Part 2 Drugs

SAFETY ALERT! acamprosate calcium

a-kam-PRO-sate

Campral

Pharmacologic class: synthetic amino acid neurotransmitter analogue

Pregnancy risk category C

AVAILABLE FORMS

Tablets (delayed-release): 333 mg

INDICATIONS & DOSAGES

Adjunct to management of alcohol abstinence

Adults: 666 mg P.O. t.i.d.

Adjust-a-dose: In patients with creatinine clearance of 30 to 50 ml/minute, give 333 mg t.i.d.

ADMINISTRATION

P.O.

•Don’t crush or break tablets.

•Give drug without regard for food.

ACTION

Restores the balance of neuronal excitation and inhibition, probably by interacting with glutamate and gamma-aminobutyric acid neurotransmitter systems, thus reducing alcohol dependence.

Route	Onset	Peak	Duration
P.O.	Unknown	3-8 hr	Unknown

Half-life: 20 to 33 hours.

ADVERSE REACTIONS

CNS: abnormal thinking, amnesia, anxiety, asthenia, depression, dizziness, headache, insomnia, paresthesia, somnolence, suicidal thoughts, syncope, tremor, pain.

CV: hypertension, palpitations, peripheral edema, vasodilation.

EENT: abnormal vision, pharyngitis, rhinitis.

GI: abdominal pain, anorexia, constipation, diarrhea, dry mouth, dyspepsia, flatulence, increased appetite, nausea, taste disturbance, vomiting.

GU: impotence.

Metabolic: weight gain.

Musculoskeletal: arthralgia, back pain, chest pain, myalgia.

Respiratory: bronchitis, dyspnea, increased cough.

Skin: increased sweating, pruritus, rash.

Other: accidental injury, chills, decreased libido, flulike symptoms, infection.

INTERACTIONS

None significant.

EFFECTS ON LAB TEST RESULTS

• May increase ALT, AST, bilirubin, blood glucose, and uric acid levels. May decrease hemoglobin level and hematocrit.

• May decrease platelet count.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients allergic to drug or its components and in those whose creatinine clearance is 30 ml/minute or less.

•Use cautiously in pregnant or breast-feeding women, elderly patients, patients with moderate renal impairment, and patients with a history of depression and suicidal thoughts or attempts.

NURSING CONSIDERATIONS

•Use only after the patient successfully becomes abstinent from drinking.

•Drug doesn’t eliminate or reduce withdrawal symptoms.

•Monitor patient for development of depression or suicidal thoughts.

•Drug doesn’t cause alcohol aversion or a disulfiram-like reaction if used with alcohol.

PATIENT TEACHING

•Tell patient to continue the alcohol abstinence program, including counseling and support.

•Advise patient to notify his prescriber if he develops depression, anxiety, thoughts of suicide, or severe diarrhea.

•Caution patient’s family or caregiver to watch for signs of depression or suicidal ideation.

•Tell patient that drug may be taken without regard to meals, but that taking it with meals may help him remember it.

•Tell patient not to crush, break, or chew the tablets but to swallow them whole.

•Advise women to use effective contraception while taking this drug. Tell patient to contact her prescriber if she becomes pregnant or plans to become pregnant.

•Explain that this drug may impair judgment, thinking, or motor skills. Urge patient to use caution when driving or performing hazardous activities until drug’s effects are known.

•Tell patient to continue taking acamprosate and to contact his prescriber if he resumes drinking alcohol.

activated charcoal

Actidose ♦, Actidose-Aqua ♦, Actidose with Sorbitol ♦, CharcoAid ♦, CharcoAid 2000 ♦, Liqui-Char ♦

charcoal

Charcoal Plus DS ♦, CharcoCaps ♦

Pharmacologic class: adsorbent Pregnancy risk category C

AVAILABLE FORMS

activated charcoal

Granules: 15 g ♦

Liquid: 12.5 g ♦, 15 g ♦^*, 25 g ♦^*,

30 g ♦^*, 50 g ♦^*

Oral suspension: 15 g ♦, 30 g ♦

Powder: 15 g ♦, 30 g ♦, 40 g ♦, 120 g ♦, 240 g ♦

charcoal

Capsules: 260 mg ♦

Tablets: 250 mg ♦

INDICATIONS & DOSAGES

Flatulence, dyspepsia, diarrhea

Adults: 500 to 520 mg (charcoal) P.O. after meals or at first sign of discomfort. Repeat as needed, up to 5 g daily.

Poisoning

Adults and children: Initially, 1 to 2 g/kg (30 to 100 g) P.O. or 10 times the amount of poison ingested as a suspension in 120 to 240 ml (4 to 8 ounces) of water.

ADMINISTRATION

P.O.

•Give after emesis is complete because activated charcoal absorbs and inactivates ipecac syrup.

•For best effect, give within 30 minutes after poison ingestion.

•Mix powder (most effective form) with tap water to consistency of thick syrup. Add small amount of fruit juice or flavoring to make mix more palatable. Don’t mix with ice cream, milk, or sherbet; these decrease adsorptive capacity of activated charcoal.

•Give by large-bore nasogastric tube after lavage, if needed.

•If patient vomits shortly after administration, repeat dose.

•Space doses at least 1 hour apart from other drugs if treatment is for indications other than poisoning.

ACTION

Adheres to many drugs and chemicals, inhibiting their absorption from the GI tract. Also reduces volume of intestinal gas and relieves related discomfort.

Route	Onset	Peak	Duration
P.O.	Immediate	Unknown	Unknown

Half-life: Unknown.

ADVERSE REACTIONS

GI: black stools, intestinal obstruction, nausea, constipation.

INTERACTIONS

Drug-drug. Acetaminophen, barbiturates, carbamazepine, digitoxin, digoxin, furosemide, glutethimide, hydantoins, methotrexate, nizatidine, phenothiazines,
phenylbutazone, propoxyphene, salicylates, sulfonamides, sulfonylureas, tetracyclines, theophyllines, tricyclic antidepressants, valproic acid: May reduce absorption of these drugs. Give charcoal at least 2 hours before or 1 hour after other drugs.

Acetylcysteine, ipecac: May inactivate these drugs. Give charcoal after vomiting has been induced by ipecac; remove charcoal by nasogastric tube before giving acetylcysteine.

Drug-food. Milk, ice cream, sherbet: May decrease adsorptive capacity of drug. Discourage use together.

EFFECTS ON LAB TEST RESULTS

None reported.

CONTRAINDICATIONS & CAUTIONS

None known.

NURSING CONSIDERATIONS

•Although there are no known contraindications, drug isn’t effective for treating all acute poisonings.

•Alert: Drug is commonly used for treating poisoning or overdose with acetaminophen, aspirin, atropine, barbiturates, dextropropoxyphene, digoxin, poisonous mushrooms, oxalic acid, parathion, phenol, phenytoin, propantheline, propoxyphene, strychnine, or tricyclic antidepressants. Check with poison control center for use in other types of poisonings or overdoses.

•Alert: Don’t aspirate or allow patient to aspirate charcoal powder; this may result in death.

•Follow treatment with stool softener or laxative to prevent constipation unless sorbitol is part of product ingredients. Preparations made with sorbitol have a laxative effect that lessens risk of severe constipation or fecal impaction.

•If preparation with sorbitol is used, maintain patient’s fluid and electrolyte needs.

•Don’t use charcoal with sorbitol in fructose-intolerant patients or in children younger than age 1.

•Alert: Drug is ineffective for poisoning or overdose of cyanide, mineral acids, caustic alkalis, and organic solvents; it’s not very effective for overdose of ethanol, lithium, methanol, and iron salts.

•Look alike-sound alike: Don’t confuse Actidose with Actos.

PATIENT TEACHING

•Explain use and administration of drug to patient (if awake) and family.

•Warn patient that stools will be black until all the charcoal has passed through the body.

•Instruct patient to drink 6 to 8 glasses of liquid per day because drug can cause constipation.

SAFETY ALERT! alprazolam

al-PRAH-zoe-lam

Apo-Alpraz†, Apo-Alpraz TS†, Niravam, Novo-Alprazol†, Xanax, Xanax XR

Pharmacologic class: benzodiazepine

Pregnancy risk category D

Controlled substance schedule IV

AVAILABLE FORMS

Oral solution: 1 mg/ml (concentrate)

Orally disintegrating tablets (ODTs):

0.25 mg, 0.5 mg, 1 mg, 2 mg

Tablets: 0.25 mg, 0.5 mg, 1 mg, 2 mg

Tablets (extended-release): 0.5 mg, 1 mg, 2 mg, 3 mg

INDICATIONS & DOSAGES

Anxiety

Adults: Usual first dose, 0.25 to 0.5 mg P.O. t.i.d. Maximum, 4 mg daily in divided doses.

Elderly patients: Usual first dose, 0.25 mg P.O. b.i.d. or t.i.d. Maximum, 4 mg daily in divided doses.

Panic disorders

Adults: 0.5 mg P.O. t.i.d., increased at intervals of 3 to 4 days in increments of no more than 1 mg. Maximum, 10 mg daily in divided doses. If using extended-release tablets, start with 0.5 to 1 mg P.O. once daily. Increase by no more than 1 mg every 3 to 4 days. Maximum daily dose is 10 mg.

Adjust-a-dose: For debilitated patients or those with advanced hepatic disease, usual first dose is 0.25 mg P.O. b.i.d. or t.i.d. Maximum, 4 mg daily in divided doses.

ADMINISTRATION

P.O.

•Don’t break or crush extended-release tablets.

•Mix oral solution with liquids or semisolid food, such as water, juices, carbonated beverages, applesauce, and puddings. Use only calibrated dropper provided with this product.

•Use dry hands to remove ODTs from bottle. Discard cotton from inside bottle.

•Discard unused portion if breaking scored ODT.

ACTION

Unknown. Probably potentiates the effects of GABA, depresses the CNS, and suppresses the spread of seizure activity.

Route	Onset	Peak	Duration
P.O.	Unknown	1-2 hr	Unknown
P.O.	Unknown	Unknown	Unknown
(extended-release)

Half-life: Immediate-release, 12 to 15 hours; extended-release, 11 to 16 hours.

ADVERSE REACTIONS

CNS: insomnia, irritability, dizziness, headache, anxiety, confusion, drowsiness, light-headedness, sedation, somnolence, difficulty speaking, impaired coordination, memory impairment, fatigue, depression, suicide, mental impairment, ataxia, paresthesia, dyskinesia, hypoesthesia, lethargy, decreased or increased libido, vertigo, malaise, tremor, nervousness, restlessness, agitation, nightmare, syncope, akathisia, mania.

CV: palpitations, chest pain, hypotension.

EENT: sore throat, allergic rhinitis, blurred vision, nasal congestion.

GI: diarrhea, dry mouth, constipation, nausea, increased or decreased appetite, anorexia, vomiting, dyspepsia, abdominal pain.

GU: dysmenorrhea, sexual dysfunction, premenstrual syndrome, difficulty urinating.

Metabolic: increased or decreased weight.

Musculoskeletal: arthralgia, myalgia, arm or leg pain, back pain, muscle rigidity, muscle cramps, muscle twitch.

Respiratory: upper respiratory tract infection, dyspnea, hyperventilation.

Skin: pruritus, increased sweating, dermatitis.

Other: influenza, injury, emergence of anxiety between doses, dependence, feeling warm.

INTERACTIONS

Drug-drug. Anticonvulsants, antidepressants, antihistamines, barbiturates, benzodiazepines, general anesthetics, narcotics, phenothiazines: May increase CNS depressant effects. Avoid using together. Azole antifungals (including fluconazole, itraconazole, ketoconazole, miconazole): May increase and prolong alprazolam level, CNS depression, and psychomotor impairment. Avoid using together.

Carbamazepine, propoxyphene: May induce alprazolam metabolism and may reduce therapeutic effects. May need to increase dose.

Cimetidine, fluoxetine, fluvoxamine, hormonal contraceptives, nefazodone: May increase alprazolam level. Use cautiously together, and consider alprazolam dosage reduction.

Tricyclic antidepressants: May increase levels of these drugs. Monitor patient closely.

Drug-herb. Kava, valerian root: May increase sedation. Discourage use together.

St. John’s wort: May decrease drug level. Discourage use together.

Drug-food. Grapefruit juice: May increase drug level. Discourage use together.

Drug-lifestyle. Alcohol use: May cause additive CNS effects. Discourage use together.

Smoking: May decrease effectiveness of drug. Monitor patient closely.

EFFECTS ON LAB TEST RESULTS

• May increase ALT and AST levels.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug or other benzodiazepines and in those with acute angle-closure glaucoma.

•Use cautiously in patients with hepatic, renal, or pulmonary disease.

NURSING CONSIDERATIONS

•The optimum duration of therapy is unknown.

•Alert: Don’t withdraw drug abruptly; withdrawal symptoms, including seizures, may occur. Abuse or addiction is possible.

•Monitor hepatic, renal, and hematopoietic function periodically in patients receiving repeated or prolonged therapy.

•Look alike-sound alike: Don’t confuse alprazolam with alprostadil. Don’t confuse Xanax with Zantac or Tenex.

PATIENT TEACHING

•Warn patient to avoid hazardous activities that require alertness and good coordination until effects of drug are known.

•Tell patient to avoid use of alcohol while taking drug.

•Advise patient that smoking may decrease drug’s effectiveness.

•Warn patient not to stop drug abruptly because withdrawal symptoms or seizures may occur.

•Tell patient to swallow extended-release tablets whole.

•Tell patient using ODT to remove it from bottle using dry hands and to immediately place it on his tongue where it will dissolve and can be swallowed with saliva.

•Tell patient taking half a scored ODT to discard the unused half.

•Advise patient to discard the cotton from the bottle of ODTs and keep it tightly sealed to prevent moisture from dissolving the tablets.

alprostadil

al-PROSS-ta-dil

Caverject, Edex, Muse

Pharmacologic class: prostaglandin Pregnancy risk category NR

AVAILABLE FORMS

Injection: 5 mcg/ml, 10 mcg/ml, 20 mcg/ml, 40 mcg/ml after reconstitution Urogenital suppository: 125 mcg, 250 mcg, 500 mcg, 1,000 mcg

INDICATIONS & DOSAGES

Erectile dysfunction of vasculogenic, psychogenic, or mixed causes

Injection

Men: Dosages are highly individualized; initially, inject 2.5 mcg intracavernously. If partial response occurs, give second dose of 2.5 mcg; then increase in increments of 5 to 10 mcg until patient achieves erection suitable for intercourse and lasting no longer than 1 hour. If patient doesn’t respond to first dose, increase second dose to 7.5 mcg within 1 hour, and then increase further in increments of 5 to 10 mcg until patient achieves suitable erection. Patient must remain in prescriber’s office until complete detumescence occurs. Don’t repeat procedure for at least 24 hours.

Urogenital suppository

Men: Initially, 125 to 250 mcg, under supervision of prescriber. Adjust dosage as needed until response is sufficient for sexual intercourse. Maximum of two administrations in 24 hours; maximum dose is 1,000 mcg.

Erectile dysfunction of neurogenic cause (spinal cord injury)

Men: Dosages are highly individualized; initially, inject 1.25 mcg intracavernously. If partial response occurs, give second dose of 1.25 mcg. Increase in increments of 2.5 mcg, to dose of 5 mcg; then increase in increments of 5 mcg until patient achieves erection suitable for intercourse and lasting no longer than 1 hour. If patient doesn’t respond to first dose, give next higher dose within 1 hour. Patient must remain in prescriber’s office until complete detumescence occurs. If there is
a response, don’t repeat procedure for at least 24 hours.

ADMINISTRATION

•For intracavernous injection, teach patient to follow instructions on package insert.

•Store injection at or below room temperature (77 F [25 C]).

•Vial is designed for a single use. Discard vial if injection solution is discolored or contains precipitate.

•Don’t shake injection contents of reconstituted vial.

•Store unopened urogenital suppositories in refrigerator (36 to 46 F [2 to 8 C]).

•Have patient urinate before inserting suppository because moisture makes it easier to insert drug in penis and will help dissolve it.

ACTION

Induces erection by relaxing trabecular smooth muscle and dilating cavernosal arteries. This leads to expansion of lacunar spaces and entrapment of blood by compressing venules against the tunica albuginea, a process referred to as the corporal veno-occlusive mechanism.

Route	Onset	Peak	Duration
Intracavernous	5-20 min	5-20 min	1-6 hr
Urogenital	10 min	16 min	1 hr

Half-life: About 5 to 10 minutes.

ADVERSE REACTIONS

CNS: headache, dizziness.

CV: hypertension, hypotension.

EENT: sinusitis, nasal congestion.

GU: penile pain, prolonged erection, penile fibrosis, rash, or edema, prostatic disorder.

Musculoskeletal: back pain.

Respiratory: upper respiratory tract infection, cough.

Skin: injection site hematoma or ecchymosis.

Other: localized trauma or pain, flulike syndrome.

INTERACTIONS

Drug-drug. Anticoagulants: May increase risk of bleeding from intracavernosal injection site. Monitor patient closely.

Cyclosporine: May decrease cyclosporine level. Monitor cyclosporine level closely.

Vasoactive drugs: Safety and effectiveness haven’t been studied. Avoid using together.

EFFECTS ON LAB TEST RESULTS

None reported.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug, in those with conditions predisposing them to priapism (sickle cell anemia or trait, multiple myeloma, leukemia) or penile deformation (angulation, cavernosal fibrosis, Peyronie disease), in men with penile implants or for whom sexual activity is inadvisable or contraindicated, in women or children, and in sexual partners of pregnant women unless condoms are used.

NURSING CONSIDERATIONS

•Stop drug in patients who develop penile angulation, cavernosal fibrosis, or Peyronie disease.

PATIENT TEACHING

•Teach patient how to prepare and give drug before he begins treatment at home. Stress importance of reading and following patient instructions in each package insert. Tell him to store unopened suppositories in refrigerator (36° to 46° F [2° to 8° C]) and store injection at or below room temperature (77° F [25° C]).

•Tell patient not to shake contents of reconstituted vial, and remind him that vial is designed for a single use. Tell him to discard vial if solution is discolored or contains precipitate.

•Instruct patient to urinate before inserting suppository because moisture makes it easier to insert drug in penis and will help dissolve it.

•Review administration and aseptic technique.

•Inform patient that he can expect an erection 5 to 20 minutes after administration, with a preferable duration of no more than 1 hour. If his erection lasts more than
6 hours, tell him to seek medical attention immediately.

•Remind patient to take drug as instructed (generally, no more than three times weekly, with at least 24 hours between each use).Warn him not to change dosage without consulting prescriber.

•Caution patient to use a condom if his sexual partner could be pregnant.

•Review possible adverse reactions. Tell patient to inspect his penis daily and to report redness, swelling, tenderness, curvature, excessive erection (priapism), unusual pain, nodules, or hard tissue.

•Urge patient not to reuse or share needles, syringes, or drug.

•Warn patient that drug doesn’t protect against sexually transmitted diseases. Also, caution him that bleeding at injection site can increase risk of transmitting blood-borne diseases to his partner.

•Remind patient to keep regular follow-up appointments so prescriber can evaluate drug effectiveness and safety.

amitriptyline hydrochloride

a-mee-TRIP-ti-leen

Pharmacologic class: tricyclic antidepressant

Pregnancy risk category C

AVAILABLE FORMS

amitriptyline hydrochloride

Injection: 10 mg/ml

Tablets: 10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg

INDICATIONS & DOSAGES

Depression

Adults: Initially, 50 to 100 mg P.O. at bedtime, increasing to 150 mg daily. Maximum, 300 mg daily, if needed. Maintenance, 50 to 100mg daily. Or, 20 to 30 mg I.M. q.i.d.

Elderly patients and adolescents: 10 mg P.O. t.i.d. and 20 mg at bedtime daily.

ADMINISTRATION

P.O.

•Give drug without regard for food.

I.M.

•Alert: Parenteral form of drug is for I.M. administration only. Drug shouldn’t be given I.V.

ACTION

Unknown. A tricyclic antidepressant that increases the amount of norepinephrine, serotonin, or both in the CNS by blocking their reuptake by the presynaptic neurons.

Route	Onset	Peak	Duration
P.O., I.M.	Unknown	2-12 hr	Unknown

Half-life: Not established, varies widely.

ADVERSE REACTIONS

CNS: stroke, seizures, coma, ataxia, tremor, peripheral neuropathy, anxiety, insomnia, restlessness, drowsiness, dizziness, weakness, fatigue, headache, extrapyramidal reactions, hallucinations, delusions, disorientation.

CV: orthostatic hypotension, tachycardia, heart block, arrhythmias, MI, ECG changes, hypertension, edema.

EENT: blurred vision, tinnitus, mydriasis, increased intraocular pressure.

GI: dry mouth, nausea, vomiting, anorexia, epigastric pain, diarrhea, constipation, paralytic ileus.

GU: urine retention, altered libido, impotence.

Hematologic: agranulocytosis, thrombocytopenia, leukopenia, eosinophilia.

Metabolic: hypoglycemia, hyperglycemia.

Skin: rash, urticaria, photosensitivity reactions, diaphoresis.

Other: hypersensitivity reactions.

INTERACTIONS

Drug-drug. Barbiturates, CNS depressants: May enhance CNS depression. Avoid using together.

Cimetidine, fluoxetine, fluvoxamine, hormonal contraceptives, paroxetine, sertraline: May increase tricyclic antidepressant level. Monitor drug levels and patient for signs of toxicity.

Clonidine: May cause life-threatening hypertension. Avoid using together. Epinephrine, norepinephrine: May increase hypertensive effect. Use together cautiously.

MAO inhibitors: May cause severe excitation, hyperpyrexia, or seizures, usually with high doses. Avoid using within 14 days of MAO inhibitor therapy.

Quinolones: May increase the risk of life-threatening arrhythmias. Avoid using together.

Drug-herb. Evening primrose: May cause additive or synergistic effect, resulting in lower seizure threshold and increasing the risk of seizures. Discourage use together.

St. John’s wort, SAM-e, yohimbe: May cause serotonin syndrome and decrease amitriptyline level. Discourage use together.

Drug-lifestyle. Alcohol use: May enhance CNS depression. Discourage use together.

Smoking: May lower drug level.Watch for lack of effect.

Sun exposure: May increase risk of photosensitivity reactions. Advise patient to avoid excessive sunlight exposure.

EFFECTS ON LAB TEST RESULTS

• May increase or decrease glucose level.

• May increase eosinophil count and liver function test values. May decrease granulocyte, platelet, and WBC counts.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug and in those who have received an MAO inhibitor within the past 14 days.

•Contraindicated during acute recovery phase of MI.

•Use cautiously in patients with history of seizures, urine retention, angle-closure glaucoma, or increased intraocular pressure; in those with hyperthyroidism, CV disease, diabetes, or impaired liver function; and in those receiving thyroid drugs.

•Use cautiously in those receiving electro-convulsive therapy.

NURSING CONSIDERATIONS

•Alert: Drug may increase the risk of suicidal thinking and behavior in children and adolescents with major depressive disorder or other psychiatric disorder. Don’t use in children younger than age 12.

•Alert: Drug may increase the risk of suicidal thinking and behavior in young adults ages 18 to 24 during the first 2 months of treatment.

•Amitriptyline has strong anticholinergic effects and is one of the most sedating tricyclic antidepressants. Anticholinergic effects have rapid onset even though therapeutic effect is delayed for weeks.

•Elderly patients may have an increased sensitivity to anticholinergic effects of drug; sedating effects of drug may increase the risk of falls in this population.

•If signs or symptoms of psychosis occur or increase, expect prescriber to reduce dosage. Record mood changes. Monitor patient for suicidal tendencies and allow only minimum supply of drug.

•Because patients using tricyclic antidepressants may suffer hypertensive episodes during surgery, stop drug gradually several days before surgery.

•Monitor glucose level.

•Watch for nausea, headache, and malaise after abrupt withdrawal of long-term therapy; these symptoms don’t indicate addiction.

•Don’t withdraw drug abruptly.

•Look alike-sound alike: Don’t confuse amitriptyline with nortriptyline or aminophylline.

PATIENT TEACHING

•Whenever possible, advise patient to take full dose at bedtime, but warn him of possible morning orthostatic hypotension.

•Tell patient to avoid alcohol during drug therapy.

•Advise patient to consult prescriber before taking other drugs.

•Warn patient to avoid activities that require alertness and good psychomotor coordination until CNS effects of drug are known. Drowsiness and dizziness usually subside after a few weeks.

•Inform patient that dry mouth may be relieved with sugarless hard candy or gum. Saliva substitutes may be useful.

•To prevent photosensitivity reactions, advise patient to use a sunblock, wear protective clothing, and avoid prolonged exposure to strong sunlight.

•Warn patient not to stop drug abruptly.

•Advise patient that it may take as long as 30 days to achieve full therapeutic effect.

aripiprazole

air-eh-PIP-rah-zole

Abilify, Abilify Discmelt

Pharmacologic class: quinolone derivative

Pregnancy risk category C

AVAILABLE FORMS

Injection: 9.75 mg/1.3 ml (7.5 mg/ml) single-dose vial

Oral solution: 1 mg/ml

Orally disintegrating tablets (ODTs): 10 mg, 15 mg, 20 mg, 30 mg

Tablets: 2 mg, 5 mg, 10 mg, 15 mg, 20 mg, 30 mg

INDICATIONS & DOSAGES

NEW INDICATION: Schizophrenia

Adults: Initially, 10 to 15 mg P.O. daily; increase to maximum daily dose of 30 mg if needed, after at least 2 weeks.

Adolescents age 13 to 17: Initially, 2 mg P.O. daily; increase to 5 mg after 2 days, then to recommended dose of 10 mg in 2 more days. May titrate to maximum daily dose of 30 mg in 5-mg increments.

Adjust-a-dose: When using with CYP3A4 inhibitors such as ketoconazole or CYP2D6 inhibitors, such as quinidine, fluoxetine, or paroxetine, give half the aripiprazole dose. When using with CYP3A4 inducers such as carbamazepine, double the aripiprazole dose. Return to original dosing after the other drugs are stopped.

Bipolar mania, including manic and mixed episodes

Adults: Initially, 30 mg P.O. once daily. May reduce dose to 15 mg daily based on patient tolerance. Safety of doses greater than 30 mg daily and treatment lasting beyond 6 weeks hasn’t been established.

Agitation associated with schizophrenia or bipolar 1 disorder, mixed or manic

Adults: 5.25 to 15 mg by deep I.M. injection. Recommended dose is 9.75 mg. May give a second dose after 2 hours, if needed. Safety of giving more frequently than every 2 hours or a total daily dose more than 30 mg isn’t known. Switch to oral form as soon as possible.

ADMINISTRATION

P.O.

•Give drug without regard for food.

•Substitute the oral solution on a milligram-by-milligram basis for the 5-, 10-, 15-, or 20-mg tablets, up to 25 mg. Give patients taking 30-mg tablets 25 mg of solution.

•Keep ODTs in blister package until ready to use. Use dry hands to carefully peel open the foil backing and remove the tablet. Don’t split tablet.

•Store oral solution in refrigerator; it can be used up to 6 months after opening.

I.M.

•Inject slowly and deep into the muscle mass.

•Don’t give I.V. or subcutaneously.

ACTION

Thought to exert partial agonist activity at D2 and serotonin 1A receptors and antagonist activity at serotonin 2A receptors.

Route	Onset	Peak	Duration
P.O.	Unknown	3-5 hr	Unknown
I.M.	Unknown	1-3 hr	Unknown

Half-life: About 75 hours in patients with normal metabolism; about 6 days in those who can’t metabolize the drug through CYP2D6.

ADVERSE REACTIONS

CNS: headache, anxiety, insomnia, light-headedness, somnolence, akathisia, increased suicide risk, neuroleptic malignant syndrome, seizures, suicidal thoughts, tremor, asthenia, depression, fatigue, dizziness, nervousness, hostility, manic behavior, confusion, abnormal gait, cogwheel rigidity, fever, tardive dyskinesia.

CV: peripheral edema, chest pain, hypertension, tachycardia, orthostatic hypotension, bradycardia.

EENT: rhinitis, blurred vision, increased salivation, conjunctivitis, ear pain.

GI: nausea, vomiting, constipation, anorexia, dry mouth, dyspepsia, diarrhea, abdominal pain, esophageal dysmotility.

GU: urinary incontinence.

Hematologic: ecchymosis, anemia.

Metabolic: weight gain, weight loss, hyperglycemia, hypercholesterolemia.

Musculoskeletal: neck pain, neck stiffness, muscle cramps.

Respiratory: dyspnea, pneumonia, cough.

Skin: rash, dry skin, pruritus, sweating, ulcer.

Other: flulike syndrome.

INTERACTIONS

Drug-drug. Antihypertensives: May enhance antihypertensive effects. Monitor blood pressure.

Carbamazepine and other CYP3A4 inducers: May decrease levels and effectiveness of aripiprazole. Double the usual dose of aripiprazole, and monitor the patient closely.

Ketoconazole and other CYP3A4 inhibitors: May increase risk of serious toxic effects. Start treatment with half the usual dose of aripiprazole, and monitor patient closely.

Potential CYP2D6 inhibitors (fluoxetine, paroxetine, quinidine): May increase levels and toxicity of aripiprazole. Give half the usual dose of aripiprazole.

Drug-food. Grapefruit juice: May increase drug level. Tell patient not to take drug with grapefruit juice.

Drug-lifestyle. Alcohol use: May increase CNS effects. Discourage use together.

EFFECTS ON LAB TEST RESULTS

• May increase CK and glucose levels.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug.

•Use cautiously in patients with CV disease, cerebrovascular disease, or conditions that could predispose the patient to hypotension, such as dehydration or hypovolemia.

•Use cautiously in patients with history of seizures or with conditions that lower the seizure threshold.

•Use cautiously in patients who engage in strenuous exercise, are exposed to extreme heat, take anticholinergics, or are susceptible to dehydration.

•Use cautiously in patients at risk for aspiration pneumonia, such as those with Alzheimer disease.

•Use cautiously in pregnant and breast-feeding women.

NURSING CONSIDERATIONS

•Alert: Neuroleptic malignant syndrome may occur. Monitor patient for hyperpyrexia, muscle rigidity, altered mental status, irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmias.

•If signs and symptoms of neuroleptic malignant syndrome occur, immediately stop drug and notify prescriber.

•Monitor patient for signs and symptoms of tardive dyskinesia. Elderly patients, especially women, are at highest risk of developing this adverse effect.

•Alert: Fatal cerebrovascular adverse events (stroke, transient ischemic attack) may occur in elderly patients with dementia. Drug isn’t safe or effective in these patients.

•Alert: Hyperglycemia may occur. Monitor patient with diabetes regularly. Patient with risk factors for diabetes should undergo fasting blood glucose testing at baseline and periodically. Monitor all patients for symptoms of hyperglycemia including increased hunger, thirst, frequent urination, and weakness. Hyperglycemia may resolve when patient stops taking drug.

•Alert: Monitor patient for symptoms of metabolic syndrome (significant weight gain and increased body mass index, hypertension, hyperglycemia, hypercholesterolemia, and hypertriglyceridemia).

•Treat patient with the smallest dose for the shortest time and periodically reevaluate for need to continue.

•Give prescriptions only for small quantities of drug, to reduce risk of overdose.

•Don’t give I.V. or subcutaneously.

PATIENT TEACHING

•Tell patient to use caution while driving or operating hazardous machinery because psychoactive drugs may impair judgment, thinking, or motor skills.

•Tell patient that drug may be taken without regard to meals.

•Advise patients that grapefruit juice may interact with aripiprazole and to limit or avoid its use.

•Advise patient that gradual improvement in symptoms should occur over several weeks rather than immediately.

•Tell patients to avoid alcohol use while taking drug.

•Advise patients to limit strenuous activity while taking drug to avoid dehydration.

•Tell patient to keep ODT in blister package until ready to use. Using dry hands, he should carefully peel open the foil backing and place tablet on the tongue. Tell him not to split tablet.

•Tell patient to store oral solution in refrigerator, and that the solution can be used for up to 6 months after opening.

aspirin (acetylsalicylic acid, ASA)

ASS-pir-in

Aspergum ◊, Bayer ◊, Ecotrin ◊, Empirin ◊, Halfprin, Heartline ◊, Norwich ◊, Novasen† ◊, St Joseph’s ◊, ZORprin ◊

Pharmacologic class: salicylate Pregnancy risk category D

AVAILABLE FORMS

Chewing gum: 227.5 mg ◊

Suppositories: 120 mg ◊, 200 mg ◊, 300 mg ◊, 600 mg ◊

Tablets: 325 mg ◊, 500 mg ◊

Tablets (chewable): 81 mg ◊

Tablets (controlled-release): 800 mg

Tablets (enteric-coated): 81 mg ◊, 165 mg ◊, 325 mg ◊, 500 mg ◊, 650 mg ◊, 975 mg

Tablets (extended-release): 650 mg ◊

INDICATIONS & DOSAGES

Rheumatoid arthritis, osteoarthritis, or other polyarthritic or inflammatory conditions

Adults: Initially, 2.4 to 3.6 g P.O. daily in divided doses. Maintenance dosage is 3.2 to 6 g P.O. daily in divided doses.

Juvenile rheumatoid arthritis

Children who weigh more than 25 kg (55 lb): 2.4 to 3.6 g P.O. daily in divided doses.

Children who weigh 25 kg or less: 60 to 130 mg/kg daily P.O. in divided doses. Increase by 10 mg/kg daily at no more than weekly intervals. Maintenance dosages usually range from 80 to 100 mg/kg daily; up to 130 mg/kg daily.

Mild pain or fever

Adults and children older than age 11: 325 to 650 mg P.O. or P.R. every 4 hours p.r.n.

Children ages 2 to 11: 10 to 15 mg/kg/dose P.O. or P.R. every 4 hours up to 80 mg/kg daily.

To prevent thrombosis

Adults: 1.3 g P.O. daily, divided b.i.d. to q.i.d.

To reduce risk of MI in patients with previous MI or unstable angina

Adults: 75 to 325 mg P.O. daily.

Kawasaki syndrome (mucocutaneous lymph node syndrome)

Children: 80 to 100 mg/kg P.O. daily, divided q.i.d. with immune globulin I.V. After the fever subsides, reduce dosage to 3 to 5 mg/kg once daily. Aspirin therapy usually continues for 6 to 8 weeks.

Acute rheumatic fever

Adults: 5 to 8 g P.O. daily.

Children: 100 mg/kg daily P.O. for 2 weeks; then 75 mg/kg daily P.O. for 4 to 6 weeks.

To reduce risk of recurrent transient ischemic attacks and stroke or death in patients at risk

Adults: 50 to 325 mg P.O. daily.

Acute ischemic stroke

Adults: 160 to 325 mg P.O. daily, started within 48 hours of stroke onset and continued for up to 2 to 4 weeks.

Acute pericarditis after MI

Adults: 160 to 325 mg P.O. daily. Higher doses (650 mg P.O. every 4 to 6 hours) may be needed.

ADMINISTRATION

P.O.

•For patient with swallowing difficulties, crush non-enteric-coated aspirin and dissolve in soft food or liquid. Give liquid immediately after mixing because drug will break down rapidly.

•Give drug with food, milk, antacid, or large glass of water to reduce GI effects.

•Give sustained-release or enteric-coated forms whole; don’t crush or break these tablets.

Rectal

•Refrigerate suppositories.

ACTION

Thought to produce analgesia and exert its anti-inflammatory effect by inhibiting prostaglandin and other substances that sensitize pain receptors. Drug may relieve fever through central action in the hypothalamic heat-regulating center. In low doses, drug also appears to interfere with clotting by keeping a platelet-aggregating substance from forming.

Route	Onset	Peak	Duration
P.O. (buffered)	5-30 min	1-2 hr	1-4 hr
P.O. (enteric-coated)	5-30 min	Variable	1-4 hr
P.O. (extended-release)	5-30 min	1-4 hr	1-4 hr
P.O. (solution)	5-30 min	15-40 min	1-4 hr
P.O. (tablet)	5-30 min	25-40 min	1-4 hr
P.R.	Unknown	3-4 hr	Unknown

Half-life: 15 to 20 minutes.

ADVERSE REACTIONS

EENT: tinnitus, hearing loss.

GI: nausea, GI bleeding, dyspepsia, GI distress, occult bleeding.

Hematologic: prolonged bleeding time, leukopenia, thrombocytopenia.

Hepatic: hepatitis.

Skin: rash, bruising, urticaria.

Other: angioedema, Reye syndrome, hypersensitivity reactions.

INTERACTIONS

Drug-drug. ACE inhibitors: May decrease antihypertensive effects. Monitor blood pressure closely.

Ammonium chloride and other urine acidifiers: May increase levels of aspirin products.Watch for aspirin toxicity.

Antacids in high doses and other urine alkalinizers: May decrease levels of aspirin products.Watch for decreased aspirin effect.

Anticoagulants: May increase risk of bleeding. Use with extreme caution if must be used together.

Beta blockers: May decrease antihypertensive effect. Avoid long-term aspirin use if patient is taking antihypertensives.

Corticosteroids: May enhance salicylate elimination and decrease drug level.Watch for decreased aspirin effect.

Heparin: May increase risk of bleeding. Monitor coagulation studies and patient closely if used together.

Ibuprofen, other NSAIDs: May negate the antiplatelet effect of low-dose aspirin therapy. Patients using immediate-release aspirin (not enteric-coated) should take ibuprofen at least 30 minutes after or more than 8 hours before aspirin. Occasional use of ibuprofen is unlikely to have a negative effect.

Methotrexate: May increase risk of methotrexate toxicity. Avoid using together.

Nizatidine: May increase risk of salicylate toxicity in patients receiving high doses of aspirin. Monitor patient closely.

Oral antidiabetics: May increase hypoglycemic effect. Monitor patient closely.

Probenecid, sulfinpyrazone: May decrease uricosuric effect. Avoid using together.

Valproic acid: May increase valproic acid level. Avoid using together.

Drug-herb. Dong quai, feverfew, ginkgo, horse chestnut, kelpware, red clover: May increase risk of bleeding. Monitor patient closely for increased effects. Discourage use together.

White willow: May increase risk of adverse effects. Discourage use together.

Drug-food. Caffeine: May increase drug absorption.Watch for increased effects.

Drug-lifestyle. Alcohol use: May increase risk of GI bleeding. Discourage use together.

EFFECTS ON LAB TEST RESULTS

• May increase liver function test values. May decrease platelet andWBC counts.

• May falsely increase protein-bound iodine level. May interfere with urine glucose analysis with Diastix, Chemstrip uG, Clinitest, and Benedict solution; with urinary 5-hydroxyindoleacetic acid
and vanillylmandelic acid tests; and with Gerhardt test for urine acetoacetic acid.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug and in those with NSAIDinduced sensitivity reactions, G6PD deficiency, or bleeding disorders, such as hemophilia, vonWillebrand disease, or telangiectasia.

•Use cautiously in patients with GI lesions, impaired renal function, hypoprothrombinemia, vitamin K deficiency, thrombocytopenia, thrombotic thrombocytopenic purpura, or severe hepatic impairment.

•Alert: Oral and rectal OTC products containing aspirin and nonaspirin salicylates shouldn’t be given to children or teenagers who have or are recovering from chickenpox or flulike symptoms because of the risk of Reye syndrome.

NURSING CONSIDERATIONS

•For inflammatory conditions, rheumatic fever, and thrombosis, give aspirin on a schedule rather than as needed.

•Because enteric-coated and sustained-release tablets are slowly absorbed, they aren’t suitable for rapid relief of acute pain, fever, or inflammation. They cause less GI bleeding andmay be better suited for long-term therapy, such as for arthritis.

•For patients who can’t tolerate oral drugs, ask prescriber about using aspirin rectal suppositories.Watch for rectal mucosal irritation or bleeding.

•Febrile, dehydrated children can develop toxicity rapidly.

•Monitor elderly patients closely because they may be more susceptible to aspirin’s toxic effects.

•Monitor salicylate level. Therapeutic salicylate level for arthritis is 150 to 300 mcg/ml. Tinnitus may occur at levels above 200 mcg/ml, but this isn’t a reliable indicator of toxicity, especially in very young patients and those older than age 60.With long-term therapy, severe toxic effects may occur with levels exceeding 400 mcg/ml.

•During prolonged therapy, assess hematocrit, hemoglobin level, PT, INR, and renal function periodically.

•Drug irreversibly inhibits platelet aggregation. Stop drug 5 to 7 days before elective surgery to allow time for production and release of new platelets.

•Monitor patient for hypersensitivity reactions, such as anaphylaxis and asthma.

•Look alike-sound alike: Don’t confuse aspirin with Asendin or Afrin.

PATIENT TEACHING

•Tell patient who’s allergic to tartrazine to avoid aspirin.

•Advise patient on a low-salt diet that 1 tablet of buffered aspirin contains 553 mg of sodium.

•Advise patient to take drug with food, milk, antacid, or large glass of water to reduce GI reactions.

•Tell patient not to crush or chew sustained-release or enteric-coated forms but to swallow them whole.

•Instruct patient to discard aspirin tablets that have a strong vinegar-like odor.

•Tell patient to consult prescriber if giving drug to children for longer than 5 days or adults for longer than 10 days.

•Advise patient receiving prolonged treatment with large doses of aspirin to watch for small, round, red pinprick spots, bleeding gums, and signs of GI bleeding, and to drink plenty of fluids. Encourage use of a soft-bristled toothbrush.

•Because of the many drug interactions with aspirin, warn patient taking prescription drugs to check with prescriber or pharmacist before taking aspirin or OTC products containing aspirin.

•Ibuprofen can interfere with the antiplatelet effect of low-dose aspirin therapy, negating its effect. Tell patient how to safely use ibuprofen in relation to aspirin therapy.

•Urge pregnant woman to avoid aspirin during last trimester of pregnancy unless specifically directed by prescriber.

•Drug is a leading cause of poisoning in children. Caution parents to keep drug out of reach of children. Encourage use of child-resistant containers.

atomoxetine hydrochloride

at-oh-MOX-ah-teen

Strattera

Pharmacologic class: selective norepinephrine reuptake inhibitor

Pregnancy risk category C

AVAILABLE FORMS

Capsules: 10 mg, 18 mg, 25 mg, 40 mg, 60 mg, 80 mg, 100 mg

INDICATIONS & DOSAGES

Attention-deficit hyperactivity disorder (ADHD)

Adults, children, and adolescents who weigh more than 70 kg (154 lb): Initially, 40 mg P.O. daily; increase after at least 3 days to a total of 80 mg/day P.O., as a single dose in the morning or two evenly divided doses in the morning and late afternoon or early evening. After 2 to 4 weeks, increase total dose to a maximum of 100 mg, if needed.

Children who weigh 70 kg or less: Initially, 0.5 mg/kg P.O. daily; increase after a minimum of 3 days to a target total daily dose of 1.2 mg/kg P.O. as a single dose in the morning or two evenly divided doses in the morning and late afternoon or early evening. Don’t exceed 1.4 mg/kg or 100 mg daily, whichever is less.

Adjust-a-dose: In patients with moderate hepatic impairment, reduce to 50% of the normal dose; in those with severe hepatic impairment, reduce to 25% of the normal dose. Poor metabolizers of CYP2D6 may require a reduced dose. In children who weigh less than 70 kg, adjust dosage to 0.5 mg/kg daily and increase to 1.2 mg/kg daily if symptoms don’t improve after 4 weeks and if first dose is tolerated. In children and adults who weigh more than 70 kg, start at 40 mg daily and increase to 80 mg daily if symptoms don’t improve after 4 weeks and if first dose is tolerated.

ADMINISTRATION

P.O.

•Give drug without regard for meals.

•Capsules should be swallowed whole and not opened.

ACTION

May be related to selective inhibition of the presynaptic norepinephrine transporter.

Route	Onset	Peak	Duration
P.O.	Rapid	1-2 hr	Unknown

Half-life: 211/2 hours.

ADVERSE REACTIONS

CNS: headache, insomnia, dizziness, somnolence, crying, irritability, mood swings, pyrexia, fatigue, sedation, depression, tremor, early-morning awakening, paresthesia, abnormal dreams, sleep disorder.

CV: orthostatic hypotension, tachycardia, hypertension, palpitations, hot flashes.

EENT: ear infection, rhinorrhea, sore throat, nasal congestion, nasopharyngitis, sinus congestion, mydriasis, sinusitis.

GI: abdominal pain, constipation, dyspepsia, nausea, vomiting, decreased appetite, gastroenteritis, dry mouth, flatulence.

GU: urinary retention, urinary hesitation, ejaculatory problems, difficulty in micturition, dysmenorrhea, erectile disturbance, impotence, delayed menses, menstrual disorder, prostatitis.

Metabolic: weight loss.

Musculoskeletal: arthralgia, myalgia.

Respiratory: cough, upper respiratory tract infection.

Skin: dermatitis, pruritus, increased sweating.

Other: influenza, decreased libido, rigors.

INTERACTIONS

Drug-drug. Albuterol: May increase CV effects. Use together cautiously.

MAO inhibitors: May cause hyperthermia, rigidity, myoclonus, autonomic instability with possible rapid fluctuations of vital signs, and mental status changes. Avoid use within 2 weeks of MAO inhibitor.

Pressor agents: May increase blood pressure. Use together cautiously.

Strong CYP2D6 inhibitors ( fluoxetine, paroxetine, quinidine): May increase atomoxetine level. Reduce first dose.

EFFECTS ON LAB TEST RESULTS

None reported.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to atomoxetine or to components of drug, in those who have taken an MAO inhibitor within the past 2 weeks, and in those with angle-closure glaucoma.

•Use cautiously in patients with hypertension, tachycardia, or CV or cerebrovascular disease, and in pregnant or breast-feeding women.

•Safety and efficacy haven’t been established in patients younger than age 6.

NURSING CONSIDERATIONS

•Use drug as part of a total treatment program for ADHD, including psychological, educational, and social intervention.

•Alert: Monitor children and adolescents closely for worsening of condition, agitation, irritability, suicidal thinking or behaviors, and unusual changes in behavior, especially the first few months of therapy or when the dosage is increased or decreased.

•Patients taking drug for extended periods must be reevaluated periodically to determine drug’s usefulness.

•Monitor growth during treatment. If growth or weight gain is unsatisfactory, consider interrupting therapy.

•Alert: Severe liver injury may occur and progress to liver failure. Notify prescriber of any sign of liver injury: yellowing of the skin or the sclera of the eyes, pruritus, dark urine, upper right-sided tenderness, or unexplained flulike syndrome.

•Monitor blood pressure and pulse at baseline, after each dose increase, and during treatment periodically.

•Monitor for urinary hesitancy or retention and sexual dysfunction.

•Patient can stop drug without tapering off.

PATIENT TEACHING

•Alert: Advise parents to call prescriber immediately about unusual behavior or suicidal thoughts.

•Tell pregnant women, women planning to become pregnant, and breast-feeding women to consult prescriber before taking atomoxetine.

•Tell patient to use caution when operating a vehicle or machinery until the effects of drug are known.

bupropion hydrochloride

byoo-PROE-pee-on

Budeprion SR,Wellbutrin,Wellbutrin SR,Wellbutrin XL, Zyban

Pharmacologic class: aminoketone

Pregnancy risk category B

AVAILABLE FORMS

Tablets (extended-release): 150 mg, 300 mg

Tablets (immediate-release): 75 mg, 100 mg

Tablets (sustained-release): 100 mg, 150 mg, 200 mg

INDICATIONS & DOSAGES

Seasonal affective disorder

Adults: Start treatment in autumn before depressive symptoms appear. Initially, 150 mg extended-release P.O. once daily in the morning. After 1 week, increase to 300 mg once daily, if tolerated. Continue 300 mg daily during the autumn and winter and taper to 150 mg daily for 2 weeks before stopping the drug in the early spring.

Depression

Adults: For immediate-release, initially, 100 mg P.O. b.i.d.; increase after 3 days to 100 mg P.O. t.i.d., if needed. If patient doesn’t improve after several weeks of therapy, increase dosage to 150 mg t.i.d. No single dose should exceed 150 mg. Allow at least 6 hours between successive doses. Maximum dose is 450 mg daily. For sustained-release, initially, 150 mg P.O. every morning; increase to target dose of 150 mg P.O. b.i.d., as tolerated, as early as day 4 of dosing. Allow at least 8 hours between successive doses. Maximum dose is 400 mg daily. For extended-release, initially, 150 mg P.O. every morning; increase to target dosage of 300 mg P.O. daily, as tolerated, as early as day 4 of dosing. Allow at least 24 hours between successive doses. Maximum is 450 mg daily.

Aid to smoking-cessation treatment

Adults: 150 mg Zyban P.O. daily for 3 days; increased to maximum of 300 mg daily in two divided doses at least 8 hours apart.

Adjust-a-dose: In patients with mild to moderate hepatic cirrhosis or renal impairment, reduce frequency and dose. In patients with severe hepatic cirrhosis, don’t exceed 75 mg immediate-release P.O. daily, 100 mg sustained-release P.O. daily, 150 mg (sustained-release) P.O. every other day, or 150 mg extended-release P.O. every other day.

ADMINISTRATION

P.O.

•Don’t crush or split tablets.

•When switching patients from regular or sustained-release tablets to extended-release tablets, give the same total daily dose (when possible) as the once-daily dosage provided.

ACTION

Unknown. Drug doesn’t inhibit MAO, but it weakly inhibits norepinephrine, dopamine, and serotonin reuptake. Noradrenergic or dopaminergic mechanisms, or both, may cause drug’s effect.

Route	Onset	Peak	Duration
P.O. (extended-release)	Unknown	5 hr	Unknown
P.O. (immediaterelease)	Unknown	2 hr	Unknown
P.O. (sustained-release)	Unknown	3 hr	Unknown

Half-life: 8 to 24 hours.

ADVERSE REACTIONS

CNS: abnormal dreams, insomnia, headache, sedation, tremor, agitation, dizziness, seizures, suicidal behavior, anxiety, confusion, delusions, euphoria, fever, hostility, impaired concentration, impaired sleep quality, akinesia, akathisia, fatigue, syncope.

CV: tachycardia, arrhythmias, hypertension, hypotension, palpitations, chest pain.

EENT: blurred vision, rhinitis, auditory disturbances, epistaxis, pharyngitis, sinusitis.

GI: constipation, nausea, vomiting, anorexia, dry mouth, taste disturbance, dyspepsia, diarrhea, abdominal pain.

GU: impotence, menstrual complaints, urinary frequency, urine retention.

Metabolic: increased appetite, weight loss, weight gain.

Musculoskeletal: arthritis, myalgia, arthralgia, muscle spasm or twitch.

Respiratory: upper respiratory complaints, increase in coughing.

Skin: excessive sweating, pruritus, rash, cutaneous temperature disturbance, urticaria.

Other: fever and chills, decreased libido, accidental injury.

INTERACTIONS

Drug-drug. Amantadine, levodopa: May increase risk of adverse reactions. If used together, give small first doses of bupropion and increase dosage gradually.

Antidepressants, antipsychotics, systemic corticosteroids, theophylline: May lower seizure threshold. Use cautiously together.

Beta blockers, class IC antiarrhythmics: May increase levels of these drugs and adverse reactions. Use a reduced dose if used with bupropion.

Carbamazepine, phenobarbital, phenytoin: May enhance metabolism of bupropion and decrease its effect. Monitor patient closely.

MAO inhibitors: May increase the risk of bupropion toxicity. Don’t use drugs within 14 days of each other.

Nicotine replacement agents: May cause hypertension. Monitor blood pressure.

Ritonavir: May increase bupropion level. Monitor patient closely for adverse reactions.

Drug-lifestyle. Alcohol use: May alter seizure threshold. Discourage use together.

Sun exposure: May increase risk of photosensitivity reactions. Advise patient to avoid excessive sunlight exposure.

EFFECTS ON LAB TEST RESULTS

• May increase liver function test values.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug, in those who have taken MAO inhibitors within previous 14 days, and in those with seizure disorders or history of bulimia or anorexia nervosa because of a higher risk of seizures.

•Contraindicated in patients abruptly stopping use of alcohol or sedatives (including benzodiazepines).

•Don’t use with other drugs containing bupropion.

•Use cautiously in patients with recent history of MI, unstable heart disease, renal or hepatic impairment, a history of seizures, head trauma, or other predisposition to seizures, and in those being treated with drugs that lower seizure threshold.

NURSING CONSIDERATIONS

•Many patients experience a period of increased restlessness, including agitation, insomnia, and anxiety, especially at start of therapy.

•Alert: To minimize the risk of seizures, don’t exceed maximum recommended dose.

•Alert: Patient with major depressive disorder may experience a worsening of depression and suicidal thoughts. Carefully monitor patient for worsening depression or suicidal thoughts, especially at the beginning of therapy and during dosage changes.

•Alert: Drug may increase the risk of suicidal thinking and behavior in children and adolescents with major depressive disorder or other psychiatric disorder.

•Alert: Drug may increase the risk of suicidal thinking and behavior in young adults ages 18 to 24 during the first 2 months of treatment.

•Closely monitor patient with history of bipolar disorder. Antidepressants can cause manic episodes during the depressed phase of bipolar disorder. This may be less likely to occur with bupropion than with other antidepressants.

•Begin smoking-cessation treatment while patient is still smoking; about 1 week is needed to achieve steady-state drug levels.

•Stop smoking-cessation treatment if patient hasn’t progressed toward abstinence by week 7. Treatment usually lasts up to 12 weeks. Patient can stop taking drug without tapering off.

•Look alike-sound alike: Don’t confuse bupropion with buspirone orWellbutrin withWellcovorin.

PATIENT TEACHING

•Alert: Explain that excessive use of alcohol, abrupt withdrawal from alcohol or other sedatives, and addiction to cocaine, opiates, or stimulants during therapy may increase risk of seizures. Seizure risk is also increased in those using OTC stimulants, in anorectics, and in diabetic patients using oral antidiabetics or insulin.

•Tell patient not to chew, crush, or divide tablets.

•Advise patient to consult prescriber before taking other prescription or OTC drugs.

•Advise patient to avoid hazardous activities that require alertness and good psychomotor coordination until effects of drug are known.

•Alert: Advise patient that Zyban and Wellbutrin contain the same active ingredient and shouldn’t be used together.

•Tell patient that it may take 4 weeks to reach full antidepressant effect.

•Alert: Advise patient to report mood swings or suicidal thoughts immediately.

•Inform patient that tablets may have an odor.

buspirone hydrochloride

byoo-SPYE-rone

BuSpar

Pharmacologic class: azaspirodecanedione derivative

Pregnancy risk category B

AVAILABLE FORMS

Tablets: 5 mg, 10 mg, 15 mg, 30 mg

INDICATIONS & DOSAGES

Anxiety disorders

Adults: Initially, 7.5 mg P.O. b.i.d. Increase dosage by 5 mg daily at 2- to 3-day
intervals. Usual maintenance dosage is 20 to 30 mg daily in divided doses. Don’t exceed 60 mg daily.

ADMINISTRATION

P.O.

•Don’t give drug with grapefruit juice.

•Give drug at the same times each day, and always with or always without food.

ACTION

May inhibit neuronal firing and reduce serotonin turnover in cortical, amygdaloid, and septohippocampal tissue.

Route	Onset	Peak	Duration
P.O.	Unknown	40-90 min	Unknown

Half-life: 2 to 3 hours.

ADVERSE REACTIONS

CNS: dizziness, drowsiness, headache, nervousness, insomnia, light-headedness, fatigue, numbness.

CV: tachycardia, nonspecific chest pain.

EENT: blurred vision.

GI: dry mouth, nausea, diarrhea, abdominal distress.

INTERACTIONS

Drug-drug. Azole antifungals: May inhibit first-pass metabolism of buspirone. Monitor patient closely for adverse effects; adjust dosage as needed.

CNS depressants: May increase CNS depression. Use together cautiously.

Drugs metabolized by CYP3A4 (erythromycin, nefazodone): May increase buspirone level. Monitor patient; decrease buspirone dosage and adjust carefully.

MAO inhibitors: May elevate blood pressure. Avoid using together.

Drug-food. Grapefruit juice: May increase drug level, increasing adverse effects. Give with liquid other than grapefruit juice.

Drug-lifestyle. Alcohol use: May increase CNS depression. Discourage use together.

EFFECTS ON LAB TEST RESULTS

None reported.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug and within 14 days of MAO inhibitor therapy.

•Drug isn’t recommended for patients with severe hepatic or renal impairment.

NURSING CONSIDERATIONS

•Monitor patient closely for adverse CNS reactions. Drug is less sedating than other anxiolytics, but CNS effects may be unpredictable.

•Alert: Before starting therapy, don’t stop a previous benzodiazepine regimen abruptly because a withdrawal reaction may occur.

•Drug shows no potential for abuse and isn’t classified as a controlled substance.

•Look alike-sound alike: Don’t confuse buspirone with bupropion.

PATIENT TEACHING

•Warn patient to avoid hazardous activities that require alertness and good coordination until effects of drug are known.

•Remind patient that drug effects may not be noticeable for several weeks.

•Warn patient not to abruptly stop a benzodiazepine because of risk of withdrawal symptoms.

•Tell patient to avoid use of alcohol during therapy.

carbamazepine

kar-ba-MAZ-e-peen

Carbatrol, Epitol, Equetro, Novo-Carbamaz†, Tegretol, Tegretol CR†, Tegretol-XR, Teril

Pharmacologic class: iminostilbene derivative

Pregnancy risk category D

AVAILABLE FORMS

Capsules (extended-release): 100 mg, 200 mg, 300 mg

Oral suspension: 100 mg/5 ml

Tablets: 200 mg

Tablets (chewable): 100 mg, 200 mg

Tablets (extended-release): 100 mg, 200 mg, 300 mg, 400 mg†

INDICATIONS & DOSAGES

Generalized tonic-clonic and complex partial seizures, mixed seizure patterns

Adults and children older than age 12: Initially, 200 mg P.O. b.i.d. (conventional or extended-release tablets), or 100 mg P.O. q.i.d. of suspension with meals. May be increased weekly by 200 mg P.O. daily in divided doses at 12-hour intervals for extended-release tablets or 6- to 8-hour intervals for conventional tablets or suspension, adjusted to minimum effective level. Maximum, 1,000 mg daily in children ages 12 to 15, and 1,200 mg daily in patients older than age 15. Usual maintenance dosage is 800 to 1,200 mg daily.

Children ages 6 to 12: Initially, 100 mg P.O. b.i.d. (conventional or extended-release tablets) or 50 mg of suspension P.O. q.i.d. with meals, increased at weekly intervals by up to 100 mg P.O. divided in three to four doses daily (divided b.i.d. for extended-release form). Maximum, 1,000 mg daily. Usual maintenance dosage is 400 to 800 mg daily; or, 20 to 30 mg/kg in divided doses three to four times daily.

Children younger than age 6: 10 to 20 mg/kg in two to three divided doses (conventional tablets) or four divided doses (suspension). Maximum dosage is 35 mg/kg in 24 hours.

Acute manic and mixed episodes associated with bipolar I disorder

Adults: Initially, 200 mg Equetro P.O. b.i.d. Increase by 200 mg daily to achieve therapeutic response. Doses higher than 1,600 mg daily haven’t been studied.

Trigeminal neuralgia

Adults: Initially, 100 mg P.O. b.i.d. (conventional or extended-release tablets) or 50 mg of suspension q.i.d. with meals, increased by 100 mg every 12 hours for tablets or 50 mg of suspension q.i.d. until pain is relieved. Maximum, 1,200 mg daily. Maintenance dosage is usually 200 to 400 mg P.O. b.i.d.

Restless legs syndrome ♦

Adults: 100 to 300 mg P.O. at bedtime.

Nonneuritic pain syndromes (painful neuromas, phantom limb pain) ♦

Adults: Initially, 100 mg P.O. b.i.d. Maintenance dose is 600 to 1,400 mg daily.

ADMINISTRATION

P.O.

•Shake oral suspension well before measuring dose.

•Contents of extended-release capsules may be sprinkled over applesauce if patient has difficulty swallowing capsules. Capsules and tablets shouldn’t be crushed or chewed, unless labeled as chewable form.

•When giving by nasogastric tube, mix dose with an equal volume of water, normal saline solution, or D₅W. Flush tube with 100 ml of diluent after giving dose.

•Don’t crush or split extended-release form or give broken or chipped tablets.

ACTION

Thought to stabilize neuronal membranes and limit seizure activity by either increasing efflux or decreasing influx of sodium ions across cell membranes in the motor cortex during generation of nerve impulses.

Route	Onset	Peak	Duration
P.O.	Unknown	1½-12 hr	Unknown
P.O. (extended-release)	Unknown	4-8 hr	Unknown

Half-life: 25 to 65 hours with single dose; 8 to 29 hours with long-term use.

ADVERSE REACTIONS

CNS: ataxia, dizziness, drowsiness, vertigo, worsening of seizures, confusion, fatigue, fever, headache, syncope.

CV: arrhythmias, AV block, heart failure, aggravation of coronary artery disease, hypertension, hypotension.

EENT: blurred vision, conjunctivitis, diplopia, dry pharynx, nystagmus.

GI: nausea, vomiting, abdominal pain, anorexia, diarrhea, dry mouth, glossitis, stomatitis.

GU: albuminuria, glycosuria, impotence, urinary frequency, urine retention.

Hematologic: agranulocytosis, aplastic anemia, thrombocytopenia, eosinophilia, leukocytosis.

Hepatic: hepatitis.

Metabolic: hyponatremia, SIADH.

Respiratory: pulmonary hypersensitivity.

Skin: erythema multiforme, Stevens-Johnson syndrome, excessive diaphoresis, rash, urticaria.

Other: chills.

INTERACTIONS

Drug-drug. Atracurium, cisatracurium, pancuronium, rocuronium, vecuronium: May decrease the effects of nondepolarizing muscle relaxant, causing it to be less effective. May need to increase the dose of the nondepolarizing muscle relaxant.

Cimetidine, danazol, diltiazem, fluoxetine, fluvoxamine, isoniazid, macrolides, propoxyphene, valproic acid, verapamil: May increase carbamazepine level. Use together cautiously.

Clarithromycin, erythromycin, troleandomycin: May inhibit metabolism of carbamazepine, increasing carbamazepine level and risk of toxicity. Avoid using together.

Doxycycline, felbamate, haloperidol, hormonal contraceptives, phenytoin, theophylline, tiagabine, topiramate, valproate, warfarin: May decrease levels of these drugs.Watch for decreased effect.

Lamotrigine: May decrease lamotrigine level and increase carbamazepine level. Monitor patient for clinical effects and toxicity.

Lithium: May increase CNS toxicity of lithium. Avoid using together.

MAO inhibitors: May increase depressant and anticholinergic effects. Avoid using together.

Phenobarbital, phenytoin, primidone: May decrease carbamazepine level.Watch for decreased effect.

Nefazodone: May increase carbamazepine levels and toxicity while reducing nefazodone levels and therapeutic benefits. Use together is contraindicated.

Drug-herb. Plantains (psyllium seed): May inhibit GI absorption of drug. Discourage use together.

EFFECTS ON LAB TEST RESULTS

• May increase BUN level. May decrease hemoglobin level and hematocrit.

• May increase liver function test values and eosinophil and WBC counts. May decrease thyroid function test values and granulocyte and platelet counts.

• May cause false pregnancy test results.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to this drug or tricyclic antidepressants and in those with a history of bone marrow suppression; also contraindicated in those who have taken an MAO inhibitor within 14 days.

•Use cautiously in patients with mixed seizure disorders because they may experience an increased risk of seizures. Also, use with caution in patients with hepatic dysfunction.

NURSING CONSIDERATIONS

•Watch for worsening of seizures, especially in patients with mixed seizure disorders, including atypical absence seizures.

•Obtain baseline determinations of urinalysis, BUN and iron levels, liver function, CBC, and platelet and reticulocyte counts. Monitor these values periodically thereafter.

•Never stop drug suddenly when treating seizures. Notify prescriber immediately if adverse reactions occur.

•Adverse reactions may be minimized by gradually increasing dosage.

•Therapeutic level is 4 to 12 mcg/ml. Monitor level and effects closely. Ask patient when last dose was taken to better evaluate drug level.

•When managing seizures, take appropriate precautions.

•Alert: Watch for signs of anorexia or subtle appetite changes, which may indicate excessive drug level.

•Look alike-sound alike: Don’t confuse Tegretol or Tegretol-XR with Topamax, Toprol-XL, or Toradol. Don’t confuse Carbatrol with carvedilol.

PATIENT TEACHING

•Instruct patient to take drug with food to minimize GI distress. Tell patient taking suspension form to shake container well before measuring dose.

•Tell patient not to crush or chew extended-release form and not to take broken or chipped tablets.

•Tell patient that Tegretol-XR tablet coating may appear in stool because it isn’t absorbed.

•Advise patient to keep tablets in the original container and to keep the container tightly closed and away from moisture. Some formulations may harden when exposed to excessive moisture, so that less is available in the body, decreasing seizure control.

•Inform patient that when drug is used for trigeminal neuralgia, an attempt to decrease dosage or withdraw drug is usually made every 3 months.

•Advise patient to notify prescriber immediately if fever, sore throat, mouth ulcers, or easy bruising or bleeding occurs.

•Tell patient that drug may cause mild to moderate dizziness and drowsiness when first taken. Advise him to avoid hazardous activities until effects disappear, usually within 3 to 4 days.

•Advise patient that periodic eye examinations are recommended.

•Advise woman of risks to fetus if pregnancy occurs while taking carbamazepine.

•Advise woman that breast-feeding isn’t recommended during therapy.

SAFETY ALERT! chloral hydrate

KLOR-al HYE-drate

Aquachloral Supprettes, Somnote

Pharmacologic class: CNS depressant

Pregnancy risk category C

Controlled substance schedule IV

AVAILABLE FORMS

Capsules: 500 mg

Suppositories: 325 mg, 500 mg, 650 mg

Syrup: 250 mg/5 ml, 500 mg/5 ml

INDICATIONS & DOSAGES

Sedation

Adults: 250 mg P.O. or P.R. t.i.d. after meals. Maximum single or daily dose is 2 g.

Children: 8 mg/kg P.O. t.i.d. Maximum dosage is 500 mg t.i.d.

Insomnia

Adults: 500 mg to 1 g P.O. or P.R. 15 to 30 minutes before bedtime. Maximum daily dose is 2 g.

Children: 50 mg/kg P.O. or P.R. 15 to 30 minutes before bedtime. Maximum single dose is 1 g.

Preoperatively to produce sedation and relieve anxiety

Adults: 500 mg to 1 g P.O. or P.R. 30 minutes before surgery.

Alcohol withdrawal

Adults: 500 mg to 1 g P.R. every 6 hours p.r.n.

Premedication for EEG

Children: 20 to 25 mg/kg P.O. or P.R. up to 500 mg/single dose. May give divided doses.

ADMINISTRATION

P.O.

•Give drug after meals.

•Give capsule with full glass of water or juice, and have patient swallow capsule whole.

•To minimize unpleasant taste and stomach irritation, dilute syrup or give with liquid such as ½ glass water, fruit juice, or ginger ale.

•Store capsules or liquid in dark container.

Rectal

•Refrigerate suppositories at least 2 hours before intended use.

•Store suppositories in refrigerator.

ACTION

Unknown. Sedative effects may be caused by drug’s main metabolite, trichloroethanol.

Route	Onset	Peak	Duration
P.O.	30 min	Unknown	4-8 hr
P.R.	Unknown	Unknown	4-8 hr

Half-life: 8 to 10 hours for trichloroethanol.

ADVERSE REACTIONS

CNS: drowsiness, nightmares, dizziness, ataxia, paradoxical excitement, hangover, somnolence, disorientation, delirium, light-headedness, hallucinations,
confusion, somnambulism, vertigo, malaise, physical and psychological dependence.

GI: nausea, vomiting, diarrhea, flatulence.

Hematologic: eosinophilia, leukopenia.

Other: hypersensitivity reactions.

INTERACTIONS

Drug-drug. CNS depressants including opioid analgesics: May cause excessive CNS depression or vasodilation reaction. Use together cautiously.

Furosemide I.V: May cause sweating, flushes, variable blood pressure, nausea, and uneasiness. Use together cautiously or use a different hypnotic drug.

Oral anticoagulants: May increase risk of bleeding. Monitor patient closely.

Phenytoin: May decrease phenytoin level. Monitor patient closely.

Drug-lifestyle. Alcohol use: May react synergistically, increasing CNS depression, or, rarely, may produce a disulfiram-like reaction. Strongly discourage alcohol use with these drugs.

EFFECTS ON LAB TEST RESULTS

• May increase eosinophil count. May decrease WBC count.

• May cause false-positive results in urine glucose tests that use cupric sulfate, such as Benedict’s reagent, and in phentolamine tests.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug and in those with hepatic or renal impairment.

•Oral administration is contraindicated in patients with gastric disorders.

•Use with caution in patients with severe cardiac disease.

•Use cautiously in patients with mental depression, suicidal tendencies, or history of drug abuse.

•Some products may contain tartrazine; use cautiously in patients with aspirin sensitivity.

NURSING CONSIDERATIONS

•Alert: Note two strengths of oral liquid form. Double-check dose, especially when giving to children. Fatal overdoses have occurred.

•Take precautions to prevent hoarding or overdosing by patients who are depressed, suicidal, or drug dependent or who have history of drug abuse.

•Long-term use isn’t recommended; drug loses its effectiveness in promoting sleep after 14 days of continued use. Long-term use may cause drug dependence, and patient may experience withdrawal symptoms if drug is suddenly stopped.

•Monitor BUN level; large doses may raise BUN level.

•Don’t give drug for 48 hours before fluorometric test.

PATIENT TEACHING

•Instruct patient to take capsule with a full glass of water or juice and to swallow capsule whole.

•Tell patient to avoid alcohol during drug therapy.

•Caution patient to avoid performing activities that require mental alertness or physical coordination.

•Advise patient to store drug in dark container and to store suppositories in refrigerator.

SAFETY ALERT! chlordiazepoxide hydrochloride

klor-dye-az-e-POX-ide

Librium

Pharmacologic class: benzodiazepine

Pregnancy risk category D

Controlled substance schedule IV

AVAILABLE FORMS

Capsules: 5 mg, 10 mg, 25 mg

Powder for injection: 100-mg ampule

INDICATIONS & DOSAGES

Mild to moderate anxiety

Adults: 5 to 10 mg P.O. t.i.d. or q.i.d.

Children older than age 6: 5 mg P.O. b.i.d. to q.i.d. Maximum, 10 mg P.O. b.i.d. or t.i.d.

Severe anxiety

Adults: 20 to 25 mg P.O. t.i.d. or q.i.d.

Elderly patients: 5 mg P.O. b.i.d. to q.i.d.

Adjust-a-dose: For debilitated patients, 5 mg P.O. b.i.d. to q.i.d.

Withdrawal symptoms of acute alcoholism

Adults: 50 to 100 mg P.O., I.V., or I.M. Repeat in 2 to 4 hours, as needed. Maximum, 300 mg daily.

Preoperative apprehension and anxiety

Adults: 5 to 10 mg P.O. t.i.d. or q.i.d. on day before surgery; or 50 to 100 mg I.M. 1 hour before surgery.

ADMINISTRATION

P.O.

•Alert: 5-mg and 25-mg capsules may look similar in color through the packaging. Verify contents and read label carefully.

I.V.

•Parenteral form isn’t recommended for children younger than age 12.

•Make sure equipment and staff needed for emergency airway management are available. Monitor respirations every 5 to 15 minutes and before each I.V. dose.

•Keep powder refrigerated and away from light; mix just before use and discard remainder.

•Injectable form comes in two ampules—diluent and powdered drug. Read directions carefully.

•Don’t give prepackaged diluent I.V. because air bubbles may form.

•Use 5 ml of normal saline solution or sterile water for injection as diluent for an ampule containing 100 mg of drug.

•Give over 1 minute.

•Incompatibilities: Other I.V. drugs.

I.M.

•For I.M. use, add 2 ml of diluent to powder and agitate gently until clear. Don’t use the supplied diluent for I.V. use. Use immediately.

• I.M. form may be absorbed erratically.

ACTION

A benzodiazepine that may potentiate the effects of GABA, depress the CNS, and suppress the spread of seizure activity.

Route	Onset	Peak	Duration
P.O.	Unknown	½-4 hr	Unknown
I.V.	1-5 min	Unknown	15-60 min
I.M.	Unknown	Unknown	Unknown

Half-life: 5 to 30 hours.

ADVERSE REACTIONS

CNS: drowsiness, lethargy, ataxia, confusion, extrapyramidal reactions, minor changes in EEG patterns.

CV: edema.

GI: nausea, constipation.

GU: menstrual irregularities.

Hematologic: agranulocytosis.

Hepatic: jaundice.

Skin: swelling and pain at injection site, skin eruptions.

Other: altered libido.

INTERACTIONS

Drug-drug. Cimetidine: May decrease chlordiazepoxide clearance and increase risk of adverse reactions. Monitor patient carefully.

CNS depressants: May increase CNS depression. Use together cautiously.

Digoxin: May increase digoxin level and risk of toxicity. Monitor patient and digoxin level closely.

Disulfiram: May decrease clearance and increase half-life of chlordiazepoxide. Monitor patient for enhanced effects. Consider dosage adjustment.

Fluconazole, itraconazole, ketoconazole, miconazole: May increase and prolong chlordiazepoxide levels, CNS depression, and psychomotor impairment. Avoid using together.

Levodopa: May decrease control of parkinsonian symptoms in patients with Parkinson disease. Use together cautiously.

Drug-herb. Kava: May increase sedation. Discourage use together.

Drug-lifestyle. Alcohol use: May cause additive CNS effects. Discourage use together.

Smoking: May decrease effectiveness of drug. Monitor patient closely.

EFFECTS ON LAB TEST RESULTS

• May increase liver function test values. May decrease granulocyte count.

• May cause a false-positive pregnancy test result. May alter urinary 17-ketosteroid (Zimmerman reaction), urine alkaloid (Frings thin-layer chromatography method), and urinary glucose determinations (with Chemstrip uG and Diastix).

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug and in pregnant women, especially in first trimester.

•Use cautiously in patients with mental depression, porphyria, or hepatic or renal disease.

NURSING CONSIDERATIONS

•In patients receiving repeated or prolonged therapy, monitor hepatic, renal, and hematopoietic function periodically.

•Alert: Use of this drug may lead to abuse and addiction. Don’t withdraw drug abruptly after long-term use because withdrawal symptoms may occur.

PATIENT TEACHING

•Warn patient to avoid hazardous activities that require alertness and coordination until effects of drug are known.

•Tell patient to avoid use of alcohol while taking drug.

•Notify patient that smoking may decrease drug’s effectiveness.

•Warn patient not to abruptly stop the drug because withdrawal symptoms may occur.

•Warnwoman to avoid use during pregnancy.

chlorpromazine hydrochloride

klor-PROE-ma-zeen

Thorazine

Pharmacologic class: phenothiazine

Pregnancy risk category C

AVAILABLE FORMS

Capsules (extended-release): 200 mg, 300 mg

Injection: 25 mg/ml

Oral concentrate: 30 mg/ml, 100 mg/ml

Suppositories: 25 mg, 100 mg

Syrup: 10 mg/5 ml

Tablets: 10 mg, 25 mg, 50 mg, 100 mg, 200 mg

INDICATIONS & DOSAGES

Psychosis, mania

Adults: For hospitalized patients with acute disease, 25 mg I.M.; may give an additional 25 to 50 mg I.M. in 1 hour if needed. Increase over several days to 400 mg every 4 to 6 hours. Switch to oral therapy as soon as possible. Or, 25 mg P.O. t.i.d. initially; then gradually increase to 400 mg daily in divided doses. For outpatients, 30 to 75 mg daily in two to four divided doses. Increase dosage by 20 to 50 mg twice weekly until symptoms are controlled.

Children age 6 months and older: 0.55 mg/kg P.O. every 4 to 6 hours or I.M. every 6 to 8 hours. Or, 1.1 mg/kg P.R. every 6 to 8 hours. Maximum I.M. dose in children younger than age 5 or who weigh less than 22.7 kg (50 lb) is 40 mg. Maximum I.M. dose in children ages 5 to 12 or who weigh 22.7 to 45.4 kg (50 to 100 lb) is 75 mg.

Nausea and vomiting

Adults: 10 to 25 mg P.O. every 4 to 6 hours, p.r.n. Or, 50 to 100 mg P.R. every 6 to 8 hours, p.r.n. Or, 25 mg I.M. initially. If no hypotension occurs, 25 to 50 mg I.M. every 3 to 4 hours may be given, p.r.n., until vomiting stops.

Acute intermittent porphyria, intractable hiccups

Adults: 25 to 50 mg P.O. t.i.d. or q.i.d. If symptoms persist for 2 to 3 days, 25 to 50 mg I.M. For hiccups, if symptoms still persist, 25 to 50 mg diluted in 500 to 1,000 ml of normal saline solution and infused slowly with patient in supine position.

Tetanus

Adults: 25 to 50 mg I.V. or I.M. t.i.d. or q.i.d.

Children age 6 months and older: 0.55 mg/kg I.M. or I.V. every 6 to 8 hours. Maximum parenteral dosage in children who weigh less than 22.7 kg (50 lb) is 40 mg daily; for children who weigh 22.7 to 45.4 kg (50 to 100 lb), 75 mg, except in severe cases. If giving I.V., dilute to 1 mg/ml with normal saline and give at a rate of 0.5 mg/minute.

Surgery

Adults: Preoperatively, 25 to 50 mg P.O. 2 to 3 hours before surgery or 12.5 to 25 mg I.M. 1 to 2 hours before surgery; during surgery, 12.5 mg I.M., repeated in 30 minutes, if needed, or fractional 2-mg doses I.V. at 2-minute intervals to maximum dose of 25 mg; postoperatively, 10 to 25 mg P.O. every 4 to 6 hours or 12.5 to 25 mg I.M., repeated in 1 hour, if needed.

Children age 6 months and older: Preoperatively, 0.55 mg/kg P.O. 2 to 3 hours before surgery or I.M. 1 to 2 hours before surgery. During surgery, 0.275 mg/kg I.M., repeated in 30 minutes if needed, or fractional 1-mg doses I.V. at 2-minute intervals to maximum of 0.275 mg/kg. May repeat fractional I.V. regimen in 30 minutes if needed. Postoperatively, 0.55 mg/kg P.O. or I.M. every 4 to 6 hours (oral dose) or 1 hour (I.M. dose), if needed and if hypotension doesn’t occur.

Elderly patients: Lower dosages are sufficient; dosage increments should be more gradual than in adults.

ADMINISTRATION

P.O.

•Wear gloves when preparing solutions and avoid contact with skin and clothing. Oral liquid forms can cause contact dermatitis.

•Slight yellowing of concentrate is common and doesn’t affect potency. Discard markedly discolored solutions.

•Protect liquid concentrate from light. Dilute with fruit juice, milk, or semisolid food just before giving.

•Don’t crush or break extended-release capsules.

I.V.

•Wear gloves when preparing solutions and avoid contact with skin and clothing. Parenteral forms can cause contact dermatitis.

•Drug is compatible with most common I.V. solutions, including D₅W, Ringer’s injection, lactated Ringer’s injection, and normal saline solution for injection.

•For direct injection, dilute with normal saline solution for injection and give into a large vein or through the tubing of a free-flowing I.V. solution.

•Don’t exceed 1 mg/minute for adults or 0.5 mg/minute for children.

•For intermittent infusion, dilute with 50 or 100 ml of a compatible solution.

•Infuse over 30 minutes.

•Incompatibilities: Aminophylline, amphotericin B, ampicillin, chloramphenicol sodium succinate, chlorothiazide, cimetidine, dimenhydrinate, furosemide, heparin sodium, linezolid, melphalan, methohexital, paclitaxel, penicillin, pentobarbital, phenobarbital, solutions with a pH of 4 to 5, thiopental.

I.M.

•Wear gloves when preparing solutions and avoid contact with skin and clothing. Parenteral forms can cause contact dermatitis.

•Slight yellowing of injection is common and doesn’t affect potency. Discard markedly discolored solutions.

•Monitor blood pressure before and after I.M. administration; keep patient supine for 1 hour afterward and have him get up slowly.

•Give deep I.M. only in upper outer quadrant of buttocks. Consider giving injection by Z-track method. Massage slowly afterward to prevent sterile abscess. Injection stings. Rotate injection sites.

Rectal

•Store suppositories in well-closed containers between 15° and 30° C (59° and 86° F).

ACTION

A piperidine phenothiazine that may block postsynaptic dopamine receptors in the brain.

Route	Onset	Peak	Duration
P.O.	30-60 min	Unknown	4-6 hr
P.O. (extended)	30-60 min	Unknown	10-12 hr
I.V., I.M.	Unknown	Unknown	Unknown
P.R.	> 1 hr	Unknown	3-4 hr

Half-life: 20 to 24 hours.

ADVERSE REACTIONS

CNS: extrapyramidal reactions, sedation, tardive dyskinesia, pseudoparkinsonism, neuroleptic malignant syndrome, seizures, dizziness, drowsiness.

CV: orthostatic hypotension, tachycardia, quinidine-like ECG effects.

EENT: ocular changes, blurred vision, nasal congestion.

GI: dry mouth, constipation, nausea.

GU: urine retention, menstrual irregularities, inhibited ejaculation, priapism.

Hematologic: leukopenia, agranulocytosis, aplastic anemia, thrombocytopenia, eosinophilia, hemolytic anemia.

Hepatic: jaundice.

Skin: mild photosensitivity reactions, pain at I.M. injection site, allergic reactions, sterile abscess, skin pigmentation changes.

Other: gynecomastia, lactation, galactorrhea.

INTERACTIONS

Drug-drug. Antacids: May inhibit absorption of oral phenothiazines. Separate antacid and phenothiazine doses by at least 2 hours.

Anticholinergics such as tricyclic antidepressants, antiparkinsonians: May increase anticholinergic activity, aggravated parkinsonian symptoms. Use together cautiously.

Anticonvulsants: May lower seizure threshold. Monitor patient closely.

Barbiturates, lithium: May decrease phenothiazine effect. Monitor patient.

Centrally acting antihypertensives: May decrease antihypertensive effect. Monitor blood pressure.

CNS depressants: May increase CNS depression. Use together cautiously.

Electroconvulsive therapy, insulin: May cause severe reactions. Monitor patient closely.

Lithium: May increase neurologic effects. Monitor patient closely.

Meperidine: May cause excessive sedation and hypotension. Don’t use together.

Propranolol: May increase levels of both propranolol and chlorpromazine. Monitor patient closely.

Warfarin: May decrease effect of oral anticoagulants. Monitor PT and INR.

Drug-herb. St. John’s wort: May cause photosensitivity reactions. Advise patient to avoid excessive sunlight exposure.

Drug-lifestyle. Alcohol use: May increase CNS depression, particularly psychomotor skills. Strongly discourage alcohol use.

Sun exposure: May increase risk of photosensitivity reactions. Advise patient to avoid excessive sunlight exposure.

EFFECTS ON LAB TEST RESULTS

• May decrease hemoglobin level and hematocrit.

• May increase liver function test values and eosinophil count. May decrease granulocyte, platelet, and WBC counts.

• May cause false-positive results for urinary porphyrin, urobilinogen, amylase, and 5-hydroxyindoleacetic acid tests and for urine pregnancy tests that use human chorionic gonadotropin.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug; in those with CNS depression, bone marrow suppression, or subcortical damage, and in those in coma.

•Use cautiously in elderly or debilitated patients and in patients with hepatic or renal disease, severe CV disease (may suddenly decrease blood pressure), respiratory disorders, hypocalcemia, glaucoma, or prostatic hyperplasia. Also use cautiously in those exposed to extreme heat or cold (including antipyretic therapy) or organophosphate insecticides.

•Use cautiously in acutely ill or dehydrated children.

NURSING CONSIDERATIONS

•Obtain baseline blood pressure measurements before therapy, and monitor regularly. Watch for orthostatic hypotension, especially with parenteral administration.

•Monitor patient for tardive dyskinesia, which may occur after prolonged use. It may not appear until months or years later and may disappear spontaneously or persist for life, despite stopping drug.

•After abrupt withdrawal of long-term therapy, gastritis, nausea, vomiting, dizziness, or tremor may occur.

•Alert: Watch for evidence of neuroleptic malignant syndrome (extrapyramidal effects, hyperthermia, autonomic disturbance), which is rare but usually fatal. It may not be related to length of drug use or type of neuroleptic; more than 60% of affected patients are men.

•If jaundice, symptoms of blood dyscrasia (fever, sore throat, infection, cellulitis, weakness), or persistent extrapyramidal reactions (longer than a few hours) develop, or if such reactions occur in children or pregnant women, withhold dose and notify prescriber.

•Don’t withdraw drug abruptly unless required by severe adverse reactions.

•Look alike-sound alike: Don’t confuse chlorpromazine with clomipramine or with chlorpropamide, a hypoglycemic.

PATIENT TEACHING

•Warn patient to avoid activities that require alertness or good coordination until effects of drug are known. Drowsiness and dizziness usually subside after first few weeks.

•Alert: Advise patient not to crush, chew, or break extended-release capsule before swallowing.

•Tell patient to avoid alcohol while taking drug.

•Have patient report signs of urine retention or constipation.

•Tell patient to use sunblock and to wear protective clothing to avoid oversensitivity to the sun. This drug is more likely to cause sun sensitivity than other drugs in its class.

•Tell patient to relieve dry mouth with sugarless gum or hard candy.

•Advise patient receiving drug by any method other than by mouth to remain lying down for 1 hour afterward and to rise slowly.

citalopram hydrobromide

si-TAL-oh-pram

Celexa

Pharmacologic class: SSRI

Pregnancy risk category C

AVAILABLE FORMS

Solution: 10 mg/5 ml

Tablets: 10 mg, 20 mg, 40 mg

Tablets (orally disintegrating): 10 mg, 20 mg, 40 mg

INDICATIONS & DOSAGES

Depression

Adults: Initially, 20 mg P.O. once daily, increasing to 40 mg daily after no less than 1 week. Maximum recommended dose is 40 mg daily.

Elderly patients: 20 mg daily P.O. with adjustment to 40 mg daily only for unresponsive patients.

Adjust-a-dose: For patients with hepatic impairment, use 20 mg daily P.O. with adjustment to 40 mg daily only for unresponsive patients.

ADMINISTRATION

P.O.

•Allow orally disintegrating tablet (ODT) to dissolve on the patient’s tongue, then be swallowed, with or without water.

•Don’t cut, break, or crush ODTs.

•Give drug without regard for food.

ACTION

Probably linked to potentiation of serotonergic activity in the CNS resulting from inhibition of neuronal reuptake of serotonin.

Route	Onset	Peak	Duration
P.O.	Unknown	4 hr	Unknown

Half-life: 35 hours.

ADVERSE REACTIONS

CNS: somnolence, insomnia, suicide attempt, anxiety, agitation, dizziness, paresthesia, migraine, impaired concentration, amnesia, depression, apathy, tremor, confusion, fatigue, fever.

CV: tachycardia, orthostatic hypotension, hypotension.

EENT: rhinitis, sinusitis, abnormal accommodation.

GI: dry mouth, nausea, diarrhea, anorexia, dyspepsia, vomiting, abdominal pain, taste perversion, increased saliva, flatulence, increased appetite.

GU: dysmenorrhea, amenorrhea, ejaculation disorder, impotence, anorgasmia, polyuria.

Metabolic: decreased or increased weight.

Musculoskeletal: arthralgia, myalgia.

Respiratory: upper respiratory tract infection, coughing.

Skin: rash, pruritus.

Other: increased sweating, yawning, decreased libido.

INTERACTIONS

Drug-drug. Amphetamines, buspirone, dextromethorphan, dihydroergotamine, meperidine, other SSRIs or SSNRIs (duloxetine, venlafaxine), tramadol, trazodone, tricyclic antidepressants, tryptophan: May increase the risk of serotonin syndrome. Avoid other drugs that increase the availability of serotonin in the CNS; monitor patient closely if used together.

Carbamazepine: May increase citalopram clearance. Monitor patient for effects.

CNS drugs: May cause additive effects. Use together cautiously.

Drugs that inhibit cytochrome P-450 isoenzymes 3A4 and 2C19: May cause decreased clearance of citalopram. Monitor patient for increased adverse effects.

Imipramine, other tricyclic antidepressants: May increase level of imipramine metabolite desipramine by about 50%. Use together cautiously.

Lithium: May enhance serotonergic effect of citalopram. Use together cautiously, and monitor lithium level.

MAO inhibitors (phenelzine, selegiline, tranylcypromine): May cause serotonin syndrome. Avoid using within 14 days of MAO inhibitor therapy.

Sumatriptan: May cause weakness, hyperreflexia, and incoordination. Monitor patient closely.

Drug-herb. St. John’s wort: May increase the risk of serotonin syndrome. Discourage use together.

Drug-lifestyle. Alcohol use: May increase CNS effects. Discourage use together.

EFFECTS ON LAB TEST RESULTS

None reported.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug or its inactive components, within 14 days of MAO inhibitor therapy, and in patients taking pimozide.

•Use cautiously in patients with history of mania, seizures, suicidal thoughts, or hepatic or renal impairment.

•Use in third trimester of pregnancy may be linked to neonatal complications at birth. Consider the risk versus benefit of treatment during this time.

•Safety and efficacy of drug haven’t been established in children.

NURSING CONSIDERATIONS

•Although drug hasn’t been shown to impair psychomotor performance, any psychoactive drug has the potential to impair judgment, thinking, or motor skills.

•The possibility of a suicide attempt is inherent in depression and may persist until significant remission occurs. Closely supervise high-risk patients at start of drug therapy. Reduce risk of overdose by limiting amount of drug available per refill.

•Alert: Drug may increase the risk of suicidal thinking and behavior in children and adolescents with major depressive disorder or other psychiatric disorders.

•Alert: Drug may increase the risk of suicidal thinking and behavior in young adults ages 18 to 24 during the first 2 months of treatment.

•At least 14 days should elapse between MAO inhibitor therapy and citalopram therapy.

•Alert: Combining triptans with an SSRI or an SSNRI may cause serotonin syndrome. Signs and symptoms may include restlessness, hallucinations, loss of coordination, fast heartbeat, rapid changes in blood pressure, increased body temperature, overactive reflexes, nausea, vomiting, and diarrhea. Serotonin syndrome may be more likely to occur when starting or increasing the dose of triptan, SSRI, or SNRI.

•Look alike-sound alike: Don’t confuse Celexa with Celebrex or Cerebyx.

PATIENT TEACHING

•Caution patient against use of MAO inhibitors while taking citalopram.

•Inform patient that, although improvement may take 1 to 4 weeks, he should continue therapy as prescribed.

•Advise patient not to stop drug abruptly.

•Tell patient that drug may be taken in the morning or evening without regard to meals. If drowsiness occurs, he should take drug in evening.

•Tell patient to allow orally disintegrating tablet to dissolve on his tongue then swallow, with or without water. Tell him not to cut, crush, or chew.

•Instruct patient to exercise caution when driving or operating hazardous machinery; drug may impair judgment, thinking, and motor skills.

•Advise patient to consult prescriber before taking other prescription or OTC drugs.

•Advise woman of childbearing age to consult prescriber before breast-feeding.

•Warn patient to avoid alcohol during drug therapy.

•Instruct woman of childbearing age to use contraceptives during drug therapy and to notify prescriber immediately if pregnancy is suspected.

clomipramine hydrochloride

kloe-MI-pra-meen

Anafranil

Pharmacologic class: tricyclic antidepressant (TCA)

Pregnancy risk category C

AVAILABLE FORMS

Capsules: 25 mg, 50 mg, 75 mg

INDICATIONS & DOSAGES

Obsessive-compulsive disorder

Adults: Initially, 25 mg P.O. daily with meals, gradually increased to 100 mg daily in divided doses during first 2 weeks. Thereafter, increase to maximum dose of 250 mg daily in divided doses with meals, as needed. After adjustment, give total daily dose at bedtime.

Children and adolescents: Initially, 25 mg P.O. daily with meals, gradually increased over first 2 weeks to daily maximum of 3 mg/kg or 100 mg P.O. in divided doses, whichever is smaller. Maximum daily dose is 3 mg/kg or 200 mg, whichever is smaller; give at bedtime after adjustment. Reassess and adjust dosage periodically.

To manage panic disorder with or without agoraphobia

Adults: 12.5 to 150 mg P.O. daily (maximum 200 mg).

Depression, chronic pain ♦

Adults: 100 to 250 mg P.O. daily.

Cataplexy and related narcolepsy ♦

Adults: 25 to 200 mg P.O. daily.

ADMINISTRATION

P.O.

•Give drug without regard for food.

ACTION

Unknown. Inhibits reuptake of serotonin and norepinephrine at the presynaptic neuron.

Route	Onset	Peak	Duration
P.O.	Unknown	2-6 hr	Unknown

Half-life: Parent compound, 32 hours; active metabolite, 69 hours.

ADVERSE REACTIONS

CNS: somnolence, tremor, dizziness, headache, insomnia, nervousness, myoclonus, fatigue, seizures, EEG changes.

CV: orthostatic hypotension, palpitations, tachycardia.

EENT: pharyngitis, rhinitis, visual changes.

GI: dry mouth, constipation, nausea, dyspepsia, increased appetite, anorexia, abdominal pain, diarrhea.

GU: urinary hesitancy, UTI, dysmenorrhea, ejaculation failure, impotence.

Hematologic: purpura.

Metabolic: weight gain.

Musculoskeletal: myalgia.

Skin: diaphoresis, rash, pruritus, dry skin.

Other: altered libido.

INTERACTIONS

Drug-drug. Barbiturates: May decrease TCA level.Watch for decreased antidepressant effect.

Cimetidine, fluoxetine, fluvoxamine, paroxetine, sertraline: May increase TCA level. Monitor drug level and patient for signs of toxicity.

Clonidine: May cause life-threatening hypertension. Avoid using together.

CNS depressants: May enhance CNS depression. Avoid using together.

Epinephrine, norepinephrine: May increase hypertensive effect. Use together cautiously.

MAO inhibitors: May cause hyperpyretic crisis, seizures, coma, or death. Avoid using within 14 days of MAO inhibitor therapy.

Quinolones: May increase the risk of life-threatening arrhythmias. Avoid using together.

Drug-herb. Evening primrose oil: May cause additive or synergistic effect, resulting in lower seizure threshold and increasing the risk of seizure. Discourage use together.

St. John’s wort, SAM-e, yohimbe: May cause serotonin syndrome. Discourage use together.

Drug-lifestyle. Alcohol use: May enhance CNS depression. Discourage use together.

Sun exposure: May increase risk of photosensitivity reactions. Advise patient to avoid excessive sunlight exposure.

EFFECTS ON LAB TEST RESULTS

None reported.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug or other tricyclic antidepressants, in those who have taken MAO inhibitors within previous 14 days, and in patients in acute recovery period after MI.

•Use cautiously in patients with history of seizure disorders or with brain damage of varying cause; in patients receiving other seizure threshold-lowering drugs; in patients at risk for suicide; in patients with history of urine retention or angle-closure glaucoma, increased intraocular pressure, CV disease, impaired hepatic or renal function, or hyperthyroidism; in patients with tumors of the adrenal medulla; in patients receiving thyroid drug or electroconvulsive therapy; and in those undergoing elective surgery.

NURSING CONSIDERATIONS

•Monitor mood and watch for suicidal tendencies. Allow patient to have only the minimum amount of drug.

•Alert: Drug may increase risk of suicidal thinking and behavior in children, adolescents, and young adults ages 18 to 24 during the first 2 months of treatment, especially in those with major depressive disorder or other psychiatric disorder.

•Don’t withdraw drug abruptly.

•Because patients may suffer hypertensive episodes during surgery, stop drug gradually several days before surgery.

•Relieve dry mouth with sugarless candy or gum. Saliva substitutes may be needed.

•Look alike-sound alike: Don’t confuse clomipramine with chlorpromazine or clomiphene, or Anafranil with enalapril, nafarelin, or alfentanil.

PATIENT TEACHING

•Warn patient to avoid hazardous activities requiring alertness and good coordination, especially during adjustment. Daytime sedation and dizziness may occur.

•Tell patient to avoid alcohol during drug therapy.

•Warn patient not to stop drug suddenly.

•Advise patient to use sunblock, wear protective clothing, and avoid prolonged exposure to strong sunlight to prevent oversensitivity to the sun.

SAFETY ALERT! clonazepam

kloe-NAZ-e-pam

Klonopin, Klonopin wafers

Pharmacologic class: benzodiazepine

Pregnancy risk category D

Controlled substance schedule IV

AVAILABLE FORMS

Tablets: 0.5 mg, 1 mg, 2 mg

Tablets (orally disintegrating): 0.125 mg, 0.25 mg, 0.5 mg, 1 mg, 2 mg

INDICATIONS & DOSAGES

Lennox-Gastaut syndrome, atypical absence seizures, akinetic and myoclonic seizures

Adults: Initially, no more than 1.5 mg P.O. daily in three divided doses. May be increased by 0.5 to 1 mg every 3 days until seizures are controlled. If given in unequal doses, give largest dose at bedtime. Maximum recommended daily dose is 20 mg.

Children up to age 10 or 30 kg (66 lb): Initially, 0.01 to 0.03 mg/kg P.O. daily (not to exceed 0.05 mg/kg daily) in two or three divided doses. Increase by 0.25 to 0.5 mg every third day to maximum maintenance dose of 0.1 to 0.2 mg/kg daily, as needed.

Panic disorder

Adults: Initially, 0.25 mg P.O. b.i.d.; increase to target dose of 1 mg daily after 3 days. Some patients may benefit from dosages up to maximum of 4 mg daily. To achieve 4 mg daily, increase dosage in increments of 0.125 to 0.25 mg b.i.d. every 3 days, as tolerated, until panic disorder is controlled. Taper drug with decrease of 0.125 mg b.i.d. every 3 days until drug is stopped.

Acute manic episodes of bipolar disorder ♦

Adults: 0.75 to 16 mg daily P.O.

Adjunct treatment for schizophrenia ♦

Adults: 0.5 to 2 mg daily P.O.

Periodic leg movements during sleep ♦

Adults: 0.5 to 2 mg P.O. at bedtime.

Parkinsonian (hypokinetic) dysarthria ♦

Adults: 0.25 to 0.5 mg daily P.O.

Multifocal tic disorders ♦

Adults: 1.5 to 12 mg daily P.O.

Neuralgias (deafferentation pain syndromes) ♦

Adults: 2 to 4 mg daily P.O.

ADMINISTRATION

P.O.

•Peel back the foil of the orally disintegrating tablet (ODT) pouch carefully. Don’t push ODT through foil.

•Give ODT to patient with or without water.

ACTION

Unknown. Probably acts by facilitating the effects of the inhibitory neurotransmitter GABA.

Route	Onset	Peak	Duration
P.O.	Unknown	1-2 hr	Unknown

Half-life: 18 to 50 hours.

ADVERSE REACTIONS

CNS: drowsiness, agitation, ataxia, behavioral disturbances, confusion, depression, slurred speech, tremor.

CV: palpitations.

EENT: abnormal eye movements, nystagmus.

GI: anorexia, change in appetite, constipation, diarrhea, gastritis, nausea, sore gums, vomiting.

GU: dysuria, enuresis, nocturia, urine retention.

Hematologic: leukopenia, thrombocytopenia, eosinophilia.

Respiratory: respiratory depression, chest congestion, shortness of breath.

Skin: rash.

INTERACTIONS

Drug-drug. Carbamazepine, phenobarbital, phenytoin: May lower clonazepam levels. Monitor patient closely.

CNS depressants: May increase CNS depression. Avoid using together.

Fluconazole, itraconazole, ketoconazole, miconazole: May increase and prolong drug levels, CNS depression, and psychomotor impairment. Avoid using together.

Drug-lifestyle. Alcohol use: May cause additive CNS effects. Discourage use together.

Smoking: May increase clearance of clonazepam. Monitor patient for decreased drug effects.

EFFECTS ON LAB TEST RESULTS

• May increase liver function test values and eosinophil count. May decrease platelet and WBC counts.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to benzodiazepines and in those with significant hepatic disease or acute angle-closure glaucoma.

•Use cautiously in patients with mixedtype seizures because drug may cause generalized tonic-clonic seizures.

•Use cautiously in children and in patients with chronic respiratory disease, open-angle glaucoma, or a history of drug or alcohol addiction.

NURSING CONSIDERATIONS

•Watch for behavioral disturbances, especially in children.

•Don’t stop drug abruptly because this may worsen seizures. Call prescriber at once if adverse reactions develop.

•Assess elderly patient’s response closely. Elderly patients are more sensitive to drug’s CNS effects.

•Monitor patient for oversedation.

•Monitor CBC and liver function tests.

•Withdrawal symptoms are similar to those of barbiturates.

•To reduce inconvenience of somnolence when drug is used for panic disorder, giving one dose at bedtime may be desirable.

PATIENT TEACHING

•Advise patient to avoid driving and other hazardous activities that require mental alertness until drug’s CNS effects are known.

•Instruct parent to monitor child’s school performance because drug may interfere with attentiveness.

•Warn patient and parents not to stop drug abruptly because seizures may occur.

•Advise patient that drug isn’t for use during pregnancy or breast-feeding.

•Tell patients to open pouch of ODTs and peel back the foil. He shouldn’t push the tablet through the foil.

•Tell patient to use dry hands when removing the ODT.

•Tell patient that ODTs can be taken with or without water.

SAFETY ALERT! clorazepate dipotassium

klor-AZ-e-pate

Gen-Xene, Novo-Clopate†, Tranxene, Tranxene-SD

Pharmacologic class: benzodiazepine

Pregnancy risk category D

Controlled substance schedule IV

AVAILABLE FORMS

Capsules: 3.75 mg, 7.5 mg, 15 mg

Tablets: 3.75 mg, 7.5 mg, 15 mg

Tablets (extended-release): 11.25 mg, 22.5 mg

INDICATIONS & DOSAGES

Acute alcohol withdrawal

Adults: Day 1, give 30 mg P.O. initially; then 30 to 60 mg P.O. in divided doses. Day 2, give 45 to 90 mg P.O. in divided doses. Day 3, give 22.5 to 45 mg P.O. in divided doses. Day 4, give 15 to 30 mg P.O. in divided doses. Then gradually reduce dosage to 7.5 to 15 mg daily. Maximum dosage is 90 mg daily.

Anxiety

Adults: 15 to 60 mg P.O. daily.

Elderly patients: Initially, 7.5 to 15 mg daily in divided doses or as a single dose at bedtime.

Adjust-a-dose: For debilitated patients, initially, 7.5 to 15 mg daily in divided doses or as a single dose at bedtime.

Adjunctive treatment for partial seizure disorder

Adults and children older than age 12: Maximum first dose is 7.5 mg P.O. t.i.d. Dosage increases shouldn’t exceed 7.5 mg weekly. Maximum daily dose is 90 mg.

Children ages 9 to 12: Maximum first dose is 7.5 mg P.O. b.i.d. Dosage increases shouldn’t exceed 7.5 mg weekly. Maximum daily dose is 60 mg.

ADMINISTRATION

P.O.

•Don’t crush or break extended-release tablets.

ACTION

Unknown. Probably potentiates the effects of GABA, depresses the CNS, and suppresses the spread of seizure activity.

Route	Onset	Peak	Duration
P.O.	Unknown	30 min-1 hr	Unknown

Half-life: 1 to 9 days.

ADVERSE REACTIONS

CNS: drowsiness, dizziness, nervousness, confusion, headache, insomnia, depression, irritability, tremor, minor changes in EEG patterns.

CV: hypotension.

EENT: blurred vision, diplopia.

GI: nausea, vomiting, abdominal discomfort, dry mouth.

GU: urine retention, incontinence.

Skin: rash.

INTERACTIONS

Drug-drug. Cimetidine: May decrease clorazepate clearance and increase risk of adverse reactions. Monitor patient carefully.

CNS depressants: May increase CNS depression. Use together cautiously.

Digoxin: May increase digoxin level and risk of toxicity. Monitor patient and digoxin level closely.

Levodopa: May decrease effectiveness of levodopa. Monitor patient closely.

Drug-herb. Kava: May increase sedation. Discourage use together.

Drug-lifestyle. Alcohol use: May cause additive CNS effects. Discourage use together.

Smoking: May decrease benzodiazepine effectiveness. Urge patient to quit smoking, and monitor patient closely.

EFFECTS ON LAB TEST RESULTS

• May increase liver function test values.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug and in those with acute angle-closure glaucoma.

•Use cautiously in patients with suicidal tendencies, renal or hepatic impairment, pulmonary disease, or history of drug abuse.

•Don’t give drug to pregnant women, especially during first trimester.

•Drug isn’t recommended for children younger than age 9.

NURSING CONSIDERATIONS

•Alert: Monitor hepatic, renal, and hematopoietic function periodically in patients receiving repeated or prolonged therapy.

•Alert: Use of this drug may lead to abuse and addiction. Don’t withdraw drug abruptly after prolonged use because withdrawal symptoms may occur.

•Look alike-sound alike: Don’t confuse clorazepate with clofibrate.

PATIENT TEACHING

•Warn patient to avoid activities that require alertness and good coordination until effects of drug are known.

•Alert: Advise patient to swallow Tranxene-SD whole and not to crush, break, or chew.

•Tell patient to avoid alcohol while taking drug.

•Advise patient that smoking may decrease drug’s effectiveness.

•Warn patient not to stop drug abruptly because withdrawal symptoms may occur.

•Warn woman of childbearing age to avoid use during pregnancy.

•Inform patient that sugarless chewing gum or hard candy can relieve dry mouth.

SAFETY ALERT! clozapine

KLOE-za-peen

Clozaril, FazaClo

Pharmacologic class: dibenzapine derivative

Pregnancy risk category B

AVAILABLE FORMS

Orally disintegrating tablets (ODTs): 12.5 mg, 25 mg, 100 mg

Tablets: 25 mg, 100 mg, 200 mg

INDICATIONS & DOSAGES

Schizophrenia in severely ill patients unresponsive to other therapies; to reduce risk of recurrent suicidal behavior in schizophrenia or schizoaffective disorders

Adults: Initially, 12.5 mg P.O. once daily or b.i.d. If using the ODT, cut in half and discard the unused half. Adjust dose upward by 25 to 50 mg daily (if tolerated) to 300 to 450 mg daily by end of 2 weeks. Individual dosage is based on clinical response, patient tolerance, and adverse reactions. Subsequent dosage shouldn’t be increased more than once or twice weekly and shouldn’t exceed 50- to 100-mg increments. Many patients respond to dosages of 200 to 600 mg daily, but some may need as much as 900 mg daily. Don’t exceed 900 mg daily.

ADMINISTRATION

P.O.

•Peel the foil from the ODT blister and gently remove the tablet immediately before giving.

•Give ODT with or without water.

ACTION

Unknown. Binds selectively to dopaminergic receptors in the CNS and may interfere with adrenergic, cholinergic, histaminergic, and serotonergic receptors.

Route	Onset	Peak	Duration
P.O.	Unknown	2½ hr	4-12 hr

Half-life: Proportional to dose; may range from 8 to 12 hours.

ADVERSE REACTIONS

CNS: drowsiness, sedation, dizziness, vertigo, headache, seizures, syncope, tremor, disturbed sleep or nightmares, restlessness, hypokinesia or akinesia, agitation, rigidity, akathisia, confusion, fatigue, insomnia, hyperkinesia, weakness, lethargy, ataxia, slurred speech, depression, myoclonus, anxiety, fever.

CV: tachycardia, cardiomyopathy, myocarditis, pulmonary embolism, cardiac arrest, hypotension, hypertension, chest pain, ECG changes, orthostatic hypotension.

EENT: visual disturbances.

GI: constipation, excessive salivation, dry mouth, nausea, vomiting, heartburn, diarrhea.

GU: urinary frequency or urgency, urine retention, incontinence, abnormal ejaculation.

Hematologic: leukopenia, agranulocytosis, granulocytopenia, eosinophilia.

Metabolic: hyperglycemia, weight gain, hypercholesterolemia, hypertriglyceridemia.

Musculoskeletal: muscle pain or spasm, muscle weakness.

Respiratory: respiratory arrest.

Skin: rash, diaphoresis.

INTERACTIONS

Drug-drug. Anticholinergics: May potentiate anticholinergic effects of clozapine. Use together cautiously.

Antihypertensives: May potentiate hypotensive effects. Monitor blood pressure.

Benzodiazepines: May increase risk of sedation and CV and respiratory arrest. Use together cautiously.

Bone marrow suppressants: May increase bone marrow toxicity. Avoid using together.

Citalopram, fluoroquinolones, fluoxetine, fluvoxamine, paroxetine, sertraline: May increase clozapine levels and toxicity. Adjust clozapine dose as needed.

Digoxin, other highly protein-bound drugs, warfarin: May increase levels of these drugs. Monitor patient closely for adverse reactions.

Phenytoin: May decrease clozapine level and cause breakthrough psychosis. Monitor patient for psychosis and adjust clozapine dosage.

Psychoactive drugs: May cause additive effects. Use together cautiously.

Ritonavir: May increase clozapine levels and toxicity. Avoid using together.

Drug-herb. St. John’s wort: May decrease drug level. Discourage use together.

Drug-lifestyle. Alcohol use: May increase CNS depression. Discourage use together.

Smoking: May decrease drug level. Urge patient to quit smoking. Monitor patient for effectiveness and adjust dosage.

EFFECTS ON LAB TEST RESULTS

• May increase glucose, cholesterol, and triglyceride levels.

• May increase eosinophil count. May decrease granulocyte and WBC counts.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients with uncontrolled epilepsy, history of clozapineinduced agranulocytosis, WBC count below 3,500/mm³, severe CNS depression or coma, paralytic ileus, and myelosuppressive disorders.

•Contraindicated in patients taking other drugs that suppress bone marrow function.

•Use cautiously in patients with prostatic hyperplasia or angle-closure glaucoma because drug has potent anticholinergic effects.

NURSING CONSIDERATIONS

•ODTs contain phenylalanine.

•Alert: Drug carries significant risk of agranulocytosis. If possible, give patient at least two trials of standard antipsychotic before starting clozapine. Obtain baseline WBC and differential counts before clozapine therapy. Baseline WBC count must be at least 3,500/mm³ and baseline antineutrophil cytoplasmic antibody (ANCA) at least 2,000/mm³. Monitor WBC and ANCA values weekly for at least 4 weeks after stopping drug, regardless of how often you were monitoring when therapy stopped.

•During the first 6 months of therapy, monitor patient weekly and dispense no more than a 1-week supply of drug. If acceptable WBC and ANCA values [WBC 3,500/mm³ or higher and ANCA 2,000/mm³ or higher] are maintained during the first 6 months of continuous therapy, reduce monitoring to every other week. After 6 months of every-other-week monitoring without interruption by leukopenia, reduce frequency of monitoring WBC and ANCA to monthly.

•If WBC count drops below 3,500/mm³ after therapy begins or if it drops substantially from baseline, monitor patient closely for signs and symptoms of infection. If WBC count is 3,000 to 3,500/mm³ and granulocyte count is above 1,500/mm³, perform WBC and differential count twice weekly. If WBC count drops to 2,000/mm³ to 3,000/mm³ or granulocyte count drops to 1,000/mm³ to 1,500/mm³, interrupt therapy and notify prescriber. Monitor WBC and differential daily until WBC exceeds 3,000/mm³ and ANCA exceeds 1,500/mm³, and monitor patient for signs and symptoms of infection. Continue monitoring WBC and differential counts twice weekly until WBC count exceeds 3,500/mm³ and ANCA exceeds 2,000/mm³. Then, restart therapy with weekly monitoring for 1 year before returning to the usual monitoring schedule of every 2 weeks for 6 months and then every 4 weeks.

•If WBC count drops below 2,000/mm³ and granulocyte count drops below 1,000/mm³, patient may need protective isolation. Bone marrow aspiration may be needed to assess bone marrow function. Future clozapine therapy is contraindicated in these patients.

•Alert: Drug increases the risk of fatal myocarditis, especially during, but not limited to, the first month of therapy. In patients in whom myocarditis is suspected (unexplained fatigue, dyspnea, tachypnea, chest pain, tachycardia, fever, palpitations, and other signs or symptoms of heart failure or ECG abnormalities, such as ST-T wave abnormalities or arrhythmias), stop therapy immediately and don’t restart.

•Alert: Drug may cause hyperglycemia. Monitor patients with diabetes regularly. In patients with risk factors for diabetes, obtain fasting blood glucose test results at baseline and periodically.

•Alert: Monitor patient for metabolic syndrome, including significant weight gain and increased body mass index, hypertension, hyperglycemia, hypercholesterolemia, and hypertriglyceridemia.

•Monitor patient for signs and symptoms of cardiomyopathy.

•Seizures may occur, especially in patients receiving high doses.

•Some patients experience transient fever with temperature higher than 100.4° F (38° C), especially in the first 3 weeks of therapy. Monitor these patients closely.

•Alert: Drug isn’t indicated for use in elderly patients with dementia-related psychoses because of an increased risk for death from CV disease or infection.

•After abrupt withdrawal of long-term therapy, abrupt recurrence of psychosis is possible.

•If therapy must be stopped, withdraw drug gradually over 1 or 2 weeks. If changes in patient’s medical condition (including development of leukopenia) require that drug be stopped immediately, monitor patient closely for recurrence of psychosis.

•If therapy is reinstated in patients withdrawn from drug, follow usual guidelines for dosage increase. Reexposure of patient to drug may increase severity and risk of adverse reactions. If therapy was stopped because WBC counts were below 2,000/mm³ or granulocyte counts were below 1,000/mm³, don’t restart.

•Look alike-sound alike: Don’t confuse clozapine with clonidine, clofazimine, or Klonopin.

PATIENT TEACHING

•Tell patient about need for weekly blood tests to check for blood-cell deficiency. Advise him to report flulike symptoms, fever, sore throat, lethargy, malaise, or other signs of infection.

•Warn patient to avoid hazardous activities that require alertness and good coordination while taking drug.

•Tell patient to check with prescriber before taking alcohol or OTC drugs.

•Advise patient that smoking may decrease drug effectiveness.

•Tell patient to rise slowly to avoid dizziness.

•Tell patient to keep ODTs in the blister package until ready to take it.

•Inform patient that ice chips or sugarless candy or gum may help relieve dry mouth.

dantrolene sodium

DAN-troe-leen

Dantrium, Dantrium Intravenous

Pharmacologic class: hydantoin derivative

Pregnancy risk category C

AVAILABLE FORMS

Capsules: 25 mg, 50 mg, 100 mg

Injection: 20 mg/vial

INDICATIONS & DOSAGES

Spasticity and sequelae from severe chronic disorders, such as multiple sclerosis, cerebral palsy, spinal cord injury, stroke

Adults: 25 mg P.O. daily. Increase by 25-mg increments, up to 100 mg t.i.d. to q.i.d. Maintain each dosage level for 7 days to determine response. Maximum, 400 mg daily.

Children: Initially, 0.5 mg/kg P.O. daily for 7 days; then 0.5 mg/kg t.i.d. for 7 days, 1 mg/kg t.i.d. for 7 days, and finally, 2 mg/kg, t.i.d. for 7 days. May increase up to 3 mg/kg b.i.d. to q.i.d. if necessary. Maximum, 100 mg q.i.d.

To manage malignant hyperthermic crisis

Adults and children: Initially, 1 mg/kg I.V. push. Repeat, as needed, up to cumulative dose of 10 mg/kg.

To prevent or attenuate malignant hyperthermic crisis in susceptible patients who need surgery

Adults and children: 4 to 8 mg/kg P.O. daily in three or four divided doses for 1 or 2 days before procedure. Give final dose 3 or 4 hours before procedure. Or, 2.5 mg/kg I.V. about 1 hour before anesthesia; infuse over 1 hour.

To prevent recurrence of malignant hyperthermic crisis

Adults: 4 to 8 mg/kg P.O. daily in four divided doses for up to 3 days after hyperthermic crisis.

ADMINISTRATION

P.O.

•Give drug with food or milk.

•Prepare oral suspension for single dose by dissolving capsule contents in juice or other liquid. For multiple doses, use acid vehicle and refrigerate. Use within several days.

I.V.

•Reconstitute drug by adding 60 ml of sterile water for injection and shaking vial until clear. Don’t use a diluent that contains a bacteriostatic drug.

•Protect solution from light, and use within 6 hours.

•Incompatibilities: D₅W, normal saline solution, other I.V. drugs mixed in a syringe.

ACTION

Acts directly on skeletal muscle to decrease excitation and contraction coupling and reduce muscle strength by interfering with intracellular calcium movement.

Route	Onset	Peak	Duration
P.O.	Unknown	5 hr	Unknown
I.V.	Unknown	Unknown	3 hr after infusion

Half-life: P.O., 9 hours; I.V., 4 to 8 hours.

ADVERSE REACTIONS

CNS: drowsiness, dizziness, malaise, fatigue, seizures, headache, light-headedness, confusion, nervousness, insomnia, fever, depression.

CV: tachycardia, blood pressure changes, phlebitis, thrombophlebitis, heart failure.

EENT: excessive lacrimation, speech disturbance, diplopia, visual disturbances.

GI: anorexia, constipation, cramping, dysphagia, metallic taste, severe diarrhea, GI bleeding, vomiting.

GU: urinary frequency, hematuria, incontinence, nocturia, dysuria, crystalluria, difficult erection, urine retention.

Hematologic: leukopenia, thrombocytopenia, lymphocytic lymphoma, anemia.

Hepatic: hepatitis.

Musculoskeletal: muscle weakness, myalgia, back pain.

Respiratory: pleural effusion with pericarditis, pulmonary edema.

Skin: eczematous eruption, pruritus, urticaria, abnormal hair growth, diaphoresis, photosensitivity.

Other: chills.

INTERACTIONS

Drug-drug. Clofibrate, warfarin: May decrease protein binding of dantrolene. Use together cautiously.

CNS depressants: May increase CNS depression. Avoid using together.

Estrogens: May increase risk of hepatotoxicity. Use together cautiously.

I.V. verapamil and other calcium channel blockers: May cause hyperkalemia, ventricular fibrillation, and myocardial depression. Stop verapamil before giving I.V. dantrolene.

Vecuronium: May increase neuromuscular blockade effect. Use together cautiously.

Drug-lifestyle. Alcohol use: May increase CNS depression. Discourage use together.

Sun exposure: May cause photosensitivity reactions. Advise patient to avoid excessive sunlight exposure.

EFFECTS ON LAB TEST RESULTS

•May increase ALT, AST, alkaline phosphatase, LDH, bilirubin, and BUN levels.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated for spasms in rheumatic disorders and when spasticity is used to maintain motor function.

•Contraindicated in breast-feeding patients and patients with upper motor neuron disorders or active hepatic disease.

•Use cautiously in women, patients older than age 35, and patients with hepatic disease (such as cirrhosis or hepatitis) or severely impaired cardiac or pulmonary function.

NURSING CONSIDERATIONS

•Start therapy as soon as malignant hyperthermia reaction is recognized.

•Liver damage may occur with long-term use. If benefits don’t occur within 45 days, stop therapy.

•Obtain liver function test results at start of therapy.

•Alert: Watch for fever, jaundice, severe diarrhea, weakness, and sensitivity
reactions, including skin eruptions.Withhold dose and notify prescriber.

•Look alike-sound alike: Don’t confuse Dantrium with Daraprim.

PATIENT TEACHING

•Instruct patient to take drug with meals or milk in four divided doses.

•Tell patient to eat carefully to avoid choking. Some patients may have trouble swallowing during therapy.

•Warn patient to avoid driving and other hazardous activities until CNS effects of drug are known.

•Advise patient to avoid combining drug with alcohol or other CNS depressants.

•Advise patient to notify prescriber if skin or eyes turn yellow, skin itches, or fever develops.

•Tell patient to avoid photosensitivity reactions by using sunblock and wearing protective clothing, to report abdominal discomfort or GI problems immediately, and to follow prescriber’s orders regarding rest and physical therapy.

desipramine hydrochloride

dess-IP-ra-meen

Norpramin

Pharmacologic class: tricyclic antidepressant (TCA)

Pregnancy risk category NR

AVAILABLE FORMS

Tablets: 10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg

INDICATIONS & DOSAGES

Depression

Adults: 100 to 200 mg P.O. daily in divided doses; increase to maximum of 300 mg daily. Or, give entire dose at bedtime.

Adolescents and elderly patients: 25 to 100 mg P.O. daily in divided doses; increase gradually to maximum of 150 mg daily, if needed.

ADMINISTRATION

P.O.

•Give drug without regard for food.

ACTION

Unknown. Increases the amount of norepinephrine, serotonin, or both in the CNS by blocking their reuptake by the presynaptic neurons.

Route	Onset	Peak	Duration
P.O.	Unknown	4-6 hr	Unknown

Half-life: Unknown.

ADVERSE REACTIONS

CNS: drowsiness, dizziness, seizures, excitation, tremor, weakness, confusion, anxiety, restlessness, agitation, headache, nervousness, EEG changes, extrapyramidal reactions.

CV: tachycardia, orthostatic hypotension, ECG changes, hypertension.

EENT: blurred vision, tinnitus, mydriasis.

GI: dry mouth, constipation, nausea, vomiting, anorexia, paralytic ileus.

GU: urine retention.

Metabolic: hypoglycemia, hyperglycemia.

Skin: rash, urticaria, photosensitivity reactions, diaphoresis.

Other: sudden death in children, hypersensitivity reactions.

INTERACTIONS

Drug-drug. Barbiturates, CNS depressants: May enhance CNS depression. Avoid using together.

Cimetidine, fluoxetine, fluvoxamine, paroxetine, sertraline: May increase desipramine level. Monitor drug levels and patient for signs of toxicity.

Clonidine: May cause life-threatening blood pressure elevations. Avoid using together.

Epinephrine, norepinephrine: May increase hypertensive effect. Use together cautiously.

MAO inhibitors: May cause severe excitation, hyperpyrexia, or seizures, usually with high doses. Avoid using within 14 days of MAO inhibitor therapy.

Quinolones: May increase the risk of life-threatening arrhythmias. Avoid using together.

Drug-herb. Evening primrose oil: May cause additive or synergistic effect, resulting in lower seizure threshold and
increasing the risk of seizure. Discourage use together.

St. John’s wort, SAM-e, yohimbe: May cause serotonin syndrome. Discourage use together.

Drug-lifestyle. Alcohol use: May enhance CNS depression. Discourage use together.

Smoking: May lower drug level. Monitor patient for lack of effect.

Sun exposure: May increase risk of photosensitivity reactions. Advise patient to avoid excessive sunlight exposure.

EFFECTS ON LAB TEST RESULTS

• May increase or decrease glucose level.

• May increase liver function test values.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug and in those who have taken MAO inhibitors within previous 14 days.

•Contraindicated during acute recovery phase after MI.

•Use with extreme caution in patients with CV disease; in those with history of urine retention, glaucoma, seizure disorders, or thyroid disease; and in those taking thyroid drug.

NURSING CONSIDERATIONS

•Monitor patient for nausea, headache, and malaise after abrupt withdrawal of long-term therapy; these symptoms don’t indicate addiction.

•Don’t withdraw drug abruptly.

•Because patients may suffer hypertensive episodes during surgery, stop drug gradually several days before surgery.

•If signs or symptoms of psychosis occur or increase, notify prescriber. Record mood changes. Monitor patient for suicidal tendencies.

•Because drug produces fewer anticholinergic effects than other TCAs, it’s often prescribed for cardiac patients.

•Recommend sugarless hard candy or gum to relieve dry mouth. Saliva substitutes may be needed.

•Alert: Norpramin may contain tartrazine.

•Look alike-sound alike: Don’t confuse desipramine with disopyramide or imipramine.

PATIENT TEACHING

•Advise patient to take full dose at bedtime to avoid daytime sedation; if insomnia occurs, tell him to take drug in the morning.

•Warn patient to avoid hazardous activities that require alertness and good coordination until effects of drug are known. Drowsiness and dizziness usually subside after a few weeks.

•Advise patient to call prescriber if fever and sore throat occur. Blood counts may need to be obtained.

•Tell patient to avoid alcohol during therapy because it may antagonize effects of drug.

•Tell patient to consult prescriber before taking other prescription or OTC drugs.

•Warn patient not to stop drug suddenly.

•To prevent sensitivity to the sun, advise patient to use sunblock, wear protective clothing, and avoid prolonged exposure to strong sunlight.

dexmethylphenidate hydrochloride

decks-meth-ill-FEN-i-date

Focalin, Focalin XR

Pharmacologic class: methylphenidate derivative

Pregnancy risk category C

Controlled substance schedule II

AVAILABLE FORMS

Capsules (extended-release): 5 mg, 10 mg, 20 mg

Tablets: 2.5 mg, 5 mg, 10 mg

INDICATIONS & DOSAGES

Attention deficit hyperactivity disorder (ADHD)

immediate-release tablets

Adults and children age 6 and older: For patients who aren’t now taking methylphenidate, initially, 2.5 mg P.O. b.i.d., given at least 4 hours apart. Increase
weekly by 2.5 to 5 mg daily, up to a maximum of 20 mg daily in divided doses.

For patients who are now taking methylphenidate, initially give half the current methylphenidate dosage, up to a maximum of 20 mg P.O. daily in divided doses.

extended-release capsules

Adults: For patients who aren’t now taking dexmethylphenidate or methylphenidate, or who are on stimulants other than methylphenidate, give 10 mg P.O. once daily in the morning. May adjust in weekly increments of 10 mg to a maximum dose of 20 mg daily.

For patients who are now taking methylphenidate, initially give half the total daily dose of methylphenidate. Patients who are now taking the immediate-release form of dexmethylphenidate may be switched to the same daily dose of extended-release form. Maximum daily dose is 20 mg.

Children ages 6 and older: For patients who aren’t now taking dexmethylphenidate or methylphenidate, or who are on stimulants other than methylphenidate, give 5 mg P.O. once daily in the morning. May adjust in weekly increments of 5 mg to a maximum daily dose of 20 mg.

ADMINISTRATION

P.O.

•Capsules may be swallowed whole or the contents sprinkled on a small amount of applesauce and eaten immediately.

•Don’t crush or divide the capsule or its contents.

ACTION

Blocks presynaptic reuptake of norepinephrine and dopamine and increases their release, increasing concentration in the synapse.

Route	Onset	Peak	Duration
P.O. (immediate-release)	Unknown	1-1 ½ hr	Unknown
P.O. (extended-release)	Unknown	1-4 hr; 4 ½ -7 hr	Unknown

Half-life: 2 to 3 hours.

ADVERSE REACTIONS

CNS: headache, anxiety, feeling jittery, nervousness, insomnia, fever, dizziness.

CV: tachycardia.

EENT: throat pain.

GI: anorexia, abdominal pain, nausea, dyspepsia, dry mouth.

Musculoskeletal: twitching (motor or vocal tics).

Other: hypersensitivity reactions.

INTERACTIONS

Drug-drug. Antacids, acid suppressants: May alter the release of extended-release form. Avoid using together.

Anticoagulants, phenobarbital, phenytoin, primidone, tricyclic antidepressants: May inhibit metabolism of these drugs. May need to decrease dosage of these drugs; monitor drug levels.

Antihypertensives: May decrease effectiveness of these drugs. Use together cautiously; monitor blood pressure.

Clonidine, other centrally acting alpha agonists: May cause serious adverse effects. Use together cautiously.

MAO inhibitors: May increase risk of hypertensive crisis. Using together within 14 days of MAO inhibitor therapy is contraindicated.

EFFECTS ON LAB TEST RESULTS

None reported.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to methylphenidate or other components.

•Contraindicated in patients with severe anxiety, tension, or agitation; glaucoma; or motor tics or a family history or diagnosis of Tourette syndrome, or within 14 days of MAO inhibitor therapy.

•Use cautiously in patients with a psychiatric illness, bipolar disorder, depression, or family history of suicide; seizures, hypertension, hyperthyroidism, heart failure, recent MI, or a history of drug or alcohol abuse.

•Use in pregnant women only if the benefits outweigh the risks; drug may delay skeletal ossification, suppress weight gain, and impair organ development in the fetus.

•Use cautiously in breast-feeding women. It’s unknown if drug appears in breast milk.

•Don’t use in children or adolescents with structural cardiac abnormalities or other serious heart problems.

NURSING CONSIDERATIONS

•Diagnosis of ADHD must be based on complete history and evaluation of the patient by psychological and educational experts.

•Obtain a detailed patient history, including a family history for mental disorders, family suicide, ventricular arrhythmias, or sudden death.

•Refer patient for psychological, educational, and social support.

•Periodically reevaluate the long-term usefulness of the drug.

•Monitor CBC and differential and platelet counts during prolonged therapy.

•Don’t use for severe depression or normal fatigue states.

•Stop treatment or reduce dosage if symptoms worsen or adverse reactions occur.

•Long-term stimulant use may temporarily suppress growth. Monitor children for growth and weight gain. If growth slows or weight gain is lower than expected, stop drug.

•Routinely monitor blood pressure and pulse.

•Monitor patient for signs of drug dependence or abuse.

•If seizures occur, stop drug.

PATIENT TEACHING

•Stress the importance of taking the correct dose of drug at the same time every day. Report accidental overdose immediately.

•Alert: Warn patient the misuse of amphetamines can have serious effects including sudden death.

•Advise patients unable to swallow capsules to empty the contents of the capsule onto a spoonful of applesauce and eat immediately.

•Alert: Tell patient not to cut, crush, or chew the contents of the extended-release beaded capsule.

•Advise parents to monitor child for medication abuse or sharing. Also inform parents to watch for increased aggression or hostility and to report worsening behavior.

•Advise parents to monitor child’s height and weight and to tell the prescriber if they suspect growth is slowing.

•Caution patient to expect blurred vision or difficulty with accommodation and to exercise caution while performing activities that require a clear visual field. Advise patient to report blurred vision to the prescriber.

dextroamphetamine sulfate

dex-troe-am-FET-a-meen

Dexedrine^*, Dexedrine Spansule, Dextroam, DextroStat

Pharmacologic class: amphetamine

Pregnancy risk category C

Controlled substance schedule II

AVAILABLE FORMS

Capsules (extended-release): 5 mg, 10 mg, 15 mg

Tablets: 5 mg, 10mg

INDICATIONS & DOSAGES

Narcolepsy

Adults: 5 to 60 mg P.O. daily in divided doses.

Children ages 6 to 12: Give 5 mg P.O. daily. Increase by 5 mg at weekly intervals as needed.

Children age 12 and older: 10 mg P.O. daily. Increase by 10 mg at weekly intervals, as needed. Give first dose on awakening; additional doses (one or two) given at intervals of 4 to 6 hours.

Attention deficit hyperactivity disorder (ADHD)

Children age 6 and older: 5 mg P.O. once daily or b.i.d. Increase by 5 mg at weekly intervals, as needed. It’s rarely necessary to exceed 40 mg/day.

Children ages 3 to 5: Give 2.5 mg P.O. daily. Increase by 2.5 mg at weekly intervals, as needed.

Short-term adjunct in exogenous obesity ♦

Adults and children age 12 and older: 5 to 30 mg P.O. daily 30 to 60 minutes before meals in divided doses of 5 to 10 mg. Or, 10- or 15-mg extended-release capsule daily in themorning.

ADMINISTRATION

P.O.

•Give drug 30 to 60 minutes before meals if used for weight reduction and at least 6 hours before bedtime to avoid sleep interference.

•Certain formulations may contain tartrazine.

ACTION

Unknown. Probably promotes nerve impulse transmission by releasing stored dopamine and norepinephrine from nerve terminals in the brain. Main sites of activity appear to be the cerebral cortex and the reticular activating system.

Route	Onset	Peak	Duration
P.O.	30-60 min	2 hr	4 hr
P.O. (extended)	60 min	2 hr	8 hr

Half-life: 10 to 12 hours.

ADVERSE REACTIONS

CNS: insomnia, nervousness, restlessness, tremor, dizziness, headache, chills, overstimulation, dysphoria, euphoria.

CV: tachycardia, palpitations, arrhythmias, hypertension.

GI: dry mouth, taste perversion, diarrhea, constipation, anorexia, other GI disturbances.

GU: impotence.

Metabolic: weight loss.

Skin: urticaria.

Other: increased libido.

INTERACTIONS

Drug-drug. Acetazolamide, alkalizing drugs, antacids, sodium bicarbonate: May increase renal reabsorption. Monitor patient for enhanced amphetamine effects.

Acidifying drugs, ammonium chloride, ascorbic acid: May decrease level and increase renal clearance of dextroamphetamine. Monitor patient for decreased amphetamine effects.

Adrenergic blockers: May inhibit adrenergic blocking effects. Avoid using together.

Chlorpromazine: May inhibit central stimulant effects of amphetamines. May use to treat amphetamine poisoning.

Insulin, oral antidiabetics: May decrease antidiabetic requirements. Monitor glucose level.

MAO inhibitors: May cause severe hypertension or hypertensive crisis. Avoid using within 14 days of MAO inhibitor therapy.

Meperidine: May potentiate analgesic effect. Use together cautiously.

Methenamine: May increase urinary excretion of amphetamines and reduce effectiveness. Monitor drug effects.

Norepinephrine: May enhance adrenergic effect of norepinephrine. Monitor patient.

Phenobarbital, phenytoin: May delay absorption of these drugs. Monitor patient closely.

Drug-food. Caffeine: May increase amphetamine and related amine effects. Urge caution.

EFFECTS ON LAB TEST RESULTS

• May increase corticosteroid level.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to or with idiosyncratic reactions to sympathomimetic amines and in those with hyperthyroidism, moderate to severe hypertension, symptomatic CV disease, glaucoma, advanced arteriosclerosis, or history of drug abuse.

•Contraindicated as first-line treatment for obesity or within 14 days of MAO inhibitor therapy.

•Use cautiously in agitated patients and patients with motor tics, phonic tics, or Tourette syndrome. Also use cautiously in patients whose underlying condition may be worsened by an increase in blood
pressure or heart rate (preexisting hypertension, heart failure, recent MI); patients with a psychiatric illness, bipolar disorder, depression, or family history of suicide; those with a seizure disorder.

•Don’t use in children or adolescents with structural cardiac abnormalities or other serious heart problems.

NURSING CONSIDERATIONS

•Obtain a detailed patient history, including a family history for mental disorders, family suicide, ventricular arrhythmias, or sudden death.

•Drug shouldn’t be used to prevent fatigue.

•Obese patients should follow a weightreduction program.

•Drug has a high abuse potential and may cause dependence.

•Alert: Overdose may cause seizures.

•If tolerance to anorexigenic effect develops, stop drug and notify prescriber.

•Monitor for growth retardation in children.

•Look alike-sound alike: Don’t confuse Dexedrine with dextran or Excedrin.

PATIENT TEACHING

•Alert: Warn patient the misuse of amphetamines can cause serious CV adverse events including sudden death.

•Tell patient to take drug 30 to 60 minutes before meals if used for weight reduction and at least 6 hours before bedtime to avoid sleep interference.

•Warn patient to avoid activities that require alertness, a clear visual field, or good coordination until CNS effects of drug are known.

•Tell patient he may get tired as drug effects wear off.

•Ask patient to report signs and symptoms of excessive stimulation.

•Inform parents that children may show increased aggression or hostility and to report worsening of behavior.

•Advise patient to consume caffeinecontaining products cautiously.

•Warn patient with a seizure disorder that drug may decrease seizure threshold. Instruct him to notify prescriber if seizures occur.

SAFETY ALERT! diazepam

dye-AZ-e-pam

Diastat, Diazemuls†, Diazepam Intensol, Novo-Dipam†, Valium

Pharmacologic class: benzodiazepine

Pregnancy risk category D

Controlled substance schedule IV

AVAILABLE FORMS

Injection: 5 mg/ml

Oral solution: 5 mg/5 ml, 5 mg/ml

Rectal gel twin packs: 2.5 mg (pediatric), 5 mg (pediatric), 10 mg, 15 mg (adult), 20 mg (adult)

Tablets: 2 mg, 5 mg, 10 mg

INDICATIONS & DOSAGES

Anxiety

Adults: Depending on severity, 2 to 10 mg P.O. b.i.d. to q.i.d. Or, 2 to 10 mg I.M. or I.V. every 3 to 4 hours, as needed.

Children age 6 months and older: 1 to 2.5 mg P.O. t.i.d. or q.i.d., increase gradually, as needed and tolerated.

Elderly patients: Initially, 2 to 2.5 mg once daily or b.i.d.; increase gradually.

Acute alcohol withdrawal

Adults: 10 mg P.O. t.i.d. or q.i.d. first 24 hours; reduce to 5 mg P.O. t.i.d. or q.i.d., as needed. Or, initially, 10 mg I.V. or I.M. Then, 5 to 10 mg I.V. or I.M. every 3 to 4 hours, as needed.

Before endoscopic procedures

Adults: Adjust I.V. dose to desired sedative response (up to 20 mg). Or, 5 to 10 mg I.M. 30 minutes before procedure.

Muscle spasm

Adults: 2 to 10 mg P.O. b.i.d. to q.i.d. Or, 5 to 10 mg I.V. or I.M. initially; then 5 to 10 mg I.V. or I.M. every 3 to 4 hours, as needed. For tetanus, larger doses up to 20 mg every 2 to 8 hours may be needed.

Children age 5 and older: 5 to 10 mg I.V. or I.M. every 3 to 4 hours, as needed.

Children ages 1 month to 5 years: 1 to 2 mg I.V. or I.M. slowly; repeat every 3 to 4 hours, as needed.

Preoperative sedation

Adults: 10 mg I.M. (preferred) or I.V. before surgery.

Cardioversion

Adults: 5 to 15 mg I.V. within 5 to 10 minutes before procedure.

Adjunct treatment for seizure disorders

Adults: 2 to 10 mg P.O. b.i.d. to q.i.d.

Children age 6 months and older: 1 to 2.5 mg P.O. t.i.d. or q.i.d. initially; increase as needed and as tolerated.

Status epilepticus, severe recurrent seizures

Adults: 5 to 10 mg I.V. or I.M. initially. Use I.M. route only if I.V. access is unavailable. Repeat every 10 to 15 minutes, as needed, up to maximum dose of 30 mg. Repeat every 2 to 4 hours, if needed.

Children age 5 and older: 1 mg I.V. every 2 to 5 minutes up to maximum of 10 mg. Repeat every 2 to 4 hours, if needed.

Children ages 1 month to 5 years: 0.2 to 0.5 mg I.V. slowly every 2 to 5 minutes up to maximum of 5 mg. Repeat every 2 to 4 hours, if needed.

Patients on stable regimens of antiepileptic drugs who need diazepam intermittently to control bouts of increased seizure activity

Adults and children age 12 and older: 0.2 mg/kg P.R., rounding up to the nearest available dose form. A second dose may be given 4 to 12 hours later.

Children ages 6 to 11: 0.3 mg/kg P.R., rounding up to the nearest available dose form. A second dose may be given 4 to 12 hours later.

Children ages 2 to 5: 0.5 mg/kg P.R., rounding up to the nearest available dose form. A second dose may be given 4 to 12 hours later.

Adjust-a-dose: For elderly and debilitated patients, reduce dosage to decrease the likelihood of ataxia and oversedation.

ADMINISTRATION

P.O.

•When using oral solution, dilute dose just before giving.

I.V.

•I.V. route is the more reliable parenteral route; I.M. route isn’t recommended because absorption is variable and injection is painful.

•Keep emergency resuscitation equipment and oxygen at bedside.

•Avoid infusion sets or containers made from polyvinyl chloride.

•If possible, inject directly into a large vein. If not, inject slowly through infusion tubing as near to the insertion site as possible. Give at no more than 5 mg/minute. Watch closely for phlebitis at injection site.

•Monitor respirations every 5 to 15 minutes and before each dose.

•Don’t store parenteral solution in plastic syringes.

•Incompatibilities: All other I.V. drugs, most I.V. solutions.

I.M.

•Use the I.M. route if I.V. administration is impossible.

Rectal

•Use Diastat rectal gel to treat no more than five episodes per month and no more than one episode every 5 days because tolerance may develop.

•Alert: Only caregivers who can distinguish the distinct cluster of seizures or events from the patient’s ordinary seizure activity, who have been instructed and can give the treatment competently, who understand which seizures may be treated with Diastat, and who can monitor the clinical response and recognize when immediate professional medical evaluation is needed should give Diastat rectal gel.

ACTION

A benzodiazepine that probably potentiates the effects of GABA, depresses the CNS, and suppresses the spread of seizure activity.

Route	Onset	Peak	Duration
P.O.	30 min	2 hr	20-80 hr
I.V.	1-5 min	1-5 min	15-60 min
I.M.	Unknown	2 hr	Unknown
P.R.	Unknown	90 min	Unknown

Half-life: About 1 to 12 days.

ADVERSE REACTIONS

CNS: drowsiness, dysarthria, slurred speech, tremor, transient amnesia, fatigue, ataxia, headache, insomnia, paradoxical
anxiety, hallucinations, minor changes in EEG patterns, pain.

CV: CV collapse, bradycardia, hypotension.

EENT: diplopia, blurred vision, nystagmus.

GI: nausea, constipation, diarrhea with rectal form.

GU: incontinence, urine retention.

Hematologic: neutropenia.

Hepatic: jaundice.

Respiratory: respiratory depression, apnea.

Skin: rash, phlebitis at injection site.

Other: altered libido, physical or psychological dependence.

INTERACTIONS

Drug-drug. Cimetidine, disulfiram, fluoxetine, fluvoxamine, hormonal contraceptives, isoniazid, metoprolol, propoxyphene, propranolol, valproic acid: May decrease clearance of diazepam and increase risk of adverse effects. Monitor patient for excessive sedation and impaired psychomotor function.

CNS depressants: May increase CNS depression. Use together cautiously.

Digoxin: May increase digoxin level and risk of toxicity. Monitor patient and digoxin level closely.

Diltiazem: May increase CNS depression and prolong effects of diazepam. Reduce dose of diazepam.

Fluconazole, itraconazole, ketoconazole, miconazole: May increase and prolong diazepam level, CNS depression, and psychomotor impairment. Avoid using together.

Levodopa: May decrease levodopa effectiveness. Monitor patient.

Phenobarbital: May increase effects of both drugs. Use together cautiously.

Drug-herb. Kava: May increase sedation. Discourage use together.

Drug-lifestyle. Alcohol use: May cause additive CNS effects. Discourage use together.

Smoking: May decrease effectiveness of drug. Monitor patient closely.

EFFECTS ON LAB TEST RESULTS

• May increase liver function test values. May decrease neutrophil count.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug or soy protein; in patients experiencing shock, coma, or acute alcohol intoxication (parenteral form); in pregnant women, especially in first trimester; and in infants younger than age 6 months (oral form).

•Diastat rectal gel is contraindicated in patients with acute angle-closure glaucoma.

•Use cautiously in patients with liver or renal impairment, depression, or chronic open-angle glaucoma. Use cautiously in elderly and debilitated patients.

NURSING CONSIDERATIONS

•Monitor periodic hepatic, renal, and hematopoietic function studies in patients receiving repeated or prolonged therapy.

•Monitor elderly patients for dizziness, ataxia, mental status changes. Patients are at an increased risk for falls.

•Alert: Use of drug may lead to abuse and addiction. Don’t withdraw drug abruptly after long-term use; withdrawal symptoms may occur.

•Look alike-sound alike: Don’t confuse diazepam with diazoxide.

PATIENT TEACHING

•Warn patient to avoid activities that require alertness and good coordination until effects of drug are known.

•Tell patient to avoid alcohol while taking drug.

•Notify patient that smoking may decrease drug’s effectiveness.

•Warn patient not to abruptly stop drug because withdrawal symptoms may occur.

•Warn woman to avoid use during pregnancy.

•Instruct patient’s caregiver on the proper use of Diastat rectal gel.

diphenhydramine hydrochloride

dye-fen-HYE-drah-meen

Allerdryl † ◊, AllerMax ◊*, Aller-Max Caplets ◊, Allernix† ◊, Altaryl Children’s Allergy† ◊, Banophen ◊, Benadryl ◊, Benadryl Allergy ◊, Children’s Pedia Care Nightime Cough† ◊, Compoz ◊, Diphen Cough ◊, Diphenhist ◊, Diphenhist Captabs ◊, Dytan ◊, Genahist ◊, Hydramine Cough ◊*, Siladryl ◊*, Silphen ◊*, Sominex ◊, Triaminic MultiSymptom ◊*, Tusstat ◊*, Twilite Caplets ◊

Pharmacologic class: ethanolamine

Pregnancy risk category B

AVAILABLE FORMS

Capsules: 25 mg ◊, 50 mg ◊

Elixir: 12.5 mg/5 ml ◊*

Injection: 50 mg/ml

Strips (orally disintegrating): 12.5 mg ◊*, 25 mg ◊*

Syrup: 12.5 mg/5 ml ◊*

Tablets: 25 mg ◊, 50 mg ◊

Tablets (chewable): 12.5 mg ◊

INDICATIONS & DOSAGES

Rhinitis, allergy symptoms, motion sickness, Parkinson’s disease

Adults and children age 12 and older: 25 to 50 mg P.O. every 4 to 6 hours. Maximum, 300 mg P.O. daily. Or, 10 to 50 mg I.V. or deep I.M. Maximum I.V. or I.M. dosage, 400 mg daily.

Children ages 6 to 11: 12.5 to 25 mg P.O. every 4 to 6 hours. Maximum dose is 150 mg daily. Or, 5 mg/kg day divided into four doses P.O., deep I.M., or I.V. Maximum dose is 300 mg daily.

Children ages 2 to 5: 6.25 mg every 4 to 6 hours. Maximum dose is 37.5 mg daily. Or, 5 mg/kg day divided into four doses P.O., deep I.M., or I.V. Maximum dose is 300 mg daily.

Children weighing less than 9.1 kg (20 lb): 5 mg/kg day divided into four doses P.O., deep I.M., or I.V. Maximum dose is 300 mg daily.

Sedation

Adults: 25 to 50 mg P.O. or deep I.M. as needed.

Nighttime sleep aid

Adults: 25 to 50 mg P.O. at bedtime.

Nonproductive cough

Adults and children age 12 and older: 25 mg (syrup) P.O. every 4 hours. Don’t exceed 150 mg daily. Or, 25 to 50 mg (liquid) every 4 hours. Don’t exceed 300 mg daily.

Children ages 6 to 11: 12.5 mg (syrup) P.O. every 4 hours. Don’t exceed 75 mg daily. Or, 12.5 to 25 mg (liquid) every 4 hours. Don’t exceed 150 mg daily.

Children ages 2 to 5: 6.25 mg (syrup) P.O. every 4 hours. Don’t exceed 25 mg daily.

Antipsychotic-induced dystonia ♦

Adults: 50 mg I.M. or I.V.

ADMINISTRATION

P.O.

•Give drug with food or milk to reduce GI distress.

I.V.

•Don’t exceed 25 mg/minute.

•Incompatibilities: Allopurinol, amobarbital, amphotericin B, cefepime, dexamethasone, foscarnet, haloperidol lactate, pentobarbital, phenobarbital, phenytoin, thiopental.

I.M.

•Give I.M. injection deep into large muscle.

•Alternate injection sites to prevent irritation.

ACTION

Competes with histamine for H1-receptor sites. Prevents, but doesn’t reverse, histamine-mediated responses, particularly those of the bronchial tubes, GI tract, uterus, and blood vessels. Structurally related to local anesthetics, drug provides local anesthesia and suppresses cough reflex.

Route	Onset	Peak	Duration
P.O.	15 min	1-4 hr	6-8 hr
I.V.	Immediate	1-4 hr	6-8 hr
I.M.	Unknown	1-4 hr	6-8 hr

Half-life: 2.4 to 9.3 hours.

ADVERSE REACTIONS

CNS: drowsiness, sedation, sleepiness, dizziness, incoordination, seizures, confusion, insomnia, headache, vertigo, fatigue, restlessness, tremor, nervousness.

CV: palpitations, hypotension, tachycardia.

EENT: diplopia, blurred vision, nasal congestion, tinnitus.

GI: dry mouth, nausea, epigastric distress, vomiting, diarrhea, constipation, anorexia.

GU: dysuria, urine retention, urinary frequency.

Hematologic: thrombocytopenia, agranulocytosis, hemolytic anemia.

Respiratory: thickening of bronchial secretions.

Skin: urticaria, photosensitivity, rash.

Other: anaphylactic shock.

INTERACTIONS

Drug-drug. CNS depressants: May increase sedation. Use together cautiously.

MAO inhibitors: May increase anticholinergic effects. Avoid using together.

Other products that contain diphenhydramine (including topical therapy): May increase risk of adverse reactions. Avoid using together.

Drug-lifestyle. Alcohol use: May increase CNS depression. Discourage use together.

Sun exposure: May cause photosensitivity reactions. Advise patient to avoid extensive sunlight exposure.

EFFECTS ON LAB TEST RESULTS

• May decrease hemoglobin level and hematocrit.

• May decrease granulocyte and platelet counts.

• May prevent, reduce, or mask positive result in diagnostic skin test.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug; newborns; premature neonates; breast-feeding women; patients with angle-closure glaucoma, stenosing peptic ulcer, symptomatic prostatic hyperplasia, bladder neck obstruction, or pyloroduodenal obstruction; and those having an acute asthmatic attack.

•Avoid use in patients taking MAO inhibitors.

•Use with caution in patients with prostatic hyperplasia, asthma, COPD, increased intraocular pressure, hyperthyroidism, CV disease, and hypertension.

•Children younger than age 12 should use drug only as directed by prescriber.

NURSING CONSIDERATIONS

•Stop drug 4 days before diagnostic skin testing.

•Dizziness, excessive sedation, syncope, toxicity, paradoxical stimulation, and hypotension are more likely to occur in elderly patients.

•Look alike-sound alike: Don’t confuse diphenhydramine with dimenhydrinate; don’t confuse Benadryl with Bentyl or benazepril.

PATIENT TEACHING

•Warn patient not to take this drug with any other products that contain diphenhydramine (including topical therapy) because of increased adverse reactions.

•Instruct patient to take drug 30 minutes before travel to prevent motion sickness.

•Tell patient to take diphenhydramine with food or milk to reduce GI distress.

•Warn patient to avoid alcohol and hazardous activities that require alertness until CNS effects of drug are known.

•Inform patient that sugarless gum, hard candy, or ice chips may relieve dry mouth.

•Tell patient to notify prescriber if tolerance develops because a different antihistamine may need to be prescribed.

•Drug is in many OTC sleep and cold products. Advise patient to consult prescriber before using these products.

•Warn patient of possible photosensitivity reactions. Advise use of a sunblock.

disulfiram

dye-SUL-fi-ram

Antabuse

Pharmacologic class: aldehyde dehydrogenase inhibitor

Pregnancy risk category NR

AVAILABLE FORMS

Tablets: 250 mg, 500 mg

INDICATIONS & DOSAGES

Adjunct to management of alcohol abstinence

Adults: 250 to 500 mg P.O. as single dose in morning for 1 to 2 weeks or in evening if drowsiness occurs. Maintenance dosage is 125 to 500 mg P.O. daily (average 250 mg) until permanent self-control is established. Treatment may continue for months or years.

ADMINISTRATION

P.O.

•Never give until patient has abstained from alcohol for at least 12 hours. He should clearly understand consequences of drug and give permission for its use. Use drug only in patients who are cooperative, well motivated, and receiving supportive psychiatric therapy.

ACTION

Blocks oxidation of alcohol at the acetaldehyde stage. Excess acetaldehyde produces a highly unpleasant reaction in the presence of even small amounts of alcohol.

Route	Onset	Peak	Duration
P.O.	1-2 hr	Unknown	14 days

Half-life: Unknown.

ADVERSE REACTIONS

CNS: drowsiness, headache, fatigue, delirium, depression, neuritis, peripheral neuritis, polyneuritis, restlessness, psychotic reactions.

EENT: optic neuritis.

GI: metallic or garlicky aftertaste.

GU: impotence.

Skin: acneiform or allergic dermatitis, occasional eruptions.

Other: disulfiram reaction precipitated by alcohol use.

INTERACTIONS

Drug-drug. Barbiturates: May prolong duration of barbiturate effect. Closely monitor patient.

CNS depressants: May increase CNS depression. Use together cautiously.

Coumarin anticoagulants: May increase anticoagulant effect. Adjust dosage of anticoagulant.

Isoniazid: May cause ataxia or marked change in behavior. Avoid using together.

Metronidazole: May cause psychotic reaction. Avoid using together.

Midazolam: May increase midazolam level. Use together cautiously.

Paraldehyde: May cause toxic level of acetaldehyde. Avoid using together.

Phenytoin: May increase toxic effect of phenytoin. Monitor phenytoin level closely, and adjust dose as necessary.

Tricyclic antidepressants, especially amitriptyline: May cause transient delirium. Closely monitor patient.

Drug-herb. Herbal preparations containing alcohol: May cause disulfiram reaction.Warn patient against using together. Alcohol reaction may occur as long as 2 weeks after single drug dose.

Drug-food. Caffeine: May increase elimination half-life of caffeine. Tell patient to watch for effects.

Drug-lifestyle. Alcohol use: May cause disulfiram reaction including flushing, tachycardia, bronchospasm, sweating, nausea and vomiting, or death.Warn patient not to use products containing alcohol, including back rub preparations, cough syrups, liniments, and shaving lotion, or to drink alcoholic beverages.

EFFECTS ON LAB TEST RESULTS

• May increase cholesterol level.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug or other thiram derivatives used in pesticides and rubber vulcanization; in those with psychoses, myocardial disease, or coronary occlusion; in those
receiving metronidazole, paraldehyde, alcohol, or alcohol-containing products; and in those experiencing alcohol intoxication or who have ingested alcohol in preceding 12 hours.

•Don’t give drug during pregnancy.

•Use with caution in patients also receiving phenytoin therapy and in those with diabetes mellitus, hypothyroidism, seizure disorder, cerebral damage, nephritis, or hepatic cirrhosis or insufficiency.

NURSING CONSIDERATIONS

•Perform complete physical examination and laboratory studies, including CBC, SMA-12, and transaminase level, before therapy and repeat regularly.

•Disulfiram reaction may result from alcohol use, with flushing, throbbing headache, dyspnea, nausea, copious vomiting, diaphoresis, thirst, chest pain, palpitations, hyperventilation, hypotension, syncope, anxiety, weakness, blurred vision, confusion, and arthropathy.

•Alert: A severe disulfiram reaction can cause respiratory depression, CV collapse, arrhythmias, MI, acute heart failure, seizures, unconsciousness, and death.

•The longer the patient remains on the drug, the more sensitive he becomes to alcohol.

•Look alike-sound alike: Don’t confuse Antabuse with Anturane.

PATIENT TEACHING

•Alert: Caution patient’s family that drug should never be given to patient without his knowledge; severe reaction or death could result if patient drinks alcohol.

•Tell patient to carry medical identification that identifies him as a disulfiram user.

•Mild reactions may occur in sensitive patient with blood alcohol levels of 5 to 10 mg/dl; symptoms are fully developed at 50 mg/dl; unconsciousness typically occurs at 125 to 150 mg/dl level. Reaction may last from 30 minutes to several hours or as long as alcohol remains in blood.

•Reassure patient that drug-induced adverse reactions (unrelated to alcohol use), such as drowsiness, fatigue, impotence, headache, peripheral neuritis, and metallic or garlic taste, subside after about 2 weeks of therapy.

•Advise patient not to drink alcoholic beverages or use products containing alcohol, including topical preparations and mouthwash.

•Have patient verify content of OTC products with pharmacist before use.

donepezil hydrochloride

doe-NEP-ah-zill

Aricept, Aricept ODT

Pharmacologic class: cholinesterase inhibitor

Pregnancy risk category C

AVAILABLE FORMS

Orally disintegrating tablets (ODTs): 5 mg, 10 mg

Tablets: 5 mg, 10mg

INDICATIONS & DOSAGES

Mild to severe Alzheimer dementia

Adults: Initially, 5 mg P.O. daily at bedtime. After 4 to 6 weeks, increase to 10 mg daily, if needed.

ADMINISTRATION

P.O.

•Allow ODT to dissolve on tongue; then follow with water.

•Give drug at bedtime, without regard for food.

ACTION

Thought to increase acetylcholine level by inhibiting cholinesterase enzyme, which causes acetylcholine hydrolysis.

Route	Onset	Peak	Duration
P.O.	Unknown	3-4 hr	Unknown

Half-life: 70 hours.

ADVERSE REACTIONS

CNS: headache, insomnia, seizures, dizziness, fatigue, depression, abnormal dreams, somnolence, tremor, irritability, paresthesia, aggression, vertigo, ataxia,
restlessness, abnormal crying, nervousness, aphasia, syncope, pain.

CV: chest pain, hypertension, vasodilation, atrial fibrillation, hot flashes, hypotension.

EENT: cataract, blurred vision, eye irritation, sore throat.

GI: nausea, diarrhea, vomiting, anorexia, fecal incontinence, GI bleeding, bloating, epigastric pain.

GU: urinary frequency.

Metabolic: weight loss, dehydration.

Musculoskeletal: muscle cramps, arthritis, bone fracture.

Respiratory: dyspnea, bronchitis.

Skin: pruritus, urticaria, diaphoresis, ecchymoses.

Other: toothache, influenza, increased libido.

INTERACTIONS

Drug-drug. Anticholinergics: May decrease donepezil effects. Avoid using together.

Anticholinesterases, cholinomimetics: May have synergistic effect. Monitor patient closely.

Bethanechol, succinylcholine: May have additive effects. Monitor patient closely.

Carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampin: May increase rate of donepezil elimination. Monitor patient.

EFFECTS ON LAB TEST RESULTS

None reported.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug or piperidine derivatives and in breast-feeding women.

•Use cautiously in pregnant women and in patients who take NSAIDs or have CV disease, asthma, obstructive pulmonary disease, urinary outflow impairment, or history of ulcer disease.

NURSING CONSIDERATIONS

•Monitor patient for evidence of active or occult GI bleeding.

•Look alike-sound alike: Don’t confuse Aricept with Ascriptin.

PATIENT TEACHING

•Stress that drug doesn’t alter underlying degenerative disease but can temporarily stabilize or relieve symptoms. Effectiveness depends on taking drug at regular intervals.

•Tell caregiver to give drug just before patient’s bedtime.

•ODTs may be taken with or without food. Have patient allow tablet to dissolve on his tongue, then swallow with a sip of water.

•Advise patient and caregiver to report immediately significant adverse effects or changes in overall health status and to inform health care team that patient is taking drug before he receives anesthesia.

•Tell patient to avoid OTC cold or sleep remedies because of risk of increased anticholinergic effects.

doxapram hydrochloride

DOCKS-a-pram

Dopram

Pharmacologic class: analeptic

Pregnancy risk category B

AVAILABLE FORMS

Injection: 20 mg/ml (benzyl alcohol 0.9%)

INDICATIONS & DOSAGES

Postanesthesia respiratory stimulation

Adults: 0.5 to 1 mg/kg as a single I.V. injection (not to exceed 1.5 mg/kg) or as multiple injections every 5 minutes, total not to exceed 2 mg/kg. Or, 250 mg in 250 ml of normal saline solution or D₅W infused at initial rate of 5 mg/minute I.V. until satisfactory response is achieved. Maintain at 1 to 3 mg/minute. Don’t exceed total dose for infusion of 4 mg/kg.

Drug-induced CNS depression

Adults: For injection, priming dose of 2 mg/kg I.V., repeated in 5 minutes and again every 1 to 2 hours until patient awakens (and if relapse occurs). Maximum daily dose is 3 g.

For infusion, priming dose of 2 mg/kg I.V., repeated in 5 minutes and again in 1 to 2 hours, if needed. If response occurs, give I.V. infusion (1 mg/ml) at 1 to 3 mg/minute until patient awakens. Don’t infuse for longer than 2 hours or give more than 3 g/day. May resume I.V. infusion after rest period of 30 minutes to 2 hours, if needed.

Chronic pulmonary disease related to acute hypercapnia

Adults: 1 to 2 mg/minute by I.V. infusion using 2 mg/ml solution. Maximum, 3 mg/minute for up to 2 hours.

ADMINISTRATION

I.V.

•Drug is compatible with D₅W, D₁₀W, and normal saline solution.

•Give slowly; rapid infusion may cause hemolysis.

•Watch for irritation and infiltration; it can cause tissue damage and necrosis.

•Incompatibilities: Aminophylline, ascorbic acid, cefoperazone, cefotaxime, cefuroxime sodium, dexamethasone sodium phosphate, diazepam, digoxin, dobutamine, folic acid, furosemide, hydrocortisone sodium phosphate, hydrocortisone sodium succinate, ketamine, methylprednisolone sodium succinate, minocycline, sodium bicarbonate, thiopental, ticarcillin disodium.

ACTION

Not clearly defined. Directly stimulates the central respiratory centers in the medulla and may indirectly act on carotid, aortic, or other peripheral chemoreceptors.

Route	Onset	Peak	Duration
I.V.	20-40 sec	1-2 min	5-12 min

Half-life: 2 ½ to 4 hours.

ADVERSE REACTIONS

CNS: headache, dizziness, seizures, apprehension, disorientation, hyperactivity, bilateral Babinski’s signs, paresthesia.

CV: chest pain and tightness, variations in heart rate, hypertension, arrhythmias, T-wave depression on ECG, flushing.

EENT: laryngospasm, sneezing.

GI: nausea, vomiting, diarrhea.

GU: urine retention, bladder stimulation with incontinence, albuminuria.

Musculoskeletal: muscle spasms.

Respiratory: bronchospasm, cough, dyspnea, rebound hypoventilation, hiccups.

Skin: pruritus, diaphoresis.

INTERACTIONS

Drug-drug. General anesthetics: May cause self-limiting arrhythmias. Avoid using doxapram within 10 minutes of an anesthetic that sensitizes the myocardium to catecholamines.

MAO inhibitors, sympathomimetics: May increase adverse CV effects. Use together cautiously.

EFFECTS ON LAB TEST RESULTS

• May increase BUN level. May decrease hemoglobin level and hematocrit.

• May decrease erythrocyte, RBC, and WBC counts.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients with seizure disorders; head injury; CV disorders; frank, uncompensated heart failure; severe hypertension; stroke; respiratory failure or incompetence secondary to neuromuscular disorders, muscle paresis, flail chest, obstructed airway, pulmonary embolism, pneumothorax, restrictive respiratory disease, acute bronchial asthma, or extreme dyspnea; or hypoxia unrelated to hypercapnia.

•Use cautiously in patients with bronchial asthma, severe tachycardia or arrhythmias, cerebral edema, increased intracranial pressure, hyperthyroidism, pheochromocytoma, or metabolic disorders.

NURSING CONSIDERATIONS

•Drug is used only in surgical or emergency department situations.

•Separate end of anesthetic treatment and start of this drug by at least 10 minutes.

•Alert: Establish an adequate airway before giving drug. Prevent patient from aspirating vomitus by placing him on his side.

•Monitor blood pressure, heart rate, deep tendon reflexes, and arterial blood gases
before giving drug and every 30 minutes afterward.

•Monitor patient for evidence of overdose, such as hypertension, tachycardia, arrhythmias, skeletal muscle hyperactivity, and dyspnea. Hold drug and notify prescriber if patient needs mechanical ventilation or shows signs of increased arterial carbon dioxide or oxygen tension.

•Look alike-sound alike: Don’t confuse doxapram with doxorubicin, doxepin, or doxazosin.

PATIENT TEACHING

•Inform family and patient about need for drug.

•Answer patient’s questions and address his concerns.

doxepin hydrochloride

DOKS-eh-pin

Sinequan

Pharmacologic class: tricyclic antidepressant (TCA)

Pregnancy risk category C

AVAILABLE FORMS

Capsules: 10 mg, 25 mg, 50mg, 75 mg, 100 mg, 150 mg

Oral concentrate: 10 mg/ml

INDICATIONS & DOSAGES

Depression; anxiety

Adults: Initially, 75 mg P.O. daily. Usual dosage range is 75 to 150 mg daily to maximum of 300 mg daily in divided doses. Or, entire maintenance dose may be given once daily with maximum dose of 150 mg.

ADMINISTRATION

P.O.

•Dilute oral concentrate with 4 ounces (120 ml) of water, milk, or juice (orange, grapefruit, tomato, prune, or pineapple, but not grape); don’t mix preparation with carbonated beverages.

•Give at bedtime, if possible, because it may cause drowsiness and dizziness.

ACTION

Unknown. Increases amount of norepinephrine, serotonin, or both in the CNS by blocking their reuptake by the presynaptic neurons.

Route	Onset	Peak	Duration
P.O.	Unknown	2 hr	Unknown

Half-life: 6 to 8 hours.

ADVERSE REACTIONS

CNS: drowsiness, dizziness, seizures, confusion, numbness, hallucinations, paresthesia, ataxia, weakness, headache, extrapyramidal reactions.

CV: orthostatic hypotension, tachycardia, ECG changes.

EENT: blurred vision, tinnitus.

GI: dry mouth, constipation, nausea, vomiting, anorexia.

GU: urine retention.

Metabolic: hypoglycemia, hyperglycemia.

Skin: diaphoresis, rash, urticaria, photosensitivity reactions.

Other: hypersensitivity reactions.

INTERACTIONS

Drug-drug. Barbiturates, CNS depressants: May enhance CNS depression. Avoid using together.

Cimetidine, fluoxetine, fluvoxamine, paroxetine, sertraline: May increase doxepin level. Monitor drug levels and patient for signs of toxicity.

Clonidine: May cause life-threatening hypertension. Avoid using together.

Epinephrine, norepinephrine: May increase hypertensive effect. Use together cautiously.

MAO inhibitors: May cause severe excitation, hyperpyrexia, or seizures, usually with high dosage. Avoid using within 14 days of MAO inhibitor therapy.

Quinolones: May increase the risk of lifethreatening arrhythmias. Avoid using together.

Drug-herb. Evening primrose oil: May cause additive or synergistic effect, resulting in lower seizure threshold and increasing the risk of seizure. Discourage use together.

St. John’s wort, SAM-e, yohimbe: May cause serotonin syndrome. Discourage use together.

Drug-lifestyle. Alcohol use: May enhance CNS depression. Discourage use together.

Sun exposure: May increase risk of photosensitivity reactions. Advise patient to avoid excessive sunlight exposure.

EFFECTS ON LAB TEST RESULTS

• May increase or decrease glucose level.

• May increase liver function test values.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug and in those with glaucoma or tendency toward urine retention; also contraindicated in those who have received an MAO inhibitor within past 14 days and during acute recovery phase of an MI.

NURSING CONSIDERATIONS

•Don’t withdraw drug abruptly.

•Monitor patient for nausea, headache, and malaise after abrupt withdrawal of long-term therapy; these symptoms don’t indicate addiction.

•Alert: Because hypertensive episodes may occur during surgery in patients receiving drug, stop it gradually several days before surgery.

•If signs or symptoms of psychosis occur or increase, expect prescriber to reduce dosage. Record mood changes. Monitor patient for suicidal tendencies and allow only a minimum supply of drug.

•Drug has strong anticholinergic effects and is one of the most sedating TCAs. Adverse anticholinergic effects can occur rapidly.

•Recommend use of sugarless hard candy or gum to relieve dry mouth.

•Look alike-sound alike: Don’t confuse doxepin with doxazosin, digoxin, doxapram, or Doxidan; don’t confuse Sinequan with saquinavir.

PATIENT TEACHING

•Tell patient to dilute oral concentrate with 4 ounces (120 ml) of water, milk, or juice (orange, grapefruit, tomato, prune, or pineapple, but not grape); preparation shouldn’t be mixed with carbonated beverages.

•Tell patient to take full dose at bedtime whenever he can, but warn him of possible morning dizziness on standing up quickly.

•Advise patient to consult prescriber before taking other prescription or OTC drugs.

•Warn patient to avoid hazardous activities that require alertness and good psychomotor coordination until effects of drug are known. Drowsiness and dizziness usually subside after a few weeks.

•Tell patient to avoid alcohol during drug therapy.

•Tell patient that maximal effect may not be evident for 2 to 3 weeks.

•Warn patient not to stop drug suddenly.

•To prevent sensitivity to the sun, advise patient to use sunblock, wear protective clothing, and avoid prolonged exposure to strong sunlight.

duloxetine hydrochloride

do-LOCKS-ah-teen

Cymbalta

Pharmacologic class: SSNRI

Pregnancy risk category C

AVAILABLE FORMS

Capsules (delayed-release): 20mg, 30 mg, 60 mg

INDICATIONS & DOSAGES

Major depressive disorder

Adults: Initially, 20 mg P.O. b.i.d.; then, 60 mg P.O. once daily or divided in two equal doses. Maximum, 60 mg daily.

NEW INDICATION: Generalized anxiety disorder

Adults: 60 mg P.O. daily. Or, 30 mg P.O. daily for 1 week; then increase to 60 mg P.O. daily.

Neuropathic pain related to diabetic peripheral neuropathy

Adults: 60 mg P.O. once daily.

Adjust-a-dose: In patients with impaired renal function, reduce starting dose and increase gradually.

ADMINISTRATION

P.O.

•Give drug whole; don’t crush or open capsule.

ACTION

May inhibit serotonin and norepinephrine reuptake in the CNS.

Route	Onset	Peak	Duration
P.O.	Unknown	6 hr	Unknown

Half-life: 12 hours.

ADVERSE REACTIONS

CNS: dizziness, fatigue, headache, insomnia, somnolence, suicidal thoughts, fever, hypoesthesia, initial insomnia, irritability, lethargy, nervousness, nightmares, restlessness, sleep disorder, anxiety, asthenia, tremor.

CV: hot flushes, hypertension, increased heart rate.

EENT: blurred vision, nasopharyngitis, pharyngolaryngeal pain.

GI: constipation, diarrhea, dry mouth, nausea, dyspepsia, gastritis, vomiting.

GU: abnormal orgasm, abnormally increased frequency of urinating, delayed or dysfunctional ejaculation, dysuria, erectile dysfunction, urinary hesitation.

Metabolic: decreased appetite, hypoglycemia, increased appetite, weight gain or loss.

Musculoskeletal: muscle cramps, myalgia.

Respiratory: cough.

Skin: increased sweating, night sweats, pruritus, rash.

Other: decreased libido, rigors.

INTERACTIONS

Drug-drug. Antiarrhythmics of type 1C ( flecainide, propafenone), phenothiazines: May increase levels of these drugs. Use together cautiously.

CNS drugs: May increase adverse effects. Use together cautiously.

CYP1A2 inhibitors (cimetidine, fluvoxamine, certain quinolones): May increase duloxetine level. Avoid using together.

CYP2D6 inhibitors ( fluoxetine, paroxetine, quinidine): May increase duloxetine level. Use together cautiously.

Drugs that reduce gastric acidity: May cause premature breakdown of duloxetine’s protective coating and early release of the drug. Monitor patient for effects.

MAO inhibitors: May cause hyperthermia, rigidity, myoclonus, autonomic instability, rapid fluctuations of vital signs, agitation, delirium, and coma. Avoid use within 2 weeks after MAO inhibitor therapy; wait at least 5 days after stopping duloxetine before starting MAO inhibitor.

Thioridazine: May prolong the QT interval and increase risk of serious ventricular arrhythmias and sudden death. Avoid using together.

Tricyclic antidepressants (amitriptyline, nortriptyline, imipramine): May increase levels of these drugs. Reduce tricyclic antidepressant dose, and monitor drug levels closely.

Triptans: May cause serotonin syndrome (restlessness, hallucinations, loss of coordination, fast heartbeat, rapid changes in blood pressure, increased body temperature, hyperreflexia, nausea, vomiting, and diarrhea). Use cautiously and with increased monitoring, especially when starting or increasing dosages.

Drug-lifestyle. Alcohol use: May increase risk of liver damage. Discourage use together.

EFFECTS ON LAB TEST RESULTS

• May increase alkaline phosphatase, ALT, AST, bilirubin, and CK levels.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients hypersensitive to drug or its ingredients, patients taking MAO inhibitors, patients with uncontrolled angle-closure glaucoma, and patients with a creatinine clearance less than 30 ml/minute. Drug isn’t recommended for patients with hepatic dysfunction or end-stage renal disease.

•Use cautiously in patients with a history of mania or seizures, patients who drink substantial amounts of alcohol, patients
with hypertension, patients with controlled angle-closure glaucoma, and those with conditions that slow gastric emptying.

NURSING CONSIDERATIONS

•Monitor patient for worsening of depression or suicidal behavior, especially when therapy starts or dosage changes.

•Treatment of overdose is symptomatic. Don’t induce emesis; gastric lavage or activated charcoal may be performed soon after ingestion or if patient is still symptomatic. Because drug undergoes extensive distribution, forced diuresis, dialysis, hemoperfusion, and exchange transfusion aren’t useful. Contact a poison control center for information.

•If taken with tricyclic antidepressants, duloxetine metabolism will be prolonged, and patient will need extended monitoring.

•Periodically reassess patient to determine the need for continued therapy.

•Decrease dosage gradually, and watch for symptoms that may arise when drug is stopped, such as dizziness, nausea, headache, paresthesia, vomiting, irritability, and nightmares.

•If intolerable symptoms arise when decreasing or stopping drug, restart at previous dose and decrease even more gradually.

•Monitor blood pressure periodically during treatment.

•Use during the third trimester of pregnancy may cause neonatal complications including respiratory distress, cyanosis, apnea, seizures, vomiting, hypoglycemia, and hyperreflexia, which may require prolonged hospitalization, respiratory support, and tube feeding. Consider potential bene-fit of drug to the mother versus risks to the fetus.

•Older patients may be more sensitive to drug effects than younger adults.

PATIENT TEACHING

•Alert: Warn families or caregivers to report signs of worsening depression (such as agitation, irritability, insomnia, hostility, impulsivity) and signs of suicidal behavior to prescriber immediately.

•Tell patient to consult his prescriber or pharmacist if he plans to take other prescription or OTC drugs or an herbal or other dietary supplement.

•Instruct patient to swallow capsules whole and not to chew, crush, or open them because they have an enteric coating.

•Urge patient to avoid activities that are hazardous or require mental alertness until he knows how the drug affects him.

•Warn against drinking alcohol during therapy.

•If patient takes drug for depression, explain that it may take 1 to 4 weeks to notice an effect.

escitalopram oxalate

ess-si-TAL-oh-pram

Lexapro

Pharmacologic class: SSRI

Pregnancy risk category C

AVAILABLE FORMS

Oral solution: 5 mg/5 ml

Tablets: 5 mg, 10 mg, 20 mg

INDICATIONS & DOSAGES

Treatment and maintenance therapy for patients with major depressive disorder; general anxiety disorder

Adults: Initially, 10 mg P.O. once daily, increasing to 20 mg if needed after at least 1 week.

Adjust-a-dose: For elderly patients and those with hepatic impairment, 10 mg P.O. daily, initially and as maintenance dosages.

ADMINISTRATION

P.O.

•Give drug without regard for food.

ACTION

Action may be linked to increase of serotonergic activity in the CNS from inhibition of neuronal reuptake of serotonin. Drug is closely related to citalopram, which may be the active component.

Route	Onset	Peak	Duration
P.O.	Unknown	5 hr	Unknown

Half-life: 27 to 32 hours.

ADVERSE REACTIONS

CNS: suicidal behavior, fever, insomnia, dizziness, somnolence, paresthesia, lightheadedness, migraine, tremor, vertigo, abnormal dreams, irritability, impaired concentration, fatigue, lethargy.

CV: palpitations, hypertension, flushing, chest pain.

EENT: rhinitis, sinusitis, blurred vision, tinnitus, earache.

GI: nausea, diarrhea, constipation, indigestion, abdominal pain, vomiting, increased or decreased appetite, dry mouth, flatulence, heartburn, cramps, gastroesophageal reflux.

GU: ejaculation disorder, impotence, anorgasmia, menstrual cramps, UTI, urinary frequency.

Metabolic: weight gain or loss.

Musculoskeletal: arthralgia, myalgia, muscle cramps, pain in arms or legs.

Respiratory: bronchitis, cough.

Skin: rash, increased sweating.

Other: decreased libido, yawning, flulike symptoms.

INTERACTIONS

Drug-drug. Aspirin, NSAIDs, other drugs known to affect coagulation: May increase the risk of bleeding. Use together cautiously.

Carbamazepine: May increase escitalopram clearance. Monitor patient for expected antidepressant effect and adjust dose as needed.

Cimetidine: May increase escitalopram level. Monitor patient for increased adverse reactions to escitalopram.

Citalopram: May cause additive effects. Using together is contraindicated.

CNS drugs: May cause additive effects. Use together cautiously.

Desipramine, other drugs metabolized by CYP2D6: May increase levels of these drugs. Use together cautiously.

Lithium: May enhance serotonergic effect of escitalopram. Use together cautiously, and monitor lithium level.

MAO inhibitors: May cause fatal serotonin syndrome. Avoid using within 14 days of MAO inhibitor therapy.

Triptans: May increase serotonergic effects, leading to weakness, hyperreflexia, incoordination, rapid changes in blood pressure, nausea, and diarrhea. Use together cautiously, especially at the start of therapy or at dosage increases.

Tramadol: May cause serotonin syndrome. Monitor patient closely.

Drug-lifestyle. Alcohol use: May increase CNS effects. Discourage use together.

EFFECTS ON LAB TEST RESULTS

None reported.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in patients taking pimozide, MAO inhibitors, or within 14 days of MAO inhibitor therapy and in those hypersensitive to escitalopram, citalopram, or any of its inactive ingredients.

•Use cautiously in patients with a history of mania, seizure disorders, suicidal thoughts, or renal or hepatic impairment.

•Use cautiously in patients with diseases that produce altered metabolism or hemodynamic responses.

•Use with caution in elderly patients because they may have greater sensitivity to drug.

•Use in third trimester of pregnancy may cause complications at birth. Consider the risk versus benefit of treatment during this time.

•Drug appears in breast milk. Patient should either stop breast-feeding or stop taking drug.

NURSING CONSIDERATIONS

•Closely monitor patients at high risk of suicide.

•Look alike-sound alike: Don’t confuse escitalopram with estazolam.

•Evaluate patient for history of drug abuse and observe for signs of misuse or abuse.

•Periodically reassess patient to determine need for maintenance treatment and appropriate dosing.

•Alert: Combining triptans with an SSRI or an SSNRI may cause serotonin syndrome. Signs and symptoms may include restlessness, hallucinations, loss of coordination, fast heart beat, rapid changes in blood pressure, increased body temperature, overactive reflexes, nausea, vomiting, and diarrhea. Serotonin syndrome may be more likely to occur when starting or increasing the dose of triptan, SSRI, or SSNRI.

PATIENT TEACHING

•Inform patient that symptoms should improve gradually over several weeks, rather than immediately.

•Tell patient that although improvement may occur within 1 to 4 weeks, he should continue drug as prescribed.

•Alert: Caution patient and patient’s family to report signs of worsening depression (such as agitation, irritability, insomnia, hostility, impulsivity) and signs of suicidal behavior to prescriber immediately.

•Tell patient to use caution while driving or operating hazardous machinery because of drug’s potential to impair judgment, thinking, and motor skills.

•Advise patient to consult health care provider before taking other prescription or OTC drugs.

•Tell patient that drug may be taken in the morning or evening without regard to meals.

•Encourage patient to avoid alcohol while taking drug.

•Tell woman to notify health care provider if she’s pregnant or breast-feeding.

esterified estrogens

ESS-tehr-eh-fide ESS-troe-jenz

Menest, Neo-Estrone

Pharmacologic class: estrogen

Pregnancy risk category X

AVAILABLE FORMS

Tablets: 0.3 mg, 0.625 mg, 1.25 mg, 2.5 mg

Tablets ( film-coated): 0.3 mg, 0.625 mg, 1.25 mg, 2.5 mg

INDICATIONS & DOSAGES

Inoperable prostate cancer

Men: 1.25 to 2.5 mg P.O. t.i.d.

Palliative treatment for metastatic breast cancer

Men and postmenopausal women: 10 mg P.O. t.i.d. for 3 or more months.

Hypogonadism

Women: 2.5 to 7.5 mg daily in divided doses in cycles of 20 days on, 10 days off.

Castration, primary ovarian failure

Women: 1.25 mg daily in cycles of 3 weeks on, 1 week off. Adjust for symptoms. Can be given continuously.

Vasomotor menopausal symptoms

Women: 1.25 mg P.O. daily in cycles of 3 weeks on, 1 week off. Dosage may be increased to 2.5 to 3.75 mg P.O. daily, if needed.

Atrophic vaginitis, atrophic urethritis

Women: 0.3 to 1.25 mg or more P.O. daily in cycles of 3 weeks on, 1 week off.

ADMINISTRATION

P.O.

•Use lowest effective dose needed for specific indication.

ACTION

Increases synthesis of DNA, RNA, and protein in responsive tissues; reduces release of follicle-stimulating and luteinizing hormones from pituitary gland.

Route	Onset	Peak	Duration
P.O.	Unknown	Unknown	Unknown

Half-life: Unknown.

ADVERSE REACTIONS

CNS: headache, dizziness, chorea, depression, stroke, seizures.

CV: thrombophlebitis, thromboembolism, hypertension, edema, pulmonary embolism, MI.

EENT: worsening myopia or astigmatism, intolerance of contact lenses.

GI: nausea, vomiting, abdominal cramps, bloating, anorexia, increased appetite, pancreatitis, increased risk of gallbladder disease.

GU: breakthrough bleeding, altered menstrual flow, dysmenorrhea, amenorrhea, increased risk of endometrial cancer, cervical erosion, altered cervical secretions, enlargement of uterine fibromas, vaginal candidiasis, testicular atrophy, impotence.

Hepatic: cholestatic jaundice, hepatic adenoma.

Metabolic: hypercalcemia, weight changes.

Skin: melasma, rash, hirsutism or hair loss, erythema nodosum, dermatitis.

Other: breast tenderness, enlargement, or secretion, gynecomastia, increased risk of breast cancer.

INTERACTIONS

Drug-drug. Carbamazepine, fosphenytoin, phenobarbital, phenytoin, rifampin: May decrease effectiveness of estrogen therapy. Monitor patient closely.

Corticosteroids: May enhance effects. Monitor patient closely.

Cyclosporine: May increase risk of toxicity. Use together with caution, and monitor cyclosporine level frequently.

Dantrolene, hepatotoxic drugs: May increase risk of hepatotoxicity. Monitor liver function closely.

Oral anticoagulants: May decrease anticoagulant effects. Adjust dosage if needed. Monitor PT and INR.

Tamoxifen: May interfere with tamoxifen effectiveness. Avoid using together.

Drug-herb. St. John’s wort: May decrease effects of drug. Discourage use together.

Drug-food. Caffeine: May increase caffeine level. Urge caution.

Grapefruit, grapefruit juice: May increase risk of adverse effects. Discourage use together.

Drug-lifestyle. Smoking: May increase risk of CV effects. If smoking continues, may need another form of therapy.

EFFECTS ON LAB TEST RESULTS

• May increase calcium, thyroid-binding globulin, serum triglyceride, serum phospholipid, and clotting factor VII, VIII, IX, and X levels.

• May increase norepinephrine-induced platelet aggregation and PT.

• May reduce metyrapone test results and cause impaired glucose tolerance.

CONTRAINDICATIONS & CAUTIONS

•Contraindicated in pregnant women, in patients hypersensitive to drug, and in patients with breast cancer (except metastatic disease), estrogen-dependent neoplasia, active thrombophlebitis, thromboembolic disorders, undiagnosed abnormal genital bleeding, or history of thromboembolic disease.

•Use cautiously in patients with history of hypertension, mental depression, cardiac or renal dysfunction, liver impairment, bone disease, migraine, seizures, or diabetes.

NURSING CONSIDERATIONS

•When used for vasomotor symptoms in menstruating women, cyclic administration is started on day 5 of bleeding.

•Make sure patient has thorough physical examination before starting estrogen therapy. Patients receiving long-term therapy should have annual examinations. Periodically monitor body weight, blood pressure, lipid levels, and hepatic function.

•Notify pathologist about patient’s estrogen therapy when sending specimens to laboratory for evaluation.

•Because of risk of thromboembolism, stop therapy at least 1 month before procedures that cause prolonged immobilization or increased risk of thromboembolism, such as knee or hip surgery.

•Glucose tolerance may be impaired. Monitor glucose level closely in patients with diabetes.

PATIENT TEACHING

•Tell patient to read package insert describing estrogen’s adverse effects; also, give patient verbal explanation.

•Emphasize importance of regular physical examinations. Postmenopausal women who use estrogen replacement for longer than 5 years to treat menopausal symptoms may be at increased risk for endometrial cancer. This risk is reduced by using cyclic rather than continuous therapy and the lowest possible estrogen dosage. Adding progestins to the regimen decreases risk of endometrial hyperplasia, but it’s unknown whether progestins affect risk of endometrial cancer.

•Alert: Warn patient to immediately report abdominal pain; pain, numbness, or stiffness in legs or buttocks; pressure or pain in chest or shortness of breath; severe headaches; visual disturbances, such as blind spots, flashing lights, or blurriness; vaginal bleeding or discharge; breast lumps; swelling of hands or feet; yellow skin or sclera; dark urine; or light-colored stools.

•Tell diabetic patient to report elevated glucose level so that antidiabetic dosage can be adjusted.

•Explain to woman receiving cyclic therapy for postmenopausal symptoms that she may experience withdrawal bleeding during week off drug. Tell her to report unusual vaginal bleeding.

•Teach woman to perform routine breast self-examination.

•Advise woman of childbearing age to consult prescriber before taking drug and to advise prescriber immediately if she becomes pregnant.

•Teach patient methods to decrease risk of blood clots.

•Encourage patient to stop smoking or reduce number of cigarettes smoked because of the risk of CV complications.

estradiol (oestradiol)

ess-tra-DYE-ole

Alora, Climara, Esclim, Estrace, Estrace Vaginal Cream, Estraderm, Estring Vaginal Ring, FemPatch, Femtrace, Femring, Gynodiol, Menostar, Vivelle, Vivelle-Dot

estradiol cypionate

Depo-Estradiol

estradiol gel

Divigel, Elestrin, EstroGel

estradiol hemihydrate

Estrasorb, Vagifem

estradiol valerate (oestradiol valerate)

Delestrogen

Pharmacologic class: estrogen

Pregnancy risk category X

AVAILABLE FORMS

estradiol

Tablets: 0.45 mg, 0.9 mg, 1.8 mg

Tablets (micronized): 0.5 mg, 1 mg, 1.5 mg, 2 mg

Transdermal: 0.014 mg/24 hours, 0.025 mg/24 hours, 0.0375 mg/24 hours, 0.05 mg/24 hours, 0.06 mg/24 hours, 0.075 mg/24 hours, 0.1 mg/24 hours

Vaginal cream (in nonliquefying base): 0.1 mg/g

Vaginal ring: 0.0075 mg/24 hours; 0.05 mg/24 hours; 0.1 mg/24 hours

estradiol cypionate

Injection (in oil): 5 mg/ml

estradiol gel

Transdermal gel: 0.06% (1.25 g/metered dose), 0.1% (in 0.25-, 0.5-, and 1-g single-dose packets)

estradiol hemihydrate

Topical emulsion: 0.25%

Vaginal tablets: 25 mcg

estradiol valerate

Injection (in oil): 10 mg/ml, 20 mg/ml, 40 mg/ml

INDICATIONS & DOSAGES

Vasomotor menopausal symptoms, female hypogonadism, female castration, primary ovarian failure

Women: 0.5 to 2 mg P.O. estradiol daily in cycles of 21 days on and 7 days off or cycles of 5 days on and 2 days off. Or, for vasomotor symptoms, 1 to 5 mg cypionate I.M. once every 3 to 4 weeks; for female hypogonadism, 1.5 to 2 mg cypionate I.M. once every month.

Transdermal patch

Women: 0.025 mg/24 hours Esclim, 0.05 mg/24 hours Estraderm, 0.0375 mg/24 hours or 0.05 mg/24 hours twice weekly Vivelle, 0.05 mg/24 hours Climara, or 0.025 mg/24 hours FemPatch once weekly. Apply to clean, dry area of the trunk. Adjust dose, if necessary, after the first 2 or 3 weeks of therapy; then every 3 to 6 months as needed. Rotate application sites weekly with an interval of at least 1 week between particular sites used. Adjust dosage as needed.

Postmenopausal urogenital symptoms

Women: One ring inserted into the upper third of the vagina. Ring is kept in place for 3 months.

Atrophic vaginitis, kraurosis vulvae

Women: 0.05 mg/24 hours Estraderm applied twice weekly in a cyclic regimen. Or, 0.05 mg/24 hours Climara applied weekly in a cyclic regimen. Or, 2 to 4 g vaginal applications of cream daily for 1 to 2 weeks. When vaginal mucosa is restored, maintenance dose is 1 g one to three times weekly in a cyclic regimen. If using Vagifem for atrophic vaginitis, give 1 tablet vaginally once daily for 2 weeks. Maintenance dose is 1 tablet inserted vaginally twice weekly. Or, 10 to 20 mg valerate I.M. every 4 weeks as needed. Or, 1 to 5 mg estradiol cypionate I.M. once every 3 to 4 weeks.

Moderate to severe vasomotor symptoms, as well as vulval and vaginal atrophy associated with menopause

Women: 1.25 g EstroGel applied once daily to skin in a thin layer from wrist to shoulder of one upper extremity.

Palliative treatment of advanced, inoperable breast cancer

Men and postmenopausal women: 10 mg P.O. estradiol t.i.d. for 3 months.

Palliative treatment of advanced, inoperable prostate cancer

Men: 30 mg valerate I.M. every 1 to 2 weeks, or 1 to 2 mg P.O. estradiol t.i.d.

To prevent postmenopausal osteoporosis

Women: Place a 6.5-cm² (0.025 mg/24 hours) Climara patch once weekly on clean, dry skin of lower abdomen or upper quadrant of buttock. Or, place a 3.25-cm² (0.014 mg/24 hours) Menostar patch once weekly to clean, dry area of the lower abdomen. For each system, press firmly in place for about 10 seconds; ensure complete contact, especially around edges. Or, 0.025-mg/24 hours Vivelle, Vivelle-Dot, or Alora system applied to a clean, dry area of the trunk twice weekly. Or, 0.5 mg P.O. daily for 21 days, followed by 7 days without drug.

Moderate to severe vasomotor symptoms from menopause

Women: Apply contents of two 1.74-g foil pouches (total 3.48 g) of Estrasorb daily. Or, Divigel 0.1% at dose of 0.25, 0.5, or 1 g/day. Start with Divigel 0.25 g daily and adjust dose based on individual patient response.

ADMINISTRATION

P.O.

•Give drug without regard for food. If stomach upset occurs, give with food.

•Don’t give drug with grapefruit juice.

•Store at controlled room temperature.

I.M.

•To give I.M. injection, make sure drug is well dispersed by rolling vial between palms. Inject deep into large muscle. Rotate injection sites to prevent muscle atrophy. Never give drug I.V.

Transdermal

•Open each pouch of Estrasorb individually and use contents of one pouch for each leg. Rub emulsion into thigh and calf for 3 minutes until thoroughly absorbed; rub emulsion remaining on hands onto the buttocks. Allow areas to dry before covering with clothing.Wash hands with soap and water to remove excess drug.

•Apply Divigel once daily on skin of either right or left upper thigh. Application surface area should be about 5 by 7 inches (about the size of two palm prints). Apply entire contents of a unit dose packet each day. To avoid potential skin irritation, apply Divigel to right or left upper thigh on alternating days. Don’t apply Divigel on face, breasts, or irritated skin, or in or around the vagina. After application, allow gel to dry before dressing. Don’t wash application site within 1 hour after applying Divigel. Avoid contact of gel with eyes.Wash hands after application.

•Apply transdermal patch to clean, dry, hairless, intact skin on abdomen or buttock. Don’t apply to breasts, waistline, or other areas where clothing can loosen patch. When applying, ensure thorough contact between patch and skin, especially around edges, and hold in place for about 10 seconds. Apply patch immediately after opening and removing protective cover. Rotate application sites.

Vaginal

•Using the applicator, insert Vagifem as far into vagina as it can comfortably go, without using force.

ACTION

Increases synthesis of DNA, RNA, and protein in responsive tissues; reduces release of follicle-stimulating and luteinizing hormones from the pituitary gland.

Route	Onset	Peak	Duration
P.O., I.M., vaginal	Unknown	Unknown	Unknown
Transdermal (Esclim)	Unknown	27-30 hr	Unknown
Transdermal (Estrasorb)	Immediate	Unknown	Unknown
Transdermal gel (EstroGel)	Immediate	1 hr	24-36 hr