ANTIPSYCHOTICS

GENERIC NAME: aripiprazole

BRAND NAME: Abilify DRUG CLASS AND MECHANISM: Aripiprazole is an anti-psychotic drug for treating psychoses. Like other anti-psychotic drugs, the mechanism of action of aripiprazole is unknown. Moreover, like other anti-psychotics, it blocks several receptors on the nerves of the brain for several neurotransmitters (chemicals that nerves use to communicate with each other). It is thought that its beneficial effect is due to its effects on dopamine and serotonin receptors. Its effects on these receptors are complex, involving stimulation of the receptors but to a lesser degree than the naturally-occurring neurotransmitters (a process called partial agonism). The FDA approved aripiprazole in November 2002. PRESCRIPTION: Yes. GENERIC AVAILABLE: No. PREPARATIONS: Tablets: 10, 15, 20, and 30 mg. Oral solution: 1 mg/mL STORAGE: Tablets should be stored at room temperature, 15-30 C (59-86 F). PRESCRIBED FOR: Aripiprazole is used to treat schizophrenia, bipolar mania and mixed manic/depressive episodes (as sole or adjunctive therapy) and as adjunctive (add-on) therapy for major depressive disorder. DOSING: Aripiprazole usually is taken once a day. The usual starting dose is 10 or 15 mg once daily. The dose may be increased over time to achieve the desired effect. Aripiprazole can be taken with or without food. DRUG INTERACTIONS: Carbamazepine (Tegretol) can markedly decrease the amount of aripiprazole in the body by increasing the rate at which the body's enzymes (particularly the liver enzyme, CYP3A4) degrade it. The manufacturer recommends that patients on aripiprazole who are started on carbamazepine double their dose of aripiprazole, under their doctor's supervision. Other drugs that can promote the activity of CYP3A4 and decrease the body's levels of aripiprazole are phenytoin (Dilantin), rifampin (Rifadin, Rimactane, Rifadin, Rifater, Rifamate), and phenobarbital. Ketoconazole (Nizoral) can increase the amount of aripiprazole in the body by blocking CYP3A4. The manufacturer of aripiprazole recommends reducing the dose of aripiprazole by one-half during ketoconazole therapy. Many other drugs also are known to block CYP3A4 and potentially could increase the levels of aripiprazole, but their actual effects on aripiprazole levels have not been studied. Such drugs include: itraconazole (Sporanox), fluconazole (Diflucan),

voriconazole (Vfend), cimetidine (Tagamet), verapamil (Calan, Isoptin), diltiazem (Cardizem, Dilacor), erythromycin, clarithromycin (Biaxin), nefazodone (Serzone), ritonavir (Norvir), saquinavir (Invirase), nelfinavir (Viracept), indinavir (Crixivan), and grapefruit juice. room temperature, 15-25 C (59-77 F). PRESCRIBED FOR: Risperidone is used to treat schizophrenia, bipolar mania [as a sole therapy or combination therapy with lithium (Eskalith, Lithobid) or valproate (Depakene, Depacon) and for the treatment of irritability associated with autistic disorder in children and adolescents. Clinical studies involving small numbers of patients have shown some benefit in using risperidone for stuttering and Tourette syndrome (non FDA-approved uses). Another nonFDA approved use of risperidone is for obsessive-compulsive disorders. DOSING: Risperidone can be administered once or twice daily. Initial dosing is generally 2 mg/day. Dose increases can occur in increments of 1-2 mg/day, as tolerated, to a recommended dose of 4-8 mg/day. In children, risperidone should be initiated at 0.5 mg once daily, and can be increased in increments of 0.5 or 1 mg/day, as tolerated, to a recommended dose of 2.5 mg/day. Risperidone can be given with or without meals. The recommended dose of Risperdal Consta is 25 mg injected into the deltoid or gluteal muscle every two weeks. Patients who have never received risperidone are started on oral risperidone in order to evaluate tolerability. Patients then may be transitioned to Risperdal Consta if oral risperidone is tolerated DRUG INTERACTIONS: Risperidone may interfere with elimination by the kidneys of clozapine (Clozaril), a different type of antipsychotic medication, causing increased levels of clozapine in the blood. This could increase the risk of side effects with clozapine. Serotonin reuptake inhibitors such as paroxetine (Paxil), Sertraline (Zoloft), and fluoxetine (Prozac) when taken with risperidone causes the metabolism (breakdown) of risperidone by the liver to be inhibited, which in turn causes elevated blood levels of risperidone, and may increase the risk of adverse reactions.

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1 2 3 Next risperidone Index Glossary risperidone on RxList

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ANTIDEPRESSANTS SSRIS

Generic Name: fluoxetine hydrochloride Brand Name: Apo-Fluoxetine (CAN), Co-Fluoxetine (CAN), Novo-Fluoxetine (CAN), PMSFluoxetine (CAN), Prozac, Prozac Pulvules, Prozac Weekly, ratio-Fluoxetine (CAN), Sarafem Other Info: Pregnancy Category C Drug class: Antidepressant, SSRI

Indications
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Treatment of depression; most effective in patients with major depressive disorder Treatment of OCD Treatment of bulimia Treatment of PMDD (Sarafem) Treatment of panic disorder with or without agoraphobia Unlabeled use: Treatment of obesity, alcoholism, numerous psychiatric disorders, chronic pain, various neuropathies

Contraindications and cautions

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Contraindicated with hypersensitivity to fluoxetine, pregnancy. Use cautiously with impaired hepatic or renal function, diabetes mellitus, lactation, seizures; history of suicide attempts.

Available forms
Tablets10, 20 mg; capsules10, 20, 40 mg; liquid20 mg/5 mL; DR capsules90 mg

Dosages
Individualize dosage; same for oral or IV routes because of rapid and almost complete absorption.

ADULTS
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Antidepressant: The full antidepressant effect may not be seen for up to 4 6 wk. Initially, 20 mg/day PO in the morning. If no clinical improvement is seen, increase dose after several weeks. Administer doses > 20 mg/day on a bid schedule. Do not exceed 80 mg/day. Once stabilized, may switch to 90-mg DR capsules once a week. OCD: Initially, 20 mg/day PO. If no clinical improvement is seen, increase dose after several weeks. Usual dosage range, 20 60 mg/day PO; may require up to 5 wk for effectiveness. Do not exceed 80 mg/day. Bulimia: 60 mg/day PO in the morning. PMDD (Sarafem): 20 mg/day PO or 20 mg/day PO starting 14 days before the anticipated beginning of menses and continuing through the first full day of menses, then no drug until 14 days before next menses; do not exceed 80 mg/day. Panic disorder (Prozac): 10 mg/day PO for the first week; increase to 20 mg/day if needed. Maximum dose, 60 mg/day.

PEDIATRIC PATIENTS 818 YR

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Major depressive disorder: 10 mg/day PO; may be increased to 20 mg/day after several weeks.

PEDIATRIC PATIENTS 717 YR

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OCD: Initially, 10 mg/day PO. After 2 wk increase to 20 mg/day. Suggested range, 20 60 mg/day PO.

PEDIATRIC PATIENTS < 7 YR

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Safety and efficacy not established.

GERIATRIC PATIENTS OR PATIENTS WITH HEPATIC OR RENAL IMPAIRMENT Give a lower or less frequent dose. Monitor response to guide dosage. Pharmacokinetics
Route Oral Onset Slow Peak 6 8 hr

Metabolism: Hepatic; T1/2: 9 days Distribution: Crosses placenta; enters breast milk Excretion: Feces, urine

Adverse effects
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CNS: Headache, nervousness, insomnia, drowsiness, anxiety, tremor, dizziness, light-headedness, agitation, sedation, abnormal gait, seizures CV: Hot flashes, palpitations Dermatologic: Sweating, rash, pruritus, acne, alopecia, contact dermatitis GI: Nausea, vomiting, diarrhea, dry mouth, anorexia, dyspepsia, constipation, taste changes, flatulence, gastroenteritis, dysphagia, gingivitis GU: Painful menstruation, sexual dysfunction, frequency, cystitis, impotence, urgency, vaginitis Respiratory: URIs, pharyngitis, cough, dyspnea, bronchitis, rhinitis Other: weight changes, asthenia, fever

Interactions
Drug-drug
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WARNING: Possible fatal reactions with MAOIs; do not administer together; 2-wk washout period needed. Increased therapeutic and toxic effects of TCAs Do not use with thioridazine (increased levels of thioridazine) Decreased effectiveness if taken while smoking Increased toxicity of lithium; avoid this combination Additive CNS effects if combined with benzodiazepines, alcohol; avoid these combinations Avoid administration with other serotonergic drugs; may lead to serotonin syndrome

Drug-alternative therapy
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Increased risk of severe reaction if combined with St. John s wort therapy

Nursing considerations
CLINICAL ALERT! Name confusion and Serophene (clomiphene); use caution. Assessment
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has

occurred

between Sarafem

(fluoxetine)

History: Hypersensitivity to fluoxetine, impaired hepatic or renal function, diabetes mellitus, lactation, pregnancy, seizures Physical: Weight, T; skin rash, lesions; reflexes, affect; bowel sounds, liver evaluation; P, peripheral perfusion; urinary output, LFTs, renal function tests

Interventions
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Arrange for lower or less frequent doses in elderly patients and patients with hepatic or renal impairment.

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BLACK BOX WARNING: Establish suicide precautions for severely depressed patients. Limit quantity of capsules dispensed; high risk in children and adolescents. Administer drug in the morning. Monitor patient for response to therapy for up to 4 wk before increasing dose. Switch to once a week therapy by starting weekly dose 7 days after last 20 mg/day dose. If response is not satisfactory, reconsider daily dosing.

Teaching points
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It may take up to 4 weeks before the full effect occurs. Take in the morning. If you feel sleepy or tired, you may take it at night. If you are taking the once-weekly capsule, mark calendar with reminders of drug day. Do not take this drug during pregnancy. If you think that you are pregnant or wish to become pregnant, consult your health care provider. Keep this drug, and all medications, out of the reach of children. You may experience these side effects: Dizziness, drowsiness, nervousness, insomnia (avoid driving or performing hazardous tasks); nausea, vomiting, weight loss (eat small frequent meals; monitor your weight loss); sexual dysfunction; flulike symptoms. Report rash, mania, seizures, severe weight loss.

TCA Generic Name: amitriptyline hydrochloride Brand Names: Endep (CAN), Tryptanol (CAN) Pregnancy Category D Drug class: TCA; tertiary amine

Therapeutic actions of Amitriptyline

Mechanism of action unknown; TCAs inhibit the reuptake neurotransmitters norepinephrine and serotonin, leading to an increase effects; anticholinergicat CNS and peripheral receptors; sedative. of in the their

Indications of Amitriptyline
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Relief of symptoms of depression (endogenous most responsive); sedative effects may help when depression is associated with anxiety and sleep disturbance. Unlabeled uses: Control of chronic pain (eg, intractable pain of cancer, central pain syndromes, peripheral neuropathies, postherpetic neuralgia, ticdouloureux); prevention of onset of cluster and migraine headaches; treatment of pathologic weeping and laughing secondary to forebrain disease (due to MS), insomnia.

Contraindications and cautions of Amitriptyline

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Contraindicated with hypersensitivity to any tricyclic drug; concomitant therapy with an MAOI; recent MI; myelography within previous 24 hr or scheduled within 48 hr; lactation. Use cautiously with electroshock therapy; preexisting CV disorders (severe coronary heart disease, progressive CHF, angina pectoris, paroxysmal tachycardia); angle-closure glaucoma, increased IOP, urinary retention, ureteral or urethral spasm; seizure disorders; hyperthyroidism; impaired hepatic, renal function; psychiatric patients (schizophrenic or paranoid patients may exhibit a worsening of psychosis with TCA therapy); manic-depressive patients; elective surgery (discontinue as long as possible before surgery).

Available forms of Amitriptyline

Injection10 mg/mL; tablets10, 25, 50, 75, 100, 150 mg

Dosages of Amitriptyline
May be given IM if patients are unable or unwilling to take oral drug. Switch to oral drug as soon as possible. ADULTS
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Depression, hospitalized patients: Initially, 100 mg/day PO in divided doses: gradually increase to 200 300 mg/day as required. May be given IM 20 30 mg qid, initially only in patients unable or unwilling to take drug PO. Replace with oral medication as soon as possible. Depression, outpatients: Initially, 75 mg/day PO, in divided doses; may increase to 150 mg/day. Increases should be made in late afternoon or at bedtime. Total daily dosage may be administered at bedtime. Initiate single daily dose therapy with 50 100 mg at bedtime; increase by 25 50 mg as necessary to a total of 150 mg/day. Maintenance dose is 40 100 mg/day, which may be given as a single bedtime dose. After satisfactory response, reduce to lowest effective dosage. Continue therapy for 3 mo or longer to lessen possibility of relapse. Chronic pain: 75 150 mg/day PO. Prevention of cluster or migraine headaches: 50 150 mg/day PO. Prevention of weeping in MS patients with forebrain disease: 25 75 mg PO.

PEDIATRIC PATIENTS > 12 YR 10 mg tid PO and then 20 mg at bedtime. PEDIATRIC PATIENTS < 12 YR Not recommended. GERIATRIC PATIENTS 10 mg tid PO with 20 mg at bedtime.

Pharmacokinetics
Route Oral Onset Varies Peak 2 4 hr Duration 2 4 wk

Metabolism: Hepatic; T1/2: 1050 hr Distribution: Crosses placenta; enters breast milk Excretion: Urine

Adverse effects of Amitriptyline

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CNS: Disturbed concentration, sedation and anticholinergic (atropine-like) effects, confusion (especially in elderly), hallucinations, disorientation, decreased memory, feelings of unreality, delusions, anxiety, nervousness, restlessness, agitation, panic, insomnia, nightmares, hypomania, mania, exacerbation of psychosis, drowsiness, weakness, fatigue, headache, numbness, tingling, paresthesias of extremities, incoordination, motor hyperactivity, akathisia, ataxia, tremors, peripheral neuropathy, extrapyramidal symptoms, seizures, speech blockage, dysarthria, tinnitus, altered EEG CV: Orthostatic hypotension, hypertension, syncope, tachycardia, palpitations, MI, arrhythmias, heart block, precipitation of CHF, CVA Endocrine: Elevated or depressed blood sugar, elevated prolactin levels, inappropriate ADH secretion GI: Dry mouth, constipation, paralytic ileus, nausea, vomiting, anorexia, epigastric distress, diarrhea, flatulence, dysphagia, peculiar taste, increased salivation, stomatitis, glossitis, parotid swelling, abdominal cramps, black tongue, hepatitis, jaundice (rare), elevated transaminase, altered alkalinephosphatase GU: Urinary retention, delayed micturition, dilation of the urinary tract, gynecomastia, testicular swelling; breast enlargement, menstrual irregularity andgalactorrhea; increased or decreased libido; impotence Hematologic: Bone marrow depression, including agranulocytosis; eosinophilia, purpura, thrombocytopenia, leukopenia Hypersensitivity: Rash, pruritus, vasculitis, petechiae, photosensitization, edema (generalized, face, tongue), drug fever Withdrawal: Symptoms on abrupt discontinuation of prolonged therapy: Nausea, headache, vertigo, nightmares, malaise Other: Nasal congestion, excessive appetite, weight change; sweating, alopecia, lacrimation, hyperthermia, flushing, chills

Interactions of Amitriptyline
Drug-drug

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Increased TCA levels and pharmacologic (especially anticholinergic) effects with cimetidine, fluoxetine Increased TCA levels with methylphenidate, phenothiazines, hormonal contraceptives, disulfiram Hyperpyretic crises, severe seizures, hypertensive episodes and deaths with MAOIs, furazolidone Increased antidepressant response and cardiac arrhythmias with thyroid medication Increased or decreased effects with estrogens Delirium with disulfiram Sympathetic hyperactivity, sinus tachycardia, hypertension, agitation with levodopa Increased biotransformation of TCAs in patients who smoke cigarettes Increased sympathomimetic (especially beta-adrenergic) effects of directacting sympathomimetic drugs (norepinephrine, epinephrine) Increased anticholinergic effects of anticholinergic drugs (including anticholinergic antiparkisonians) Increased response (especially CNS depression) to barbiturates Decreased antihypertensive effect of guanethidine, clonidine, other antihypertensives Decreased effects of indirect-acting sympathomimetic drugs (ephedrine)

Nursing considerations of Amitriptyline

Assessment
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History: Hypersensitivity to any tricyclic drug; concomitant therapy with an MAOI; recent MI; myelography within previous 24 hr or scheduled within 48 hr; lactation; EST; preexisting CV disorders; angle-closure glaucoma, increased IOP, urinary retention, ureteral or urethral spasm; seizure disorders; hyperthyroidism; impaired hepatic, renal function; psychiatric patients; manic-depressive patients; elective surgery Physical: Weight; T; skin color, lesions; orientation, affect, reflexes, vision and hearing; P, BP, orthostatic BP, perfusion; bowel sounds, normal output, liver evaluation; urine flow, normal output; usual sexual function, frequency of menses, breast and scrotal examination; LFTs, urinalysis, CBC, ECG

Interventions
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Restrict drug access for depressed and potentially suicidal patients. Give IM only when oral therapy is impossible. Do not administer IV. Administer major portion of dose at bedtime if drowsiness, severe anticholinergic effects occur (note that the elderly may not tolerate single-daily-dose therapy). Reduce dosage if minor side effects develop; discontinue if serious side effects occur. Arrange for CBC if patient develops fever, sore throat, or other sign of infection.

Teaching points
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Take drug exactly as prescribed; do not stop abruptly or without consulting health care provider. Avoid using alcohol, other sleep-inducing drugs, over-the-counter drugs.

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Avoid prolonged exposure to sunlight or sunlamps; use a sunscreen or protective garments. You may experience these side effects: Headache, dizziness, drowsiness, weakness, blurred vision (reversible; if severe, avoid driving and tasks requiring alertness while these persist); nausea, vomiting, loss of appetite, dry mouth (eat frequent small meals; use frequent mouth care and suck on sugarless candies); nightmares, inability to concentrate, confusion; changes in sexual function. Report dry mouth, difficulty in urination, excessive sedation during amitriptyline therapy.

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