Classifications: psychotherapeutic agent; antipsychotic, atypical; Therapeutic: atypical antipsychotic
Pregnancy Category: B
25 mg, 50 mg, 100 mg tablets and 12.5 mg, 25 mg, 50 mg, 100 mg orally disintegrating tablets
Interferes with binding of dopamine to D1 and D2 receptors in the limbic region of brain. It binds primarily to nondopaminergic sites (e.g., alpha-adrenergic, serotonergic,
and cholinergic receptors).
Limited to treatment of schizophrenia uncontrolled by other agents.
Management of severely ill schizophrenic patients who have failed to respond to other neuroleptic agents.
Schizo-affective disorder, severe obsessive-compulsive disorder, bipolar disorder, dementia-related behavioral disorders.
Severe CNS depression, blood dyscrasia, history of bone marrow depression; patients with myeloproliferative disorders, uncontrolled
epilepsy; clozapine-induced agranulocytosis, severe granulocytosis, chemotherapy, coma, leukemia, leukopenia, neutropenia,
myocarditis, concurrent administration of benzodiazepines or other psychotropic drugs; renal failure, dialysis, hepatitis,
jaundice; infants, lactation.
Arrhythmias, GI disorders, narrow-angle glaucoma, hepatic and renal impairment, prostatic hypertrophy, history of seizures;
patients with cardiovascular and/or pulmonary disease; cerebrovascular disease, cardiac arrhythmias, tachycardia, dehydration,
neurological disease, tardive dyskinesia, previous history of agranulocytosis; surgery, glaucoma, infection, pregnancy (category
B); older adults. Safety and efficacy in children <9 y have not been established.
Route & Dosage
Adult (>16 y): PO Initiate at 12.5 mg q.d. or b.i.d. then increase by 2550 mg/d and titrate to a target dose of 350450 mg/d in
3 divided doses, further increases (not more than twice weekly) can be made if necessary, max of 900 mg/d
- Drug is usually withdrawn gradually over 12 wk if therapy must be discontinued.
- Store the drug away from heat or light.
Adverse Effects (≥1%) CV:
Orthostatic hypotension, tachycardia,
ECG changes, increased risk of myocarditis especially during first month of therapy, pericarditis, pericardial effusion,
cardiomyopathy, heart failure, MI, mitral insufficiency. GI:
Nausea, dry mouth, constipation
, hypersalivation. Hematologic: Agranulocytosis. CNS:
Seizures, transient fever,
sedation, neuroleptic malignant syndrome (rare),
dystonic reactions (rare). Metabolic:
Urinary retention. Other: Increased mortality from severe hematologic, cardiovascular, and respiratory adverse effects.
and other cns depressants
compound depressant effects; anticholinergic agents
potentiate anticholinergic effects; antihypertensive agents
may potentiate hypotension. Herbal: St. John's wort
may increase sedation.
Readily absorbed from GI tract. Onset:
24 wk. Peak:
2.5 h. Distribution:
Possibly distributed into breast milk. Metabolism:
In liver. Elimination:
50% in urine, 30% in feces. Half-Life:
Assessment & Drug Effects
- Lab tests: Baseline WBC and absolute neutrophil count must be made before initial treatment, every week for first 6 mo,
then every 2 wk for next 6 mo, then every 4 wk, and weekly for 4 wk after the drug is discontinued. Periodically monitor
- Monitor diabetics for loss of glycemic control.
- Monitor for seizure activity; seizure potential increases at the higher dose level.
- Closely monitor for recurrence of psychotic symptoms if the drug is being discontinued.
- Monitor cardiovascular and respiratory status, especially during the first month of therapy. Report promptly S&S of CHF and
other potential cardiac problems.
- Monitor for development of tachycardia or hypotension, which may pose a serious risk for patients with compromised cardiovascular
- Monitor daily temperature and report fever. Transient elevation above 38° C (100.4° F), with peak incidence during
first 3 wk of drug therapy, may occur.
Patient & Family Education
- Carefully monitor blood glucose levels if diabetic.
- Do not engage in any hazardous activity until response to the drug is known. Drowsiness and sedation are common adverse
- Due to the risk of agranulocytosis (see Appendix F) it is important to comply with blood test regimen. Report flulike symptoms,
fever, sore throat, lethargy, malaise, or other signs of infection.
- Rise slowly to avoid orthostatic hypotension.
- Report immediately any of the following: unexplained fatigue, especially with activity; shortness of breath, sudden weight
gain or edema of the lower extremities.
- Take drug exactly as ordered.
- Do not use OTC drugs or alcohol without permission of physician.