Clozapine(kloe’ za peen)
Apo-Clozapine (CAN), Clozaril, FazaClo, Gen-Clozapine (CAN)
PREGNANCY CATEGORY B
Drug Classes
Antipsychotic
Dopaminergic blocker
Therapeutic Actions
Mechanism not fully understood: Blocks dopamine receptors in the brain, depresses the RAS; anticholinergic, antihistaminic (H1), and alpha-adrenergic blocking activity may contribute to some of its therapeutic (and adverse) actions. Clozapine produces fewer extrapyramidal effects than other antipsychotics.
Indications
Management of severely ill schizophrenics who are unresponsive to standard antipsychotic drugs
Reduction of the risk of recurrent suicidal behavior in patients with schizophrenia or schizoaffective disorder (not orally disintegrating tablet)
Contraindications and Cautions
Contraindicated with allergy to clozapine, myeloproliferative disorders, history of clozapine-induced agranulocytosis or severe granulocytopenia, severe CNS depression, comatose states, history of seizure disorders, lactation, therapy with other drugs that cause bone marrow suppression.
Use cautiously with CV disease, narrow-angle glaucoma, pregnancy.
Available Forms
Tablets—12.5, 25, 50, 100, 200 mg; orally disintegrating tablets—12.5, 25, 100, 150, 200 mg
Dosages
Adults
Initial therapy: 12.5 mg PO once or twice daily. Continue to 25 mg PO daily or bid; then gradually increase with daily increments of 25–50 mg/day, if tolerated, to a dose of 300–450 mg/day by the end of second week. Adjust later dosage no more often than twice weekly in increments of less than 100 mg. Do not exceed 900 mg/day.
Maintenance: Maintain at the lowest effective dose for remission of symptoms.
Discontinuation of therapy: Gradual reduction over a 1- to 2-wk period is preferred. If abrupt discontinuation is required, carefully monitor patient for signs of acute psychotic symptoms.
Reinitiation of treatment: Follow initial dosage guidelines, use extreme care; increased risk of severe adverse effects with re-exposure.
Pediatric patients
Safety and efficacy in patients younger than 16 yr not established.
Pharmacokinetics
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