Land: Kanada
Språk: engelska
Källa: Health Canada
CLOZAPINE
PHARMASCIENCE INC
N05AH02
CLOZAPINE
25MG
TABLET
CLOZAPINE 25MG
ORAL
100
Prescription
ATYPICAL ANTIPSYCHOTICS
Active ingredient group (AIG) number: 0122583001; AHFS:
CANCELLED POST MARKET
2011-01-20
PRODUCT MONOGRAPH PR PMS-CLOZAPINE (Clozapine Tablets) 25 mg and 100 mg ANTIPSYCHOTIC AGENT PHARMASCIENCE INC. Date of Preparation: 6111 Royalmount Avenue, Suite #100, 1999.07.28 Montréal, Quebec Date of Revision: H4P 2T4 September 16, 2004 Control #93035 - 2 - PRODUCT MONOGRAPH PR PMS-CLOZAPINE (Clozapine) THERAPEUTIC CLASSIFICATION Antipsychotic Agent ACTION AND CLINICAL PHARMACOLOGY pms-CLOZAPINE (clozapine), a dibenzodiazepine derivative, is an atypical antipsychotic drug because its profile of binding to dopamine receptors and its effects on various dopamine-mediated behaviours differ from those exhibited by conventional antipsychotics. In contrast to conventional antipsychotics, clozapine produces little or no prolactin elevation. Clozapine exerts potent anticholinergic, adrenolytic, antihistaminic and antiserotoninergic activity. Controlled clinical trials indicate that clozapine improves both positive and negative symptoms. Patients on rare occasions may report an intensification of dream activity during clozapine therapy. Rapid eye movement (REM) sleep was found to be increased to 85% of the total sleep time. In these patients, the onset of REM sleep occurred almost immediately after falling asleep. As is true of more typical antipsychotic drugs, clinical EEG studies have shown that clozapine increases delta and theta activity and slows dominant alpha frequencies. Enhanced synchronization occurs, and sharp wave activity and spike and wave complexes may also develop. - 3 - P HARMACOKINETICS The absorption of orally administered clozapine is 90 to 95%. Food does not affect either the rate or the extent of absorption. Clozapine is subject to first-pass metabolism, resulting in an absolute bioavailability of 50 to 60%. Plasma concentrations show large inter-individual differences, with peak concentrations occurring approximately 2.5 hours (range: 1 to 6 hours) after dosing. In a dose range of 37.5 mg bid to 150 mg bid, the area under the curve (AUC) and the peak plasma concentration (C max ) increase linear Läs hela dokumentet