Disposition of clozapine and desmethylclozapine in schizophrenic patients.
The disposition of the atypical clozapine and its desmethyl metabolite were evaluated in fourteen male chronic patients. A single 100 mg dose of clozapine was administered and blood sampling performed over the following 72 hours. The mean (SD) oral clearance and half-life of clozapine were 55.4 (29.7) L/hr and 13.7 (9.9) hours, respectively. The mean (SD) AUC for clozapine and desmethylclozapine was 2389.9 (1406) and 751.1 (622.9) ng.hr/mL, respectively. The elimination of the metabolite is rate limited by its formation from cloza-pine. A wide interpatient variability in clozapine and desmethylclozapine pharmacokinetics was observed.
Lin
S K
SK
Taipei City Psychiatric Center, Taiwan, Republic of China.
Chang
W H
WH
Chung
M C
MC
Lam
Y W
YW
Jann
M W
MW
D000328:Adult; D002908:Chronic Disease; D003024:Clozapine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D003915:Dextromethorphan / Q000652:urine; D006207:Half-Life; D006719:Homovanillic Acid / Q000097:blood; D006801:Humans; D008297:Male; D008657:Metabolic Clearance Rate; D008875:Middle Aged; D010641:Phenotype; D012559:Schizophrenia / Q000378:metabolism*
C058272:norclozapine; D003915:Dextromethorphan; D003024:Clozapine; D006719:Homovanillic Acid