Clinical pharmacokinetics of clozapine in chronic schizophrenic patients

The clinical pharmacokinetics of clozapine, an atypical neuroleptic, was evaluated in 10 chronic schizophrenic male patients after intravenous and oral administration. The mean equilibrium-state concentration ratio between blood and plasma was experimentally determined to be 0.87. The average values...

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Veröffentlicht in:European journal of clinical pharmacology 1988-01, Vol.34 (5), p.445-449
Hauptverfasser: CHENG, Y. F, LUNDBERG, T, BONDESSON, U, LINDSTRÖM, L, GABRIELSSON, J
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container_end_page 449
container_issue 5
container_start_page 445
container_title European journal of clinical pharmacology
container_volume 34
creator CHENG, Y. F
LUNDBERG, T
BONDESSON, U
LINDSTRÖM, L
GABRIELSSON, J
description The clinical pharmacokinetics of clozapine, an atypical neuroleptic, was evaluated in 10 chronic schizophrenic male patients after intravenous and oral administration. The mean equilibrium-state concentration ratio between blood and plasma was experimentally determined to be 0.87. The average values for blood clearance, hepatic extraction ratio and oral bioavailability were 250 ml/min, 0.2 and 0.27, respectively. Plasma concentration peaked on average at 3 h. The mean volume of distribution at steady-state and the terminal half-life was 1.6 l/kg and 10.3 h, respectively. A large fraction of the dose is most probably metabolized by some extrahepatic presystemic routes. The large inter-individual variability in the bioavailability and clearance is probably the main reason for large variation in the steady-state plasma level in patients receiving the same oral dosage regimen.
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subjects Administration, Oral
Adult
Biological and medical sciences
Chronic Disease
Clozapine - administration & dosage
Clozapine - pharmacokinetics
Clozapine - therapeutic use
Dibenzazepines - pharmacokinetics
Humans
Injections, Intravenous
Male
Medical sciences
Neuropharmacology
Pharmacology. Drug treatments
Psycholeptics: tranquillizer, neuroleptic
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Schizophrenia - drug therapy
Schizophrenia - metabolism
title Clinical pharmacokinetics of clozapine in chronic schizophrenic patients
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