Clozapine disposition covaries with CYP1A2 activity determined by a caffeine test.
作者： L Bertilsson , JA Carrillo , ML Dahl , A Llerena , C Alm
DOI: 10.1111/J.1365-2125.1994.TB04385.X
关键词: CYP1A2 、 Caffeine 、 Chemistry 、 Xanthine oxidase 、 Pharmacology 、 Oral administration 、 Clozapine 、 Debrisoquine 、 Hydroxylation 、 Pharmacokinetics
摘要: In a previous study we showed that the disposition of clozapine after single oral dose is unrelated to either debrisoquine or S-mephenytoin hydroxylation polymorphism. The same 14 healthy subjects studied in investigation were given 150 mg caffeine. reciprocal plasma AUC (0,24), was correlated with an index N3-demethylation caffeine (rs = 0.84; P 0.0024), used as measure cytochrome P4501A2 (CYP1A2) activity. N1- and N7-demethylation indices also reflect CYP1A2 activity clearance 0.89 0.85; 0.0013 0.0023; respectively). No significant relationships xanthine oxidase N-acetyl transferase activity, assessed by test, found. This suggests metabolised major extent.
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