作者: Thomas J. Raedler , Kim Hinkelmann , Klaus Wiedemann
DOI: 10.1097/WNF.0B013E31815CBA61
关键词: Active metabolite 、 Negative correlation 、 Pharmacology 、 In vivo metabolism 、 In vivo 、 Plasma levels 、 Schizophrenia 、 Medicine 、 Clozapine 、 High variability
摘要: Objectives: Clozapine, the gold standard of antipsychotic treatment in treatment-refractory patients with schizophrenia, is metabolized vivo to clozapine-N-oxide and N-desmethylclozapine (NDMC = norclozapine). an active metabolite clozapine combines unique pharmacological properties. Because little known about rate metabolic conversion vivo, we assessed association between dose plasma levels for NDMC. Methods: Plasma NDMC were measured 485 blood samples from 108 schizophrenia treated clozapine. %NDMC, ratio total + clozapine), was used as a measure metabolism Results: Daily doses correlated significantly levels, whereas %NDMC showed weaker negative correlation dose. The mean value 37.0% ± 16.8%, high variability subjects. Repeated measurements subjects same within-subject %NDMC. Conclusions: Our results suggest degree between-subject vivo. Direct administration may be preferable reliably achieve sufficient this compound.