用放射受体分析法与高效液相色谱法测定血清中氯氮平：羟基代谢物的可能检测

Determination of clozapine in serum by radioreceptor assay versus high-performance liquid chromatography: possible detection of hydroxy-metabolites.

作者信息

Odou P, Frimat B, Fontaine B, Luyckx M, Brunet C, Robert H, Dine T, Gressier B, Cazin M, Cazin J C

机构信息

Laboratoire de Pharmacie Clinique, Pharmacocinétique et de Pharmacologie Faculté des Sciences Pharmaceutiques et Biologiques, Lille, France.

出版信息

J Clin Pharm Ther. 1996 Oct;21(5):337-42. doi: 10.1111/j.1365-2710.1996.tb00028.x.

DOI:10.1111/j.1365-2710.1996.tb00028.x

PMID:9119916

Abstract

Clozapine is an antipsychotic drug with few extra-pyramidal motor side-effects, used to treat schizophrenia which is resistant to classical neuroleptic therapy. This report shows that norclozapine but not clozapine-N-oxide has the same D2 receptor affinity as clozapine. Assay results suggest a bimodal distribution which may be explained by CYP1A2 polymorphism. Extensive metabolizers could produce other active metabolites, probably other hydroxy-clozapine derivatives.

摘要

氯氮平是一种锥体外系运动副作用较少的抗精神病药物，用于治疗对传统抗精神病药物治疗无效的精神分裂症。本报告显示，去甲氯氮平而非氯氮平 -N- 氧化物与氯氮平具有相同的 D2 受体亲和力。检测结果表明存在双峰分布，这可能由 CYP1A2 基因多态性解释。快代谢者可能会产生其他活性代谢物，可能是其他羟基氯氮平衍生物。