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氯巴占和N-去甲基氯巴占的血清及脑脊液浓度

Serum and cerebrospinal fluid concentration of clobazam and N-desmethylclobazam.

作者信息

Laux G, Koeppen D

出版信息

Int J Clin Pharmacol Ther Toxicol. 1984 Jul;22(7):355-9.

PMID:6147313
Abstract

Twelve adult neurological patients undergoing lumbar puncture for diagnostic purposes received acute or repeated doses of the 1,5-benzodiazepine clobazam 20-40 mg/day. In one patient, additional ventricle cerebrospinal fluid samples were collected in the course of the diagnostic procedure and the respective concentrations of clobazam and N-desmethylclobazam were determined. The serum and lumbar cerebrospinal fluid concentrations of clobazam and its main metabolite N-desmethylclobazam were compared. The concentrations of both clobazam and N-desmethylclobazam were higher in serum than in cerebrospinal fluid (CSF). Clobazam and N-desmethylclobazam showed similar increase and decline in the ventricle CSF of one patient. This result differed from the pharmacokinetics of clobazam and its main metabolite in the blood which is characterized by a slower increase and a more prolonged elimination of N-desmethylclobazam, as opposed to the parent compound.

摘要

12名因诊断目的接受腰椎穿刺的成年神经科患者接受了20 - 40毫克/天的1,5 - 苯二氮䓬类药物氯巴占的急性或重复剂量给药。在一名患者中,在诊断过程中额外采集了脑室脑脊液样本,并测定了氯巴占和N - 去甲基氯巴占的各自浓度。比较了氯巴占及其主要代谢物N - 去甲基氯巴占的血清和腰椎脑脊液浓度。氯巴占和N - 去甲基氯巴占的血清浓度均高于脑脊液(CSF)。在一名患者的脑室脑脊液中,氯巴占和N - 去甲基氯巴占呈现出相似的升降变化。这一结果与氯巴占及其主要代谢物在血液中的药代动力学不同,其特征是N - 去甲基氯巴占的上升较慢且消除时间更长,与母体化合物相反。

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