吗氯贝胺治疗会使司巴丁代谢率大幅升高。丹麦大学抗抑郁药研究小组。
Moclobemide treatment causes a substantial rise in the sparteine metabolic ratio. Danish University Antidepressant Group.
作者信息
Gram L F, Brøsen K
机构信息
Department of Clinical Pharmacology, Odense University, Denmark.
出版信息
Br J Clin Pharmacol. 1993 Jun;35(6):649-52. doi: 10.1111/j.1365-2125.1993.tb04196.x.
Abstract
A sparteine test was carried out immediately before (n = 37) and during (n = 33) moclobemide treatment (200 mg twice daily) in 37 patients participating in a controlled clinical trial. The sparteine metabolic ratio (MR) did not correlate with the plasma concentration of moclobemide and/or its oxidized metabolite Ro 12-8095, and four sparteine poor metabolisers (PM, MR > 20) had plasma moclobemide concentrations similar to those in extensive metabolisers (EM, MR < 20). The Ro 12-8095/moclobemide ratio tended to correlate negatively with the sparteine MR before and during treatment (rs = -0.32, -0.37). During moclobemide treatment the sparteine MR rose substantially by a factor of 1-103 (median 4.7), and two EM became phenotypically PM. In the PM subjects as well as in one EM patient on cimetidine during both tests, no change in sparteine MR occurred.
摘要
在一项对照临床试验的37例患者中，在莫洛贝胺治疗前（n = 37）和治疗期间（n = 33）（每日两次，每次200 mg）立即进行了司巴丁试验。司巴丁代谢率（MR）与莫洛贝胺及其氧化代谢产物Ro 12 - 8095的血浆浓度无关，并且四名司巴丁慢代谢者（PM，MR > 20）的血浆莫洛贝胺浓度与快代谢者（EM，MR < 20）相似。在治疗前和治疗期间，Ro 12 - 8095/莫洛贝胺比值与司巴丁MR呈负相关（rs = -0.32，-0.37）。在莫洛贝胺治疗期间，司巴丁MR大幅上升，升高了1 - 103倍（中位数为4.7），两名EM在表型上转变为PM。在PM受试者以及在两次试验期间服用西咪替丁的一名EM患者中，司巴丁MR没有变化。
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