Reynolds G P, Riederer P, Sandler M
J R Soc Med. 1981 Sep;74(9):649-52. doi: 10.1177/014107688107400905.
The tranylcypromine stereoisomers have been investigated in a series of comparative trials in Parkinsons' disease and the results indicate that doses below 3 mg/day, of the (+)-isomer in particular, are effective as adjuvant anti-parkinsonian therapy. Biochemical results, monitoring platelet monoamine oxidase (MAO) activity and plasma concentrations of drugs and phenylethylamine, an MAO substrate, showed such low doses of the (+)-isomer to inhibit MAO without inducing the hypertensive reaction sometimes observed at higher dosage. These findings, along with the observation of substantial pharmacokinetic differences between the two isomers are discussed, particularly in relation to reports on their efficacy in depressive illness.
在一系列针对帕金森病的对比试验中对反苯环丙胺立体异构体进行了研究,结果表明,每日剂量低于3毫克,尤其是(+)-异构体,作为辅助抗帕金森病治疗是有效的。生化结果监测血小板单胺氧化酶(MAO)活性以及药物和MAO底物苯乙胺的血浆浓度,结果显示,如此低剂量的(+)-异构体可抑制MAO,而不会引发有时在高剂量时观察到的高血压反应。讨论了这些发现以及两种异构体之间存在显著药代动力学差异的观察结果,特别是与它们在抑郁症治疗中的疗效报告相关的内容。