Hrdina P D, Lapierre Y D, McIntosh B, Oyewumi L K
Clin Pharmacol Ther. 1983 Jun;33(6):757-62. doi: 10.1038/clpt.1983.103.
We studied mianserin kinetics after a single (60 mg) dose in eight inpatients suffering from depression. There was a considerable interpatient variability in plasma levels. Mean peak plasma levels (+/- SEM) were 114 +/- 26 ng/ml and were reached between 1 and 3 hr. The decline of mianserin levels in plasma was biphasic. The mean elimination t 1/2 was 21.6 +/- 3.1 hr and ranged from 10.7 to 40.8 hr. The estimated first-pass loss ranged from 26% to 48% (mean, 37%) and was lower than that reported for tertiary amine tricyclic antidepressants. The mean apparent volume of distribution (15.7 +/- 2.2 l/kg; 9.7 to 28.8 l/kg) was in the range of that for imipramine but somewhat lower than for maprotiline. Apparent total body clearance ranged from 0.33 to 0.81 l/hr/kg (mean +/- SEM, 0.52 +/- 0.05 l/hr/kg) and was of the order of that after maprotiline. Our results indicate that mianserin kinetics are in most respects similar to those of tertiary amine tricyclic antidepressants (e.g., imipramine) and the tetracyclic maprotiline.
我们对8名抑郁症住院患者单次服用60毫克米安色林后的药代动力学进行了研究。患者之间血浆水平存在相当大的差异。平均血浆峰浓度（±标准误）为114±26纳克/毫升，在1至3小时之间达到。血浆中米安色林水平的下降呈双相性。平均消除半衰期为21.6±3.1小时，范围为10.7至40.8小时。估计的首过损失范围为26%至48%（平均为37%），低于叔胺类三环抗抑郁药的报告值。平均表观分布容积为15.7±2.2升/千克（9.7至28.8升/千克），与丙咪嗪的范围相当，但略低于马普替林。表观全身清除率范围为0.33至0.81升/小时/千克（平均±标准误，0.52±0.05升/小时/千克），与马普替林后的清除率相当。我们的结果表明，米安色林的药代动力学在大多数方面与叔胺类三环抗抑郁药（如丙咪嗪）和四环类马普替林相似。
