Calvo B, García M J, Pedraz J L, Mariño E L, Domínguez-Gil A
Int J Clin Pharmacol Ther Toxicol. 1985 Apr;23(4):180-5.
The plasma concentrations of amoxapine and its active metabolites, 8-hydroxyamoxapine and 7-hydroxyamoxapine were determined in 8 healthy volunteers receiving a single oral dose of 100 mg of the drug. Considerable interindividual variation was seen in the plasma levels of the three substances. Amoxapine reached maximum levels of 67.4 +/- 35.8 ng/ml between 1 and 2 h after administration. The decline of amoxapine levels in plasma was biphasic. The mean elimination half-life was 9.8 +/- 2.6 h and the estimated first-pass loss ranged between 0.18 and 0.54. The peak levels of the metabolites were reached between 1 and 3 h after administration, with 8-hydroxyamoxapine levels significantly higher than those of 7-hydroxyamoxapine. The mean elimination half-lives were 30.8 and 5.1 h for 8-hydroxyamoxapine and 7-hydroxyamoxapine respectively. The margins of the plasma concentrations reached at steady-state were calculated according to pharmacokinetics parameters for a dosage interval of 8 h.
在8名接受单次口服100毫克阿莫沙平的健康志愿者中，测定了阿莫沙平及其活性代谢物8-羟基阿莫沙平和7-羟基阿莫沙平的血浆浓度。这三种物质的血浆水平存在相当大的个体间差异。给药后1至2小时内，阿莫沙平达到最高水平，为67.4±35.8纳克/毫升。血浆中阿莫沙平水平的下降呈双相性。平均消除半衰期为9.8±2.6小时，估计首过损失在0.18至0.54之间。给药后1至3小时内达到代谢物的峰值水平，8-羟基阿莫沙平水平显著高于7-羟基阿莫沙平。8-羟基阿莫沙平和7-羟基阿莫沙平的平均消除半衰期分别为30.8小时和5.1小时。根据8小时给药间隔的药代动力学参数计算稳态时达到的血浆浓度范围。
