Haglund K, Seideman P, Collste P, Borg K O, von Bahr C
Clin Pharmacol Ther. 1979 Sep;26(3):326-9. doi: 10.1002/cpt1979263326.
Induction of microsomal enzymes with barbiturates in rats has little effect on the metabolism of metoprolol, compared with propranolol and alprenolol, which undergo extensive hepatic extraction in animals and man. Our study was designed to examine whether the metabolism of metoprolol is inducable by barbiturate in man. In 8 healthy subjects the area under the plasma concentration/time curve after 0.1 gm metoprolol was reduced by a mean of 32% after treatment with 0.1 gm pentobarbital at bedtime for 10 days. There was considerable interindividual variability in the reduction after pentobarbital treatment (2% to 46%).
与普萘洛尔和阿普洛尔相比,用巴比妥酸盐诱导大鼠微粒体酶对美托洛尔的代谢影响很小,普萘洛尔和阿普洛尔在动物和人体内会经历广泛的肝脏摄取。我们的研究旨在检查美托洛尔的代谢在人体内是否可被巴比妥酸盐诱导。在8名健康受试者中,睡前服用0.1克戊巴比妥10天,服用0.1克美托洛尔后血浆浓度/时间曲线下面积平均降低了32%。戊巴比妥治疗后降低程度存在相当大的个体间差异(2%至46%)。