Ishida R, Usui T, Fukushima Y, Fujita S, Suzuki T
J Pharm Sci. 1985 May;74(5):578-81. doi: 10.1002/jps.2600740520.
The effect of vitamin K3, which inhibits electron transfer from NADPH to cytochrome P-450 via cytochrome c reductase, on the metabolism of propranolol was studied in the rat in vitro and in vivo. For in vitro experiments using rat liver microsomes, the metabolism of propranolol was inhibited by vitamin K3. For in vivo experiments, the area under the blood concentration-time curve and the maximum concentration of propranolol were markedly increased following intraportal infusion of propranolol with vitamin K3, but intraportal administration of vitamin K3 had little effect on propranolol kinetics when propranolol was infused intravenously. Thus, it was concluded that vitamin K3 inhibited the first-pass metabolism of propranolol.
研究了维生素K3对大鼠体内外普萘洛尔代谢的影响，维生素K3可通过细胞色素c还原酶抑制电子从NADPH向细胞色素P-450的转移。在体外实验中，使用大鼠肝微粒体，维生素K3抑制了普萘洛尔的代谢。在体内实验中，门静脉内输注普萘洛尔与维生素K3后，普萘洛尔的血药浓度-时间曲线下面积和最大浓度显著增加，但当静脉输注普萘洛尔时，门静脉内给予维生素K3对普萘洛尔动力学影响不大。因此，得出结论：维生素K3抑制了普萘洛尔的首过代谢。
