Lukienko P I, Bushma M I, Nikitin V S
Farmakol Toksikol. 1983 Nov-Dec;46(6):74-8.
It has been shown in experiments on male rats that administration of cordiamine per os in a dose of 73 mg/kg for 45 days provokes hepatomegaly, proliferation of smooth endoplasmic reticulum in hepatocytes, an increase in the microsomal fraction release, rise in the content of cytochrome P450 and in the rate of N-demethylation of ethylmorphine and p-hydroxylation of aniline in liver microsomes. The spectral magnitude of cytochrome P450 binding with aniline and cordiamine does not change under the effect of the latter drug, while interaction of the enzyme with ethylmorphine decreases. The rate of the recovery of the cytochrome P450-ethylmorphine complex increases 3-fold. It is assumed that an increase in the content of cytochrome and in the rate of xenobiotic hydroxylation in microsomes after prolonged administration of cordiamine might be regarded as substrate induction in nature.
在雄性大鼠实验中已表明,以73毫克/千克的剂量口服可拉明45天,会引发肝肿大、肝细胞中滑面内质网增殖、微粒体部分释放增加、细胞色素P450含量升高以及肝微粒体中乙基吗啡的N - 去甲基化速率和苯胺的对羟基化速率提高。在可拉明的作用下,细胞色素P450与苯胺和可拉明结合的光谱幅度不变,而该酶与乙基吗啡的相互作用减弱。细胞色素P450 - 乙基吗啡复合物的恢复速率增加3倍。据推测,长期给予可拉明后微粒体中细胞色素含量增加和异生物质羟基化速率提高在本质上可能被视为底物诱导。