[苯二氮䓬类药物作为大鼠肝微粒体中细胞色素P - 450和细胞色素b5诱导剂的研究]
[Benzodiazepines as cytochrome P-450 and cytochrome b5 inductors in rat liver microsomes].
作者信息
Pachecka J, Kobylińska K, Bicz W
机构信息
Zakładu Metabolizmu Leków Instytutu Biofarmacji, Akademii Medycznej w Warszawie.
出版信息
Folia Med Cracov. 1990;31(3):209-15.
Among the benzodiazepines tested (diazepam, oxazepam, clonazepam, nitrazepam and chlordiazepoxide ) chlordiazepoxide is the most potent inducer of cytochrome P-450, diazepam is a poor inducer, whereas clonazepam and nitrazepam do not possess a capacity to induce of cytochrome P-450. On the other hand, microsomal cytochrome b5 is induced by diazepam only. The extent of induction of cytochrome P-450 and cytochrome b5 depends on the environmental temperature. Chlordiazepoxide is the most potent inducer of cytochrome P-450 in rats exposed to an ambient temperature of 28 degrees C, whereas diazepam have the highest induction ability in rats exposed to 35 degrees C. On the other hand, nitrazepam increased the content of cytochrome b5 in rats exposed to temperature of 35 degrees C only; diazepam was the most potent inducer of cytochrome b5 in rats exposed to temperature of 21 degrees C. These results indicate that high ambient temperature is a factor modifying the ability of benzodiazepines to induce of microsomal cytochrome P-450 and cytochrome b5.
在所测试的苯二氮䓬类药物（地西泮、奥沙西泮、氯硝西泮、硝西泮和氯氮卓）中，氯氮卓是细胞色素P - 450最有效的诱导剂，地西泮是较弱的诱导剂，而氯硝西泮和硝西泮不具备诱导细胞色素P - 450的能力。另一方面，微粒体细胞色素b5仅由地西泮诱导。细胞色素P - 450和细胞色素b5的诱导程度取决于环境温度。在环境温度为28摄氏度的大鼠中，氯氮卓是细胞色素P - 450最有效的诱导剂，而在环境温度为35摄氏度的大鼠中，地西泮具有最高的诱导能力。另一方面，硝西泮仅在环境温度为35摄氏度的大鼠中增加了细胞色素b5的含量；在环境温度为21摄氏度的大鼠中，地西泮是细胞色素b5最有效的诱导剂。这些结果表明，高环境温度是改变苯二氮䓬类药物诱导微粒体细胞色素P - 450和细胞色素b5能力的一个因素。
Zotero 插件