Briatico G, Guiso G, Jori A, Ravazzani C
Br J Pharmacol. 1976 Oct;58(2):173-81. doi: 10.1111/j.1476-5381.1976.tb10393.x.
The effect on liver microsomal enzyme activity of three steroid contraceptive drug (SCD) combinations was compared in rats, mice and guinea-pigs. Lynestrenol plus mestranol, norethisterone plus mestranol and norethynodrel plus mestranol were given orally for 4 consecutive days (acute treatment) or 30 days (chronic treatment) at various doses eliciting an experimentally controlled antifertility activity which varied in its extent. In rats and mice all the combined treatments (with the exception of norethynodrel plus mestranol in mice) were active as inducers of liver microsomal enzymes. This induction seems to be mediated mainly by the progestogenic compounds. Oestrogens showed a very poor effect bordering on significance only in a few cases. No effect on liver microsomal protein or cytochrome P 450 concentration was obtained after treatment with doses capable of increasing the microsomal enzyme activity. The activity of the liver microsomal enzymes did not appear to be reduced immediately (2 h) after the last administration of the SCD given during 4 or 30 days. Contraceptive treatments at doses capable of eliciting complete antifertility activity were inactive on liver microsomal enzyme activity in guinea-pigs.
在大鼠、小鼠和豚鼠中比较了三种甾体避孕药（SCD）组合对肝脏微粒体酶活性的影响。炔雌醇甲醚炔诺酮、炔诺酮加炔雌醇甲醚和异炔诺酮加炔雌醇甲醚以不同剂量连续口服4天（急性治疗）或30天（慢性治疗），这些剂量可引发实验控制的抗生育活性，其程度各不相同。在大鼠和小鼠中，所有联合治疗（小鼠中异炔诺酮加炔雌醇甲醚除外）均作为肝脏微粒体酶的诱导剂具有活性。这种诱导似乎主要由孕激素化合物介导。雌激素仅在少数情况下显示出非常微弱的影响，几乎没有统计学意义。用能够增加微粒体酶活性的剂量治疗后，未观察到对肝脏微粒体蛋白或细胞色素P 450浓度的影响。在连续4天或30天给予SCD后最后一次给药后2小时内，肝脏微粒体酶的活性似乎没有立即降低。能够引发完全抗生育活性的剂量的避孕治疗对豚鼠肝脏微粒体酶活性没有影响。
