Kulcsár A, Kulcsár-Gergely J
Arzneimittelforschung. 1977;27(9):1694-7.
Experiments on female rats were performed to observe the effects of progesterone and two synthetic progestens: ethinodiol-diacetate and methylestrenolone on liver function. In acute experiments animals were treated for the duration of one sexual cycle. All three compounds prolonged the hexobarbital biotransformation time. This effect is reversible and normalised 48 h after stopping treatment. The testosterone inducement of microsomal mixed function oxydases remained at the level of controls after methylestrenolone pretreatments and was even higher in the ethinodiol-diacetate and progesterone pretreated animals. Subacute and chronical treatments lasting for two or more sexual cycles resulted in the same slight inhibition of hexobarbital biotransformation when performed with the two progestogens. Chronical progesterone administration prolonged significantly hexobarbital biotransformation time. This impairement is also reversible. Our results pertain to a moderate, transitive inhibition of hexobarbital metabolism during short-term and prolonged progesterone and progestogen treatment. This effect may be easily suspended by interrupting drug administration or inducing microsomal enzymes with a single dosage of testosterone. In our progesterone experiments the inhibition of liver function increased with dosage and exposition time. In case of the two examined progestogens exposition time has not been proven as a predisposing factor for impairing liver function.
对雌性大鼠进行实验，以观察孕酮及两种合成孕激素——双醋炔诺醇和甲基炔诺酮对肝功能的影响。在急性实验中，动物接受一个性周期时长的治疗。所有这三种化合物均延长了己巴比妥的生物转化时间。这种作用是可逆的，在停止治疗后48小时恢复正常。经甲基炔诺酮预处理后，睾酮诱导的微粒体混合功能氧化酶水平维持在对照水平，而经双醋炔诺醇和孕酮预处理的动物中该水平甚至更高。用两种孕激素进行持续两个或更多性周期的亚急性和慢性治疗，导致己巴比妥生物转化受到同样轻微的抑制。长期给予孕酮显著延长了己巴比妥的生物转化时间。这种损害也是可逆的。我们的结果表明，在短期和长期的孕酮及孕激素治疗期间，己巴比妥代谢受到中度、短暂的抑制。通过中断给药或单次给予睾酮诱导微粒体酶，这种作用可能很容易被消除。在我们的孕酮实验中，肝功能的抑制随剂量和暴露时间增加。对于所检测的两种孕激素，暴露时间尚未被证明是损害肝功能的一个诱发因素。
