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醋酸甲羟孕酮不会诱导比格犬体内安替比林清除率增加,且只会微弱增加α1-酸性糖蛋白。

Medroxyprogesterone acetate does not induce antipyrine clearance and only weakly increases alpha 1-acid glycoprotein in beagle dogs.

作者信息

Abramson F P, Moore C F, Hill M D

出版信息

Res Commun Chem Pathol Pharmacol. 1986 Jul;53(1):65-78.

PMID:2944196
Abstract

The synthetic progestin medroxyprogesterone acetate (MPA) has previously been shown to be an inducer of hepatic microsomal cytochrome P-450 in both man and the rat. We have assessed the ability of a variety of oral doses of MPA to induce either hepatic cytochrome P-450 as measured by antipyrine clearance or alpha 1-acid glycoprotein (AGP) in beagle dogs. Over the range of 25 mg/d to 400 mg/d, MPA did not induce antipyrine clearance. The concentration of AGP only increased at the 400 mg/d level, and was effected to a much smaller extent than has been previously observed for other inducing agents. MPA was also tested as a promoter of induction by combining it with a course of rifampin capable of substantially elevating both antipyrine clearance and AGP. MPA was without effect. The results of these experiments are discussed in light of the toxicology of MPA in beagles.

摘要

合成孕激素醋酸甲羟孕酮(MPA)先前已被证明在人和大鼠中都是肝微粒体细胞色素P - 450的诱导剂。我们评估了不同口服剂量的MPA诱导比格犬肝细胞色素P - 450(通过安替比林清除率测定)或α1 - 酸性糖蛋白(AGP)的能力。在25毫克/天至400毫克/天的范围内,MPA未诱导安替比林清除率。AGP浓度仅在400毫克/天的水平增加,且其受影响程度比先前观察到的其他诱导剂小得多。还通过将MPA与能大幅提高安替比林清除率和AGP的利福平疗程联合使用,来测试MPA作为诱导促进剂的作用。MPA没有效果。根据MPA在比格犬中的毒理学对这些实验结果进行了讨论。

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