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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。

相似文献

1
Medroxyprogesterone acetate does not induce antipyrine clearance and only weakly increases alpha 1-acid glycoprotein in beagle dogs.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。
Res Commun Chem Pathol Pharmacol. 1986 Jul;53(1):65-78.
2
The kinetics of induction by rifampin of alpha 1-acid glycoprotein and antipyrine clearance in the dog.利福平诱导犬体内α1-酸性糖蛋白及安替比林清除率的动力学研究
Drug Metab Dispos. 1986 Jan-Feb;14(1):46-51.
3
Antipyrine metabolism and liver function in patients treated with high-dose medroxyprogesterone.接受大剂量甲羟孕酮治疗患者的安替比林代谢与肝功能
Biomedicine. 1979 Sep;31(5):135-8.
4
Parallel induction of plasma alpha 1-acid glycoprotein concentration and antipyrine clearance by drugs.
Prog Clin Biol Res. 1989;300:427-35.
5
Relationship between metabolic clearance rate of antipyrine and hepatic microsomal drug-oxidizing enzyme activities in humans without liver disease.无肝脏疾病人群中安替比林代谢清除率与肝微粒体药物氧化酶活性之间的关系。
Gastroenterology. 1981 Jan;80(1):112-8.
6
Metabolism of medroxyprogesterone acetate and hepatic drug metabolism activity.醋酸甲羟孕酮的代谢与肝脏药物代谢活性
Res Commun Chem Pathol Pharmacol. 1985 Feb;47(2):305-8.
7
The effects of phenytoin dosage on the induction of alpha 1-acid glycoprotein and antipyrine clearance in the dog.苯妥英钠剂量对犬体内α1-酸性糖蛋白诱导及安替比林清除率的影响。
Eur J Drug Metab Pharmacokinet. 1986 Apr-Jun;11(2):135-43. doi: 10.1007/BF03189839.
8
Parallel induction of plasma alpha 1-acid glycoprotein concentration and antipyrine clearance by various doses of phenobarbital in the dog.犬体内不同剂量苯巴比妥对血浆α1-酸性糖蛋白浓度和安替比林清除率的平行诱导作用。
Drug Metab Dispos. 1988 Nov-Dec;16(6):890-1.
9
Increased clearance of antipyrine and d-propranolol after phenobarbital treatment in the monkey. Relative contributions of enzyme induction and increased hepatic blood flow.苯巴比妥治疗后猴子体内安替比林和d-普萘洛尔清除率增加。酶诱导和肝血流量增加的相对作用。
J Clin Invest. 1974 Apr;53(4):1101-7. doi: 10.1172/JCI107647.
10
Phenobarbital in the genetically obese Zucker rat. II. In vivo and in vitro assessments of microsomal enzyme induction.苯巴比妥对遗传性肥胖的 Zucker 大鼠的影响。II. 微粒体酶诱导的体内和体外评估。
J Pharmacol Exp Ther. 1984 Dec;231(3):654-9.

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