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抗雄激素醋酸环丙孕酮对脂质和脂蛋白代谢的矛盾作用。

Paradoxical effects of the anti-androgen cyproterone acetate on lipid and lipoprotein metabolism.

作者信息

Wynn V, Godsland I F, Seed M, Jacobs H S

出版信息

Clin Endocrinol (Oxf). 1986 Feb;24(2):183-91. doi: 10.1111/j.1365-2265.1986.tb00761.x.

DOI:10.1111/j.1365-2265.1986.tb00761.x
PMID:2940034
Abstract

The effects on fasting serum lipids of the potent anti-androgen, cyproterone acetate (CA) and the oestrogen, ethinyl oestradiol (EO) given both alone and in combination were examined in women acting as their own controls. Cyproterone acetate alone caused significant reductions in total cholesterol, high density lipoprotein subfraction 2 cholesterol (HDL2) and low density lipoprotein cholesterol (LDL). Ethinyl oestradiol alone significantly increased triglycerides, HDL and HDL2 and reduced LDL, and there was also a significant increase in the HDL/LDL and HDL2/LDL ratios. The two steroids were administered in combination according to a reverse sequential regime. The 28-day treatment cycle thus included Phase A during which both drugs were given followed by Phase B when EO alone was given. Triglycerides rose significantly in Phases A and B to the same extent as for the group taking EO alone. High density lipoprotein cholesterol was unchanged but HDL2 was reduced in both phases and this effect could not be overcome by increasing the dose of oestrogen. Low density lipoprotein cholesterol fell and the HDL/LDL ratio rose during the two Phases and these changes were significant during Phase A. The effects of EO demonstrated in this study are consistent with previous reports. Cyproterone acetate, however, has properties conventionally ascribed to both synthetic androgens (e.g. lowering of HDL2) and oestrogens (e.g. lowering of LDL). The limitations of the terms androgenic and oestrogenic activity in relation to their conventional associations with changes in lipid and lipoprotein levels are discussed.

摘要

在以自身作为对照的女性中,研究了强效抗雄激素醋酸环丙孕酮(CA)和雌激素炔雌醇(EO)单独及联合使用对空腹血脂的影响。单独使用醋酸环丙孕酮可使总胆固醇、高密度脂蛋白亚组分2胆固醇(HDL2)和低密度脂蛋白胆固醇(LDL)显著降低。单独使用炔雌醇可使甘油三酯、HDL和HDL2显著升高,LDL降低,并且HDL/LDL和HDL2/LDL比值也显著升高。两种甾体激素按照反向序贯方案联合给药。28天的治疗周期包括A期,在此期间两种药物都给药,随后是B期,此时仅给予EO。甘油三酯在A期和B期均显著升高,升高程度与单独服用EO的组相同。高密度脂蛋白胆固醇未发生变化,但HDL2在两个阶段均降低,并且增加雌激素剂量也无法克服这种影响。低密度脂蛋白胆固醇降低,HDL/LDL比值在两个阶段均升高,且在A期这些变化具有显著性。本研究中显示的EO的作用与先前的报道一致。然而,醋酸环丙孕酮具有通常归因于合成雄激素(如降低HDL2)和雌激素(如降低LDL)的特性。讨论了与脂质和脂蛋白水平变化的传统关联相关的雄激素活性和雌激素活性术语的局限性。

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