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屈螺酮:一种新型孕激素,用作不含雌激素成分的口服避孕药。

Drospirenone: a novel progestogen used as an oral contraceptive without an estrogen component.

作者信息

Paton D M

机构信息

Professor Emeritus of Pharmacology, University of Auckland, Auckland, New Zealand and Professor Emeritus of Oral Biology, University of Alberta, Edmonton, Alberta, Canada.

出版信息

Drugs Today (Barc). 2020 May;56(5):321-328. doi: 10.1358/dot.2020.56.5.3134788.

Abstract

Drospirenone (DRSP) was synthesized as an analogue of spironolactone with the aim of producing a fourth-generation progestogen that differed from earlier progestogens in that it had antiandrogenic and little or no androgenic activity and lacked estrogenic effects while retaining some antimineralocorticoid activity. Since then, DRSP has been included in several oral contraceptive preparations together with an estrogen. However, increasing evidence has demonstrated that DRSP 4 mg on its own inhibits ovulation. It was thus a logical development to determine the efficacy of a tablet that only included DRSP 4 mg as an oral contraceptive. This proved successful and this product has now been approved by the Food and Drug Administration (FDA).

摘要

屈螺酮(DRSP)是作为螺内酯的类似物合成的,目的是生产一种第四代孕激素,它与早期孕激素的不同之处在于具有抗雄激素活性且几乎没有或没有雄激素活性,缺乏雌激素作用,同时保留了一些抗盐皮质激素活性。从那时起,DRSP就与一种雌激素一起被纳入了几种口服避孕药制剂中。然而,越来越多的证据表明,单独使用4毫克DRSP就能抑制排卵。因此,确定一种仅含有4毫克DRSP的片剂作为口服避孕药的疗效是一个合乎逻辑的发展。这一尝试被证明是成功的,该产品现已获得美国食品药品监督管理局(FDA)的批准。

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