的孕激素屈螺antimineralocorticoid属性:一个简短的回顾。
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Oelkers W
的孕激素屈螺antimineralocorticoid属性:一个简短的回顾。
摩尔细胞性。2004年3月31日,217 (2):255 - 61。doi: 10.1016 / j.mce.2003.10.030。
- PubMed ID
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15134826 (在PubMed]
- 文摘
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未标记的:孕酮(P)具有高亲和力的盐皮质激素受体(MCR),它是一个MCR拮抗剂。几乎所有合成孕激素缺乏这antimineralocorticoid (anti-MC)的效果。他们无法对抗盐保留雌激素的影响。这可能是一个原因的体重和血压的增加使用口服避孕药(OC)和相结合,在一些敏感的女性,绝经后雌激素/孕激素治疗。本课程的目的是评估的临床研究结果,屈(DRSP),一个新的孕激素由先灵葆雅A.G.,anti-MCR活动。DRSP 17-alpha-spirolactone的导数。老鼠,兔子和人,这是一个PR-agonist和MCR - androgen-R拮抗剂对glucocorticoid-R和estrogen-R没有影响。通常在经期女性,2-3mg DRSP每天从第五天到25的循环,抑制排卵,导致轻微的尿钠排泄,轻微的补偿性renin-aldosterone系统的激活。相比之下,一个包含30 OC microg炔雌醇(EE)和150 microg levonorgestrel,结合3毫克DRSP 30 microg EE 6个月了导致轻微下降,体重和血压。减少平均体重的结合与EE DRSP相比传统OC可以证实在900年的一项研究超过26个月的年轻女性。 The OC containing DRSP has favorable effects in patients suffering from the premenstrual syndrome (PMS), and, partly due to the antiandrogenic effect of DRSP, in those with acne vulgaris. For postmenopausal women, a combination of DRSP with estradiol has been developed with the expectation that the slight blood pressure lowering and weight reducing effects will minimize cardiovascular morbidity in patients needing hormone treatment because of hot flushes and other climacteric symptoms. CONCLUSIONS: DRSP, by its anti-MCR effect and its potential to slightly decrease body weight and blood pressure, shares many pharmacodynamic properties with progesterone, and it is a candidate for reducing cardiovascular morbidity in women using OCs or postmenopausal hormone treatment.