Pharmacology of Different Progestogens: The Special Case of Drospirenone

    January 2005 in “ Climacteric ”
    Régine Sitruk-Ware
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    TLDR Drospirenone is a unique progestin with anti-water retention and potential blood pressure benefits, used in birth control and hormone therapy.
    The document discusses the pharmacological properties of progestins, highlighting that small structural changes can significantly affect their function. It notes that the specificity of progestins to progesterone receptor isoforms PR-A or PR-B is unclear, and the clinical relevance of this specificity remains unknown. New progestins with improved receptor-selectivity profiles have been developed, including drospirenone, which is unique due to its antimineralocorticoid activity, leading to decreased salt and water retention and potentially lower blood pressure. Drospirenone binds to the mineralocorticoid receptor with five times the affinity of aldosterone and exhibits partial antiandrogenic activity, which could benefit hair growth and body composition in postmenopausal women. With a terminal half-life of about 32 hours and a bioavailability of 76%, drospirenone is used in oral contraceptives and hormone replacement therapy, available in products like Yasmin® and Angeliq® by Schering AG.
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