Antimineralocorticoid activity of a novel oral contraceptive containing drospirenone, a unique progestogen resembling natural progesterone.
Sex hormones are known to interfere with the renin-angiotensin-aldosterone system (RAAS) in two ways. First, estrogens strongly stimulate the production of renin substrate (angiotensinogen), leading to increased levels of angiotensin and aldosterone, and sodium retention. Second, progesterone is a potent aldosterone antagonist, which acts on the mineralocorticoid receptor to prevent sodium retention. In combined oral contraceptives, progestogens devoid of antimineralocorticoid and antiandrogenic activity are unable to counteract the sodium-retaining effect of the ethinylestradiol component. As a consequence, these preparations may increase fluid retention, and promote related symptoms such as edema and body weight. Drospirenone is a new progestogen with antimineralocorticoid and antiandrogenic activity. The relationship between the progestogenie and antimincralocorticoid potency of drospirenone is similar to that of endogenous progesterone. At a dosage that suppresses ovulation, drospirenone induces mild natriuresis, which is followed by compensatory stimulation of the RAAS (comparable to a low sodium diet). An oral contraceptive containing 3 mg drospirenone and 30 microg ethinylestradiol. (Yasmin, Schering AG, Berlin, Germany) provides reliable contraception and, due to a lack of sodium retention, may counteract cyclical weight gain and other symptoms related to estrogen-induced fluid retention.
Oelkers
W
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Division of Endocrinology, Department of Medicine, Klinikum Benjamin Franklin, Freie Universität Berlin, Berlin, Germany.
D000736:Androstenes / Q000008:administration & dosage*; D003267:Contraception / Q000379:methods; D003277:Contraceptives, Oral, Combined / Q000008:administration & dosage*; D018849:Controlled Clinical Trials as Topic; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D005260:Female; D006801:Humans; D008901:Mineralocorticoids / Q000378:metabolism*; D010349:Patient Compliance; D011247:Pregnancy; D011275:Pregnancy, Unwanted / Q000706:statistics & numerical data; D011374:Progesterone; D045167:Progesterone Congeners; D012084:Renin-Angiotensin System / Q000187:drug effects* / Q000502:physiology; D012680:Sensitivity and Specificity
D000736:Androstenes; D003277:Contraceptives, Oral, Combined; D008901:Mineralocorticoids; D045167:Progesterone Congeners; D011374:Progesterone; C035144:drospirenone