Antimineralocorticoid activity of a novel oral contraceptive containing drospirenone, a unique progestogen resembling natural progesterone.

Abstract

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.

• Authors: W Oelkers
• Journal: The European journal of contraception & reproductive health care : the official journal of the European Society of Contraception (Eur J Contracept Reprod Health Care) Vol. 7 Suppl 3 Pg. 19-26; discussion 42-3 (Dec 2002) ISSN: 1362-5187 [Print] England
• PMID: 12659403 (Publication Type: Journal Article, Review)

Chemical References

• Androstenes
• Contraceptives, Oral, Combined
• Mineralocorticoids
• Progesterone Congeners
• Progesterone
• drospirenone

Topics

• Androstenes (administration & dosage)
• Contraception (methods)
• Contraceptives, Oral, Combined (administration & dosage)
• Controlled Clinical Trials as Topic
• Dose-Response Relationship, Drug
• Drug Administration Schedule
• Female
• Humans
• Mineralocorticoids (metabolism)
• Patient Compliance
• Pregnancy
• Pregnancy, Unwanted (statistics & numerical data)
• Progesterone
• Progesterone Congeners
• Renin-Angiotensin System (drug effects, physiology)
• Sensitivity and Specificity