Drospirenone: pharmacology and pharmacokinetics of a unique progestogen

Drospirenone: pharmacology and pharmacokinetics of a unique progestogen The pharmacology and pharmacokinetics of drospirenone, a unique progestogen, are reviewed in this paper. Unlike other progestogens, drospirenone, an analogue of spironolactone, has biochemical and pharmacologic profiles similar to endogenous progesterone, especially regarding antimineralocorticoid and antiandrogenic activities. Drospirenone counteracts the estrogen-induced stimulation of the renin-angiotensin-aldosterone system and blocks testosterone from binding to androgen receptors. Because of these characteristics, it has the potential to reduce body weight, blood pressure, and low-density lipoprotein levels and to enhance high-density lipoprotein levels. As a combination oral contraceptive, drospirenone with ethinyl estradiol is effective and has positive effects on weight and lipid levels. Additionally, it relieves menstrually related symptoms (e.g., negative affect and water retention) that are commonly observed with other combination oral contraceptives. Based on the biochemical and pharmacodynamic data, drospirenone appears to be a viable alternative to the currently available progestogens. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Contraception Elsevier

Drospirenone: pharmacology and pharmacokinetics of a unique progestogen

Contraception, Volume 62 (1) – Jul 1, 2000

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Publisher
Elsevier
Copyright
Copyright © 2000 Elsevier Science Inc.
ISSN
0010-7824
DOI
10.1016/S0010-7824(00)00133-5
Publisher site
See Article on Publisher Site

Abstract

The pharmacology and pharmacokinetics of drospirenone, a unique progestogen, are reviewed in this paper. Unlike other progestogens, drospirenone, an analogue of spironolactone, has biochemical and pharmacologic profiles similar to endogenous progesterone, especially regarding antimineralocorticoid and antiandrogenic activities. Drospirenone counteracts the estrogen-induced stimulation of the renin-angiotensin-aldosterone system and blocks testosterone from binding to androgen receptors. Because of these characteristics, it has the potential to reduce body weight, blood pressure, and low-density lipoprotein levels and to enhance high-density lipoprotein levels. As a combination oral contraceptive, drospirenone with ethinyl estradiol is effective and has positive effects on weight and lipid levels. Additionally, it relieves menstrually related symptoms (e.g., negative affect and water retention) that are commonly observed with other combination oral contraceptives. Based on the biochemical and pharmacodynamic data, drospirenone appears to be a viable alternative to the currently available progestogens.

Journal

ContraceptionElsevier

Published: Jul 1, 2000

References

  • Effects of estrogens and progestogens on the renin-aldosterone system and blood pressure
    Oelkers, W.K.
  • The androgenicity of progestins
    Darney, P.D.
  • The novel progestin drospirenone and its natural counterpart progesterone
    Fuhrmann, U.; Krattenmacher, R.; Slater, E.P.; Fritzemeier, K.H.

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