Drospirenone: pharmacology and pharmacokinetics of a unique progestogen

Contraception. 2000 Jul;62(1):29-38. doi: 10.1016/s0010-7824(00)00133-5.

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.

Publication types

  • Review

MeSH terms

  • Androstenes / pharmacokinetics
  • Androstenes / pharmacology*
  • Androstenes / therapeutic use
  • Animals
  • Contraceptive Agents, Female
  • Female
  • Humans
  • Menstruation / drug effects
  • Menstruation / physiology
  • Menstruation Disturbances / drug therapy
  • Progesterone / physiology
  • Progesterone Congeners / pharmacokinetics
  • Progesterone Congeners / pharmacology*
  • Progesterone Congeners / therapeutic use
  • Receptors, Androgen / drug effects
  • Receptors, Androgen / physiology
  • Receptors, Steroid / drug effects
  • Receptors, Steroid / physiology
  • Renin-Angiotensin System / drug effects
  • Testosterone / metabolism

Substances

  • Androstenes
  • Contraceptive Agents, Female
  • Progesterone Congeners
  • Receptors, Androgen
  • Receptors, Steroid
  • Testosterone
  • Progesterone
  • drospirenone