Drospirenone: a Novel Progestogen with Antimineralocorticoid and Antiandrogenic Activity

  title={Drospirenone: a Novel Progestogen with Antimineralocorticoid and Antiandrogenic Activity},
  author={Peter Muhn and Ulrike Fuhrmann and Karl Heinrich Fritzemeier and Rolf Krattenmacher and Ekkehardt Schillinger},
  journal={Annals of the New York Academy of Sciences},
Drospirenone (ZK 30595; 6 beta, 7 beta, 15 beta, 16 beta-dimethylen-3-oxo-17 alpha-pregn-4-ene-21, 17-carbolactone) is a novel progestogen under clinical development. Drospirenone is characterized by an innovative pharmacodynamic profile which is very closely related to that of progesterone. Potential applications include oral contraception, hormone replacement therapy and treatment of hormonal disorders. The pharmacological properties of drospirenone were investigated in vitro by receptor… 

Drospirenone, a progestogen with antimineralocorticoid properties: a short review

  • W. Oelkers
  • Medicine, Biology
    Molecular and Cellular Endocrinology
  • 2004

Drospirenone and its antialdosterone properties

The combined actions of drospirenone on sodium and water retention and cardiovascular parameters make it a more attractive therapeutic option as a component of hormone replacement therapy than other synthetic progestins.

Drospirenone in combination with estrogens: for contraception and hormone replacement therapy

  • W. Oelkers
  • Medicine, Biology
    Climacteric : the journal of the International Menopause Society
  • 2005
Drospirenone is not only a safe option for women using oral contraceptives or HRT, but it may offer new medical benefits, via its antimineralocorticoid and antialdosterone effects and its potential to decrease water retention and blood pressure.

Pharmacology of different progestogens: the special case of drospirenone

  • R. Sitruk-Ware
  • Biology, Medicine
    Climacteric : the journal of the International Menopause Society
  • 2005
Drospirenone, which has pharmacodynamic properties very similar to those of progesterone, has been developed as a combined oral contraceptive and may counteract the negative effect of androgens on hair growth, lipid changes, insulin and, possibly, body composition in postmenopausal women.

Antiadipogenic effects of the mineralocorticoid receptor antagonist drospirenone: potential implications for the treatment of metabolic syndrome.

Drospirenone exerts a potent antiadipogenic effect that is related to an alteration of the transcriptional control of adipogenesis via an antagonistic effect on the MR, and has promise as a novel therapeutic option for the control of excessive adipose tissue deposition and its related metabolic complications.



Dihydrospirorenone, a new progestogen with antimineralocorticoid activity: effects on ovulation, electrolyte excretion, and the renin-aldosterone system in normal women.

It is concluded that DHSP may be a suitable partner of ethinyl estradiol as a constituent of an oral contraceptive, since its progestogenic and antialdosterone profile is similar to that of progesterone.

Interaction of synthetic progestagens with renal mineralocorticoid receptors.

The decreased affinity of synthetic progestins for mineralocorticoid receptors explains in part the lack of natriuretic activity of these compounds.

Progestogens with antimineralocorticoid activity.

Gestodene may be regarded as the first progestogen of the nortestosterone series exhibiting a more natural, progesterone-like profile of activity and the antimineralocorticoid activity of the steroids tested could also be demonstrated after oral administration.

Effects of progesterone and four synthetic progestagens on sodium balance and the renin-aldosterone system in man.

The influence of treatment with progesterone and with 4 synthetic progestagens for 6 days on sodium balance and on different factors of the renin-aldosterone system was investigated in 20 young healthy men on a fixed sodium intake.

Relation Between Estrogen Inhibitory Activity and Binding to Cytosol of Rabbit and Human Uterus

It is suggested that all these inhibitors are weak estrogens competing effectively for uterine receptors when in high concentration, but rapidly lost from the target organ as a result of their low association constants for the specific binding site.

The metabolic effects of progesterone in man.

It has been demonstrated that progesterone induces growth in the sebaceous glands of rats, and in a man with Addison's disease who was maintained with added salt, 30 mg.