Drospirenone: pharmacology and pharmacokinetics of a unique progestogen.

Article Details

Citation

Krattenmacher R

Drospirenone: pharmacology and pharmacokinetics of a unique progestogen.

Contraception. 2000 Jul;62(1):29-38.

PubMed ID
11024226 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
DrospirenoneAndrogen receptorProteinHumans
Yes
Antagonist
Details
DrospirenoneGlucocorticoid receptorProteinHumans
Unknown
Binder
Details
DrospirenoneMineralocorticoid receptorProteinHumans
Yes
Antagonist
Details
DrospirenoneProgesterone receptorProteinHumans
Yes
Agonist
Details
Drug Reactions
Reaction
Details