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Abstract
The pharmacological properties of progestins used in contraception and hormone replacement therapy (HRT) vary, depending upon the molecules from which they are derived. Very small structural changes may induce considerable differences in effects. It is unclear if the currently available progestins are able to bind specifically to the progesterone receptors, PR-A or PR-B. The clinical relevance of more specific binding to one or the other isoforms of the progesterone receptor is still unknown. The development of new generations of progestins, with improved receptor-selectivity profiles, has been a great challenge. Steroidal and non-steroidal progesterone agonists have also been synthesized, although these molecules are at a very early stage of development. Several new progestins have been synthesized in the past decade, including dienogest, drospirenone, Nestorone, nomegestrol acetate and trimegestone.
Drospirenone differs from the classic progestins in its derivation from spirolactone. The major effect of drospirenone is antimineralocorticoid activity. By that property, drospirenone causes decreased salt and water retention, and thus lowering of blood pressure. The affinity of drospirenone for the mineralocorticoid receptor is about five times that of aldosterone, the naturally occurring mineralocorticoid. In addition, drospirenone has no androgenic effect, but does exhibit partial antiandrogenic activity; its antiandrogenic potency is about 30% of that of cyproterone acetate, the progestin with the most potent antiandrogenic activity. This property, shared by several new progestins, may counteract the negative effect of androgens on hair growth, lipid changes, insulin and, possibly, body composition in postmenopausal women.
Drospirenone has a long terminal half-life (about 32 hours), and its bioavailability is about 76%. Drospirenone, which has pharmacodynamic properties very similar to those of progesterone, has been developed as a combined oral contraceptive (30 μg ethinylestradiol/3 mg drospirenone; Yasmin®, Schering AG, Berlin, Germany). Drospirenone is also available in combination with estradiol as an HRT preparation (1 mg 17β-estradiol/2 mg drospirenone; Angeliq®, Schering AG).