Evolution of progestins. Focus on the novel progestin drospirenone.

Combination oral contraceptives have changed considerably since they were introduced, in 1960. Although ethinyl estradiol has been the primary estrogen in combination oral contraceptives for years, a number of progestogenic agents have been developed. All of the progestins currently used in combination oral contraceptives are derived from 19-nortestosterone. The exception is a new progestin derived from 17 alpha-spirolactone--drospirenone. As compared with that of other progestins used in combination oral contraceptives, drospirenone pharmacology more closely resembles the pharmacology endogenous progesterone. Its antiandrogenic and antimineralocorticoid activities result in special benefits--e.g., improvement in androgen-related disorders (such as acne and hirsutism) and avoidance of estrogen-related fluid retention.