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.
Thorneycroft
Ian H
IH
Mobile Obstetrics and Gynecology Center, University of South Alabama College of Medicine, One Mobile Infirmary Circle, Mobile, AL 36607, USA.
D000726:Androgen Antagonists; D000736:Androstenes / Q000494:pharmacology / Q000627:therapeutic use; D003277:Contraceptives, Oral, Combined; D004997:Ethinyl Estradiol / Q000008:administration & dosage; D005260:Female; D006801:Humans; D008901:Mineralocorticoids / Q000037:antagonists & inhibitors; D045167:Progesterone Congeners / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use
D000726:Androgen Antagonists; D000736:Androstenes; D003277:Contraceptives, Oral, Combined; D008901:Mineralocorticoids; D045167:Progesterone Congeners; D004997:Ethinyl Estradiol; C035144:drospirenone