Oral Contraceptives: Their Mode of Action and Dermatologic Applications

Milena Pitashny, MD; Helena Martinez de Morentin, MD; Sarah Brenner, MD


Skinmed. 2005;4(2):101-104, 106. 

In This Article


The first contraceptive pill available for human use in 1960 contained the estrogen mestranol, an ethinyl-estradiol precursor, in a very high concentration (150 mg), and norethynodrel, a 19-nortestos-terone derivate progestin.[1] The high dose of estrogen in these pills was implicated in the development of cardiovascular and thromboembolic events, and starting in 1970 the doses of ethinyl estradiol were significantly reduced. Modern pills, known as "low-dose oral contraceptives (OCs)," contain ethinyl estradiol at concentrations of 20-35 µg. The subsequent discovery of deleterious effects of progestin on the lipid profile prompted a flurry of research into OCs that led to an understanding of the mechanism of action of the combination of estrogen and progestin, its influence on androgenic metabolism, and the development of new synthetic progestins to replace the "old" ones. These innovative OCs were found to be safe in young healthy women without risk factors for heart disease, lipid disorders, or glucose metabolism disorders.

OCs have also been found useful in the treatment of several gynecological and dermatological disorders. It has been known for years that the interference of OCs in hormonal metabolism benefits acne treatment, and today they are an accepted treatment for mild-to-moderate acne as well as hirsutism in healthy women.

It is well known that androgens in the pilosebaceous unit promote skin problems such as acne, seborrhea, hirsutism, and androgenetic alopecia (AGA) ( Table 1 ). Androgen receptors are localized in the basal layer of the sebaceous gland and in keratinocytes of the outer sheath of the hair follicle. Androgens that interact with these receptors are mainly testosterone and dihydrotestosterone; the latter is 5-10 times more potent than the former.


Comments on Medscape are moderated and should be professional in tone and on topic. You must declare any conflicts of interest related to your comments and responses. Please see our Commenting Guide for further information. We reserve the right to remove posts at our sole discretion.