Acne vulgaris and hirsutism are important signs related to hyperandrogenaemia and present a serious medical problem for the patients and a challenge for doctors in terms of effective treatment.

Using hormonal contraception to treat acne vulgaris and hirsutism requires knowledge of the mechanism of antiandrogenic actions and the possible contraindications and complications.

Antiandrogenic properties of combined contraception are related to both components of the pill: oestrogen and progestin. Oestrogen stimulates sex hormone binding globulin (SHBG) liver synthesis that in turn reduces the amount of biologically active androgens, induces oestrogen receptor expression, and decreases gonadotrophin secretion that inhibits LH-related testosterone production by theca cells in the ovaries. Progestins block 5α-reductase activity, and decrease testosterone receptor expression and gonadotrophin (FSH, LH) synthesis. 5α-reductase is responsible for the conversion of testosterone into DHT.

Both components of combined contraception lower the levels of adrenocorticotropic hormone (ACTH) that in consequence has inhibitory effect on adrenal androgenesis (dehydroepiandrosterone and dehydroepiandrosterone sulphate production).

Results of clinical studies

The progestins of documented antiandrogenic activity are as follows: levonorgestrel, norethindrone acetate, norgestimate, chlormadinone acetate, dro-spirenone, dienogest, and cyproterone acetate. Cyproterone acetate (2mg of cyproterone acetate and 0.35 of ethinyl oestradiol) after three months of treatment caused subjective improvement in hirsutism in 83%, improvement in trichoscopy in 77%, visible improvement in acne in 40%, and very good cosmetic effect in 26% of patients. 86% of patients finished the study, which suggests very good compliance and tolerability. It showed the stronger antiandrogen activity than dro-spirenone after 12 months of therapy (there was no difference after six months of therapy).

Chlormadinone acetate (2mg of chlormadinone acetate and 0.03mg of ethinyl oestradiol) was effective in the treatment of mild to moderate acne and hirsutism, caused visible improvement in hirsutism and seborrhoea after 12 months of treatment, improvement of acne after three, six, and 12 months of treatment, and a relevant decrease of percentage of patients suffering from acne from 46% to 14% after 13 cycles of treatment.

Chlormadinone acetate reduced the number of patients with skin problems (–55%), reduced the number of patients seeking dermatological treatment (–67%) and concealer cosmetics (–55%) and the number of patients who felt that their self-esteem was restricted due to skin problems (–67%). It was more effective in the treatment of acne than levonorgestrel and was more antiandrogenic than dienogest.

Drospirenone (3mg of drospirenone and 0.02mg of ethinyl estradiol) caused improvement in acne after six months of treatment, significant improvement in the trunk acne (improvement >50%) after six months of treatment and significant reduction of skin problems treatment costs. Drospirenone was more effective in the treatment of acne than norgestimate. It was more effective than chlormadinone acetate in the treatment of skin changes such as seborrhoea, acne, increased hair, hydration, homogeneity, and overall quality of the skin. Dienogest significantly improved acne in 52% of treated patients in one study and in 66% of treated patients in another one and its antiandrogenic properties were also seen in a meta-analysis of 56 clinical studies. It was more antiandrogenic than both drospirenone and chlormadinone acetate.

Reference

Słopień R, Milewska E, Rynio P, et al. Use of oral contraceptives for management of acne vulgaris and hirsutism in women of reproductive and late reproductive age. Prz Menopauzalny. 2018;17:1-4. doi: 10.5114/pm.2018.74895. Epub 2018 Apr 11. PMID: 29725277; PMCID: PMC5925193.