Oral contraceptives studied in acne
Oral contraceptives generally contain an estrogen (most commonly ethinyl estradiol) and a progestin. In their early formulations, oral contraceptives contained over 100 mg of estrogen. In these and higher doses, estrogens themselves can suppress sebum production. Estrogens also act on the liver to increase the synthesis of sex hormone-binding globulin that binds testosterone and lowers the circulating levels of free testosterone. In addition, oral contraceptives inhibit the ovarian production of androgens by suppressing ovulation. This, in turn, decreases serum androgen levels and reduces sebum production. The concentrations of estrogen in oral contraceptives have decreased over the years from 150 to 35 mg, and in the most recent forms, to 20 mg, in order to reduce the side effects associated with estrogen. Oral contraceptives containing low doses of estrogen are listed in Table 1.
TABLE 1: Oral Contraceptives Containing Low Doses of Estrogen
Ethinyl estradiol 20 mg/Levonorgestrel 0.1 mg (AlesseTM)
Ethinyl estradiol 20, 10 mg/Desogestrel 0.15 mg (MircetteTM)
Ethinyl estradiol 20, 30, 35 mg/norethindrone 1.0 mg (Estrostepw)
Ethinyl estradiol 20 mg/norethindrone acetate 1.0 mg (Lo-Estrinw 1/20)
Ethinyl estradiol 20 mg/drospirenone 3.0 mg (YazTM)
Many oral contraceptives have been studied in the treatment of acne (Table2 ). These include those containing ethinyl estradiol in combination with cyproterone acetate (Diane, Dianette), ethynodiol diacetate (Demulen), levonorgestrel (TriPhasil, Alesse), norgestimate (Ortho Tri-Cyclenw), desogesterel (Desogen), and drosperinone (Yasmin, Yaz). Numerous studies point to the efficacy of ethinyl estradiol/cyproterone acetate oral contraceptives (Diane and Dianette) in the treatment of acne. Reductions in inflammatory lesion count on the order of 50% to 75% have been reported. Two large studies involving a total of approximately 500 women with moderate acne were conducted with ethinyl estradiol 35 mg/norgestimate (Ortho Tri-Cyclen). Improvement in inflammatory lesions, total lesions, and global assessment was noted with this oral contraceptive after six months of treatment (46,47). There was a 50% to 60% improvement in inflammatory lesions. Decreases in serum free testosterone and an increase in sex hormone-binding globulin were noted in the active group. Two large, six-month, placebo-controlled trials (350 and 371 women, respectively) were conducted
TABLE 2 Oral Contraceptives Studied in Acne
Demulen (ethinyl estradiol 35 mg/ethynodiol diacetate)
Diane, Dianette (ethinyl estradiol 50, 35 mg/cyproterone acetate)
Estrostep (ethinyl estradiol 20, 25, 30 mg/norethindrone)
Alesse (ethinyl estradiol 20 mg/levonorgestrel)
Ortho Tri-Cyclen (ethinyl estradiol 35 mg/norgestimate)
Desogen (ethinyl estradiol 30 mg/desogestrel)
Yasmin (ethinyl estradiol 30 mg/drospirenone)
Yaz (ethinyl estradiol 20 mg/drospirenone)
Triphasil (ethinyl estradiol 30 mg, 40 mg/levonorgestrel)
using ethinyl estradiol 20 mg/levonorgestrel (Alesse) in the treatment of acne. In each study, the oral contraceptive demonstrated significantly greater reduction in acne lesion counts and improvement in global assessment scores compared with placebo. The reduction in inflammatory lesion count was on the order of 47%. A study of 128 women with mild-to-moderate acne compared the efficacy of ethinyl estradiol 30 mg/drospirenone (Yasmin) and ethinyl estradiol 35 mg/cyproterone acetate (Diane-35) in the treatment of acne for nine cycles (50). Both treatments produced comparable reductions in acne lesion counts, with an approximate 60% reduction in inflammatory lesion count. Both treatments also reduced sebum production and yielded comparable increases in sex hormone-binding globulin. Two large placebo-controlled studies involving a total of approximately 593 women with moderate acne, found improvement in inflammatory lesions, total lesions, global assessment, and quality of life in women who were treated for six months with a triphasic oral contraceptive that contains doses of 20 to 35 mg of ethinyl estradiol in combination with 1.0 mg norethindrone acetate (Estrostep). In these studies, inflammatory lesion counts were reduced by approximately 47% .
Oral contraceptives that have been approved for the treatment of acne in the United States include ethinyl estradiol 35 mg/norgestimate (Ortho Tri-Cyclen) ethinyl estradiol 20 to 35 mg/norethindrone acetate (Estrostep), and ethinyl estradiol 20 mg/drospirenone (Yaz).
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