Progestins

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The progestins contained in oral contraceptives include estranges and gonanes, which are derivatives of 19-nortestosterone, cyprotereone acetate, and a novel progestin, drosperinone. Members of the estrane and gonane class of progestins (Table 2) can cross-react with the androgen receptor, which can lead to increased androgenic effects and could aggravate acne, hirsutism, or androgenic alopecia. These progestins can also cause changes in lipid metabolism and can increase serum glucose, leading to glucose intolerance, as well as possibly interfering with the beneficial effect of estrogen on the sex hormone-binding globulin. However, the third generation progestins, including norgestimate, desogestrel, and gesto-dene, are more selective for the progesterone receptor rather than the androgen receptor. The biological relevance of these differences, however, is uncertain. For

TABLE 1 Oral Contraceptives Containing Low Doses of Estrogen

Ethinyl estradiol 20 mg/Levonorgestrel 0.1 mg (Alesse™) Ethinyl estradiol 20, 10 mg/Desogestrel 0.15 mg (Mircette™) Ethinyl estradiol 20, 30, 35 mg/norethindrone 1.0 mg (Estrostep®) Ethinyl estradiol 20 mg/norethindrone acetate 1.0 mg (Lo-Estrin® 1 /20) Ethinyl estradiol 20 mg/drospirenone 3.0 mg (Yaz™)

TABLE 2 Progestins: 19-Nortestosterone Derivatives

Estranes Norethindrone Norethindrone acetate Ethynodiol diacetate

Gonanes Norgestrel

Levonorgestrel

Desogestrel Gestodene

Norgestimate years, it has been known that almost all oral contraceptives are beneficial in the treatment of acne (42). It is possible that some women are more sensitive to the androgenic effects of a progestin, but it is more likely that the effect of progestin may be offset by estrogen. All oral contraceptives, regardless of the type of progestin, will inhibit serum androgen levels. Moreover, although some progestins might be more androgenic than others, there is an increase in sex hormone-binding globulin with the use of any oral contraceptives and an improvement of the acne in women who are treated with them.

Drospirenone is a novel progestin that is derived from 17a-spironolactone. It possesses antiandrogenic and antimineralocorticoid activity, which can be of benefit in androgenic-related conditions such as acne and hirsutism and in the estrogen-related fluid retention associated with some oral contraceptives (43).

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