Ebling F J, Randall V A
J Steroid Biochem. 1983 Jul;19(1B):587-90. doi: 10.1016/0022-4731(83)90222-4.
Antiandrogens, such as cyproterone acetate, and oestrogens both inhibit sebaceous secretion in rats and have a potentiality for the treatment of hirsutism and acne in the human female. However, they act at different points. In castrated rats treated with testosterone, 3 micrograms/day oestradiol produced a greater decrease in sebum secretion than a dose of cyproterone acetate over 1000 times larger; moreover the antiandrogen reduced the incidence of sebaceous mitoses whereas the oestradiol did not. In hirsute women, oral administration of 100 mg of cyproterone acetate daily caused a 40% reduction in sebum secretion within 10 days; a further 20% was subsequently produced by combined therapy with cyproterone acetate and ethinyloestradiol. Significant decreases in the diameter and rate of growth of thigh hairs were not established until around the fourth monthly cycle of treatment. The actions were believed to be mainly peripheral, though contributory factors could also have been the small but significant reductions in plasma androgens produced by the antiandrogen, and the marked rise in sex hormone binding globulin produced by the oestrogen. That it is theoretically possible for cyproterone acetate or oestradiol to act locally follows from an unequivocal demonstration that either compound produced a local depression of sebum secretion when applied topically to rats.
抗雄激素药物，如醋酸环丙孕酮，以及雌激素均可抑制大鼠的皮脂腺分泌，并且具有治疗女性多毛症和痤疮的潜力。然而，它们的作用点不同。在用睾酮治疗的去势大鼠中，每天3微克的雌二醇比剂量超过其1000倍的醋酸环丙孕酮使皮脂分泌的减少幅度更大；此外，抗雄激素药物降低了皮脂腺有丝分裂的发生率，而雌二醇则没有。在多毛女性中，每天口服100毫克醋酸环丙孕酮可在10天内使皮脂分泌减少40%；随后，醋酸环丙孕酮与炔雌醇联合治疗又使其进一步减少了20%。直到治疗大约第四个月周期左右，大腿毛发的直径和生长速度才出现显著下降。这些作用被认为主要是外周性的，不过促成因素也可能是抗雄激素药物使血浆雄激素出现的虽小但显著的降低，以及雌激素使性激素结合球蛋白显著升高。从明确的证据可知，当将醋酸环丙孕酮或雌二醇局部应用于大鼠时，这两种化合物都会使局部皮脂分泌减少，因此从理论上讲它们有可能在局部发挥作用。
