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Clin Ther. 1990 Sep-Oct;12(5):447-55.

Clinical significance of the androgenicity of progestins in hormonal therapy in women.

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Department of Obstetrics and Gynecology, Saint Joseph Hospital, Evanston, Illinois.


Optimal efficacy has been achieved in both oral contraception and postmenopausal replacement therapy. The current challenge is to minimize the side effects and metabolic impact of the administered hormones in both oral contraceptives and hormone replacement agents. When the dose of estrogen in oral contraceptives was reduced the risk of thromboembolism decreased, but the androgenic side effects of the progestin became increasingly apparent. The addition of progestins to hormone replacement therapy reduces the risk of endometrial cancer associated with unopposed estrogen, but their androgenicity offsets the favorable effects of estrogen on lipid metabolism. Androgens not only cause troublesome clinical side effects but also induce changes in blood levels of lipoproteins that have been associated with an increased risk of atherogenesis and coronary heart disease, as well as alterations in glucose and insulin levels. Both the side effects and the adverse effects on lipoprotein and glucose metabolism can be reduced by the use of less androgenic progestins.


In order to offset the undesirable clinical effects of progestins in oral contraceptives (OCs) or in hormone replacement therapy, effort has been made to reduce the amount of progestin used and to use progestins with lower androgenicity. It is pointed out that the androgenicity is related to the structural relationship between progestins and 19-nortestosterone. Based on the relative binding affinities (RBAs) for rat prostatic androgen receptors and for sex hormone binding globulin (SHBG), it has been noted that levonorgestrel, which is the active isomer of norgestrel, has twice the androgenicity of norethisterone. There have been research results which confirm OCs with progestins with reduced androgenicity; research shows norethindrone in Ortho-Novum 7/7/7 and levonorgestrel in Triphasil both minimize the effect on lipid metabolism. Another study shows only those more androgenic progestins reduce HDL. The newest low dose progestins in OCs are norgestimate, desogestrel, and gestodene. The action of progestins is on lipid and carbohydrate metabolism.

[Indexed for MEDLINE]

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