Preclinical profiles of progestins used in formulations of oral contraceptives and hormone replacement therapy.

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Hammond GL, Rabe T, Wagner JD

Preclinical profiles of progestins used in formulations of oral contraceptives and hormone replacement therapy.

Am J Obstet Gynecol. 2001 Aug;185(2 Suppl):S24-31.

PubMed ID

11521119 [ View in PubMed

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Abstract

Progestins used in oral contraceptive formulations available in the United States include norgestimate, desogestrel, norethindrone, norethindrone acetate, and levonorgestrel. Progestins used in the United States in continuous and intermittent formulations of hormone replacement therapy are norgestimate, medroxyprogesterone acetate, and norethindrone acetate. The chemical structure of a progestin determines its relative binding affinity for the progesterone and androgen receptors, as well as the sex hormone binding globulin in human serum, and determines its clinical profile. Overall, the properties of levonorgestrel or norethindrone acetate in this regard differ from norgestimate and are more conducive to androgenic stimulation. Estrogen replacement offers cardioprotective effects in postmenopausal women. Progestins are added to hormone replacement therapy to counteract the well-known increased risk of endometrial hyperplasia associated with the use of unopposed estrogen. Animal models show that for some parameters, including improvement of lipid profiles, progestins can diminish the cardioprotective effect of estrogen. Initial animal studies of norgestimate combined with estrogen do not show an attenuation of estrogenic effects.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Levonorgestrel	Sex hormone-binding globulin	Protein	Humans	Unknown	Inhibitor Binder	Details
Norgestrel	Progesterone receptor	Protein	Humans	Yes	Binder	Details