Profile of the progesterone derivative chlormadinone acetate - pharmocodynamic properties and therapeutic applications

René Druckmann


Chlormadinone acetate (CMA) is a derivative of progesterone (17alpha-acetoxy-6-chloro-4,6-pregnadiene-3,20-dione), first synthesized in 1961 and is used as an orally effective progestogen in hormone replacement therapy (HRT), and in combination with ethinyl estradiol (EE) in contraception since 1999. Chlormadinone acetate has a strong progestogenic effect - about one-third higher than that of progesterone - and may vary depending on the previous effect of an estrogen, i.e., estrogens may promote the formation of progesterone receptors and proliferation of the endometrium. Like progesterone, it is anti-estrogenic and has no partial androgenic effect (at the doses used for contraception and HRT). In contrast to progesterone, it has a slight glucocorticoid effect, a pronounced anti-androgenic effect and no anti-mineralocorticoid effect. No pregnancy-maintaining effect of CMA has been demonstrated in humans. The anti-androgenic effect of CMA is presumed to be the result of both its binding to androgen receptors - competitively inhibiting the effect of endogenous testosterone and dihydrotestosterone - and the competitive inhibition of 5alpha-reductase. In this respect, dosing of CMA is crucial; agonistic effects are observed when do...Continue Reading


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