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Orally active progesteron Chlormadinone acetate
Orally active progesteron Chlormadinone acetate Used in combinations as an oral contraceptiveSynonyms: 17-(Acetyloxy)-6-chloropregna-4,6-diene-3,20-dioneCAS: 302-22-7Einecs:206-118-0 MF: C23H29ClO4MW: 404.93Standard: CP2000, JP13 Appearance: white crystalline powder Assay: 99% Packing: Foil bagUsage: Orally active progesteron with antiandrogenic activity; has been used in combinations as an oral contraceptive. Progestogen; antineoplastic (hormonal)Chlormadinone acetate (INN, USAN, BAN, JAN) (sold under brand names including Clordion, Gestafortin, Lormin, Non-Ovlon, Normenon, Verton, and many others), sometimes abbreviated as CMA, and also known as 17α-acetoxy-6-chloro-6-dehydroprogesterone, is a steroidal progestin with additional antiandrogen and antigonadotropic (and by extension antiestrogenic) effects.It is used clinically as a hormonal contraceptive, and in part due to its capacity to lower estrogen levels, but also for improved effectiveness in contraception, chlormadinone is frequently combined with ethinyl estradiol for this purpose.It is the acetate ester of chlormadinone.Like other steroidal progestins with antiandrogen properties such as cyproterone acetate, medroxyprogesterone acetate, and megestrol acetate, as well as spironolactone (a steroidal antimineralocorticoid with antiandrogen and progestogen properties), but unlike non-steroidal antiandrogens such as flutamide and bicalutamide, chlormadinone acetate is not a silent antagonist of the androgen receptor (AR) but rather a weak partial agonist of the AR with the capacity to activate the receptor in the absence of more efficacious agonists such as testosterone.Similarly to other 17-hydroxyprogesterone derivatives such as cyproterone acetate, medroxyprogesterone acetate, and megestrol acetate, chlormadinone acetate is a weak glucocorticoid, and has the potential to cause adrenal insufficiency upon abrupt discontinuation of the drug at sufficient dosages.Chlormadinone acetate is a competitive inhibitor of 5α-reductase.
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