High purity Progesterone Estrogen Steroids Powder Chlormadinone Acetate CAS 302-22-7 for Contraceptive
Place of Origin:ShenZhen, China (Mainland)
Grade Standard:Medicine Grade
Model Number:a 302-22-7
Product name:Chlormadinone acetate
Chlormadinone acetate (CMA), sold under the brand names Belara, Lutéran, and Prostal among others, is a progestin and antiandrogen medication which is used in birth control pills to prevent pregnancy, as a component of menopausal hormone therapy, and in the treatment of gynecological disorders as well as androgen-dependent conditions like enlarged prostate and prostate cancer in men and acne and hirsutism in women. It is available both at a low dose in combination with an estrogen in birth control pills and, in a few countries like France and Japan, at low, moderate, and high doses alone for various indications. It is taken by mouth.
Side effects of the combination of an estrogen and CMA include menstrual irregularities, headaches, nausea, breast tenderness, vaginal discharge, and others. At high dosages, CMA can cause sexual dysfunction, demasculinization, adrenal insufficiency, and changes in carbohydrate metabolism among other adverse effects. The drug is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It is also an antiandrogen, and hence is an antagonist of the androgen receptor, the biological target of androgens like testosterone and dihydrotestosterone. Due to its progestogenic activity, CMA has antigonadotropic effects. The medication has weak glucocorticoid activity and no other important hormonal activity.
CMA was discovered in 1959 and was introduced for medical use in 1965. It may be considered a "first-generation" progestin. The medication was withdrawn in some countries in 1970 due to concerns about mammary toxicity observed in dogs, but this turned out not to apply to humans. CMA is available widely throughout the world in birth control pills, but is notably not marketed in any predominantly English-speaking countries. It is available alone in only a few countries, including France, Mexico, Japan, and South Korea.
CMA is used at a low dose in combination with ethinylestradiol (EE), an estrogen, in combined birth control pills. It has also been used in the treatment of gynecological conditions including vaginal bleeding, oligomenorrhea, polymenorrhea, hypermenorrhea, dysmenorrhea, secondary amenorrhea, and endometriosis and in France (under the brand name Lutéran) in menopausal hormone therapy in combination with an estrogen. CMA is used at dosages of 1 to 2 mg/day in combined birth control pills and at dosages of 2 to 10 mg/day in the treatment of gynecological disorders. Combined birth control pills containing EE and CMA have been found to be useful in reducing androgen-dependent symptoms such as skin and hair conditions. Dosages of CMA of 15 to 20 mg/day have been found to improve hot flashes.
CMA has been widely used as a means of androgen deprivation therapy in the treatment of prostate cancer and benign prostatic hyperplasia (BPH) in Japan and South Korea, but has seen little use for these indications elsewhere in the world. It is used at dosages of 50 to 100 mg/day in the treatment of prostate diseases. Similarly to cyproterone acetate (CPA), CMA shows a lower risk of hot flashes than gonadotropin-releasing hormone analogues (GnRH analogues). The medication is the only other steroidal antiandrogen besides CPA that has been approved and used for the treatment of prostate cancer; megestrol acetate has also been researched, but has not been approved.
CMA has also been found to be effective in the treatment of other androgen-dependent conditions such as acne, seborrhea, hirsutism, and pattern hair loss in women, similarly to CPA. It has been studied at moderate dosages of 4 to 12 mg/day in the treatment of precocious puberty in girls. It showed similar benefits as those of medroxyprogesterone acetate in these girls and was found to reduce, but not abolish premature development such as breast growth and menstruation. Only slight or no axillary hair growth was observed in the girls. CMA has also been used as a component of hormone therapy for transgender women, similarly to CPA and spironolactone, albeit mostly only in Japan.
See also: Cyproterone acetate § Side effects, Progestin § Side effects, and Antiandrogen § Side effects
The most common side effects of birth control pills containing EE and low-dose CMA have been found to include menstrual abnormalities, headache (37%), nausea (23%), breast tenderness (22%), and vaginal discharge (19%) among others. These formulations do not adversely affect sexual desire or function in women and show little or no risk of depression, mood swings, or weight gain. High-dosage CMA is associated with sexual dysfunction (e.g., reduced libido, erectile dysfunction), reduced body hair, adrenal insufficiency, and alterations in carbohydrate metabolism. Conversely, it does not share adverse effects of estrogens such as breast discomfort and gynecomastia. CMA does not increase the risk of venous thromboembolism. There is a case report of autoimmune progesterone dermatitis with CMA. Similarly to other progestins but in contrast to progesterone, CMA has been found to significantly increase the risk of breast cancer when used in combination with an estrogen in menopausal hormone therapy.No abnormalities in liver function tests have been observed in women taking combined birth control pills containing CMA or CPA. Unlike CPA, high-dosage CMA does not seem to be associated with hepatotoxicity.
Similarly to megestrol acetate and medroxyprogesterone acetate, CMA appears to show less potential for liver genotoxicity and carcinogenicity than CPA in bioassays. This seems to be related to the lack of the C1α,2α methylene group of CPA in these steroids. A case of hepatocellular carcinoma has been reported in a woman taking a birth control pill containing CMA. However, the incidence of liver tumors in women in association with CMA-containing birth control pills appears to be similar to that for birth control pills containing other progestins.