CPA has also been available in combination with estradiol valerate (brand name Femilar) as a combined birth control pill in Finland since 1993.
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The formulation is taken once daily for 21 days, followed by a 7-day free interval. This birth control combination has been available since 1978. Birth control ĬPA is used with ethinylestradiol as a combined birth control pill to prevent pregnancy. The steroidal antiandrogen and progestin chlormadinone acetate is used as an alternative to CPA in Japan, South Korea, and a few other countries. Examples of such medications include gonadotropin-releasing hormone modulators (GnRH modulators) like leuprorelin and degarelix, nonsteroidal antiandrogens like flutamide and bicalutamide, the diuretic and steroidal antiandrogen spironolactone, the progestin medroxyprogesterone acetate, and the 5α-reductase inhibitors finasteride and dutasteride. In the United States, where CPA is not available, other medications with antiandrogenic effects are used to treat androgen-dependent conditions instead. It is used both at low doses and at higher doses.
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Specifically, CPA is used in combined birth control pills, in the treatment of androgen-dependent skin and hair conditions such as acne, seborrhea, excessive hair growth, and scalp hair loss, high androgen levels, in transgender hormone therapy, to treat prostate cancer, to reduce sex drive in sex offenders or men with paraphilias or hypersexuality, to treat early puberty, and for other uses. ĬPA is used as a progestin and antiandrogen in hormonal birth control and in the treatment of androgen-dependent conditions. An exception is the United States, where it is not approved for use. CPA is available widely throughout the world. It has been described as a "first-generation" progestin and as the prototypical antiandrogen. A few years later, in 1978, CPA was introduced as a progestin in a birth control pill. CPA was first marketed, as an antiandrogen, in 1973, and was the first antiandrogen to be introduced for medical use.
In 1965, the antiandrogenic effects of CPA were discovered. It was originally developed as a progestin. It can also produce weak cortisol-like effects at very high doses. In addition, it has progesterone-like effects by activating the progesterone receptor (PR).
CPA blocks the effects of androgens such as testosterone in the body, which it does by preventing them from interacting with their biological target, the androgen receptor (AR), and by reducing their production by the gonads, hence their concentrations in the body. CPA can also cause adrenal insufficiency as a withdrawal effect if it is discontinued abruptly from a high dosage. Rare but serious adverse reactions of CPA include blood clots, liver damage, and certain types of benign brain tumors. At very high doses in older individuals, significant cardiovascular complications can occur. In both men and women, possible side effects of CPA include low sex hormone levels, reversible infertility, sexual dysfunction, fatigue, depression, weight gain, and elevated liver enzymes. CPA is taken by mouth one to three times per day.Ĭommon side effects of high-dose CPA in men include gynecomastia (breast development) and feminization. It is formulated and used both alone and in combination with an estrogen. Cyproterone acetate ( CPA), sold alone under the brand name Androcur or with ethinylestradiol under the brand names Diane or Diane-35 among others, is an antiandrogen and progestin medication used in the treatment of androgen-dependent conditions such as acne, excessive body hair growth, early puberty, and prostate cancer, as a component of feminizing hormone therapy for transgender women, and in birth control pills.