Cyproterone acetate (CPA) was first introduced as a medication in the 1970s. It was initially used primarily as a treatment for prostate cancer due to its antiandrogenic properties. However, over time, CPA has also been found to be effective for a variety of other conditions. This article will mainly focus on the uses cyproterone acetate in dermatolgy. It has been used in dermatology for the treatment of various skin conditions, particularly those that are related to hormonal imbalances. Cyproterone acetate (CPA) is a synthetic progestogen that acts as both an antiandrogen and an inhibitor of gonadotrophin secretion.
Mechanism of action of cyproterone acetate
- The mechanism of action of cyproterone acetate (CPA) is related to its ability to block the androgen receptor, which reduces the effects of androgens in the body.
- It also has progestogenic activity, which can help to regulate the menstrual cycle. CPA is often used in combination with an estrogen-containing oral contraceptive pill.
- Cyproterone acetate (CPA) can inhibit gonadotropin secretion. Gonadotropins are hormones that are produced by the pituitary gland and play a key role in regulating the function of the reproductive system.
What are the indications of cyproterone acetate in dermatology?
- Acne: CPA is often used in combination with an estrogen-containing oral contraceptive pill to treat moderate to severe acne in women with seborrhea . The combination of CPA and estrogen helps to reduce the production of sebum, which can contribute to acne.
- Hirsutism: CPA may be used to treat excessive hair growth in women (hirsutism) that is caused by an excess of androgens. CPA helps to block the effects of androgens on the hair follicles, which can reduce hair growth.
- Femal pattern hair loss: CPA may be used to treat androgenetic alopecia in women. CPA helps to block the effects of androgens on the hair follicles, which can slow or stop hair loss.
- Hyperandrogenism: CPA may be used to treat hyperandrogenism, which is an excess of androgens in the body. This condition can cause a variety of symptoms, including acne, hirsutism, and hair loss.
What is the doage of cyproterone acetate?
Cyproterone acetate should be taken on the first or fifth day of the menstrual cycle and end on the fourteenth day, right before ovulation. The suggested dose is 50 to 100 mg per day is advised for use when taken alone.
Two forms of CPA are usually used
- Cyproterone acetate (2 mg) and ethinyl estradiol (35 or 50 mcg) are combined together in contraceptive formulation. e.g Diane-35 should be started on the first day of the menstrual cycle (i.e. the first day of menstruation) and subsequent tablets should be taken daily at approximately the same time each day for 21 days, with or without food, there is usually a seven-day break during which no tablets are taken. During this break, a withdrawal bleed similar to a period usually occurs. Regardless of whether the withdrawal bleed has stopped or not. The first tablet of the new cycle is taken on the eighth day.
- Cyproterone acetate (50-100) alone formulations are also available e.g Androcur 50 mg per day may be taken for 10 days each month, typically starting on the first day of the menstrual cycle. The dose can be modified according to response.
The combination of CPA and a contraceptive may provide better control of androgen levels and menstrual cycles, as well as reliable contraception.
What are the side effects of Cyproterone acetate?
Side effects are more frequent with higher dosage.
Common side effects
- Breast tenderness or enlargement (in both men and women)
- Irregular menstrual bleeding (in women)
- Nausea and vomiting
- Headache
- Fatigue
- Dizziness
Rare side effects
- Decreased libido (sex drive)
- Mood changes, such as depression or anxiety
- Liver problems, including jaundice
- Blood clots or other cardiovascular problems (rare).
What are the contraindications of Cyproterone acetate?
Cyproterone acetate `s contraindications are the same as for the contraceptive pill. Venous thromboembolism is the adverse effect of greatest medical signifcance. Other contraindications include :
- History of liver disease: CPA can cause liver problems, so it is contraindicated in people with a history of liver disease or liver problems.
- Breast cancer: CPA is not recommended for use in people with a history of breast cancer or current breast cancer.
- Pregnancy: CPA is contraindicated during pregnancy, as it can cause feminization of a male fetus
It should be halted before trying to get pregancy. - Allergies: CPA is contraindicated in people who are allergic to cyproterone acetate or any of the other ingredients in the medication.
Can cyproterone acetate be used by postmenopausal women?
Cyproterone acetate, with or without oestrogens, may be taken continuously
by postmenopausal women.
What are the forms of Cyproterone acetate in the market?
Cyproterone acetate (CPA) is available in several forms for different indications. Here are some of the forms of CPA that are available in the market:
- Oral tablets: CPA is commonly available in the form of oral tablets, which are taken by mouth. These tablets may be available in various strengths, depending on the indication for which they are being used.
- Combination tablets: CPA is often used in combination with other medications for the treatment of certain conditions, such as acne and hirsutism in women. Combination tablets that contain CPA and ethinyl estradiol (EE), a form of estrogen, are available as oral contraceptives.
- Topical cream/gel: CPA is also available in the form of a topical cream or gel for the treatment of acne and other dermatological conditions. These formulations are applied directly to the affected area of the skin.
- Injectable solution: CPA is available as an injectable solution for the treatment of prostate cancer.
What are the brand names of cyproterone acetate?
Cyproterone acetate (CPA) is available under different brand names depending on the country and manufacturer. Here are some of the common brand names for CPA:
- Androcur: This is a brand name for CPA that is available in many countries, including Europe, Canada, and Australia. Androcur is available in various strengths and formulations, including tablets and injections.
- Diane-35: This is a combination drug that contains CPA and ethinyl estradiol, a form of estrogen. Diane-35 is used primarily as an oral contraceptive but is also approved for the treatment of acne and hirsutism in women. Diane-35 is available in many countries, including Europe, Canada, and Australia.
- Cyprostat: This is a brand name for CPA that is available in the United Kingdom. Cyprostat is available as an oral tablet and is used primarily for the treatment of prostate cancer.
- Siterone: This is a brand name for CPA that is available in some countries, including Australia and India. Siterone is available as an oral tablet and is used primarily for the treatment of prostate cancer.
It is important to note that the availability and specific formulations of CPA may vary depending on the country and healthcare system.