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Hair Removal Prescription Oral Medications

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6 Hair Removal Prescription Oral Medications - 2

1. Spironolactone (Aldactone)
2. Finasteride (marketed as Propecia and Proscar)
3. Flutamide
4. Cyproterone acetate (not available in the US)
5. Ketoconazole
6. Gonadotrophin releasing hormone agonists

3. Flutamide
   Flutamide is a potent antiandrogen that strongly binds to androgen receptors on cells in hair follicles. The binding of Flutamide to cell androgen receptors blocks androgens from stimulating hair growth.

   Studies that compare flutamide to spironolactone or cyproterone acetate suggest that overall the beneficial effects on reducing hirsutism are similar. Some suggest flutamide is slightly superior and others say it is slightly less superior. Initially flutamide was given to patients at high dose rates of up to 250mg three times a day. However more recent studies indicate that a similar improvement in hirsutism can be obtained with flutamide doses as low as 62.5mg a day. The reduction in dose significantly reduces the risk of side effects.

   For a small subgroup of women flutamide and other oral antiandrogens are highly toxic. Between February 1989 and December 1994 the Food and Drug Administration (FDA) received reports of 20 patients who died and 26 who were hospitalized for hepatotoxicity due to flutamide, a rate around 3 per 10,000 flutamide users.

   Early symptoms of hepatotoxicity include nausea, vomiting, fatigue and jaundice and if such symptoms occur they must be immediately reported to a doctor. Dermatologists generally recommend that serial blood aminotransferase levels should be monitored during the first few months of flutamide treatment. Any adverse aminotransferase level changes suggest that hepatotoxicity is a significant risk and flutamide use should be stopped. For this and other reasons, some dermatologists do not use flutamide to treat hirsutism however, the side effect risk of flutamide is no better or worse than other oral antiandrogens

4. Cyproterone Acetate (not available in the US)
   Cyproterone acetate (CPA) was first used to treat hirsutism experimentally in 1965 and was brought to the attention of dermatologists by Hammerstein and colleagues in Germany. Since then it has become a very popular oral antiandrogen in Europe, Canada, and South America. Flutamide may have slightly a superior ability to reduce hirsutism as compared to CPA, but CPA is significantly cheaper than Flutamide and so is a popular choice in those countries where CPA is available.

   Some dermatologists suggest that the effects of spironolactone are somewhat inferior to cyproterone acetate (CPA). However, CPA is not available in the US.

   Several different treatment approaches have been tried with CPA. 50-100mg per day of CPA orally on days 1-10 of the menstrual cycle along with a triphasic oral contraceptive is a popular treatment regime with some dermatologists, particularly in Mediterranean countries. However, this is regarded as overkill by some Northern European dermatologists who specialize in treating hair conditions. Dosages of 100mg CPA per day are used for people with ovarian tumors or for sex offenders, but may not be necessary for treating idiopathic hirsutism. Several studies comparing different CPA dosage rates have shown no significant difference in the treatment of hirsutism when using 100mg or 2mg of CPA. A few dermatologists use high dose CPA initially and then drop the dosage for long term use.

   Low dose CPA treatment protocols include; oral ingestion of 2mg CPA plus estradiol on days 5-25 of the menstrual cycle, or just 1mg of CPA on days 12 to 21 of the menstrual cycle plus estradiol for 21 days. Low dose CPA use reduces the risk of side effects while having similar positive benefits in treating hirsutism. There are many other protocols for treating hirsutism using different CPA doses or different times of application during the monthly cycle. No clear advantage has been demonstrated for a particular CPA treatment regime and the personal preference of the dermatologist seems to be the greatest factor in deciding CPA dose levels.
   CPA is not available in the US in any form and only certain formulations of CPA are available in other countries.

   The most commonly available form of CPA is in combination with estradiol in tablets called Diane (Diane 35) or Dianette (Diane 50) both of which are advertised for treating acne in women, but have been utilized for treating other androgen based conditions such as hirsutism. However, while both Diane and Dianette are available in Canada, only Diane is available in the UK. CPA in its various forms is made by the Germany based Schering AG pharmaceutical company.

   Both Diane and Dianette contain 2mg of CPA but Diane contains 35mg of estradiol and Dianette contains 50mg of estradiol. The Dianette tablets have a significant property in that they increase sex hormone binding globulin (SHBG) levels in the blood whereas the lower estradiol dose in Diane does not. The increase in SHBG has a positive benefit as SHBG binds to testosterone and stops it from being converted to dihydrotestosterone and having an affect on hair follicles. However, high dose estradiol is potentially toxic and some women are unable to tolerate the negative effects of Dianette.

   CPA and estradiol combined also has potential to induce other side effects. Some suspicions have been cast on long term CPA and estradiol use and the potential for a reduction in bone mass. However, recent research studies suggest there are no apparent negative effects. Other side effect risks include weight gain, fatigue, nausea, headaches, depression, and impairment of liver function. Some dermatologists recommend testing vitamin B12 levels in CPA users. CPA can cause B12 levels to drop and this can lead to depression or anxiety problems. Vitamin B12 supplements can rectify the problem.
   As with all systemic antiandrogens, serious side effects will develop in a male embryo of a pregnant user. Although CPA is a powerful proestrogen it does not necessarily stop ovulation. Consequently, contraception with cyclical estrogen supplements is vital when using CPA.

1. Spironolactone (Aldactone); 2. Finasteride (marketed as Propecia and Proscar)
5. Ketoconazole; 6. Gonadotrophin releasing hormone agonists