oral medications

Oral meds work as one of the hair removal methods by reducing the production of androgens (e.g. testosterone), binding to the cell's androgen receptors, and reducing the conversion of androgens to hair follicle stimulating chemicals (i.e. Dihydrotestosterone - DHT). They act to inhibit the growth of hair rather than to remove hairs per se.

The main types of oral medication are Spironolactone, Finasteride, Flutamide, Cyproterone Acetate, Ketoconazole and Gonadotrophin.

A note of caution, there are various side effects in using these medications, such as diuretic symptoms, breast enlargement, increased libido (decreased in men), and foetus abnormalities.

Spironolactone (also known as Aldactone) is arguably the number 1 excess hair growth (hirsutism) treatment of choice for dermatologists. Spironolactone has several properties that make it effective in treating hirsutism. It interferes with and limits the production of androgens and it increases the metabolism of any testosterone that is produced. Spironolactone binds to the cell's androgen receptors and blocks them from binding to naturally produced androgens. With long term use, there is a gradual reduction in type 2 isozyme 5-alpha-reductase activity. It is this activity that converts testosterone to the more potent, hair follicle stimulating, Dihydrotestosterone (DHT)

Treatment protocols may require continuous Spironolactone use at 50mg to 200mg per day or periodic use. Combining this method with an oral contraceptive pill or Dexamethasone appears to have an improved beneficial effect on hirsutism, and limits and removes some of the side effects.

Spironolactone is a diuretic, so it is advised to drink plenty of water during the therapy. The side effects with Spironolactone are generally transient. As with all anti-androgens, Spironolactone therapy should be avoided during pregnancy and in women who have a family history of breast cancer, although there is no proven association between Spironolactone and breast malignancy.

Promoted for use in treating pattern baldness in men, it is a type 2, 5-alpha-reductase inhibitor. This enzyme blocks the conversion of testosterone to the follicles of hairs, stimulating the chemical dihydrotestosterone (DHT).

When Finasteride was first tested on postmenopausal women with pattern baldness there was very little or no response in the subjects. However, in trials for hirsutism, Finasteride has shown some promise. Results with using Finasteride in some hair removal trials have been comparable with other oral anti-androgens. However, a combination of Finasteride plus another anti-androgen have shown an improved effect over using the treatments separately.

Although Finasteride may not be an appropriate treatment in all situations, it is readily available and a relatively safe method. The most significant side effect is experienced by pregnant women with male foetuses, where the male foetus can develop with female genitalia. Professional dermatologists will ensure 1 or more forms of birth control are used by any woman using Finasteride. Other side effects reported in trials include breast enlargement and an increased libido (or decreased libido in men).

Flutamide is a potent anti-androgen that strongly binds to the cell's androgen receptors in hair follicles. The binding of Flutamide to cell's androgen receptors blocks the androgens from stimulating hair growth.

Studies that compare Flutamide to Spironolactone or Cyproterone acetate suggest that overall the effects on reducing excess growth of hairs are similar. Initially Flutamide was given to patients at high dose rates of up to 750mg a day. However more recent studies indicate that a dose as low as 63mg a day is just as effective. Also, the reduction in dose significantly reduces the risk of side effects.

Some users will find Flutamide and other oral anti-androgens are highly toxic. The FDA received reports that 20 patients died and 26 were hospitalised between 1989 and 1994 due to hepatotoxicity as a result of taking Flutamide. Early symptoms of hepatotoxicity include fatigue, nausea, vomiting, and jaundice. Dermatologists usually recommend that aminotransferase levels should be monitored during the first few months of Flutamide treatment. Any increase in aminotransferase levels suggest that hepatotoxicity is a significant risk and Flutamide treatment should be stopped. For this reasons, some dermatologists do not recommend Flutamide to treat hirsutism however, the risk of side effects of Flutamide is no better or worse than other oral anti-androgen hair removal methods.

Cyproterone acetate was first used to treat hirsutism back in 1965. Since then it has become a very popular oral anti-androgen in various parts of Europe, Canada, and South America. Flutamide has a slightly superior ability to reduce hirsutism as compared to CPA, but CPA is significantly cheaper than Flutamide. Some dermatologists suggest that the removal effects of CPA are superior to Spironolactone.

Several different treatment approaches are used with CPA. For example, 50-100mg per day of CPA taken on days 1-10 of the menstrual cycle along with a triphasic oral contraceptive, is a popular treatment regime with some dermatologists. Dosages of 100mg CPA per day are recommended for people with ovarian tumours or for sex offenders. Several studies have compared different CPA dosage rates (100mg to 2mg) and have reported that there are no significant difference in the effectiveness on hair, but low dosages have the benefit that they reduce the risk of side effects. Some dermatologists suggest a high dose of CPA initially and then drop the dosage for long term use.

Low dose treatments 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. Dermatologists will recommend various protocols for treating hirsutism using different doses or different times of treatment during the monthly cycle. There is no clear advantage of one protocol over another; the personal preference of the dermatologist seems to be the greatest factor in deciding CPA dose levels and timings.

The most common method of hair treatment with CPA is in combination with Estradiol in tablets called Diane (Diane 35) or Dianette (Diane 50). Both are marketed for treating acne in women, but have been utilised for treating other androgen based conditions such as hirsutism. Both Diane and Dianette contain 2mg of CPA but Dianette contains more Estradiol. The Dianette tablets, having more Estradiol, increases the sex hormone binding globulin (SHBG) levels in the blood. The increase in SHBG has a positive benefit as it decrease the production of Dihydrotestosterone (DHT) - the chemical that stimulates hair growth. However, a high dosage of Estradiol is potentially toxic and some women are unable to tolerate the stronger Dianette.

Not all countries sell CPA (it is not available in the US) and some only sell certain formulations. However, CPA in all its various forms is available from the German based Schering AG pharmaceutical company. As with all anti-androgen methods, serious side effects will develop in a male embryo of a pregnant user. Consequently, Dermatologists recommend contraception with cyclical Estrogen supplements when using CPA.

Ketoconazole is 1 of the newer hair removal treatments and is a particularly potent anti-androgen drug. Since 1985 there have been various studies that suggest Ketoconazole could be used to treat hirsutism. Ketoconazole works by stopping the production of hormones by the ovaries and the adrenal glands.

As with most other anti-androgen drugs, there are several different research reports that claim a reduction in hirsutism with different drug use regimes. These regimes vary the amount of Ketoconazole from 200mg to 400mg a day.

Some dermatologists believe the risk of side effects from using Ketoconazole is greater than with other anti-androgen drugs due to its potency. Dermatologists are particularly concerned with the risk of hepatotoxicity when using Ketoconazole as with CPA. Most dermatologists only use Ketoconazole when the hirsutism is particularly pronounced, and even then only prescribed the drug for a brief period of time before switching to other anti-androgen drugs.

There are many different types of GnRH agonists but the most commonly used are Leuprolide Acetate, Buserelin and Decapeptyl. GnRH agonists are drugs that reduce ovarian steroid production and some studies show that GnRH agonists could also be very effective for treating hirsutism where ovarian hyperandrogenism (too much androgen production by the ovaries) is the main problem. However, the effect of GnRH agonists is on ovarian production so they are not very effective if the route cause of hirsutism is over activity of the adrenal glands.

Some studies suggest that using a combination of GnRH agonists with another anti-androgen drug prolongs remission of hair growth. GnRH agonists have to be taken along with hormone replacement therapy as the GnRH agonist shuts down virtually all ovarian hormone production, including the production of hormones that are still required. GnRH agonists drugs are still quite expensive compared to Cyproterone Acetate or Spironolactone.