Prescription oral medications Basic facts
Some prescription oral medications have been found to affect
hair growth. They can be helpful in reducing hair growth in some
conaumers, but it's important to discuss possible unwanted side
effects with your physician.
Drugs that can reduce hair growth
 Spironolactone (Aldactone)
Spironolactone (also known as Aldactone) is arguably the number
one hirsutism treatment of choice for dermatologists in the
US. Spironolactone has antiandrogenic effects that may enhance
treatment of several androgen-excess conditions, particularly
severe hirsutism.
Spironolactone has several properties that make it suitable
for use in treating hirsutism. It interferes with the production
of testosterone and it increases the metabolism of any testosterone
that is produced. Spironolactone binds to cell androgen receptors
and blocks them from binding to naturally produced androgens.
In addition with long term spironolactone use, there is a gradual
reduction in 5 alpha reductase activity. It is this enzyme that
converts testosterone to the more potent, hair follicle stimulating,
dihydrotestosterone.
Treatment protocols may involve continuous spironolactone use
at 50mg to 200mg per day or cyclic use. For example 50mg or
100mg twice daily from the 4th to the 22nd day of the menstrual
cycle. Numerous treatment protocols involving spironolactone
have been used in different studies, but no particular treatment
approach has been shown to be significantly superior. Combination
therapy with an oral contraceptive pill or dexamethasone appears
to have an improved beneficial effect on hirsutism and limits
side effects.
Spironoolactone is a diuretic, so it's advised to drink plenty
of water while taking it. Side effects with spironolactone are
generally transient. As with all antiandrogens , spironolactone
use 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.
Finasteride (marketed as Propecia and Proscar)
Promoted for use in treating pattern baldness and benign prostate
hyperplasia, respectively, it's a type II 5alpha reductase inhibitor.
This enzyme blocks the conversion of testosterone to dihydrotestosterone
(DHT), a potent stimulator of hair loss in scalp follicles and
hair growth in body hair follicles that have androgen receptors.
When finasteride was tested on postmenopausal women with pattern
baldness there was little or no response. However, in trials
for hirsutism finasteride has some significant promise. Results
with finasteride alone in some trials have been comparable with
oral antiandrogens, and the combination of finasteride plus
other antiandrogens have shown an improved effect over using
treatments separately. Although it may not be an appropriate
treatment in every situation, finasteride is a readily available
and relatively safe treatment option. The most significant side
effect is that male fetuses will develop with female genitalia
in any pregnant woman using finasteride. Consequently, dermatologists
ensure one or more forms of birth control are used by any woman
using finasteride. Other side effects reported include breast
enlargement and increased libido (in contrast to decreased libido
in men).
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
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 35 and Dianette- actually the exact same drug, just marketed under different names. In Canada, it is called Diane 35. In the UK and Europe it is called Dianette. Both have 35 mcg of ethinylestradiol and 2 mg CPA. Diane 50 has 50 mcg of ethinylestradiol and 2 mg CPA. However, this drug is NOT available in Canada. CPA in its various
forms is made by the Germany based Schering AG pharmaceutical
company.
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.
Ketoconazole
Ketoconazole is a relatively new and particularly potent anti
androgen drug. Since 1985 there have been various studies suggesting
that ketoconazole could be used to treat hirsutism. Ketoconazole
works by blocking the production of hormones by the ovaries
and the adrenal glands.
As with other antiandrogen drugs, there are several different
research reports that claim a reduction in hirsutism with different
drug use protocols. The intake of ketoconazole may range from
200mg to 400mg a day.
Although the list of references below might seem to suggest
that ketoconazole is a popular treatment for hirsutism, most
dermatologists are wary of using it on a regular basis. Because
it is such a powerful anti androgen, some dermatologists believe
the risk of side effects is greater than with other antiandrogen
drugs. Dermatologists are particularly concerned with the risk
of hepatotoxicity when using ketoconazole. Most dermatologists
only use ketoconazole when the hirsutism is particularly pronounced
and even then the drug is only prescribed for a brief period
of time before switching to other antiandrogen drugs.
Gonadotrophin releasing hormone agonists
Gonadotrophin releasing hormone agonists (GnRH) have been suggested
as potential treatments for hirsutism. The most common GnRH
agonists used are leuprolide acetate, buserelin and decapeptyl.
GnRH agonists are drugs that decrease ovarian steroid production
and some studies show that GnRH agonists could be very effective
for treating hirsutism where ovarian hyperandrogenism (too much
androgen production by the ovaries) is the problem. However,
the effect of GnRH agonists is on ovarian production so they
are not very effective for hirsutism where the root cause is
over activity of the adrenal glands.
GnRH agonists are still primarily an experimental treatment.
Some studies suggest that addition of GnRH agonists to treatment
using antiandrogen drugs prolongs remission of hirsutism. GnRH
agonists have to be taken along with hormone replacement therapy
(often called "add back treatment") as the GnRH agonist
shuts down ovarian hormone production almost completely so while
androgens are no longer produced, neither are estrogens and
progesterones. Hormone replacement is particularly important
as using GnRH agonists without estrogen and progesterone supplements
bone density decreases significantly.
The greatest barrier to wide spread use of GnRH agonists is
that the drugs are quite expensive compared to cyproterone acetate
or spironolactone.
For a bibliography , see the discussion of medical data
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