Finasteride (marketed as Proscar, Propecia,
Fincar, Finpecia, Finax, Finast, Finara, Prosteride) is an antiandrogen
which acts by inhibiting 5-alpha reductase, the enzyme that converts
testosterone to dihydrotestosterone. It is used as a treatment in
benign prostatic hyperplasia (BPH) in low doses, and in prostate
cancer in higher doses. It is also indicated for use in combination
with doxazosin therapy to reduce the risk for symptomatic progression
of BPH. Additionally, it is registered in many countries for male-pattern
baldness.
Finasteride was approved initially in 1992 as Proscar, a treatment
for prostate enlargement, but the sponsor had studied 1 mg of finasteride
and demonstrated hair growth in male pattern hair loss. In December
22, 1997, FDA approved finasteride to treat male pattern hair loss.
The Prostate Cancer Prevention Trial (PCPT) showed at a dosage
of 5mg per day, as is commonly prescribed for BPH, though much higher
than the 1mg generally prescribed for hair loss, participants taking
finasteride were 25% less likely to have developed prostate cancer
at the end of the trial compared to those taking a placebo.[1] However,
the cancers that developed in the men taking finasteride looked
like they were more likely to grow and spread. The reason for this
is not known. The study researchers are continuing to watch these
men to see if these cancers truly are more aggressive. At lower
doses, this effect is less well-defined.
Recognised side-effects, experienced by around 6%-19% of users,
include erectile dysfunction, and less often gynecomastia (breast
gland enlargement). [1] In trial studies, side effects ceased after
dosage was discontinued. An undetermined percentage of men have
also reported unwanted side effects remaining months or even years
after discontinuing the usage of Propecia.
Brand names
Drug trade names include Propecia and Proscar, both products of
Merck & Co. (the former is marketed for hair loss in male pattern
baldness, and the latter for BPH). There is 1 mg of finasteride
in Propecia and 5 mg in Proscar
Cipla is also manufacturing finasteride (trade names Fincar and
Finpecia), as is Dr. Reddy's (trade names Finax and Finast), Ranbaxy
(trade name Finara), and Aleppo Pharmaceutical (trade name Prosteride).
On June 19, 2006, Merck's patents on Proscar and Propecia expired
and the FDA approved a first-time generic formulation for finasteride
5 mg tablets.
Side effects
Finasteride is not indicated for use by women. Finasteride is in
the FDA pregnancy category X. This means that it is known to cause
birth defects in an unborn baby. Women who are or who may become
pregnant must not handle crushed or broken finasteride tablets,
because the medication could be absorbed through the skin. Finasteride
is known to cause birth defects in a developing male baby. Exposure
to whole tablets should be avoided whenever possible, however exposure
to whole tablets is not expected to be harmful as long as the tablets
are not swallowed. It is not known whether finasteride passes into
breast milk, and thus should not be taken by breastfeeding women.
It appears that finasteride can pass into the semen of men, thus,
at certain dosages, caution should be used to avoid ingestion of
semen during oral sex if a woman is pregnant or may become pregnant.
Finasteride can also be used to mask steroid abuse, and many professional
sports have banned finasteride use for this reason.
Use as a treatment for hair loss
Finasteride is taken orally and has a reported 0–5% success
rate (vs 17-45% in patients receiving a placebo). It is effective
only for as long as it is taken; the hair gained or maintained is
lost within 6-12 months of ceasing therapy (Rossi, 2004). In clinical
studies, Propecia, like minoxidil, was shown to work on both the
crown area and the hairline, but is most successful in the crown
area.
Some users, in an effort to save money, buy Proscar instead of
Propecia, and split the Proscar pills to approximate the Propecia
dosage.
Propecia has been shown to be ineffective for treating hair loss
in women.[citation needed] However, Propecia's supporters respond
that the study was on post-menopausal women whose hairloss was more
likely related to the loss of estrogen versus a sensitivity to testosterone.
Other studies[citation needed] have shown that Propecia is effective
for many women with follicular sensitivity to androgens. Many doctors
do prescribe it for women, but not without either careful birth
control measures or assurance that the woman
Possible health concerns
The UC Berkeley Wellness Letter expressed concern in March 2003
about the unproven long-term safety of Propecia and recommended
cutting a standard 1 milligram dose of Propecia into quarters to
reduce the cost without reducing its effectiveness. This claim appears
to be supported by clinical pharmacological data reviewed by the
FDA during Propecia's approval process that suggested that the advantage
of taking 1 mg per day over 0.2 mg per day is statisticially small.
Some people have unsuccessfully petitioned the FDA to re-examine
the approved dosage in light of the statistical evidence and unknown
long-term risks. The FDA responded and said that just because the
level of DHT found in the scalp was not significantly different
does not mean there is a correlation with hair loss. A study would
have to show that the benefits of using 0.2 mg and 1 mg were not
statistically different. According to the FDA such a study has been
performed and a 1 mg dose has a greater benefit.
Supporters of Propecia respond that while the drug must be taken
for a lifetime in order to avoid losing hair, future treatments
are widely expected by baldness specialists to replace Propecia,
which would end the need for continued use. In addition, Propecia
is widely considered safe enough to prescribe by health professionals,
and is one of the only two FDA-approved baldness treatment products
on the market.
Propecia's effects in detail
DHT is a derivative hormone (metabolite) of testosterone that has
been shown to be critical to the initiation and progression of follicular
miniaturization and eventual destruction of hair follicles in male
pattern baldness. DHT is a steroid hormone just like testosterone
but with greater affinity for the androgen receptor. Converting
Testosterone to DHT thus increases many of its effects.
While the mechanism by which DHT is involved in hair loss is not
confirmed, many dermatologists and research scientists specializing
in hair loss believe DHT molecules may diffuse into the interior
of hair follicle cells (the cytoplasm or cytosol) and bind with
androgen receptors. This complex, both the receptor and the DHT
molecule, then enters the nucleus of the cell. In the nucleus of
the hair follicle cell this complex could then alter the rate of
protein synthesis in men who are genetically predisposed to baldness.
[citation needed]
However, DHT also plays an important role in the functioning of
the central nervous system (the brain), the testicles and prostate,
and almost everything but muscle tissue. In muscle tissue testosterone
is the dominant hormone, which is why some bodybuilders inject testosterone
derivatives to aid in muscular development.
Propecia (and other products containing finasteride) cause a rise
in testosterone levels because testosterone that would normally
be converted into DHT remains testosterone. Continual high levels
of testosterone in the body could possibly have negative side effects.
Artificially low levels of DHT in the body could cause some unwanted
conditions. DHT is an antagonist of estrogen. Men’s bodies
also produce the female hormone estrogen in the adrenal glands,
although this is just one-tenth of the estrogen that premenopausal
women produce in their ovaries. By reducing DHT with drugs, a man’s
protection from the effects of estrogen may also be reduced. This
could result in gynecomastia.
Even though both finasteride and dutasteride were developed to combat
benign prostatic hyperplasia by reducing DHT in prostate tissue,
some scientists question the wisdom of using these 5-alpha reductase
inhibitors in younger men who have no problem with their prostates.
A research chemist, Pat Arnold, says “Evidence is mounting
that the existence of a high estrogen/androgen ratio – a condition
common in older men – is highly correlated with the development
of benign prostatic hyperplasia.”
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