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Finasteride
Identification
Apperance: white or off-white crystalline powder
Molecular Formula: C23H36N2O2
Molecular Weight; 372.55
CAS Registry Number: 98319-26-7
Molecular Structure:
Instroduction:
Finasteride is an antiandrogen which acts by inhibiting
type II 5-alpha reductase, the enzyme that converts testosterone
to dihydrotestosterone (DHT). It is used as a treatment in benign
prostatic hyperplasia (BPH) in low doses, and 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 androgenetic
alopecia (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. On December 22, 1997, the 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. Further,
finasteride increased the specificity and selectivity of prostate
cancer detection, thus, a seemly increased rate of high Gleason
grade tumor.
Recognized
side effects, experienced by around >1% of users, include erectile
dysfunction, and less often gynecomastia (breast gland enlargement).As
expected from its short 6-8 hour half-life, in trial studies,
side effects ceased after dosage was discontinued.
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. Finasteride may pass into
the semen of men, but Merck states that a pregnant woman's contact
with the semen of a man taking finasteride is not an issue for
concern.
Finasteride
has been linked with depression.The drug also caused reductions
in allopregnanolone, a potent, endogenous positive modulator of
the GABA-A receptor, in very large doses in rodent studies.
Finasteride
can also be used to mask steroid abuse, and many professional
sports have banned finasteride use for this reason.
Finasteride
is under investigation by the Swedish Medical Products Agency
for possibly causing irreversible sexual side effects.
Use as a treatment for hair loss
In a 5-year study of men with mild to moderate hair loss, 48%
of those treated with Propecia (finasteride 1mg) experienced some
regrowth of hair, and 42% had no further loss. Average hair count
in the treatment group remained above baseline, and showed an
increasing difference from hair count in the placebo group, for
all five years of the study. Propecia is effective only for as
long as it is taken; the hair gained or maintained is lost within
6-12 months of ceasing therapy.[9] 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. Doing so is generally considered unadvisable
if women of pregnancy age are in the household; this is because
finasteride, even in small concentrations, can cause birth defects
in a developing male fetus. The birth defects involve the development
of male genitalia (no such effects have been noted in developing
female fetuses). On most product inserts, it will be mentioned
that the dust or crumbs from broken Propecia tablets should be
kept away from pregnant women.
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 hair loss was more likely related
to the loss of estrogen versus a sensitivity to testosterone.
Many doctors prescribe it for women, but not without either careful
birth control measures or assurance that the woman cannot become
pregnant.
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