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by Bill Roberts - Clomid is the anti-estrogen
of choice for improving recovery of natural testosterone
production after a cycle, improving testosterone
production of endurance athletes, and is also effective
in reducing risk of gynecomastia during a cycle
employing aromatizable steroids.
While it has been claimed that Clomid "stimulates"
production of LH and therefore of testosterone,
in fact Clomid’s activity is achieved not by stimulation
of the hypothalamus and pituitary, but by blocking
their inhibition by estrogen.
Clomid is a
mixed estrogen agonist/antagonist (activator/blocker)
which, when bound to the estrogen receptor, puts
it in a somewhat different conformation (shape)
than does estradiol. The estrogen receptor requires
binding of an estrogen or drug at its binding site
and also the binding of any of several cofactors
at different sites. Without the binding of
the cofactor, the estrogen receptor is inactive.
Different tissues use different cofactors. Some
of these cofactors are able to bind to the estrogen
receptor/Clomid complex, but others are blocked
due to the change in shape. The result is
that in some tissues Clomid acts as an antagonist
-- the cofactor used in that tissue cannot bind
and so the receptor remains inactive -- and in others
Clomid acts as an agonist (activator), because the
cofactors used in that tissue are able to bind.
Clomid is an effective antagonist in the hypothalamus
and in breast tissue. It is an effective agonist
in bone tissue, and for improving blood cholesterol.
Clomid also has the property of reducing the
adverse effect of exercise-induced damage of muscle
tissue. This is very significant for endurance athletes
but is not very significant, if at all significant,
with reasonable weight training. Clomid does not
perceptibly affect gains of the weight trainer either
favorably or adversely in my experience.
The drug seems to have estrogenic effects on
mood, which can be beneficial (improving relationships
with women by improving empathy) or can yield depression
or PMS-like symptoms, but for most users there is
no significant effect either way.
The claim that duration of intake should not
exceed 10-14 days is incorrect. Clinical studies
with male patients have been for periods of a year
or longer. This error probably originates from the
fact that, for use in women, due to the menstrual
cycle there would obviously be no point in trying
to stimulate ovulation all four weeks of the month.
Thus, use in women is limited to 10-14 days. That
limitation is not because of toxicity.
Clomid is in fact useful throughout a cycle if
aromatizable drugs are being used. I do think however
that to be conservative, one should use it no more
than 2/3 of the time throughout the year or a little
less.
Clomiphene citrate is
the chemical name of active ingredient in Clomid.
Clomid is a registered trademark of Merrell
Dow Pharmaceuticals in the United States and/or
other countries.
Clomid Resources
Clomid Pictures
Clomid Prescribing Information
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| Trivial name |
Clomiphene |
| Systematic name |
Ethanamine, 2-(4-(2-chloro-1,2-diphenylethenyl)phenoxy)-N,N-diethyl- |
| CAS number |
911-45-5
or 50-41-9 (citrate (1:1))
|
| ATC code |
G03GB02 |
| Merck Index Number |
2410 |
| Chemical formula |
C26H28ClNO
or C32H36ClNO8
(citrate) |
| Molecular weight |
405.9663
g/mol (without citrate)
598.0913 g/mol (with citrate) |
| Bioavailability |
High (>90%) |
| Metabolism |
Hepatic (with enterohepatic circulation) |
| Elimination half-life |
5-7 days |
| Excretion |
Mainly renal, some biliary |
| Pregnancy category |
X |
| Legal status |
Prescription only (US) |
| Controlled substance |
No |
| Routes of administration |
Oral |
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