akn
Musclechemistry Member
Description:
Clomiphene citrate is an anti-estrogenic drug that is
prescribed to women to treat anovulatory infertility
(inability to ovulate). In clinical medicine it is specifically
referred to as a nonsteroidal ovulatory stimulant. The drug
works by interacting with estrogen receptors, often in an
antagonistic manner, in various tissues of the body
including the hypothalamus, pituitary, ovary,
endometrium, vagina, and cervix. One main focus is that
the drug will oppose the negative feedback of estrogens
on the hypothalamic-pituitary-ovarian axis, enhancing the
release of gonadotropins (LH and FSH). This surge in
gonadotropins may cause egg release (follicular rupture),
ideally leading to conception. Clomiphene citrate is
chemically a synthetic estrogen with both
agoniist/antagonist properties, and in this regard is very
similar in structure and action to Nolvadex®. It is believed
that both the estrogenic and anti-estrogenic properties of
clomiphene citrate play a role in its ability to support
femal,e fertility.
In men, clomiphene citrate also acts as a partial antiestrogen,
and may be used to counter some of the side
effects of aromatizable steroid use including gynecomastia
and increased water retention. As an anti-estrogenic drug,
clomiphene citrate may also produce an elevation of
follicle stimulating hormone, and luteinizing hormone
levels, which can elevate testosterone production. This
effect is especially beneficial at the conclusion of a steroid
cycle, when endogenous testosterone levels are
depressed. Here, clomiphene citrate is most often applied
in combination with HCG and tamoxifen, in an effort to
restore endogenous testosterone production more quickly
(see PCT: Post-Cycle Therapy). If testosterone levels are not
brought back to normal in a short period of time, a
significant loss in size and strength may occur.This is due to
the fact that without testosterone (or other
anabolic/androgenic steroids) to impart an ongoing
anabolic message, the catabolic hormone cortisol
becomes the dominant force affecting muscle protein
synthesis. Often referred to as the post-steroid crash, when
not corrected this state of imbalance in the endocrine
system can quickly reduce muscle mass levels, diminishing
the long-term return on anabolic/androgenic steroid
therapy.
Note that the triphenylethylene compounds (toremifene
citrate, tamoxifen citrate, clomiphene citrate) tend to be
somewhat intrinsically estrogenic in the liver. This means
that while they can block estrogenic activity in some areas
of the body, they can actually act as estrogens in this other key area. Estrogenic action in the liver is important in the
regulation of serum cholesterol (it tends to support HDL
synthesis and LDL reductions). Since steroid-using
bodybuilders are already dealing with the negative
cardiovascular effects of these drugs, compounding the
issue with aromatase inhibitors (which will lower total
serum estrogen levels) may not always be the best option.
Using a drug that blocks gynecomastia, for example, while
at the same time supporting improved cholesterol values,
might be much more ideal.
History:
Clomiphene citrate is a fertility drug with a substantial
history of use in the United States. It first gained
widespread acceptance during the early 1970s, and has
been a drug common to the fertility practice ever since.
The drug is now considered a standard medication for
certain forms of fertility therapy, and has been adopted as
such far outside U.S. border. Clomiphene citrate is presently
available in most nations worldwide.The two most popular
brand names one is likely to encounter are Clomid and
Serofene, although the drug can be found under numerous
other trade names as well including (but not limited to)
Sepafar, Omifin, Pergotime, Gonaphene, Duinum, Clostil,
Ova.-Mit, and Clostibegyt. Clomiphene citrate is generally a
very inexpensive medication compared to stronger antiestrogens
such as the newer selective third-generation
aromatase inhibitors. It, likewise, remains a very popular
agent of use among bodybuilders and athletes.
How Supplied:
Clomiphene citrate is most commonly supplied in tablets
of 50 mg.
Structural Characteristics:
Clomiphene citrate is classified as a selective estrogen
receptor modulator, with both agonist and antagonist
properties. It has the chemical designation 2-[4-(2-chloro1,2-
diphenylvinyl)phenoxy]triethylamine dihydrogen
citrate.
Some patients using clomiphene citrate notice blurring or
other visual disturbances such as spots or flashes. These
symptoms occur more frequently at higher doses or
longer durations of therapy, and often disappear within a
few days or weeks of use. Prolonged visual disturbances
have been reported after the discontinuation of
clomiphene citrate therapy, however, and in some cases
may be irreversible. Those taking clomiphene citrate
should be warned that these symptoms might make
activities like driving a car or operating heavy machinery
more hazardous than usual.While the exact cause of these
visual symptoms is not yet understood, it is advisable to
discontinue treatment and have a thorough
medical/opthalmological examination should they occur.
Side Effects:
Clomiphene citrate appears to be well tolerated, with a
low incidence of significant side effects. Common adverse
reactions during clinical trails included ovarian
enlargement (13.6%), vasomotor flushes (10.4%),
abdominal discomfort (5.5%), nausea/vomiting (2.2%),
breast discomfort (2.1 %), visual symptoms (1.50/0),
headache (1.30/0), and abnormal uterine bleeding (1.30/0).
Data also suggests that the prolonged use of clomiphene
citrate may increase the chance of ovarian tumor.
Clomiphene citrate is occasionally associated with a
serious and potentially life threatening side effect called
ovarian hyperstimulation syndrome (OHSS). Early warning
signs of OHSS include abdominal pain and distention,
nausea, diarrhea, and weight gain.
Administration:
Clomiphene citrate is FDA approved for the treatment of
women with ovulatory dysfunction preventing
pregnancy.The recommended dosage is 50 mg daily for 5
days, which is initiated approximately 5 days into the
menstrual cycle. If ovulation does not occur, follow up
cycles may use a dosage of 100 mg per day for 5 days.
Many clinicians recommend a limit of 6 courses of therapy.
When used by men (off-label) to mitigate the estrogenic
side effects of anabolic/androgenic steroid use, a daily
dosage of 50-100 mg (1-2 tablets) is usually administered
while any offending steroids are taken. Note, however, that
tamoxifen is usually given preference over clomiphene
citrate for this purpose. More commonly, clomiphene
citrate is used by men at a dosage of 50-100 mg per day
for 30 days at the conclusion of a steroid cycle, in an effort
to bring natural testosterone production back to normal
levels. Here, it is usually deemed most appropriate to use
as part of a multi-component post-cycle recovery
program (see PCT: Post-Cycle Therapy). Female athletes
occasionally use clomiphene citrate for the reduction of
estrogenicity near the time of a bodybuilding contest. In
some instances this may aid in increasing fat loss and
muscularity, particularly in female trouble areas such as
the hips and thighs. The drug, however, often produces
very troubling side effects in pre-menopausal women,
and is likewise not in very high demand among this
group.
Availability:
Clomiphene citrate is widely available on the international
market in a variety of brand names. It generally sells for a
reasonable price, and is of low interest to counterfeiters.
Clomiphene citrate is an anti-estrogenic drug that is
prescribed to women to treat anovulatory infertility
(inability to ovulate). In clinical medicine it is specifically
referred to as a nonsteroidal ovulatory stimulant. The drug
works by interacting with estrogen receptors, often in an
antagonistic manner, in various tissues of the body
including the hypothalamus, pituitary, ovary,
endometrium, vagina, and cervix. One main focus is that
the drug will oppose the negative feedback of estrogens
on the hypothalamic-pituitary-ovarian axis, enhancing the
release of gonadotropins (LH and FSH). This surge in
gonadotropins may cause egg release (follicular rupture),
ideally leading to conception. Clomiphene citrate is
chemically a synthetic estrogen with both
agoniist/antagonist properties, and in this regard is very
similar in structure and action to Nolvadex®. It is believed
that both the estrogenic and anti-estrogenic properties of
clomiphene citrate play a role in its ability to support
femal,e fertility.
In men, clomiphene citrate also acts as a partial antiestrogen,
and may be used to counter some of the side
effects of aromatizable steroid use including gynecomastia
and increased water retention. As an anti-estrogenic drug,
clomiphene citrate may also produce an elevation of
follicle stimulating hormone, and luteinizing hormone
levels, which can elevate testosterone production. This
effect is especially beneficial at the conclusion of a steroid
cycle, when endogenous testosterone levels are
depressed. Here, clomiphene citrate is most often applied
in combination with HCG and tamoxifen, in an effort to
restore endogenous testosterone production more quickly
(see PCT: Post-Cycle Therapy). If testosterone levels are not
brought back to normal in a short period of time, a
significant loss in size and strength may occur.This is due to
the fact that without testosterone (or other
anabolic/androgenic steroids) to impart an ongoing
anabolic message, the catabolic hormone cortisol
becomes the dominant force affecting muscle protein
synthesis. Often referred to as the post-steroid crash, when
not corrected this state of imbalance in the endocrine
system can quickly reduce muscle mass levels, diminishing
the long-term return on anabolic/androgenic steroid
therapy.
Note that the triphenylethylene compounds (toremifene
citrate, tamoxifen citrate, clomiphene citrate) tend to be
somewhat intrinsically estrogenic in the liver. This means
that while they can block estrogenic activity in some areas
of the body, they can actually act as estrogens in this other key area. Estrogenic action in the liver is important in the
regulation of serum cholesterol (it tends to support HDL
synthesis and LDL reductions). Since steroid-using
bodybuilders are already dealing with the negative
cardiovascular effects of these drugs, compounding the
issue with aromatase inhibitors (which will lower total
serum estrogen levels) may not always be the best option.
Using a drug that blocks gynecomastia, for example, while
at the same time supporting improved cholesterol values,
might be much more ideal.
History:
Clomiphene citrate is a fertility drug with a substantial
history of use in the United States. It first gained
widespread acceptance during the early 1970s, and has
been a drug common to the fertility practice ever since.
The drug is now considered a standard medication for
certain forms of fertility therapy, and has been adopted as
such far outside U.S. border. Clomiphene citrate is presently
available in most nations worldwide.The two most popular
brand names one is likely to encounter are Clomid and
Serofene, although the drug can be found under numerous
other trade names as well including (but not limited to)
Sepafar, Omifin, Pergotime, Gonaphene, Duinum, Clostil,
Ova.-Mit, and Clostibegyt. Clomiphene citrate is generally a
very inexpensive medication compared to stronger antiestrogens
such as the newer selective third-generation
aromatase inhibitors. It, likewise, remains a very popular
agent of use among bodybuilders and athletes.
How Supplied:
Clomiphene citrate is most commonly supplied in tablets
of 50 mg.
Structural Characteristics:
Clomiphene citrate is classified as a selective estrogen
receptor modulator, with both agonist and antagonist
properties. It has the chemical designation 2-[4-(2-chloro1,2-
diphenylvinyl)phenoxy]triethylamine dihydrogen
citrate.
Some patients using clomiphene citrate notice blurring or
other visual disturbances such as spots or flashes. These
symptoms occur more frequently at higher doses or
longer durations of therapy, and often disappear within a
few days or weeks of use. Prolonged visual disturbances
have been reported after the discontinuation of
clomiphene citrate therapy, however, and in some cases
may be irreversible. Those taking clomiphene citrate
should be warned that these symptoms might make
activities like driving a car or operating heavy machinery
more hazardous than usual.While the exact cause of these
visual symptoms is not yet understood, it is advisable to
discontinue treatment and have a thorough
medical/opthalmological examination should they occur.
Side Effects:
Clomiphene citrate appears to be well tolerated, with a
low incidence of significant side effects. Common adverse
reactions during clinical trails included ovarian
enlargement (13.6%), vasomotor flushes (10.4%),
abdominal discomfort (5.5%), nausea/vomiting (2.2%),
breast discomfort (2.1 %), visual symptoms (1.50/0),
headache (1.30/0), and abnormal uterine bleeding (1.30/0).
Data also suggests that the prolonged use of clomiphene
citrate may increase the chance of ovarian tumor.
Clomiphene citrate is occasionally associated with a
serious and potentially life threatening side effect called
ovarian hyperstimulation syndrome (OHSS). Early warning
signs of OHSS include abdominal pain and distention,
nausea, diarrhea, and weight gain.
Administration:
Clomiphene citrate is FDA approved for the treatment of
women with ovulatory dysfunction preventing
pregnancy.The recommended dosage is 50 mg daily for 5
days, which is initiated approximately 5 days into the
menstrual cycle. If ovulation does not occur, follow up
cycles may use a dosage of 100 mg per day for 5 days.
Many clinicians recommend a limit of 6 courses of therapy.
When used by men (off-label) to mitigate the estrogenic
side effects of anabolic/androgenic steroid use, a daily
dosage of 50-100 mg (1-2 tablets) is usually administered
while any offending steroids are taken. Note, however, that
tamoxifen is usually given preference over clomiphene
citrate for this purpose. More commonly, clomiphene
citrate is used by men at a dosage of 50-100 mg per day
for 30 days at the conclusion of a steroid cycle, in an effort
to bring natural testosterone production back to normal
levels. Here, it is usually deemed most appropriate to use
as part of a multi-component post-cycle recovery
program (see PCT: Post-Cycle Therapy). Female athletes
occasionally use clomiphene citrate for the reduction of
estrogenicity near the time of a bodybuilding contest. In
some instances this may aid in increasing fat loss and
muscularity, particularly in female trouble areas such as
the hips and thighs. The drug, however, often produces
very troubling side effects in pre-menopausal women,
and is likewise not in very high demand among this
group.
Availability:
Clomiphene citrate is widely available on the international
market in a variety of brand names. It generally sells for a
reasonable price, and is of low interest to counterfeiters.
