akn
Musclechemistry Member
Description:
Raloxifene hydrochloride is a second-generation Selective
Estrogen Receptor Modulator (SERM) of the
benzothiophene family. This drug is similar in effect to
tamoxifen, exhibiting estrogen receptor antagonist
(blocking) properties in some tissues while acting as an
estrogen receptor agonist (activator) in others. The main
point of variation between these two agents is their tissue
selectivity. While raloxifene hydrochloride is a strong antiestrogen
in breast and uterine tissues, it appears to be
estrogenic in bone. This allows it to protect bone density,
mimicking the beneficial effects of endogenous estradiol.
This is quite different from tamoxifen, which is antiestrogenic
in both breast and bone. In a role that was novel
for an anti-estrogen, raloxifene hydrochloride was
approved by the FDA for the prevention and treatment of
osteoporosis in post-menopausal women. It is also being
investigated for several other potential uses, including the
treatment and prevention of cardiovascular disease, breast
cancer, gynecomastia, prostate cancer, acromegaly, and
uterine cancer.
As an anti-estrogen, athletes and bodybuilders may use
this compound to combat the estrogenic side effects
caused by aromatizable or estrogenic steroids. The
principle among these side effects is gynecomastia, a
purpose for which raloxifene hydrochloride seems better
suited than tamoxifen. This was demonstrated in a July
2004 study in the Journal ofPediatrics, which looked at how
these two agents compared in the treatment of persistent
pubertal gynecomastia.832 The investigation involved a
group of 38 patients, averaging 15 years of age and
suffering from gynecomastia for a little over 2 years.
Treatment for 3 to 9 months with either agent had a high
success rate for seeing "some improvement" (91 % for
raloxifene and 86% for Nolvadex). However, a significant
reduction of gynecomastia was seen in more than twice as
many patients with raloxifene hydrochloride (86%
compared to 41 %). Given its relative potency, raloxifene
hydrochloride may offer an alternative to surgery for some
cases of gynecomastia.
Typical of an anti-estrogen, raloxifene hydrochloride
should also offer some benefit as a testosteronestimulating
compound. We see this effect demonstrated in
studies on a group of older men (aged 60-70 years), where
daily doses of 120 mg were able to increase serum and
bioavailable (unbound) testosterone by 20%.833 Though
t~ese figures are not dramatic, they do demonstrate an
anti-estrogenic effect instead of an estrogenic (negative)
one when it comes to testosterone production. This drug
may, therefore, be of some value when utilized as an
adjunct to HCG injections during a post-cycle testosterone
recovery program. This same study above also showed
raloxifene hydrochloride to have at least a partial
estrogenic effect on serum lipids, exhibiting a trend toward
decreases in all cholesterol values (total, LDL, and HDL).lt is
difficult to discern if there are any real benefits to male
bodybuilders when it comes to using raloxifene
hydrochloride to counteract the negative cardiovascular
side effects of steroid use. As discussed in its respective
profile, this may be a notable benefit with the use of
Nolvadex, a first-generation SERM agent shown to improve
HDL (good) cholesterol levels in many patients.
There are some negatives to inhibiting the actions of
estrogen that should be addressed. For one, estrogen is a
beneficial hormone when it comes to IGF-1 levels. In
studies with acromegaly patients that suffer from GH
hypersecretion, 60 mg of raloxifene hydrochloride twice
daily was able to reliably suppress IGF-1 levels by an
average of 16%.834 Estrogen is also understood to exert
positive anabolic effects in regards to increasing androgen
receptor concentrations in certain tissues, and enhancing
enzymes involved in the utilization of glucose for tissue
growth and repair. This is further support for the belief that
anti-estrogens should not be used unless there is a defined
reason for doing so. When used for simple side-effect
prevention (without visible side effects occurring), the
drug may inadvertently lessen the total anabolic potency
of steroid therapy.
history:
Raloxifene hydrochloride was developed by Eli Lilly &
Company, and FDA approved for u.S. sale in 1997. Its first
indicated use was as that of an osteoporosis treatment,
owing to its ability to increase bone density. In 2007, the
FDA expanded the indicated uses for the drug to include
reducing the risk of invasive breast cancer in two
populations: postmenopausal women with osteoporosis
and postmenopausal women at high risk for invasive
breast cancer. Today, raloxifene hydrochloride is a fairly
popular drug in clinical medicine, and is approved for sale
in over 50 countries. The Evista brand from Eli Lilly &
Company dominates the global market, although a small
number of other brands can be found including Ketidin,
Oseofem, and Raxeto (Argentina), Bonmax, Estroact, and
Ralista (India), and Optruma (Spain, France, Italy).
How Supplied:
Raloxifene hydrochloride is most commonly supplied in
tablets of 60 mg.
Structural Characteristics:
Raloxifene hydrochloride is classified a selective estrogen
receptor modulator, with both agonist and antagonist
properties. It has the chemical designation 6-Hydroxy-2(
p-hyd roxyphenyl) benzo[bJthien-3-yl-p-(2piperidinoethoxy)
phenyl ketone hydrochloride.
Warnings (Stroke):
The FDA mandates that the following warning be present
on the prescribing information for Evista (raloxifene
hydrochloride): "WARNING: INCREASED RISK OF VENOUS
THROMBOEMBOLISM AND DEATH FROM STROKE.
Increased risk of deep vein thrombosis and pulmonary
embolism have been reported with Evista. Women with
active or past history of venous thromboembolism should
not take Evista. Increased risk of death due to stroke
occurred in a trial in postmenopausal women with
documented coronary heart disease or at increased risk
for magor coronary events. Consider risk-benefit balance in
women at risk for stroke."
Side Effects:
Common side effects associated with the use of raloxifene
hydrochloride include hot flashes/flushing, headache,
malaise, weakness, cramping, edema, sweating,
depression, weight gain, and gastrointestinal disturbances
such as nausea, vomiting, indigestion, and diarrhea. Less
comm!on side effects include breast pain, vaginal
bleeding, thrombophlebitis (inflammation of vein
associated with blood clot), and visual disturbances. In
rare cases raloxifene hydrochloride use has been
associated with stroke, narrowing of the arteries (transient
ischaelmic attack), pulmonary embolus, deep-vein
thrombosis, low white blood cell or platelet count, upper
gastrointestinal hemorrhage, or ulcer. Antiestrogens may
harm the developing fetus, and should never be used
duringl pregnancy.
Administration:
Raloxifene hydrochloride is FDA approved for the
treatment and prevention of osteoporosis in
postmenopausal women, reducing the risk of invasive
breast cancer in postmenopausal women with
osteoporosis, and reducing the risk of invasive breast
cancer in postmenopausal women at high risk for invasive
breast cancer.The recommended dose is one 60 mg tablet
administered once per day, without regard to meals.When
used (off-label) to mitigate the estrogenic side effects of
anabolic/androgenic steroid use, male athletes and
bodybuilders often take 30 mg to 60 mg per day.
Availability:
Raloxifene hydrochloride is available in over 50 countries.
Aside from a small number of other brands, the Evista
product from Eli Lilly & Company is most likely to be
encountered. Price is often a concern, as raloxifene
hydrochloride is considerably more expensive than some
of the anti-estrogens bodybuilders and athletes are
already accustomed to such as Nolvadex and Clomid.The
price per individual daily dose of raloxifene hydrochloride
(1 tablet) can exceed $2. That would add up to $200 or
more per 100 doses. A hundred tablets of generic
tamoxifen (20 mg) often sell for approximately $50. This is
about 50 cents per dose, or , /4th the price of raloxifene
hydrochloride. Thus far, price, not availability, seem to be
preventing the more widespread diversion of raloxifene
hydrochloride for black market sale.
Raloxifene hydrochloride is a second-generation Selective
Estrogen Receptor Modulator (SERM) of the
benzothiophene family. This drug is similar in effect to
tamoxifen, exhibiting estrogen receptor antagonist
(blocking) properties in some tissues while acting as an
estrogen receptor agonist (activator) in others. The main
point of variation between these two agents is their tissue
selectivity. While raloxifene hydrochloride is a strong antiestrogen
in breast and uterine tissues, it appears to be
estrogenic in bone. This allows it to protect bone density,
mimicking the beneficial effects of endogenous estradiol.
This is quite different from tamoxifen, which is antiestrogenic
in both breast and bone. In a role that was novel
for an anti-estrogen, raloxifene hydrochloride was
approved by the FDA for the prevention and treatment of
osteoporosis in post-menopausal women. It is also being
investigated for several other potential uses, including the
treatment and prevention of cardiovascular disease, breast
cancer, gynecomastia, prostate cancer, acromegaly, and
uterine cancer.
As an anti-estrogen, athletes and bodybuilders may use
this compound to combat the estrogenic side effects
caused by aromatizable or estrogenic steroids. The
principle among these side effects is gynecomastia, a
purpose for which raloxifene hydrochloride seems better
suited than tamoxifen. This was demonstrated in a July
2004 study in the Journal ofPediatrics, which looked at how
these two agents compared in the treatment of persistent
pubertal gynecomastia.832 The investigation involved a
group of 38 patients, averaging 15 years of age and
suffering from gynecomastia for a little over 2 years.
Treatment for 3 to 9 months with either agent had a high
success rate for seeing "some improvement" (91 % for
raloxifene and 86% for Nolvadex). However, a significant
reduction of gynecomastia was seen in more than twice as
many patients with raloxifene hydrochloride (86%
compared to 41 %). Given its relative potency, raloxifene
hydrochloride may offer an alternative to surgery for some
cases of gynecomastia.
Typical of an anti-estrogen, raloxifene hydrochloride
should also offer some benefit as a testosteronestimulating
compound. We see this effect demonstrated in
studies on a group of older men (aged 60-70 years), where
daily doses of 120 mg were able to increase serum and
bioavailable (unbound) testosterone by 20%.833 Though
t~ese figures are not dramatic, they do demonstrate an
anti-estrogenic effect instead of an estrogenic (negative)
one when it comes to testosterone production. This drug
may, therefore, be of some value when utilized as an
adjunct to HCG injections during a post-cycle testosterone
recovery program. This same study above also showed
raloxifene hydrochloride to have at least a partial
estrogenic effect on serum lipids, exhibiting a trend toward
decreases in all cholesterol values (total, LDL, and HDL).lt is
difficult to discern if there are any real benefits to male
bodybuilders when it comes to using raloxifene
hydrochloride to counteract the negative cardiovascular
side effects of steroid use. As discussed in its respective
profile, this may be a notable benefit with the use of
Nolvadex, a first-generation SERM agent shown to improve
HDL (good) cholesterol levels in many patients.
There are some negatives to inhibiting the actions of
estrogen that should be addressed. For one, estrogen is a
beneficial hormone when it comes to IGF-1 levels. In
studies with acromegaly patients that suffer from GH
hypersecretion, 60 mg of raloxifene hydrochloride twice
daily was able to reliably suppress IGF-1 levels by an
average of 16%.834 Estrogen is also understood to exert
positive anabolic effects in regards to increasing androgen
receptor concentrations in certain tissues, and enhancing
enzymes involved in the utilization of glucose for tissue
growth and repair. This is further support for the belief that
anti-estrogens should not be used unless there is a defined
reason for doing so. When used for simple side-effect
prevention (without visible side effects occurring), the
drug may inadvertently lessen the total anabolic potency
of steroid therapy.
history:
Raloxifene hydrochloride was developed by Eli Lilly &
Company, and FDA approved for u.S. sale in 1997. Its first
indicated use was as that of an osteoporosis treatment,
owing to its ability to increase bone density. In 2007, the
FDA expanded the indicated uses for the drug to include
reducing the risk of invasive breast cancer in two
populations: postmenopausal women with osteoporosis
and postmenopausal women at high risk for invasive
breast cancer. Today, raloxifene hydrochloride is a fairly
popular drug in clinical medicine, and is approved for sale
in over 50 countries. The Evista brand from Eli Lilly &
Company dominates the global market, although a small
number of other brands can be found including Ketidin,
Oseofem, and Raxeto (Argentina), Bonmax, Estroact, and
Ralista (India), and Optruma (Spain, France, Italy).
How Supplied:
Raloxifene hydrochloride is most commonly supplied in
tablets of 60 mg.
Structural Characteristics:
Raloxifene hydrochloride is classified a selective estrogen
receptor modulator, with both agonist and antagonist
properties. It has the chemical designation 6-Hydroxy-2(
p-hyd roxyphenyl) benzo[bJthien-3-yl-p-(2piperidinoethoxy)
phenyl ketone hydrochloride.
Warnings (Stroke):
The FDA mandates that the following warning be present
on the prescribing information for Evista (raloxifene
hydrochloride): "WARNING: INCREASED RISK OF VENOUS
THROMBOEMBOLISM AND DEATH FROM STROKE.
Increased risk of deep vein thrombosis and pulmonary
embolism have been reported with Evista. Women with
active or past history of venous thromboembolism should
not take Evista. Increased risk of death due to stroke
occurred in a trial in postmenopausal women with
documented coronary heart disease or at increased risk
for magor coronary events. Consider risk-benefit balance in
women at risk for stroke."
Side Effects:
Common side effects associated with the use of raloxifene
hydrochloride include hot flashes/flushing, headache,
malaise, weakness, cramping, edema, sweating,
depression, weight gain, and gastrointestinal disturbances
such as nausea, vomiting, indigestion, and diarrhea. Less
comm!on side effects include breast pain, vaginal
bleeding, thrombophlebitis (inflammation of vein
associated with blood clot), and visual disturbances. In
rare cases raloxifene hydrochloride use has been
associated with stroke, narrowing of the arteries (transient
ischaelmic attack), pulmonary embolus, deep-vein
thrombosis, low white blood cell or platelet count, upper
gastrointestinal hemorrhage, or ulcer. Antiestrogens may
harm the developing fetus, and should never be used
duringl pregnancy.
Administration:
Raloxifene hydrochloride is FDA approved for the
treatment and prevention of osteoporosis in
postmenopausal women, reducing the risk of invasive
breast cancer in postmenopausal women with
osteoporosis, and reducing the risk of invasive breast
cancer in postmenopausal women at high risk for invasive
breast cancer.The recommended dose is one 60 mg tablet
administered once per day, without regard to meals.When
used (off-label) to mitigate the estrogenic side effects of
anabolic/androgenic steroid use, male athletes and
bodybuilders often take 30 mg to 60 mg per day.
Availability:
Raloxifene hydrochloride is available in over 50 countries.
Aside from a small number of other brands, the Evista
product from Eli Lilly & Company is most likely to be
encountered. Price is often a concern, as raloxifene
hydrochloride is considerably more expensive than some
of the anti-estrogens bodybuilders and athletes are
already accustomed to such as Nolvadex and Clomid.The
price per individual daily dose of raloxifene hydrochloride
(1 tablet) can exceed $2. That would add up to $200 or
more per 100 doses. A hundred tablets of generic
tamoxifen (20 mg) often sell for approximately $50. This is
about 50 cents per dose, or , /4th the price of raloxifene
hydrochloride. Thus far, price, not availability, seem to be
preventing the more widespread diversion of raloxifene
hydrochloride for black market sale.
