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View Full Version : CytadrenŽ (aminoglutethimide) anti estrogen profie and use



akn
05-20-2014, 06:07 PM
Descrilption:
Aminoglutethimide is mainly identified as an inhibitor of
adrenocortical steroid synthesis. Its primary function is to
block the conversion of cholesterol to pregnenolone,
which is required for the biosynthesis of adrenal
glucocorticoids, mineralocorticoids, estrogens, and
androgens. Aminoglutethimide is a nonspecific inhibitor,
and also blocks several other steps in steroid synthesis
including hydroxylation at C-ll, C-18, and C-21, and the
aromatization of androgens to estrogens.The drug may be
used clinically to treat estrogen dependent breast cancer,
and to treat Cushing's syndrome, which is a condition
where the body overproduces the hormone cortisol. The
effect that aminogluthethimide can have on cortisol and
estrogen production is what makes this a drug of interest
to athlletes and bodybuilders.
Cortisol Inhibition: While cortisol is an essential hormone
for life, its levels may also vary greatly within "normal"
ranges depending on the individual, their training and
dietary status, and many other personal metabolic factors.
It has been a common pursuit in the sports community to
find ways to control (limit) cortisol production. This is
because while androgens give your muscle cells a message
to increase protein synthesis, cortisol (a catabolic
hormone) imparts a message to breakdown and release
amino acids. If one can limit this catabolic message, net
protein synthesis should, in theory, be increased.
Aminoglutethimide has been used by a number of athletes
and bodybuilders for this purpose, usually in combination
with anabolic/androgenic steroids because it has a low
level of androgen inhibition. Together with even a
relatively small dose, it was thought one could shift the
ratio of anabolic to catabolic hormones in favor of the
former, the goal being new muscle growth. The results for
this use have been mixed.
When first looked at in the realm of athletics, however,
research was bare as to the best way to use
aminoglutethimide as a cortisol lowering anti-catabolic.
Dubbed the "adrenal escape phenomenon': it has been
noted that after a short period of regular use your body
often reacts to lowered cortisol levels by increasing the
release of another hormone, ACTH (adrenocorticotropic
hormone). Increased ACTH could overcome the activity of
aminoglutethimide, resulting in your body resuming its
original levels of cortisol production (negating the benefits
of cortisol inhibition)829.A moderate amount of
hydrocortisone (20-30 mg daily) is given to patients when
this occurs. This can keep glucocorticoid activity from
compl,etely diminishing, preventing the ACTH response
and allowing the drug to retain its effect. For athletes,
however, supplementing glucocorticoids would probably
be counterproductive given the desired goal.A 2-day-on 2day-
off regime of administration was, therefore,
implemented as a way to delay or even avoid the adrenal
escape phenomenon. This strategy is based on theory and
experimentation, however, and no clinical studies have
evaluated aminiglutethimide as an anti-catabolic agent.
It is important to note that while many people believe they
have used this drug as an anti-catabolic, few have actually
taken the correct dosage. Four tablets per day, or 1,000 mg,
appears necessary to significantly inhibit the demolase
enzyme (the enzyme responsible for converting
cholesterol to pregnenolone, and the target when reduced
cortisol is desired). Those who do venture this high
commonly report fatigue and discomfort, stating that the
drug is intolerable for any type of prolonged use. Today,
many athletes and bodybuilders are accepting that the
original proposed use of aminogluthethimide as a nonsteroidal
muscle-building agent does not seem to be a
plausible one. The only instances this author has really
heard of this drug ever being used at such doses
consistently with any type of positive response were
competitive bodybuilders partaking in high-dosed
Cytadren shortly before a contest. They claimed the shortterm
rise in androgen to corticosteroid ratio greatly aided
their abilities to bring out a show-ready hard and dense
physique, and credit the drug as genuinely being a very
effective pre-contest agent. In speaking with the late Paul
Borresen he summed up the pre-contest use of Cytadren
by stating, "1 have had considerable experience with the high
dose use. It makes athletes sleepy and weak. It seems to help
the last ten days before a show, and this is tried and tested."
Aromatase Inhibition: Aminoglutethimide is an efficient
aromatase inhibitor, and tends to inhibit the activity of this
enzyme at a much lower dosage from that what is required
for inhibition of corticosteroid production.830 831 While a
daily dosage of 1000 mg is typically needed to inhibit
cortisol, maximum suppression of aromatase and estrogen
levels is typically achieved at a dosage between 250 mg
and 500 mg, a point where strong adrenal steroid
blockage is not noted. There also seems to be no added
benefit by adding cortisol in terms of survival/response
rate among breast cancer patients, pointing to the fact
that the "adrenal escape phenomenon" bears little relation
to its abilities as an aromatase inhibitor. Ultimately, it
appears that not only do we need a higher dose (1,000 mg
or 4 tablets per day minimum) to really inhibit cortisol
production, but also that there is no need for an athlete to
implement a rotating dose schedule if the drug is being
used as an anti-estrogen.
Aminoglutethimide is usually regarded highly among
athletes and bodybuilders as an estrogen maintenance
agent. Studies have shown it to be capable of decreasing
aromatase activity by as much as 920/0 after administration
of 250 mg per day. Patient response rates also show
aminoglutethimide to be at least as effective as tamoxifen
therapy in treating estrogen dependent cancer cells, and
more effective under certain conditions. Due to its
discussed broad range of non-specific activity, however,
including the potential inhibition of not only estrogens,
but corticosteroids, aldosterone, and androgens as well, it
is not regarded as highly as newer (second and third
generation) aromatase inhibitors in terms of patient
comfort and efficacy, and is not widely used for this
purpose today. Athletes, however, still tend to consider it
to be an effective remedy for estrogenic side effects like
gynecomastia, increased water retention, and fat gain.
History:
Aminoglutethimide was FDA approved as an
anticonvulsant drug in 1960. Side effects were common
with treatment, however, including drowsiness, dizziness,
and partial loss of motor control. In 1966 reports of
adrenal insufficiency subsequent to aminoglutethimide
use were reported. The drug was withdrawn from the U.S.
market as an anticonvulsant that same year due to its
recently understood effects on the adrenal gland. By
1967, however, the drug was reintroduced for a new
purpose, namely inhibition of aromatase activity and the
treatment of breast cancer. It was one of the first
aromatase inhibitors sold, and is identified alongside
testolactone as a "first-generation" agent of this type.
Given its novel effects on adrenal steroid production, the
U.S. FDA also granted approval for the use of
aminoglutethimide for the treatment of Cushing's
syndrome.
At one time aminoglutethimide was available under
numerous brand names and in more than 2-dozen
countries. Ciba's Cytadren and Orimeten preparations
were by far the most common, and could be found in such
nations as Argentina, Australia, Austria, Brazil, Canada,
Chile, Czech Republic, France, Germany, Hong Kong,
Ireland, Israel, Italy, Malaysia, Netherlands, Norway, New
Zealand, Russia, South Africa, Spain, Sweden, Switzerland,
United Kingdom, and the United States. Additionally, the
drug could be found on occasion under other names
including Aminoblastin, Rodazol, and Mamomit. The vast
majority of original aminoglutethimide preparations have
since been discontinued, however. Today, the drug
remains available in a very small number of countries,
most notably the United States (Cytadren), Russia
(Mamomit), Hong Kong (Orimetene), and Australia
(Cytadren).
How Supplied:
Aminoglutethimide is most commonly supplied in tablets
of250 mg.
Structural Characteristics:
Aminoglutethimide is an analog of glutethimide. It has
the chemical designation 2-(4-Aminophenyl)-2ethylglutarimide;
3-(4-Aminophenyl)-3-ethylpiperidine2,6-
dione.
Side Effects:
Frequent side effects associated with aminoglutethimide
include fatigue, dizziness, skin rashes, fever, and nausea.
Other side effects may include sleep disorder, apathy,
depression, vomiting, stomach upset, thyroid dysfunction,
virilization, jaundice, elevated cholesterol levels, changes
in blood cell counts,and high blood pressure. Additionally,
those bodybuilders and athletes taking it at a dosage high
enough to promote cortisol suppression often note that
reduced levels of this hormone bring about more aches
and pains in the joints when trying to lift heavy weights. It
seems logical that this might lead to an increased
susceptibility to injury. Users should be careful not to
overexert themselves during the short periods in which
this drug is used in high doses. Most of the listed side
effects listed here are most common with higher dosed
regimens that inhibit the adrenal production of cortisol,
and are less common with athletes taking one or two
tablets per day as an anti-estrogen. Even in low doses
aminoglutethimide may cause birth defects, and should
never be taken during pregnancy.
Administration:
Aminoglutethimide is medically indicated for the
treatment of Cushing's syndrome, metastatic breast
cancer in postmenopausal women, and palliative
treatment in men with advanced prostate cancer. When
used to treat Cushings syndrome, the dosage used may
range from 1,000 mg to 2,000 mg per day, often in
conjunction with 20-30 mg of hydrocortisone to avoid the
aforementioned adrenal escape phenomenon. Athletes
and bodybuilders using aminoglutethimide for cortisol
inhibition will commonly take a dosage of 1,000 mg per
day, usually for brief periods of 2-3 weeks or less (10 days
of use pre-contest is reported with some bodybuilders). A
schedule of 2-days on, 2-days off may be used in an
attempt to extend the effectiveness of
aminoglutethimide for longer periods, but such use is
usually discarded in place of daily short-term
administration. The dosage most commonly used for
mitigating the estrogenic side effects of
anabolic/androgenic steroid use ranges from 125 mg to
500 mg per day (1/2 to 2 tablets), with 1 tablet (250 mg)
per day appearing to be the most common dosage
selected.
Availability:
Aminoglutethimide is produced in a small number of
countries, and is a fairly expensive pharmaceutical. As
such, it may sell for as much as $2 per tablet on the black
market. This, combined with limited availability, has
severely limited its more widespread use

guardianactual
05-20-2014, 06:22 PM
It's like Letro only it lowers cortisol as well! too bad it's kinda toxic.

akn
05-20-2014, 06:34 PM
i am a big letro fan but shit is expensive and i think if ur not gyno prone or estrogen sensitive we should stay away from ai and if willing to use start with a really low dose and if its working fine no need to bump it just my opinion

guardianactual
05-20-2014, 06:44 PM
I keep hearing letro's expensive but I dont think it is LMAO I paid like $30 for 75mg. I mean comparedd to Adex yes... but exemastane cost more.

akn
05-20-2014, 06:52 PM
your lucky bro , over her in pharmacies its like 258 $ for 30 tabs of 2.5 mg femra , i have to ask friends to bring it from different countries

bigdaddyo1617
05-20-2014, 08:59 PM
Wow that's a big difference

akn
05-20-2014, 09:07 PM
first time i had gyno symptoms and this price of letro was nightmare lol

Presser
02-14-2016, 10:18 AM
yeah letrozole is pretty affordable now days