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Cytadren
Pharmaceutical Name: Aminoglutethimide
Drug Class: Cortisol and Aromatase Inhibitor
Active Life: approximately 24 hours
Aminoglutethimide is a non-steroidal compound that works to inhibit both
cortisol production as well as the aromatization of androgens. It works to
block the production of cortisol by stopping the conversion of cholesterol to
pregnenolone (1). This along with the ability to inhibit aromatization of any
androgens that a steroid user may be administering would obviously be
beneficial for those hoping to not only minimize estrogenic side effects but
also lowering the levels of the catabolic hormone cortisol.
The medical use of aminoglutethimide is primarily to treat
hyperadrenocorticism, also known as Cushing�s syndrome, which is the excessive
production of cortisol by the body. To a lesser extent the drug has also been
used in the treatment of breast cancer, as is the case with other aromatase
inhibiting drugs. However since there are far superior drugs now available
aminoglutethimide is not a popular drug in cancer treatment.
In terms of research conducted in athletes or those looking to use the drug
for athletic or cosmetic purposes, there is of course very little as is the
case with many drugs used by bodybuilders and strength athletes. For this
reason we are left to extrapolate the best methods to use aminoglutethimide
from anecdotal information as well as trying to form the available research to
fit into our needs.
A significant aspect of aminoglutethimide is that along with its ability to
inhibit both cortisol and aromatization, it also suppresses the production of
adrenal androgens (2). Obviously this would be a negative for someone that was
not using exogenous hormones, but since it is unlikely that athletes or other
steroid users would be administering aminoglutethimide without also using
anabolic steroids this is likely not to be a concern for most.
The cortisol inhibiting effect of aminoglutethimide is short lived in the body
due to the body�s ability to adapt to the action of the drug. By lowering the
natural production of cortisol the body will begin to produce
adrenocorticotropic hormone. The hormone sparks an increase in cortisol
production in the body to help normalize its levels causing the action of the
drug to become basically moot (3). It is believed by some that if one staggers
their use of the drug to a schedule similar to two days on and then two days
off that this may be enough to ward off the body�s response to the lowered
cortisol levels while still reaping the benefit of partial suppression. There
is little research to indicate that this is true however.
Use/Dosing of Cytadren
To achieve the two primary actions of aminoglutethimide, namely aromatase
inhibition and cortisol reduction; two very different dosing ranges are used.
For aromatase inhibition, maximum estrogen suppression is achieved at 250 to
500 milligrams per day. In some studies it has been demonstrated that as
little as 250 milligrams of aminoglutethimide can suppress aromatase activity
by 92% in some users, with larger doses only providing minimally improved
results. In contrast, for cortisol suppression dosages typically run in excess
of one gram of aminoglutethimide per day. While running a larger dose the
enzyme that is responsible for converting cholesterol into prognenolone and
thereby creating cortisol, the demolase enzyme, should be maximally inhibited
(3).
As noted earlier however, when running the drug for cortisol suppression, it
will provide diminishing results if run consistently. For this reason
administering the drug for only two or three days consecutively should be the
norm for most users. Any more then that and the body will begin to produce
more cortisol to compensate. As for dosing for aromatase inhibition, doses
ranging from approximately 250 to 500 milligrams per day, these should be
moderate enough to not affect cortisol levels and therefore there is no need
to skip days of administering the drug. Every day administration at that
dosage should not negatively impact the user.
As for the duration of the cycles that include aminoglutethimide, it again
depends on the dosages used. If the user is using doses in the range of 250 to
500 milligrams per day, a duration of six to eight weeks should be safe for
the majority of users. However if one is using it at doses of approximately
one gram per day the user will want to limit their use of the drug to only a
few weeks, possibly prior to a competition. This is due to the potential for
liver toxicity that comes with aminoglutethimide, as will be discussed further
in the Risks/Side Effects portion of this profile below.
As a side note, it should be mentioned that unlike many other aromatase
inhibitors or other drugs that are said to have �anti-estrogenic� qualities,
aminoglutethimide does not raise other beneficial hormones for strength
athletes and bodybuilders in the body such as luteinizing hormone,
gonadotropin releasing hormone and/or testosterone, among others. For this
reason there is no real reason to run this drug during post-cycle therapy as
there are countless other compounds that offer additional benefits that the
user should take advantage of.
Risks/Side Effects of using Cytadren
It appears that there is a significant risk of hepatoxicity with
aminoglutethimide when used over extended periods of time even at relatively
moderate dosages (4). For this reason lengthy use of the drug would not be
recommended for most users and even short cycles of it are likely to increase
liver values.
Other potential negative side effects include apathy, insomnia,
gastrointestinal distress, and thyroid dysfunction. As well, like other
aromatase inhibitors, cholesterol levels in both men and women may be
negatively affected with long term usage of the drug. With cortisol
suppression it is likely that users will also experience joint discomfort when
training along with a feeling of malaise. This is a common side effect and
often reported when users are administering significantly large enough doses
of the drug to achieve cortisol suppression. However, these cortisol-related
side effects will only become noticeable if the doses administered are high
enough to produce such an effect. If run at lower doses exclusively for the
aromatase inhibitor effect, these will be less likely to occur.
References
1. Lonning PE. Oestrogen suppression--lessons from clinical
studies. Best Pract Res Clin Endocrinol Metab. 2004 Mar;18(1):33-45.
2. Schmid P, Possinger K. Interactions of antioestrogens and aromatase
inhibitors. Forum (Genova). 2002;12(1):45-59.
3. Dexter RN, Fishman LM, Ney RC et al. Inhibition of adrenal corticosteroid
synthesis by aminoglutethimide: Studies on the mechanism of action. J Clin
Endocrinol 27 (1967) 473-80.
4. Perez AM, Guerrero B, Melian C, Ynaraja E, Pena L. Use of aminoglutethimide
in the treatment of pituitary-dependent hyperadrenocorticism in the dog. J
Small Anim Pract. 2002 Mar;43(3):104-8.
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