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Substance
Letrozole
Active Dosage
2,5mg/tablet
Form
30 Tablets x 2,5mg.
Category
Oral
Classification
Non-steroidal aromatase inhibitor
Half Life
2 days
Dosage
0,5-2,5 mg/day
Acne
No
Water Retention
No
HBR
No
Aromatization
No
Hepatoxity
No
Description
Letrozole
is an anti-estrogen of the Aromatase Inhibitor (AI) family and is one
of the most potent and powerfully effective of all AI’s. In fact,
its potency is sometimes too much for some to handle when used for
off label use. Letrozole first gained U.S. FDA approval in 1997 and
would hit the market under the brand name Femara through Novartis.
Although Femara is the dominating trade name of the AI, unlike most
AI’s it is the only one generally known by its chemical name
Letrozole far more commonly than its dominating brand name.
Letrozole
was first developed in an effort to combat breast cancer in
post-menopausal women. In fact, it would prove to be virtually
identical to the already popular AI in Arimidex (Anastrozole). While
intended for breast cancer treatment, like many AI’s, it has found
a welcomed home among anabolic steroid users. Letrozole is one of the
most commonly used anti-estrogens among steroid users during steroid
use to combat possible estrogenic related side effects. It is so
effective as an anti-estrogen in this regard many anabolic steroids
have effectively reversed gynecomastia symptoms with Letrozole.
Letrozole
Functions & Traits:
Letrozole
is an AI, which holds the purpose of blocking the aromatase enzyme,
which is in turn responsible for the production of estrogen. By
inhibiting estrogen production, this lowers total serum estrogen
levels in the body. This will be useful to the breast cancer patient
on the basis of such cancer often feeding off the estrogen hormone.
It will be beneficial to the anabolic steroid user as excess estrogen
often leads to some of the most commonly associated side effects of
anabolic steroid use.
Letrozole
also carries the ability to increase natural testosterone production
through an increase in Luteinizing Hormone (LH) and Follicle
Stimulating Hormone (FSH). There have been physicians who have chosen
Letro as it’s often known to treat low testosterone conditions, but
this is normally not the preferred method of treatment. Without
question, when it comes to low testosterone treatment exogenous
testosterone is generally the only thing that makes sense. However,
Letrozole can be useful in such a plan in conjunction with exogenous
testosterone in order to combat possible side effects. We will look
into this in the effects section.
Effects
of Letrozole:
Letrozole
as an anti-estrogen is extremely beneficial to breast cancer
patients. Many forms of breast cancer actively feed off the estrogen
hormone. By inhibiting the production of estrogen, which in turn
lowers the amount of circulating estrogen in the body, this has the
ability to starve the cancer. For years Nolvadex was the preferred
form of treatment for this purpose. Nolvadex actively binds to the
estrogen receptor, thereby preventing estrogen from binding. However,
it does not inhibit or lower production. Nolvadex is still extremely
valuable in breast cancer treatment plans, but many physicians,
especially in extreme cases have begun to use AI’s first. Once the
cancer is in remission, at this stage a SERM like Nolvadex may
replace the AI in an effort to protect against the cancer
reappearing.
For
the anabolic steroid user, the same anti-estrogenic effect provided
by Letrozole is tremendously beneficial. Many anabolic steroids have
the ability to increase estrogen levels due to testosterone’s
interaction with the aromatase enzyme. As estrogen levels rise, this
can lead to gynecomastia and excess water retention. If water
retention becomes severe, this can in turn promote high blood
pressure. While many anabolic steroids have the ability to aromatize
and promote an increase in estrogen, not all anabolic steroids carry
this ability. However, many common steroids carry this ability
including Methandrostenolone (Dianabol) as well as all forms of
testosterone. The Nandrolone (Deca Durabolin, Durabolin, NPP, etc.)
and Boldenone (Equipoise) hormone also carry the ability to aromatize
to a degree. Nandrolone will aromatize at approximately 20% the rate
of testosterone and Boldenone at approximately 50%. While both
aromatize significantly less than testosterone, it is enough to
promote estrogenic related side effects. The probability is increased
with Nandrolone as it carries a strong progestin nature. Progesterone
has the ability to stimulate the estrogenic mechanism and can lead to
gynecomastia. AI’s like Letrozole can be useful when using all the
aforementioned steroids.
By
including Letrozole in a cycle that contains aromatizing anabolic
steroids, this can prevent the estrogenic related side effects. This
will protect the individual from gynecomastia and water retention.
Further, while many steroids can promote high blood pressure despite
aromatization, an AI will improve the individual’s odds when water
retention is the culprit. Heavy excess water retention is normally
the number one cause of high blood pressure among steroid users.
Undeniably,
AI’s like Letrozole are the most effect means at combating
estrogenic related side effects. However, they can also have a
negative impact on cholesterol. Alone AI’s do not appear to have a
strong, negative effect on cholesterol, but when coupled with an
aromatizing steroid like testosterone the adverse cholesterol effect
is enhanced. For this reason, many will find SERM’s like Tamoxifen
Citrate (Nolvadex) should be their first choice in estrogen
protection. SERM’s will not negatively affect cholesterol; in fact,
SERM’s, while anti-estrogenic, actively act as estrogens in the
liver, and in turn, promote healthier cholesterol levels. We’ll
look at this in more detail in the side effect section, and while
Letrozole can be used without an adverse cholesterol effect, it will
take some effort on your part.
With
its ability to promote natural testosterone production, Letrozole is
often an appealing choice for Post Cycle Therapy (PCT) plans. This
can also make it appealing for low testosterone treatment, but it’s
often not enough. However, for PCT purposes, while it can be
effective it’s generally not recommended. The primary purpose of
PCT is stimulating natural testosterone production, which Letrozole
can do very well. However, part of the purpose of PCT is also
normalization, which will be difficult with severely suppressed
estrogen levels. Estrogen is an important hormone as it promotes a
stronger immune system and healthier cholesterol levels. For the
anabolic steroid user, his best bet for PCT is sticking with SERM’s
for his natural testosterone production needs.
Side
Effects of Letrozole:
The
side effects of Letrozole will cover a wide breadth and will be very
similar to Arimidex. Both weakness and fatigue are two of the most
common side effects of Letrozole use. However, for the anabolic
steroid user this will normally not be an issue. The use of anabolic
steroids should prevent such states so as long as estrogen
suppression isn’t taken too far. The exception would be its use
during a hard bodybuilding contest prep cycle. During a harsh
bodybuilding diet, the individual will normally be very weak and
fatigue at the end of his diet due to tremendously intense training
and very low caloric intake. Beyond possible energy issues, the most
common side effects of Letrozole use include:
- Headaches
- High Blood Pressure
- Hot Flashes
- Joint Pain
- Depression