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Nolvadex Profile
Pharmaceutical Name: Tamoxifen Citrate
Drug Class: Selective Estrogen Receptor Modulator
Active Life: 5-7 days
Tamoxifen citrate is a selective estrogen receptor modulator. Selective estrogen
receptor modulators can act as estrogen receptor agonists or antagonists (1).
This activity of tamoxifen citrate is tissue selective, effecting those estrogen
receptors located in the liver, breast, and bone. When the tamoxifen molecule
binds to this receptor, the estrogen is blocked and can not have any influence,
thereby remaining inactive in that tissue. By doing so, an "anti-estrogenic"
effect is achieved. The drug was developed and still used to treat breast
cancer. It is often used as a first option due to its mild nature in comparison
to aromatase inhibitors (2). Of course one would want to use the mildest
compound possible when dealing with estrogen levels in women, but one could
afford to be more aggressive in dealing with male strength athletes or
bodybuilders.
In terms of its use in steroid users, tamoxifen citrate can help in two ways.
Firstly due to the binding affinity of the compound it is able to help in the
prevention of gynocomastia (3). Tamoxifen will compete with estrogen for the
estrogen receptors in certain tissues, including the breast, and if it can bind
to the receptor estrogen will not have an opportunity to interact with receptor
and therefore gynocomastia should not be able to develop. When using anabolic
steroids that can convert to estradiol (estrogen) this protection against
gynocomastia can be invaluable. However it should be noted that tamoxifen
citrate will not eliminate the estrogen or disallow the conversion to occur.
Instead it attempts to counteract the effects of circulating estrogen in the
body in those tissues that the drug effects. Therefore there is no evidence that
tamoxifen citrate has any effects counteracting etrogenic side effects that are
unrelated to the tissues that are not in the breast, liver or bone. Namely there
is no real causal connection to any reduction in water retention and acne in
users that begin taking tamoxifen citrate as it relates to estrogen.
The second, and possibly more beneficial, aspect of tamoxifen citrate for
steroid users is its ability to increase the production of luteinizing hormone
and follicle stimulating hormone, and therefore increasing testosterone (4).
This ability is why it is often used by steroid users during their post-cycle
therapy. There are numerous studies that indicate that tamoxifen citrate can
increase the levels of these hormones quite dramatically. Tamoxifen citrate does
this by blocking the negative feedback inhibition caused by estrogen at the
hypothalamus and pituitary, and this in turn will help to increase the
production of these hormones. Unlike clomiphine citrate, tamoxifen citrate has
also been shown to increase luteinizing hormone responsiveness to gonadotropin
releasing hormone. Clomiphine citrate can lower this responsiveness over time.
Use and Dosing Nolvadex
In terms of dosing for combating gynocomastia that has begun to form, there is
very little research. The limited research that does exist does point to the
fact that doses of 20-40mgs per day are effective in treating the existing
condition (3). However, anecdotally users have reported sometimes using doses of
60-80mgs per day. These doses may have more to do with users� impatience rather
than the need for higher doses, as no research indicates that such doses are
needed. It should be noted as well however that tamoxifen citrate may have no
effect on existing gynocomastia in some individuals. Many users have indicated
that the compound will only help alleviate symptoms if the gynocomstia has not
been apparent for a long period of time. Of course, this is all subjective and
the effectiveness of the drug can only be determined on a trial and error basis.
For use during post-cycle therapy users have anecdotally indicated that doses
ranging between 20 and 40mgs per day are average. These doses have been shown to
significantly raise levels of testosterone, luteinizing hormone and follicle
stimulating hormone (4). Most users have reported when using tamoxifen citrate
for their post-cycle therapy they will administer the drug for a minimum of
three weeks. A maximum length has not necessarily been established due to the
few side effects associated with the compound. In this case, this compound can
be run for as long as wanted with little to no concern being needed to be paid
to potential side effects. See the below section for more details.
Some users have used tamoxifen citrate for the purpose of helping raise their
HDL (good) cholesterol values. In theory it is thought that since the compound
is an estrogen agonist in the liver and therefore is capable of activating the
estrogen receptor and mimicking the actions of the hormone in the organ that it
may help improve cholesterol levels as estrogen does. However this effect is
rather slight and won�t significantly improve a user�s HDL levels very
noticeably at all. This is especially true when one factors in the dramatic
effect that most anabolic steroids have on these levels. For this reason,
tamoxifen citrate should not be relied upon for this purpose.
Risks and Side Effects while using Nolvadex
One of the possible side effects associated with use of tamoxifen citrate is the
possible reduction of insulin-like growth factor levels. If these levels are
reduced this could suppress the gains an individual can make slightly. However
this reduction, if it actually exists, would not be overly significant with
gains in muscle mass only being marginally reduced for the most part.
Another effect of use of tamoxifen citrate may be vision problems. Recently,
there has been some information from researchers that indicates corneal, retinal
and optic nerve abnormalities seen in patients using the drug could be related
to its use (5). Anecdotally a small number of steroid users have reported that
they have suffered from visual problems while using this drug as well. After
discontinuation of the drug these symptoms seemingly dissipate. However there is
simply not enough research on the subject to know whether permanent damage could
occur. More research needs to be conducted.
Other than these concerns, there is little in the way that long-term use of
tamoxifen citrate could cause damage to in the human body. It is seemingly safe
in terms of possible effects to the body�s hormonal production, other than the
one relating to insulin-like growth factor, and endocrine system (4). For the
vast majority of users the compound is relatively side effect free and well
tolerated.
References
1. Bruning PF, Bonfrer JM, Hart AA, de Jong-Bakker M, Linders D,
van Loon J, Nooyen WJ. Tamoxifen, serum lipoproteins and cardiovascular risk. Br
J Cancer. 1988 Oct;58(4):497-9
2. Konig R, Schonberger W, Neumann P, Benes P, Grimm W. [Treatment of marked
gynecomastia in puberty with tamoxifen] Klin Padiatr. 1987 Nov-Dec;199(6):389-91
3. Schopman W, Slager E, Hackeng WH, Mulder H. Stimulation of calcitonin
secretory capacity by increased serum levels of testosterone in men treated with
tamoxifen. Int J Androl. 1987 Dec;10(6):747-51
4. van Bergeijk L, Gooren LJ, van der Veen EA, de Vries CP. Effects of short-
and long-term administration of tamoxifen on hCG-induced testicular
steroidogenesis in man: no evidence for an oestradiol-induced steroidogenic
lesion. Int J Androl. 1985 Feb;8(1):28-36
5. Isherwood, Dana. Tamoxifen and Your Eyes. Breast Cancer Action. Newsletter
#25�August 1994
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