Nolvadex — tamoxifen citrate

Tamoxifen citrate is a non-steroidal anti-estrogenic drug, used widely in clinical medicine. It is specifically a Selective Estrogen-Receptor Modulator (SERM) of the triphenylethylene family, and possesses both estrogen agonist and antagonist properties. As such, it may act as an estrogen in some tissues while blocking the action of estrogen in others. In breast tissue tamoxifen citrate is a strong anti-estrogen, and as a result it is commonly used in the treatment of hormone-responsive breast cancer in women. In some cases it is even utilized as a preventative measure, taken by women with an extremely high familial tendency for breast cancer. In male bodybuilders and athletes, tamoxifen citrate is commonly used (off-label) to counter the side effects caused by elevated estrogens subsequent to the use of certain anabolic/androgenic steroids.

The primary worry among the athletic/bodybuilding population is gynecomastia, or the very unsightly development of female breast tissue in men. This can be first noticed by the appearance of swelling or a small lump under the nipple. If left to progress, this can develop into a large hard-tissue gynecomastia that may be an irreversible occurrence without surgery. The estrogen can also lead to an increase in the level of water retained in the body, resulting in a notable loss of definition as the muscles begin to look smooth (even bloated) due to the retention of subcutaneous fluid. Fat storage may also be increased as estrogen levels rise in men. In fact, differences in the estrogen/androgen ratio are one of the reasons women have a higher body fat percentage, and different fat distribution (hips/thighs), than men.

Tamoxifen citrate also possesses the ability to increase production of FSH (follicle stimulating hormone) and LH (luteinizing hormone). This is accomplished by blocking negative feedback inhibition caused by estrogen at the hypothalamus, which (via the actions of GnRH) fosters the release of the mentioned pituitary hormones. This is very similar to the function ofClomid and cyclofenil, tamoxifen citrate can have a positive impact on one’s serum testosterone level. This “testosterone stimulating” effect is an added benefit when preparing to conclude a steroid cycle. Since anabolic/androgenic steroids tend to suppress endogenous testosterone production, tamoxifen citrate can help restore a balance in hormone levels. It is most commonly used as part of a comprehensive post cycle recovery program (see Post-Cycle Recovery).

Note that like some other triphenylethylene compounds, tamoxifen citrate can act as an estrogen in the liver . Estrogenic action in the liver is important in the regulation of serum cholesterol, and tends to support HDL (good) cholesterol synthesis and LDL (bad) cholesterol reductions. Since steroid-using bodybuilders are already dealing with the negative cardiovascular effects of these drugs, compounding the issue with aromatase inhibitors (which will lower total serum estrogen levels) may not always be the best option. Using a drug that blocks gynecomastia, for example, while at the same time supporting improved cholesterol values, might be much more ideal. It is important to note that tamoxifen citrate is not sufficient to stabilize serum cholesterol at healthy levels with the use of c-17alpha alkylated orals or high doses of steroids in general. The effect it would have on cholesterol values would likely be one of degrees, and cannot be relied upon to eliminate cardiovascular disease risk from anabolic/androgenic steroid use.

Brand name Nolvadex, Tamoxifen citrate

Tamoxifen Citrate History

Tamoxifen citrate was first synthesized in 1962 by ICI . It was made commercially available in the U.S. not long after, but was initially used to treat certain forms of female infertility, a purpose for which tamoxifen citrate does not seemed ideally suited. In 1971, the first clinical trials evaluating the effectiveness of tamoxifen citrate in breast cancer patients were undertaken . Two years later, noting the link between estrogen and breast cancer and the success of early trials, ICI pursued marketing the drug in the U.S. to treat breast cancer. It was not until 1977 that FDA approval for this use would finally be granted. Tamoxifen citrate was sold by ICI in a wide number of countries under the Nolvadex brand name (the company would later become known as AstraZeneca). A number of generics and other brands followed, presently too numerous to list. In 1998, the FDA approved expanding the indicated uses of tamoxifen citrate to include breast cancer prevention for women at high risk for developing the disease. In spite of continued clinical success with the drug for both cancer treatment and prevention, in June 2006 AstraZenica finally discontinued the sale of Nolvadex in the U.S. A number of generic versions are still available in this country, however, ensuring easy patient access to the drug. Tamoxifen citrate is presently the most popular anti-estrogen used by athletes and bodybuilders.

How is Tamoxifen Citrate Supplied

Tamoxifen citrate is most commonly supplied in tablets of 10 mg or 20 mg.

Structural Characteristics of Tamoxifen Citrate

Tamoxifen citrate is classified as a selective estrogen receptor modulator, with both agonist and antagonist properties (also known as an estrogen agonist/angagonist). It has the chemical designation (Z)2- [4-(1,2-diphenyl-1-butenyl) phenoxy]-N, Ndimethylethanamine 2- hydorxy-1,2,3- propanetricarboxylate (1:1).

Tamoxifen Citrate Side Effects

Common side effects associated with the administration of tamoxifen citrate include hot flashes, vaginal bleeding, vaginal discharge, vaginal itching, upset stomach, headache, lightheadedness, edema, and hair loss. Other listed adverse reactions include skin rash, reduced platelet or white blood cell count, visual disturbances, uterine fibroids, endometriosis and other endometrial changes, deep vein thrombosis and pulmonary embolism, changes in liver enzyme levels, and increased triglyceride levels. An increased incidence of endometrial cancer and uterine sarcoma has been reported in association with tamoxifen citrate. Tamoxifen citrate may cause birth defects and should not be taken during pregnancy.

Tamoxifen Citrate Administration

Tamoxifen citrate is indicated for:

  • the treatment of metastatic breast cancer in women and men
  • adjuvant treatment of node-negative breast cancer following breast surgery and radiation
  • adjuvant treatment of node-positive breast cancer in postmenopausal women following breast surgery and radiation
  • reduction in incidence of contralateral breast cancer (in the other breast) in the adjuvant setting
  • reduction in incidence of invasive breast cancer in women with DCIS (Ductal Carcinoma in Situ) following breast surgery and radiation
  • reduction in incidence of breast cancer in women at high risk for breast cancer

In women and men with metastatic breast cancer, a dose of 10-20 mg is administered twice a day (morning and evening). When used by men (off-label) to mitigate the estrogenic effects of anabolic/androgenic steroid use, a daily dosage of 10-30 mg (1-3 tablets) is usually administered while any offending steroids are taken, or as part of a comprehensive post-cycle hormone recovery program.

It is important to note that anti-estrogen use may slightly reduce gains made during a steroid cycle, as many androgenic/anabolic steroids seem to exhibit their most powerful anabolic effects when accompanied by a sufficient level of estrogen (See Estrogen Aromatization). This may be one reason why gains made with a strong aromatizable androgen like testosterone are usually more pronounced than those achieved with anabolic steroids that aromatizes to a lower (or no) degree. Therefore, it is usually advised to identify a specific need for tamoxifen citrate before committing to its use during a cycle. Many people, in fact, find the use of an anti-estrogen unnecessary, even when utilizing problematic compounds such as testosterone or methandrostenolone. Others, however, find they are troubled by water retention and gynecomastia even with milder (less estrogenic) drugs like Deca-Durabolin and Equipoise. The estrogenic response to steroid use is very individual, and may be influenced by factors such as age and body fat percentage (adipose tissue is a primary site of aromatization).

Tamoxifen Availability

Tamoxifen citrate is widely manufactured, and can be found in virtually every developed nation of the world. The drug is also commonly circulated on the black market. Given its relatively low price and high availability, counterfeit product do not appear to be a large issue.

Tamoxifen is produced by Swiss Remedies and available across Europe. Due to numerous fakes of this product, Swiss Remedies offers a convenient online product checker.

Magnus Pharmaceuticals makes the product Tamoxifen primarily for the EU and UK markets. Due to fake products appearing on the market, Magnus offers an online checker that lets steroid users verify their product originality.

Bodybuilders reference

Nolvadex is a drug commonly referred to as an anti-estrogen. This would suggest less or no estrogen is produced due to the drug's actions as in the case of Teslac. Actually, Nolvadex is an estrogen antagonist, meaning it competes with estrogen at estrogen receptor- sites. This prevents the active estrogen from entering its receptor and creating an estrogenic complex capable of activity. Since many AAS aromatize (covert to estrogen) to some degree, the control of feminizing side effects (males should pay attention here) is important. Males normally have a very low estrogen level. During AAS cycles, due to aromatization, estrogen levels rise considerably. This elevated estrogen level can cause feminizing side effects such as increased fat deposits, water retention, and gynecomastia (growth of breast gland tissue and painful tumors under the nipple). As a rule, it is more the ratio of androgens-to-estrogens than the simple increase in estrogen that actually initiates feminizing side effects.

It is important that the reader realizes that Nolvadex does not decrease estrogen production and that it simply blocks estrogen receptors. For this reason the sudden discontinuance of Nolvadex will allow the increased level of circulating estrogen to merge with the newly freed receptors and do feminine things to the body.

"Enter Proviron". At the end of a steroid cycle, the body's natural testosterone production can be impaired. Due to the aromatization of the AAS estrogen levels are significantly higher than normal and Nolvadex only helps by blocking the estrogen receptors. If an athlete abruptly ends an AAS protocol without regeneration of the HPTA under these conditions, much of the hard earned gains would disappear due to estrogen becoming the dominant hormone. So what did the boys (that didn’t want to be a girl) do?

Proviron is an anti-estrogen (*See "Proviron" for more info) that helps to prevent estrogen production while elevating androgen levels. During the last week of an AAS cycle, some male bodybuilders began a HCG protocol (*See HCG) and administered 25- mg Proviron/10-20-mg Novladex 1-2 times daily. This was commonly noted to almost completely suppress post-cycle estrogen and its activity. Since Nolvadex increases the body's own testosterone production, as does HCG, much of the cycle gains were retained quite well. Nolvadex has a direct effect on the hypothalamus and therefore increases the release of Gonadotropic hormones to a minor degree. (The hormones that tell the Leydig cells in the testes to produce androgens such as testosterone are refereed to as Gonadotropics) Many added Clomid (*See Clomid) to their post-cycle stacks beginning 6-10 days after HCG and continued for the average reported two week duration. In most cases the result was athletes with normal (or above) sex drive and androgen production!

*High dosage use of Nolvadex can inhibit natural testosterone production. This is due to inhibition of enzymes needed for testosterone production by the testes.

Nolvadex was normally layered into any protocol utilizing high aromatizing steroids such as testosterone, Dianabol, or those that are progesterone receptor stimulators such as Anadrol-50. Those who were prone to high fat deposits, water retention, and gyno consistently reported inclusion of Nolvadex. Many are were to obtain excellent estrogenic activity suppression with only 10-mg daily while others noted the need for as much as 60-mg daily (20mg 3 times daily). The best results and guidelines were obtained by starting low and increasing dosages only when necessary.

It is important for the reader to realize that AAS must have some estrogen present in order to achieve their full positive potential effectiveness and provide the best commonly desired results. This is why many AAS lose their anabolic qualities when combined with anti-estrogens. It is also why Methandriol magnifies the effects of the same AAS. Those who used high anabolic/moderate-low androgenic steroids such as nandrolones, Primobolan, or Winstrol, and did not combine them with high aromatizing steroids (such as testosterone) often considered not using Nolvadex during cycles the best choice when increased mass was the primary intent.

Women who used Nolvadex usually did so because it aids in fat loss due to less estrogenic activity. I have yet to see a female compete whom was able to achieve truly cut legs with out it. Women athletes often combined 10-20mg of Nolvadex with 50-75mg Proviron daily for the last few weeks of dieting. Due to availability of Clenbuterol, Proviron dosages were reported lower as of late, at least in female fitness competitors. Women should be aware that birth control is an estrogen and Novladex will block its effectiveness. Women have note irregular menstrual cycles, weaker menstrual bleeding, and sometimes skip periods all together during Nolvadex use. I know several women who use Nolvadex for this reason and can not say I disagree with their choice. After all, the use of progestin type birth control as a means of regulating or even stopping menstruation is becoming accepted in the medical circles at last.

A few athletes have experienced a paradox when using high dosages of Nolvadex. Instead of lowering estrogenic activity, it increased it. What happened was that the Adrenal glands went into over drive producing a pro-hormone called DHEA. DHEA is actually an adrenal androgen normally secreted in lower levels. As circulating levels increased enzymic factors came into play. Research shows DHEA readily converts into androstenedione, and to some extent, estrogens in males. (That sucks!) The female endocrine system usually favors testosterone production from converted DHEA or androstenedione. The newly formed estrogen then overwhelmed the estrogen receptors blocking the intended qualities of Novladex. In this case, Proviron, and especially Teslac where notably better choices.

*Gyno that fails to react to these drugs normally must be removed by surgery. DHT derivatives can cause increases endogenous estrogen production also in some individuals. Cytadren was a commonly co-administered drug with Nolvadex.

Anabolic Steroid Guide reference

This remedy is somewhat different from others since it is not an anabolic/androgenic steroid. For male and female bodybuilders, how-ever, it is a very useful and recommended compound which is con-firmed by its widespread use and mostly positive results. Nolvadex belongs to the group of sex hormones and is a so-called antiestrogen. The normal application of Nolvadex is in the treatment of certain forms of breast cancer in female patients. With Nolvadex it is pos-sible to reverse an existing growth process of deceased tissue and prevent further growth. The growth of certain tissues is stimulated by the body's own estrogen hormone. This is especially true for the breast glands in men and women since the body has a large number of estrogen receptors at these glands which can bond with the estro-gens present in the blood. If the body's own estrogen level is unusu-ally high an undesired growth of breast glands occurs. However, in healthy women and particularly in men this is not the case. Despite this, it is mostly male bodybuilders who use Nolvadex, and fewer women. At first sight this seems somewhat inconceivable but when taking a closer look, the reasons are clear. Bodybuilders who take Nolvadex also use anabolic steroids at the same time. Since most steroids aromatize more or less strongly, i.e. part of the substance is converted into estrogens, male bodybuilders can experience a sig-nificant elevation in the normally very low estrogen level. This can lead to feminization symptoms such as gynecomastia (growth of breast glands), increased fat deposits and higher water retention.

The antiestrogen Nolvadex works against this by blocking the es-trogen receptors of the effected body tissue, thereby inhibiting a bonding of estrogens and receptor. It is, however, important to un-derstand that Nolvadex does not prevent the aromatization but only acts as an estrogen antagonist. This means that it does not prevent testosterone and its synthetic derivatives (steroids) from converting into estrogens but only fights with them in a sort of "competition" for the estrogen receptors. This characteristic has the disadvantage that after the discontinuance of Nolvadex a "rebound effect" can occur which means that the suddenly freed estrogen receptors are now able to absorb the estrogen present in the blood. For this reason the combined intake of Proviron is suggested (see Proviron.) Nolvadex is also useful during a diet since it helps in the burning of fat. Al-though Nolvadex has no direct fatburning effect its antiestrogenic effect contributes to keeping the estrogen level as low as possible. Nolvadex should especially be taken together with the strong an-drogenic steroids Dianabol and Anadrol 50, and the various test-osterone compounds. Athletes who have a tendency to retain water and who have a mammary dysfunction should take Nolvadex as a prevention during every steroid intake. Since Nolvadex is very affective in most cases it is no wonder that several athletes can take Anadrol 50 and Dianabol until the day of a competition, and in combination with a diuretic still appear totally ripped in the. limelight. Those who already have a low body fat content will achieve a visibly improved muscle hardness with Nolvadex.

Several bodybuilders like to use Nolvadex at the end of a steroid cycle since it increases the body's own testosterone production -which will be discussed in more detail in the following-to counter-act the side effects caused by the estrogens. These can occur after the discontinuance of steroids when the androgen level in relationship to the estrogen concentration is too low and estrogen becomes the dominant hormone. A very rare but all the more serious problem of Nolvadex is that in some cases it does not lower the estrogen level but can increase it. Another disadvantage is that it can weaken the anabolic effect of some steroids. The reason is that Nolvadex, as we know, reduces the estrogen level. The fact is, however, that certain steroids - especially the various testosterone compounds-can only achieve their full effect if the estrogen level is sufficiently high. Those who are used to the intake of larger amounts of various steroids do not have to worry about this. Athletes however, who predominantly use mild steroids such as Primobolan, Winstrol, Oxandrolone, and Deca-Durabolin should carefully consider whether or not they should take Nolvadex since, due to the compound's already moderate ana-bolic effect, an additional loss of effect could take place, leading to unsatisfying results.

A rarely observed but welcome characteristic of Nolvadex is that it has a direct influence on the hypothalamus and thus, by an in-creased release of gonadotropine, it stimulates the testosterone pro-duction in the testes. This does not result in a tremendous but still a measurable increase of the body's own testosterone. This effect, however, is not sufficient to significantly increase the testosterone production reduced by anabolic/androgenic steroids.

The side effects of Nolvadex are usually low in dosages of up to 30 mg/day In rare cases nausea, vomiting, hot flashes, numbness, and blurred vision can occur. In women irregular menstrual cycles can occur which manifest themselves in weaker menstrual bleeding or even complete missing of a period. Women should also be careful not to get pregnant while taking Nolvadex. It is important for fe-male athletes that Nolvadex and the "pill" not be taken together since the antiestrogen Nolvadex and the estrogen-containing pill nega-tively counterfeit each other. The normal daily dosage taken by athletes corresponds more or less to the dosage indications of the manufacturer and is 10-30 mg/day To prevent estrogenic side ef-fects normally 10 mg/day are sufficient, a dosage which also keeps low the risk of reducing the effect of simultaneously-taken ste-roids. Often it is sufficient if the athlete begins this preventive intake of Nolvadex only three to four weeks after the intake of anabolics. Athletes who have tendencies toward gynecomastia, strong water retention, and increased fat deposits with steroids such as Dianabol, Testosterone, Anadrol 50, and Deca-Durabolin usually take 20-30 mg/day The combined application of Nolvadex 20-30 mg/day and Proviron 25-50 mg/day in these cases leads to excellent results. The same is true for athletes who are in competition, and for women. Women, however, should do without the intake of Proviron or at least reduce the dose to one 25 mg tablet per day. Unfortunately, in most cases, a very pronounced gynecomastia ("bitch tits") cannot be reduced by taking Nolvadex so that often surgery is required, surgery which is not paid for by health insurance. First signs of a possible gynecomastia are light pain when touching the nipples. The tablets are usually taken 1-2x daily, swallowed whole without chewing, with some liquid during meals.

Nolvadex unfortunately is a very expensive compound. Some ex-amples: In Germany one hundred 20 mg tablets cost $192. In Spain the prices are fixed by the govern-ment and it makes no difference whether it is an original Nolvadex or a generic compound. One hundred 20 mg tablets cost approx. $60 in Spain. In Greece the same quantity costs about $85. The athlete should look for the 20-mg version since, from its price, it is the most economical. On the black-market, mostly the foreign Nolvadex can be found costing about $2 - 3 per 20 mg tablet. Origi-nal Nolvadex tablets can be easily identified since, on the front, ICI (name of the manufacturer) is stamped and, on the back, the name "Nolvadex". Most of the time the tablet strength is also imprinted. Ten tablets are included in an unusually large push-through strip. In the U.S. original Nolvadex is packaged by the manufacturer, ICI Pharma, in small, white plastic boxes with a childproof screw cap. So far there are no fakes of Nolvadex and its generic products.

Newbies Research Guide reference

10 mg/tab 60 or 250/bottle. This drug is a potent nonsteroidal anti-estrogen. It is indicated for use in estrogen dependent tumors, i.e. breast cancer. Steroid users take Nolvadex to prevent the effects of estrogen in the body. This estrogen is most often the result of aromatizing steroids. Nolvadex can aid in preventing edema, gynecomastia, and female pattern fat distribution, all of which might occur when a man’s estrogen levels are too high. Also, these effects can occur when androgen levels are too low, making estrogen the predominant hormone. This can occur when endogenous androgens have been suppressed by the prolonged use of exogenous steroids. Nolvadex works by competitively binding to target estrogen sites like those at the breast. This drug is not toxic nor have any side effects been seen in athletes who used the drug’ as an anti-estrogen. This drug is the most popular anti-estrogen amongst steroid users. Although it does not turn out to be 100% effective for everyone, it does seem to exhibit some level of effectiveness for the majority. It works so well for some bodybuilders they can take drugs like Anadrol right up to a contest as long as they stack it with Nolvadex. It would seem wise to take this drug in conjunction with any steroid cycle. Most reported a dosage of 10 mg to 20 mg daily got the job done. Availability of Nolvadex has been fair on the black market.

References

Wlliam Llewellyn (2011) - Anabolics
L. Rea (2002) - Chemical Muscle Enhancement Bodybuilders Desk Reference
Anabolic Steroid Guide
Newbies Research Guide

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