Tamoxifen in bodybuilding after a course of steroids: side effects and instructions for use

Tamoxifen (alternatively Nolvadex, informally Tamox) was originally developed for the treatment of women. Its medical purpose is to prevent the development of malignant tumors in the mammary gland. Today the drug is actively used among athletes. In bodybuilding, the drug is used to reduce estrogen levels and prevent gynecomastia in men. Some athletes combine it with anabolic steroids, others take it as a recovery agent after a steroid cycle.

Tamoxifen - what is it?

The drug "Tamoxifen" also has another name. It is also called "Nolvadex"

Tamoxifen is popularly known as Tamox. In pharmacology, this medicine is used by women. It suppresses estrogen levels in the body and fights breast cancer.

But, as you may have guessed, athletes began to use Tamox for slightly different purposes. It should be used during a course of steroids. Tamoxifen helps keep estrogen levels low and prevents gynecomastia in men.

For those who don't know, gynecomastia is swelling of the breasts in men due to the growth of the mammary glands. In simple words, a man's breasts become similar to a woman's.

In what form is it produced?

The drug Tamoxifen is available in the form of coated tablets with a total mass of active substance of 10 and 20 mg.

The tablets are placed in plastic bottles, which are packed in cardboard boxes. The drug is dispensed only with a prescription from the attending physician. The average cost of 1 package of Tamoxifen is 1200 rubles.

Advantages of the drug

Tamoxifen has a number of benefits:

1. Low cost compared to analogues.
2. High efficiency.
3. No side effects when used correctly.
4. Low toxicity of the drug.
5. Reduces cholesterol levels in the body.

In addition, Tamox has many functions, such as: increasing strength, burning fat, increasing muscle mass, etc. In fact, this is an exaggeration and tamoxifen does not perform any of these functions.

Links[edit | edit code]

1. Hormonal effects of an antiestrogen, Tamoxifen, in normal and oligospermic men. Vermeulen, Comhaire. Fertil and Steril 29 (1978) 320-7
2. Vermeulen A., Comhaire F., Hormonal effects of an anti-estrogen, tamoxifen, in normal and oligospermic men, Fertil. Ster. 29 (1978) 320-27
3. https://theoncologist.alphamedpress.org/content/7/2/163.full
4. https://www.ncbi.nlm.nih.gov/pubmed/18193254
5. Hormonal effects of an antiestrogen, Tamoxifen, in normal and oligospermic men. Vermeulen, Comhaire. Fertil and Steril 29 (1978) 320-7
6. Bruning PF, Bronfer JMG, Hart AAM, Jong-Bakker M, tamoxifen, serum lipoproteins and cardiovascular risk, Br. J Cancer 1988 Oct, 58 (4) 497-9
7. The effect of Clomiphene citrate on sex hormone binding globulin in normospermic and oligozoospermic men. Adamopoulos, Kapolla et al. Int J Androl 4 (1981) 639-45
8. De Leo V. et al. Clomiphene citrate increases insulin-like growth factor binding protein-1 and reduces insulin-like growth factor-I without correcting insulin resistance associated with polycystic ovarian syndrome //Human Reproduction. – 2000. – T. 15. – No. 11. – pp. 2302-2305.
9. C. WANG, G. F. ERICKSON, B. HOPPER, A. J. W. HSUEH. Direct Inhibitory Effect of Enclomiphene Citrate and Estradiol on Testis Functions in Hypophysectomized Rats. BIOLOGY OF REPRODUCTION 22, 64-653 (1980)
10. https://joe.endocrinology-journals.org/content/53/2/261
11. https://community.breastcancer.org/forum/78/topic/733162
12. https://www.nature.com/eye/journal/v17/n2/full/6700317a.html

Side effects

Tamoxifen has more advantages than disadvantages. It is a fairly calm and harmless drug. But, like any medicine, it should be used correctly to avoid side effects.

Side effects of tamoxifen:

• Exceeding dosages causes increased body temperature and nausea.
• Large dosages have a detrimental effect on kidney function.
• Long-term use is harmful to vision and can significantly worsen it.

If tamoxifen is used wisely and according to the instructions, then there will be no complications; it is a very “mild” drug. Athletes, in most cases, do not violate the rules of administration, and, therefore, side effects are extremely rare.

Action

A distinctive feature of the anti-estrogen drug Tamoxifen is that it has a gradual effect on the functioning of the endocrine glands and is not capable of causing a sharp imbalance of sex hormones. When taken orally, the active substance of the drug is well absorbed in the gastrointestinal tract.

The maximum concentration of Tamoxifen in the blood serum is observed 7 hours after the start of therapy. Optimal accumulation of the chemical in muscle fibers and connective tissue is achieved after 6 weeks of taking the drug.

The antiestrogenic effect of tamoxifen is achieved after the active substance of the drug reaches the receptors responsible for identifying the hormones of the estradiol group.

The action of female sex hormones - estrogens - is blocked. The drug is equally effective regardless of whether it is taken on an empty stomach or after a meal. In this case, the pharmacokinetics of the drug does not change.

Metabolism of Tamoxifen occurs in the liver tissue, and chemicals formed during the breakdown of the drug are excreted in bile. About 3% of the active components of the drug are found in urine. During the metabolism of tamoxifen, citrate breaks down into desmethyltamoxifen, which is converted into the desdimethyl metabolite through demethylation.

During the breakdown of tamoxifen citrate into its constituent components, an additional load is created on the liver tissue. In this regard, the drug can disrupt the functioning of this organ, causing its systemic dysfunction.

Tamoxifen during a course of steroids

Some athletes use tamoxifen for its intended purpose - to lower estrogen levels in the body.

The scheme is very simple : steroids increase testosterone levels, along with it estrogen increases, and Tamox prevents it from doing this.

The result : high levels of male hormones and low levels of female hormones.

Tamoxifen is cheap and that's its advantage. But you have to drink it every day, and for some this is a great inconvenience. A more expensive and effective analogue for suppressing estrogen levels is anastrozole. This drug is more powerful, more effective and it is enough to drink it once every 4 days. But its cost is 4 times higher than that of tamoxifen.

Afterword

From our side - the facts, from yours - the decision.

Common sense cannot remain silent and shouts that the use of pharmacology is madness.

The crazy thing is that “athletes” are looking for a solution to eliminate gynecomastia as a consequence of taking steroids, adding another drug to the list of pharmacological crap, instead of just finally removing the cause of this gynecomastia - pharmacology - and along with it a whole bunch of other potential side effects.

Tamoxifen – as PCT

Some believe that tamoxifen is effective after a cycle.

How it works: at the end of the steroid cycle, the athlete begins to use tamoxifen, which allows the testicles to work faster and release their own testosterone.

As a result : the body’s own production of male hormone is normalized, thereby maintaining muscle mass.

But here's the rub. The direct function of tamoxifen is to suppress the level of estrogen in the body. And producing your own testosterone is a conclusion made by the athletes themselves. Moreover, among its disadvantages is the slow functioning of the testicles. This means that using Tamox on PCT is unwise, since its effectiveness at this stage has not been proven.

There is a very effective drug for PCT - Clomid, which does its job perfectly. True, its cost is 2-3 times higher than that of tamoxifen, but the result is much better.

General disadvantages[edit | edit code]

• Both drugs inhibit the production of insulin-like growth factor-1[8]
• Directly suppress testicular function[9]
• Increase sex hormone binding globulin[10]
• Increase the concentration of estrogen several times
• Causes visual impairment with long-term use[11][12]
• In some cases, when using Clostilbegit (Clomid) for a month at a dosage of 25 mg per day, after 2 weeks after the end of the course, a decrease in total testosterone was observed by 16-17% (while a decrease in estradiol was observed by 13.5%)
• It is important to understand that in some people the pituitary-hypothalamus-testicular (PHT) arc may not respond to stimulation with Clomid (clomiphene) or Nolvadex (tamoxifen).

How to take tamoxifen correctly

We conclude that tamoxifen is most effective while taking steroids rather than after. This means that it must be used throughout the course.

Rules of use:

1. We start using tamoxifen a week after starting a course of steroids. This is due to the fact that the first signs of gynecomastia appear no earlier than after 2 weeks. But it’s better to play it safe and start taking it within a week.
2. We take 1 tablet a day, no more is required. Even 20 mg copes with its task 100%.
3. After stopping taking steroids, continue taking tamoxifen for another 2 weeks. Since during this time a high level of testosterone is maintained in the body, it needs to be controlled with Tamox.

Contraindications

Tamoxifen in bodybuilding is a drug that is not recommended for use by athletes with a number of chronic diseases and pathological conditions of the body.

The drug is contraindicated in the following cases:

• individual intolerance to the active component - tamoxifen citrate, which is expressed in allergic reactions of any kind;
• leukopenia, accompanied by a further decrease in the level of leukocytes in the blood (this restriction on taking the drug is associated with a high risk of malignant diseases of the blood and lymphatic system);
• severe form of thrombocytopenia, which is associated with increased fragility of blood vessels, poor circulation, and periodic occurrence of internal bleeding (taking Tamoxifen can provoke an exacerbation of the disease, as well as aggravate the symptoms of cellular blood balance);
• hypercalcemia, the development of which is associated with metabolic disorders and diseases of internal organs;
• acute or chronic renal failure;
• severe diseases of liver tissue, which are associated with their gradual decay and death of hepatocytes (cirrhosis, malignant neoplasms, viral or intoxicating hepatitis).

Tamoxifen is contraindicated for use by women who are pregnant and continue to engage in bodybuilding. Also, the drug is not recommended for use by athletes who suffer from thrombophlebitis, have signs of varicose veins, or have pathologies of the great vessels.

Failure to comply with the above contraindications may lead to a deterioration in general health.

Photos before and after taking the drug

Reviews of tamoxifen

Tamoxifen is a very controversial drug, and therefore there are varied reviews about it:

• According to some experienced athletes, tamoxifen is a thing of the past. Now there are more modern and effective drugs, so there is no point in using it.

• Most athletes who use tamoxifen as an aromatase inhibitor are happy with it. In their opinion, Tamox perfectly blocks the increase in estrogen and copes with its task.
• All who prefer tamoxifen agreed that side effects are extremely rare or do not occur at all. This drug is very “soft” and does not harm the body.
• When using a large number of steroid drugs, it is still recommended to use anastrozole as an estrogen blocker. This drug is more powerful, but also more expensive.
• As a PCT, tamoxifen is quite weak, as athletes claim. After a steroid course, it works well only in conjunction with Proviron.
• Tamoxifen removes water from the body, which once again emphasizes its need during steroid use, and not after.

Drug interactions

Tamoxifen in bodybuilding is taken in compliance with the rules of drug interactions with other drugs and anabolic steroids.

When taking the drug, the following pharmacological properties of tamoxifen citrate must be taken into account:

• Tamoxifen reduces the effect of other medications that contain sex hormones of the estradiol group;
• the medication enhances the pharmacological effect of drugs that are classified as coumarin anticoagulants;
• simultaneous therapy with Tamoxifen and drugs that are platelet aggregation inhibitors increases the risk of internal bleeding;
• co-administration of Tegafur may cause progressive hepatitis or cirrhosis of the liver;
• therapy with Allopurinol increases the risk of developing hepatotoxic reactions;
• the active components of cytotoxic drugs can enter into chemical reactions with tamoxifen citrate and cause thromboembolic complications;
• simultaneous administration of Bromocriptine enhances the anti-estrogenic effect of Tamoxifen, and also increases the concentration of its metabolites in the blood serum.

Food items included in a bodybuilder’s daily diet do not affect the absorption process of tamoxifen citrate and do not change the pharmacokinetic properties of the drug.

Summarize

Much has been said today about this drug, but let’s put it all together:

1. Tamoxifen is a remedy that is effective during a course of steroids.
2. It is not suitable for post-cycle therapy.
3. Tamox, when taken correctly, has no side effects.
4. Its cost is low, which makes it very attractive.

Tamoxifen blocks the aromatization of testosterone, as a result of which estrogen does not increase. The male body will not accept female properties: swelling in unnecessary places, lethargy, weak libido.

Tamoxifen is cheap and cheerful. If you have the opportunity to buy more expensive drugs, such as anastrozole, then it makes sense to do just that.

Analogs

Level 4 ATX code matches:
Nolvadex

Fareston

Vero-Tamoxifen

Structural analogues of Tamoxifen: Vero-Tamoxifen , Tamoxifen Hexal , Tamoxifen Lachema , Tamoxifen-Ferein , Tamoxifen-Ebewe .

Faslodex and Fareston have a similar mechanism of action .

Fareston or Tamoxifen - which is more effective?

Fareston is an antitumor antiestrogenic non-steroidal drug based on the substance toremifene . Main features of the medicine:

• the presence of a chlorine atom in its chemical structure (which makes the drug more stable compared to Tamoxifen);
• lack of oncogenic effect ;
• ability to induce apoptosis;
• effectiveness in ER-negative tumors .

According to clinical observations conducted over six months, it was found that when taking Fareston:

• changes in hormonal homeostasis are an order of magnitude more favorable than when taking Tamoxifen;
• changes that are less dangerous for the patient in terms of cancer risk develop;
• Undesirable side effects occur an order of magnitude less frequently.

The studies also led to the conclusion that, as part of a complex treatment, the effect of Fareston on the tumor process in progressive breast cancer is more effective than the effect of its analogue: with its use, patients experienced complete remission much more often, and disease progression began at 1.2 a month later.

In addition, the antitumor effect during treatment with Fareston was observed in a larger number of patients.