Tamoxifen citrate is a SERM (selective estrogen receptor modulator), which means that this drug can act as an estrogen in some parts of the body and have antiestrogenic effects elsewhere.

It was developed in the 1960s initially to treat female infertility and in the late 1970s it was approved for the treatment of breast cancer. Guru Dan Duchaine claims to have introduced tamoxifen in bodybuilding in 1981 for the purpose of treating gynecomastia, due to its anti-estrogenic effect on breast tissue. Until that time, bodybuilders did not have drugs to prevent this side effect and for this reason they avoided abusing testosterone. Tamoxifen is also anti-estrogenic in the hypothalamus and pituitary gland, works by blocking estrogen receptors in this region and thereby preventing negative estrogen feedback. By inhibiting the negative feedback effect of estrogen on the hypothalamus and pituitary gland, tamoxifen stimulates the release of gonadotropins LH and FSH by the pituitary gland, and therefore can stimulate testosterone synthesis and spermatogenesis in the testicles after discontinuing steroid use, and by this is a very effective drug in post-cycle therapy.

Other benefits of tamoxifen for steroid users refer to its estrogenic activity in the liver, having beneficial effects on cholesterol metabolism, unlike aromatase inhibitors, which, by reducing estrogen levels, may impair the lipid profile. TAMOXIFENO is a drug that offers little risk of side effects in male steroid users. Some users claim that tamoxifen can hinder cycle gains, perhaps because this drug reduces serum levels of IGF-1, but there is no direct evidence for this gain-reducing effect.

The usual doses to treat gynecomastia and use in CPT vary from 20 to 40 mg per day, but it can be effective even in doses of 10 mg per day. Most gurus and experts consider tamoxifen to be more effective than clomiphene in steroid users. It does not appear to have proven benefits in women using steroids, except to stimulate ovulation after discontinuing steroid use.

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