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Facts About TAMOXIFEN You Didn't Know!

5/1/2020

This is another classic anti estrogen that's been used by the bodybuilding community and men that are using anabolic androgenic steroids for many years. Actually, since the 1990s.

The utility of this drug is more focused than the other drugs. This is specifically for uncycle or PCT gynecomastia and specifically as a regimen with other drugs for post cycle therapy. The drugs that are obviously used with this are classic estrogenic anabolic androgenic steroids like esters of testosterone and drugs like Dianabol and Anadrol draw but it's used with many other steroids as men use steroids together in stacks. So, it's also interesting that unlike aromatase inhibitors anti-aging clinics really don't use this drug so much. Although, I do see it used from time to time and I think over time we see more polypharmacy coming out of these clinics and I do see men getting put on this drug inappropriately.

The history of Tamoxifen

First synthesized by ICI pharmaceuticals in 1962 was cleared by the FDA in the mid-60s initially for female infertility. Now this is interesting because this is a SARM like clomiphene that now today is much stronger for that utility. After many years in study by 1977 the FDA cleared this drug for what it's used for today. Medically which is hormone receptor positive breast cancer in 1998 the FDA gave it a second clearance for breast cancer prevention and high-risk individuals, that would be a woman or a man, that has breast cancer unilaterally and they want to protect against having breast cancer in the second breast. Also used classically in more commonly women that have breast cancer of risks familiar risks and classically genetic risks with the classic gene BRCA1 and 2.

The mechanism of action of Tamoxifen

It's a classic and the oldest non-steroidal anti estrogen drugs and a class called selective estrogen receptor modulators. This specific drug falls under the triphenyl Eveline family. And as the SORMs do it has both estrogenic agonistic and estrogenic antagonistic blocking effects, depending on what receptor and what part of the body system were looking at.

So, for an example properties of anti-estrogenic you would classically see the blocking effects the estrogen site of breast tissue where we see breast cancer. That's a very strong blocking effect in that point and that part of the body. Also, in this CNS like clomiphene you also see the blocking of a hypothalamus and you see a reflex increase in FSH and LH, again like clomiphene, but definitely not as strong in this effect as clomiphene. As far as pro atherogenic effects in the body we know medically and classically for decades it is going to have positive effects estrogenic like in the liver. And it's very interesting that and I'll discuss later the effects on cholesterol and classically the HDL. Also, in the liver and throughout the body it's thought that this drug is a pro estrogen can be hyper coagulating to DVTs pulmonary embolisms and strokes. This is very interesting and needs to be paid attention to. Also, as a pro estrogen is in the bones and there are other and more specific classes of SERMs that are used for postmenopausal women classically that have osteopenia and osteoporosis, or they want prevention.

Facts About TAMOXIFEN You Didn't Know!

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