Tamoxifen Mechanism of Action

Tamoxifen Citrate (often sold as brand name Nolvadex but there are numerous other brands too) is a Selective Estrogen Receptor Modulator (SERM). This is orally active medicine that is FDA approved and has various uses in medical settings.

But Tamoxifen is very often used either as an anti estrogen or as a Post Cycle Therapy (PCT) drug by bodybuilders. More specifically – by anabolic steroid users who run them for their physique and performance enhancement purposes.

  • In fact, Nolvadex (Tamoxifen) is so important for steroid users that the compound can be considered a “must” for everyone who is running or plans to run steroids.

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You should learn more about the Tamoxifen mechanism of action. If you’re wondering why Tamoxifen has so many uses like infertility treatment in women, breast cancer drug treatment and preventative, gynecomastia drug, PCT drug, etc. – then again, you’ve got to learn more about Tamoxifen mechanism of action.

How Does Tamoxifen Work?

In short, Tamoxifen, as its class name suggests, selectively works on certain parts of the body and that’s why it has various uses. But as you may notice, Nolvadex is having lots of different uses when talking about breast tissues. That’s why the compound is very valuable both in medical settings and in the bodybuilding industry for its great effects.

Tamoxifen mostly works in breast tissues taken into consideration that it binds to estrogen receptors in this particular part of the body. This compound is not reducing the total estrogen levels and doesn’t stop aromatization. It stops certain estrogen receptors from doing their job.

At the same time, Tamoxifen Citrate was found effective in working as an estrogen agonist in other parts of the body (such as the liver, etc.). This means that it boosts the effects of estrogen receptors.

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SERMs vs AIs

Before we continue talking more about the Tamoxifen mechanism of action, is very important for you to understand the difference between Selective Estrogen Receptor Modulators (SERMs) and Aromatase Inhibitors (AIs).

Both these types of drugs are known to reduce estrogens activity.

  • That’s why they are both considered anti-estrogens and both are highly valuable in the bodybuilding industry.

Both SERMs and AIs can be used during cycles of steroids to prevent estrogen related issues from occurring or as a part of PCT plans to assist in restoring natural testosterone production.

Nonetheless, there’s a huge difference between how SERMs and AIs are working and the way they are affecting estrogen.

  • AIs are known to reduce aromatization by binding to aromatase enzymes. Therefore the total estrogen flow in the body is reduced.
  • On the other hand, SERMs (where you can find Clomiphene CitrateClomid, but also Tamoxifen CitrateNolvadex) are only targeting certain parts of the body. They bind to estrogen receptors blocking their activity. So whilst you’re still going to have estrogen, the activity of this hormone in certain areas of your body would be inhibited. But estrogen activity in other tissues would be boosted.

That’s why AIs are considered a better option for on-cycle needs (as they are able to control a wider range of estrogen related issues than SERMs).

But on the other hand, SERMs are much better for Post Cycle Therapy (PCT) plans. That’s because they are boosting testosterone levels more effectively without suppressing estrogen too much.

So, both SERMs and AIs are very effective at treating or preventing gynecomastia.

But SERMs are not very helpful for fighting off water retention for example, whilst AIs are not very helpful for recovering back natural hormonal balance.

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Tamoxifen Mechanism For PCT Plans

Tamoxifen (Nolvadex) exactly as Clomiphene (Clomid) is great for Post Cycle Therapy. That’s because, after the use of steroids, when the body’s LH level is near zero. Therefore it doesn’t produce testosterone. Yet, these compounds stimulate your hypothalamus. This results in more release of gonadotropins. From this point, it is easy to understand why you get more testosterone. It results in more LH and FSH and therefore more testosterone production in your body.

Why does it happen? Your hypothalamus is receiving signals that there is too much estrogen. That’s because a part of testosterone is converted into estrogen. So it stops releasing gonadotropins. Tamoxifen is blocking the estrogens from reaching your hypothalamus. That’s why it continues to release.

  • Keep in mind that Tamoxifen doesn’t mimic LH as HCG does. Plus is not a steroid that can boost testosterone levels.

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That’s why Tamoxifen (Nolvadex) is very effective for PCT plans specifically. Or for gynecomastia treatment specifically.

You get off steroids, then go on PCT with Nolvadex. It keeps high testosterone levels. When you get off PCT and all steroids are flushed out of your body, your HPTA recovers back to normal. And levels of hormones are getting in the normal range.

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