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Last Updated on May 30, 2023

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The drug Tamoxifen is used in the treatment of breast cancer. It acts selectively on the docking sites (receptors) of female sex hormones (estrogen and Progesterone) and thus can inhibit the growth of hormone-dependent tumors. Compared with other drugs to treat cancer, Tamoxifen has a clear side effect potential. It is therefore often used for breast cancer treatment especially since the expiry of patent protection in the year of 2002. Here you can read everything relevant to effect of Tamoxifen, side effects and use.

How Tamoxifen works

The endogenous female hormone estrogen (also: Estrogen) determines not only the cycle of the woman, but also has other functions in the body. Among other things, it ensures strong bones (a lack of estrogen can lead to osteoporosis) and stimulates the immune system. If estrogens distributed in the body, they pass through the bloodstream to the target tissue. Once there, they specifically influence the target cell and can stimulate cell growth, among other things. Has a cell many docking (receptors) for estrogens, she is particularly sensitive to the hormone.

In a large part of breast tumors, there is an increased number of estrogen receptors. The already degenerated cells will continue to grow and divide, ie propagating, stimulated by the natural estrogen, causing the tumor grows unchecked.

Tamoxifen and especially its metabolite hydroxy Tamoxifen can bind to the estrogen receptors without cell division and proliferation stimulating. Thus, the existing receptors are blocked and can no longer be activated by the natural estrogen.

Pharmacokinetics and metabolism of Tamoxifen

After taking Tamoxifen tablets of the drug is well absorbed in the intestine and reaches its maximum blood levels after four to seven hours. The metabolism, which takes place mainly in the liver, resulting in many cases more effective degradation products. These are then excreted mainly in the feces, but this takes some time: It was only after about a week, the active ingredient broken down and excreted half

When should you use Tamoxifen?

The drug Tamoxifen is approved for the treatment of hormone-dependent breast tumors: It can be used to support after a primary treatment of breast cancer or breast cancer, which has already secondary tumors (metastases) formed. The application usually takes place over a longer period.

How is Tamoxifen used

The active ingredient is administered in pill form. The usual dosage is Tamoxifen twenty milligrams per day, but can be increased if necessary up to forty milligrams. To be taken with a meal, to mitigate adverse effects such as nausea.

What are the side effects of Tamoxifen?

Tamoxifen side effects in more than every tenth woman treated include nausea, fluid accumulation in the tissues, vaginal discharge and bleeding, cycle changes and menopausal symptoms such as hot flashes and fatigue.

For each hundredth to tenth patient leads to drowsiness, hypersensitivity reactions, muscle pain, leg cramps, blood clots, temporary anemia and itching on the genitals. Another side effect of Tamoxifen, a change in laboratory parameters (elevated blood lipids, altered liver enzymes) occur.

What should I watch for while taking Tamoxifen?

Due to the Tamoxifen therapy the effect of the body’s own estrogen to be reduced. An additional estrogen intake in the form of hormonal contraceptives (eg “the pill”) would not make sense and should therefore be avoided.

Tamoxifen affects the blood coagulation by reducing the number of platelets. Be given additional anticoagulant drugs, the anticoagulant effect may increase. Such “anticoagulant” are, for example, aspirin and other antiplatelet agents and anticoagulants such as coumarin-like warfarin and phenprocoumon.

Tamoxifen is converted by certain liver enzymes in the active form of action. Drugs that inhibit these enzymes or promote their activity, can thus affect the metabolism and thus the effectiveness of the cancer drug. So can reduce the effectiveness of Tamoxifen as antidepressants from the group of selective serotonin reuptake inhibitors (SSRIs, such as Paroxetine and Fluoxetine) and the antidepressant Bupropion by enzyme inhibition. The concomitant use of such drugs should be avoided if possible.

Since the use of Tamoxifen in pregnancy and lactation is little data, the drug during this period should not be taken. In animal trials, by taking Tamoxifen damage the unborn child.

Also, due to lack of knowledge use in children and adolescents does not appear (is contraindicated).

How to get Tamoxifen

preparations containing Tamoxifen, are a prescription at the pharmacy to purchase.

Since when Tamoxifen is known?

Even researched in the late 1950s, pharmaceutical companies active on antiestrogens (ie agents which inhibit the estrogen effect) for effective contraception. It developed Dr. Dora Richardson, Associate an English pharmaceutical company, in 1966 the drug Tamoxifen. For contraception, this however was not suitable, so he came back first into oblivion. Later it was discovered that estrogens also may accelerate the growth of breast cancer. As a result, in 1971 the Christie Hospital in Manchester, one of the largest cancer clinics in Europe, a clinical trial with Tamoxifen started. Due to the positive study results Tamoxifen in 1973 was marketed to treat breast cancer in late stage.

More interesting facts about Tamoxifen

Tamoxifen is used by male athletes misused as a doping agent: It can increase the level of testosterone, which stimulates muscle growth. In addition, prevents Tamoxifen a common side effect of anabolic steroids, the so-called “man boobs” (gynecomastia).