Last Updated on June 12, 2023
Tamoxifen is a medication that is primarily used to treat breast cancer. It works by blocking the effect of estrogen, a hormone that can promote the growth of breast cancer cells. In addition to its use in breast cancer treatment, tamoxifen can also be used to prevent breast cancer in women who are at high risk.
While tamoxifen is a prescription medication, there has been some discussion as to whether it should be available over the counter in the UK. Proponents argue that making tamoxifen more widely available could help to increase access to this life-saving medication, particularly for women who may not have easy access to a doctor or who may be hesitant to seek medical attention due to financial concerns.
However, there are also concerns about making tamoxifen available over the counter. Some experts worry that without proper medical supervision, women may not use the medication correctly or may not receive the appropriate screening and follow-up care. Others worry that making tamoxifen available over the counter could lead to an increase in misuse or abuse of the medication. Ultimately, the decision about whether to allow tamoxifen to be sold over the counter will need to weigh these potential benefits and risks carefully.
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What is tamoxifen?
Tamoxifen is used to treat breast cancer. It acts selectively on the receptors for female sex hormones (oestrogen and progesterone) and can inhibit the growth of hormone-dependent tumours. Compared with other cancer drugs, tamoxifen has a clear potential for side effects. This is why it is often used to treat breast cancer, especially since it went off patent in 2002. Here you can read all about the effects, side effects and use of tamoxifen.
How does tamoxifen work?
The female hormone oestrogen (also known as estrogen) not only controls the menstrual cycle, but also has other functions in the body. These include maintaining strong bones (a lack of oestrogen can lead to osteoporosis) and stimulating the immune system. When oestrogens are distributed in the body, they travel through the bloodstream to the target tissue. Once there, they specifically affect the target cell and can stimulate cell growth, among other things. If a cell has many docking sites (receptors) for oestrogen, it is particularly sensitive to the hormone.
A large proportion of breast tumours have an increased number of oestrogen receptors. The already degenerated cells continue to grow and divide, i.e. multiply, stimulated by natural oestrogen, causing the tumour to grow unchecked.
Tamoxifen, and especially its metabolite hydroxy-tamoxifen, can bind to the estrogen receptors without stimulating cell division and proliferation. The existing receptors are blocked and can no longer be activated by natural oestrogen.
Pharmacokinetics and metabolism of tamoxifen
The female hormone estrogen not only controls the menstrual cycle, but also has other functions in the body. These include maintaining strong bones (a lack of estrogen can lead to osteoporosis) and stimulating the immune system. When estrogens are distributed in the body, they travel through the bloodstream to the target tissue. Once there, they specifically affect the target cell and can stimulate cell growth, among other things. If a cell has many docking sites (receptors) for estrogens, it is particularly sensitive to the hormone.
A large proportion of breast tumors have an increased number of estrogen receptors. The already degenerated cells will continue to grow and divide, i.e. multiply, stimulated by the natural estrogen, causing the tumor to grow unchecked.
Tamoxifen, and especially its metabolite hydroxy tamoxifen, can bind to the estrogen receptors without stimulating cell division and proliferation. The existing receptors are blocked and can no longer be activated by natural estrogen.
When should you use tamoxifen?
Tamoxifen is approved for the treatment of hormone-dependent breast cancer: It may be used as an adjunct after primary treatment for breast cancer or for breast cancer that has already formed secondary tumors (metastases). Tamoxifen is usually used over a long period of time.
How is tamoxifen used?
The drug is given in pill form. The usual dosage of Tamoxifen is twenty milligrams per day, but can be increased to forty milligrams if necessary. To be taken with a meal to reduce side effects such as nausea.
What are the side effects of tamoxifen?
Tamoxifen side effects in more than one in ten women treated include nausea, fluid retention in the tissues, vaginal discharge and bleeding, cycle changes, and menopausal symptoms such as hot flashes and fatigue.
For every one 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?
Tamoxifen therapy reduces the effect of the body’s own estrogen. An additional intake of estrogen in the form of hormonal contraceptives (e.g. the pill) would not make sense and should therefore be avoided.
Tamoxifen affects blood clotting by reducing the number of platelets. If additional anticoagulant drugs are given, the anticoagulant effect may be increased. Such “anticoagulants” include aspirin and other antiplatelet agents and anticoagulants such as coumarin-like warfarin and phenprocoumon.
Tamoxifen is converted to its active form by certain liver enzymes. Drugs that inhibit these enzymes or promote their activity may affect the metabolism and thus the effectiveness of the anticancer drug. For example, antidepressants from the group of selective serotonin reuptake inhibitors (SSRIs, such as paroxetine and fluoxetine) and the antidepressant bupropion may reduce the effectiveness of tamoxifen through enzyme inhibition. Concomitant use of these medications should be avoided if possible.
Since there is little data on the use of tamoxifen during pregnancy and lactation, the drug should not be taken during this period. In animal studies, the use of tamoxifen caused harm to the unborn child.
Also, due to lack of knowledge, use in children and adolescents does not appear (is contraindicated).
How to get tamoxifen?
Tamoxifen can be bought at the pharmacy with a prescription.
When was tamoxifen introduced?
As early as the late 1950s, pharmaceutical companies were researching anti-oestrogens (i.e. agents that inhibit the effect of oestrogen) for effective contraception. Dr Dora Richardson, an employee of an English pharmaceutical company, developed the drug tamoxifen in 1966. However, it was not suitable for use as a contraceptive, so it was initially forgotten. It was later discovered that oestrogen can also accelerate the growth of breast cancer. In 1971, the Christie Hospital in Manchester, one of the largest cancer clinics in Europe, began a clinical trial of tamoxifen. Based on the positive results of the trial, tamoxifen was approved for use in late-stage breast cancer in 1973.
More interesting facts about tamoxifen
Tamoxifen is used as a doping agent by male athletes: It can increase the level of testosterone, which stimulates muscle growth. Tamoxifen also prevents a common side effect of anabolic steroids, so-called “man boobs” (gynecomastia).