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- Active ingredient: Tamoxifen
- Type: Selective estrogen receptor modulator
- Form: Oral (tablets)
Description
Tamoxifen is an antiestrogen belonging to the triphenylethylene group. It is classified as a selective estrogen receptor modulator with mixed agonist and antagonist properties. This means that, in certain tissues, it blocks the action of estrogen by binding to receptors. There is one exception—bone tissue, where it activates estrogen receptors, thus being useful in preventing osteoporosis. In men, the drug acts as an antiestrogen, blocking receptors throughout the body, including its ability to interfere with the negative feedback of estrogen to the hypothalamus and stimulate increased production of GnRH (gonadoliberin), which in turn causes the pituitary gland to produce the hormones LH and FSH, which trigger the synthesis of testosterone and sperm in the testicles.
Research conducted in the late 1970s at the University of Ghent in Belgium illuminated the benefits of tamoxifen over clomiphene in increasing testosterone levels. Researchers analyzed the endocrine effects of tamoxifen and clomiphene in healthy men, as well as in those with oligospermia. It was also found that tamoxifen, when used for 10 days at a dosage of 20 mg per day, increased serum testosterone levels by 142% compared to baseline, which was comparable to the effect of 150 mg of clomiphene per day over the same period.
Difference with clomiphene
Tamoxifen has no effect on blood estrogen levels. Its mechanism of action is limited to blocking estrogen receptors, including in the pituitary gland. However, clomiphene is the most selective blocker, being more specific to the pituitary gland, while tamoxifen is less selective. While clomiphene binds to estrogen receptors primarily in the pituitary gland and testes, tamoxifen binds to them uniformly throughout most of the body. This is why tamoxifen is the best solution for estrogen-induced gynecomastia in men.
Clomiphene acts as an estrogen antagonist and eliminates its inhibitory effect on the hypothalamus and pituitary gland, contributing to a faster restoration of their functions. Tamoxifen blocks receptors in almost all tissues and also helps the body begin to restore its own testosterone. It is important to note that tamoxifen is less capable of blocking estrogen receptors in the pituitary gland than clomiphene. Neither clomiphene nor tamoxifen affect estrogen metabolism, so during use of these medications, estrogen continues to be destroyed by liver enzymes and does not accumulate in the body.
Notices
Tamoxifen increases the number of progesterone receptors, so it cannot be used if the cycle is based on progestin-only medications (nandrolone, trenbolone). In this case, clomiphene should be used.
Dosages
The typical recommended dosage of Tamoxifen is 10–40 mg per day, taken in one or two doses.
Effects
- Estrogen receptor blockade
- Increase endogenous testosterone production (as part of PCT or anti-aging therapy)
- Strengthens bones
- Prevents estrogen-induced gynecomastia
- Tamoxifen lowers cholesterol levels, which is important when using steroids.
Side effect
- Breast tenderness or discomfort
- Headache
- Nausea
- Diarrhea
- Discharge
- Blurred vision or other visual disturbances
- Please note that side effects of tamoxifen are very rare.
Profile
- Half-life: 5-7 days
- Frequency of intake: 1 time a day
Contraindications
- Anticoagulant therapy, chemotherapy, stroke, thromboembolism
- Endometrial cancer, endometrial hyperplasia, new primary malignancy, uterine cancer
- Anemia, bone marrow suppression, leukopenia, neutropenia, thrombocytopenia
- Cataracts, visual disturbances, visual impairment
- Hypercalcemia
How to store
- Keep out of reach of children
- Keep in a cool, dry place, away from direct sunlight.
- Store at room temperature
- Do not use after expiration date.