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Tamoxifen is a non-steroidal selective estrogen receptor modulator (SERM). It binds to estrogen receptors (ER), altering their structure and blocking or modifying the transcription of estrogen-responsive genes. This action leads to reduced DNA polymerase activity, decreased thymidine uptake, inhibited estradiol binding, and reduced estrogen response. Depending on the tissue, Tamoxifen can exert both estrogenic and anti-estrogenic effects by interacting with coactivators or corepressors and binding to ER-alpha or ER-beta receptors.
Tamoxen may cause both estrogen-related and general side effects, including:
Rarely, elevated triglycerides, potentially leading to pancreatitis
Adults (including elderly):
The recommended daily dosage is 20 to 40 mg, taken as a single dose or divided into two doses.
Coumarin anticoagulants: Concurrent use may increase anticoagulant effect, requiring close monitoring.
Cytotoxic agents: Co-administration may raise the risk of thromboembolic events.
Pregnancy: Tamoxen should not be taken during pregnancy.
Hypersensitivity: Not for use in patients allergic to tamoxifen or any of its components.
Pregnancy: Tamoxen is contraindicated during pregnancy. Although some birth defects and fetal deaths have been reported, no direct link has been established. Patients should avoid pregnancy while taking Tamoxen and for at least two months after stopping. Non-hormonal contraceptives are advised.
Lactation: It’s unclear if tamoxifen is excreted in breast milk. Use is not recommended while breastfeeding. A healthcare provider should assess the importance of continuing the drug for the mother.
Menstrual irregularities may occur in premenopausal women.
Increased risk of endometrial cancer has been observed, possibly due to estrogen-like effects of tamoxifen.
Any abnormal gynecological symptoms, especially vaginal bleeding, should be evaluated.
Rare reports of secondary tumors (excluding the endometrium or opposite breast) have been noted; their significance is unclear.
Store at 20–25°C, away from light.
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