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What is the role of tamoxifen?
- Sep 06, 2019-

Tamoxifen is used to treat advanced breast and ovarian cancer. In the clinical treatment of breast cancer, the effective rate is generally 30%, the estrogen receptor-positive patients have better efficacy (49%), and the negative patients have poor efficacy (7%). Both premenopausal and postmenopausal patients can be used, and postmenopausal and 60 years of age or older are better than premenopausal and younger patients. From the point of view of the lesion, the skin, lymph nodes and soft tissues are effective, and the effect of bone and visceral metastasis is poor.

After oral administration of 20 mg of tamoxifen, the peak concentration of blood was 4 to 7 hours, which was 0.14 μg/ml. A second peak occurs in the enterohepatic circulation after 4 days or more of administration. The half-life β phase is greater than 7 days, and the alpha phase is 7 to 14 hours. 4 to 10 weeks after administration, the objective signs are improved, and if there is bone metastasis, it is effective for several months. A single dose of antiestrogenic effect lasts for several weeks. The drug is metabolized in the liver. The main metabolites are N-desmethyl tamoxifen and 4-hydroxy tamoxifen, and also have a role in binding to the estrogen receptor. Most of the drug is excreted in the form of a conjugate and a small amount is excreted from the urine. The half-life of the parent compound of this product is 5-7 days, and the metabolite nitrogen-desmethyltamoxifen is 14 days.

Tamoxifen Citrate(Nolvadex)_副本.jpgtamoxifen


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