Tamoxifen

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In medicine, tamoxifen is "one of the selective estrogen receptor modulators with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the endometrium.

Until the introduction of the aromatase inhibitors, tamoxifen was the gold standard for chemotherapy of breast cancer, and remains important in its treatment, especially of premenopausal women. It is also used to treat other hormonally sensitive cancers, such as melanoma.

Pharmacology

Administration

Distribution

Metabolism

Tamoxifen is metabolized in the liver by cytochrome P-450 CYP2D6 to active metabolites.

Excretion

Toxicity

Drug interactions

Paroxetine may increase death from breast cancer among women taking tamoxifen due to inhibiting metabolism of tamoxifen to its active metabolite by cytochrome P-450 CYP2D6.[1]

References

  1. Kelly, Catherine M; David N Juurlink, Tara Gomes, Minh Duong-Hua, Kathleen I Pritchard, Peter C Austin, Lawrence F Paszat (2010-02-08). "Selective serotonin reuptake inhibitors and breast cancer mortality in women receiving tamoxifen: a population based cohort study". BMJ 340 (feb08_1): c693. DOI:10.1136/bmj.c693. Retrieved on 2010-02-10. Research Blogging.