Gynecology Book

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Tamoxifen

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  1. See Also
    1. Selective Estrogen Receptor Modulator
  2. Indications
    1. Breast Cancer in post-menopausal women
      1. Estrogen Receptor positive
  3. Contraindications
    1. Thromboembolism history
    2. Perioperative period
    3. Prolonged immobilization
  4. Efficacy
    1. Estrogen Receptor Positive Breast Cancer
      1. Reduces Breast Cancer recurrence (29%)
      2. Reduces mortality from Breast Cancer (20%)
    2. Reference
      1. (1992) Lancet 339:1
  5. Course
    1. Recommended for five years (exact course unclear)
  6. Benefits
    1. Anti-Estrogen
      1. Reduces Breast Cancer recurrence rate
    2. Preserves Bone Mineral Density
      1. Only applies to post-menopausal patients
      2. Bone Mineral Density decreases if premenopausal
    3. Lowers Total Cholesterol and LDL Cholesterol
      1. Only applies to post-menopausal patients
      2. No effect on lipids if premenopausal
  7. Adverse Effects
    1. Thromboembolism
      1. Tamoxifen significantly increases risk
      2. See contraindications
    2. Endometrial Cancer
      1. Markedly increased risk if used more than 5 years
      2. Relative risk for 2 to 5 years of use: 2.0
      3. Relative risk for 5 or more years of use: 6.9
  8. Drug Interactions
    1. CYP2D6 Inhibitors (e.g. Paroxetine, Fluoxetine)
      1. May decrease Tamoxifen efficacy
  9. References
    1. (2002) Lancet 360:817
    2. Bergman (2000) Lancet 356:881

Tamoxifen (C0039286)

Definition (MSH)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.
Definition (CSP)selective estrogen receptor modulator; it is agonist for bone tissue and cholesterol metabolism but antagonist in mammary and uterine tissues.
Definition (NCI)An antineoplastic nonsteroidal selective estrogen receptor modulator (SERM). Tamoxifen competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA. The result is a reduction in DNA synthesis and cellular response to estrogen. In addition, tamoxifen up-regulates the production of transforming growth factor B (TGFb), a factor that inhibits tumor cell growth, and down-regulates insulin-like growth factor 1 (IGF-1), a factor that stimulates breast cancer cell growth.
Definition (NCI)An anticancer drug that belongs to the family of drugs called antiestrogens. Tamoxifen blocks the effects of the hormone estrogen in the body. It is used to prevent or delay the return of breast cancer or to control its spread.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishTAM, Tamoxifen, TAMOXIFEN PREPARATION, TMX
Spanishtamoxifeno
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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