Tamoxifen: Uses, Dosage & Side Effects

10 min read

Quick Facts

What Is Tamoxifen?

Tamoxifen is a selective estrogen receptor modulator that acts as an estrogen antagonist in breast tissue while having agonist effects in bone and cardiovascular tissue. It remains a gold standard for hormone receptor-positive breast cancer.

How Tamoxifen Works
Tamoxifen competitively binds to estrogen receptors in breast cancer cells, blocking estrogen-stimulated growth and proliferation. Its selective action preserves beneficial estrogen effects in bone density maintenance and lipid profiles.

Indications

  • Adjuvant treatment of node-negative and node-positive breast cancer
  • Metastatic breast cancer in postmenopausal women
  • Breast cancer risk reduction in high-risk women (BRCA mutations, strong family history)
  • Ductal carcinoma in situ (DCIS)
  • Prevention of contralateral breast cancer

Dosage and Administration

Standard Dosing:

  • 20 mg once daily or 10 mg twice daily
  • Take with or without food
  • Treatment duration typically 5 years; may extend to 10 years in selected cases

Adjuvant Therapy:

  • Initiated after surgery, radiation, and/or chemotherapy
  • Continuous daily dosing for entire treatment period
Clinical Note
Baseline gynecologic assessment is recommended before initiation. Annual gynecologic exams and awareness of endometrial symptoms is essential during treatment.

Side Effects

Common: Hot flashes, vaginal discharge/bleeding, nausea, weight gain, mood changes Serious: Endometrial cancer (2-3 fold increased risk), thromboembolic events (DVT/PE), stroke, cataracts, retinal deposits

Warning
Tamoxifen significantly increases the risk of endometrial cancer and thromboembolic events. Women should be monitored for abnormal vaginal bleeding. Baseline and periodic ophthalmologic examination is recommended, particularly with doses >120 g cumulative dose. Risk-benefit assessment is essential, especially in women with prior thromboembolism.

Contraindications

  • Pregnancy or concurrent use in women of childbearing potential (highly teratogenic)
  • Active thromboembolism
  • Undiagnosed vaginal bleeding
  • History of thromboembolic events (relative contraindication; requires careful risk assessment)
  • Concurrent warfarin therapy (relative)

Drug Interactions

  • CYP2D6 inhibitors (paroxetine, fluoxetine, bupropion): reduce tamoxifen efficacy by decreasing active metabolite (endoxifen) formation
  • Warfarin: increased anticoagulant effect; monitor INR closely
  • Aromatase inhibitors: sequential or concurrent use in some protocols
  • Megestrol acetate: additive effects for advanced disease

Key Clinical Evidence

NSABP B-24 trial (JNCI 2004) demonstrated tamoxifen reduces recurrence and mortality in early breast cancer. IBIS-I trial demonstrated 38% risk reduction for contralateral breast cancer in high-risk women. Emergence of aromatase inhibitors has shifted treatment paradigms for postmenopausal women.

Monitoring Parameters

  • Baseline assessment before initiating therapy
  • Regular clinical follow-up per indication
  • Laboratory parameters as specified in sections above
  • Drug interaction screening at each visit

Special Populations

Dosing adjustments may be necessary in:

  • Renal impairment
  • Hepatic impairment
  • Elderly patients
  • Pregnancy and lactation
  • Pediatric patients

Patient Counseling

  • Take exactly as directed; do not modify dose without consulting healthcare provider
  • Report any unusual symptoms or adverse effects
  • Maintain regular follow-up appointments
  • Store at room temperature away from moisture and light
  • Keep out of reach of children

Disclaimer: This information is for educational purposes only and should not substitute for professional medical advice. Always consult with a qualified healthcare provider before starting, stopping, or modifying any medication.

Sources

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Last updated: 2024-01-01Sources: 2

The content on Medical Atlas is for informational purposes only. It is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider.