Tamoxifen

Indications
Oral
Breast cancer
Adult: 20 mg daily as a single dose or in 2 divided doses. Max: 40 mg/day.
Oral
Reduction of breast cancer incidence in women at high risk
Adult: 20 mg daily for 5 yr.
Oral
Anovulatory infertility
Adult: 20 mg daily on days 2-5 of the menstrual cycle. Max: 80 mg/day.
Contraindications
Pregnancy and lactation. History of thromboembolic events.
Warnings / Precautions
Perform routine haematological and liver function tests in long-term therapy. Gynaecological monitoring is necessary in women.
Adverse Reactions
Hot flushes, oedema, fluid retention, dry skin, vaginal bleeding, vaginal discharge, pruritus vulvae, GI upsets, nausea, dizziness, rashes, blurred vision, loss of acuity, alopecia, increased liver enzymes, hypertriglyceridaemia, uterine fibroids and endometrial hyperplasia.
Potentially Fatal: Blood dyscrasias, cholestasis, hepatitis, hypercalcaemia in patients with bone metastasis, thromboembolic events. Increased risk of endometrial cancer and uterine sarcoma.
Drug Interactions
Aminoglutethimide reduces plasma-tamoxifen concentration.
Potentially Fatal: Concurrent use increased anticoagulant effect of warfarin; increased risk of thromboembolic events with other cytotoxic drugs.
See Below for More tamoxifen Drug Interactions
Lab Interactions
False increase of serum thyroxine concentration. False negative estrogen receptor determinations if performed within 4-6 wk after discontinuation of drug.
Mechanism of Actions
Tamoxifen, a triphenylethylene derivative, produces a nuclear complex by competitively binding to oestrogen receptors on tumours and other tissue targets thus, decreasing DNA synthesis and inhibiting oestrogen effect. It is only cytostatic rather than cytotoxic due to accumulation of cell in G0 and G1 phases.
Absorption: Well absorbed from the GIT; peak plasma concentrations after 4-7 hr (oral).
Distribution: Distributed into uterus (high concentrations), endometrial and breast tissues. Protein-binding: Extensive.
Metabolism: Extensively metabolised in liver by the cytochrome P450 isoenzymes CYP3A4, CYP2C9, and CYP2D6, converted to desmethyltamoxifen; undergoes enterohepatic recycling.
Excretion: Faeces (as conjugates), urine (small amounts); 7 days (terminal half-life).
Storage Conditions
Oral: Store between 20-25°C.
Storage
Oral: Store between 20-25°C.
Available As
  • Tamoxifen 10 mg
  • Tamoxifen 100 mg
  • Tamoxifen 20 mg
  • Tamoxifen 50 mg
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    Tamoxifen is used in following diseases

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