Tamoxifen

Tamoxifen (TAMOPLEX®)

🔴 Red Flag (Important Information)

Increased risk of venous thromboembolism and stroke – higher risk with chemotherapy, surgery, or prior clot history
Risk of endometrial pathology (hyperplasia, polyps, endometrial cancer) – investigate any vaginal bleeding immediately
Contraindicated in pregnancy and breastfeeding – teratogenic
Visual disturbances and cataracts may occur – ophthalmology review if symptoms develop
Hypercalcaemia can occur, especially in patients with bone metastases
Interacts with CYP2D6 inhibitors (e.g. paroxetine, fluoxetine) – may reduce efficacy
Tumour flare may occur early in treatment
Avoid in patients with active or high-risk thromboembolic disease unless benefits outweigh risks


1. Basic Information

Generic name: Tamoxifen (as tamoxifen citrate)
Brand name: TAMOPLEX®
Drug class: Selective oestrogen receptor modulator (SERM)
Formulation: Oral tablets
Strength: 20 mg
Scheduling status: S4

Mechanism of action:
Tamoxifen acts as an oestrogen antagonist in breast tissue by competitively binding to oestrogen receptors, inhibiting oestrogen-mediated tumour growth. It has partial agonist effects in bone and endometrium.


2. Indications (FULL)

Breast cancer:
• Treatment of breast cancer in adult patients


3. Dosing and Administration

Adults (including elderly):
20 mg orally once daily

Administration:
• Swallow tablet whole with water
• Do not crush or chew
• Duration of treatment is determined by the treating clinician

Children:
• Not recommended


4. Dose Modifications

• No routine dose adjustment required
• Interrupt or discontinue if severe thromboembolic events, severe visual disturbance, or significant endometrial pathology occurs
• Clinical judgement required in patients with hepatic dysfunction or low blood counts


5. Contraindications

• Hypersensitivity to tamoxifen or any excipients
Premenopausal status
• Pregnancy or breastfeeding


6. Monitoring Requirements

• Monitor for signs of thromboembolism (leg swelling, chest pain, dyspnoea)
• Gynaecological review if vaginal bleeding, pelvic pain, or menstrual irregularities occur
• Visual symptoms – assess for cataracts or retinal changes
• Periodic blood counts if clinically indicated
• Monitor calcium levels in patients with bone metastases


7. Side Effects

Very common and common:
• Hot flushes
• Nausea and vomiting
• Fatigue
• Headache
• Alopecia
• Vaginal irritation or discharge
• Menstrual irregularities
• Muscle pain and leg cramps
• Weight gain
• Endometrial hyperplasia

Serious:
• Venous thromboembolism (DVT, PE)
• Stroke or transient ischaemic attack
• Endometrial cancer
• Severe visual disturbance or loss of vision
• Hepatotoxicity
• Interstitial pneumonitis
• Severe allergic reactions


8. Drug Interactions

• Anticoagulants (e.g. warfarin) – increased bleeding risk
• CYP2D6 inhibitors (e.g. paroxetine, fluoxetine, bupropion, quinidine) – reduced tamoxifen efficacy
• Rifampicin – reduced tamoxifen levels
• Other cytotoxic chemotherapy – increased thromboembolic risk


9. Use in Special Populations

• Pregnancy: Contraindicated
• Breastfeeding: Contraindicated
• Premenopausal women: Contraindicated
• Elderly: No dose adjustment required
• Hepatic impairment: Use with caution
• Renal impairment: No specific adjustment required


10. Duration of Use and When to Stop

Continue treatment for the duration prescribed by the treating clinician.

Permanently discontinue if:
• Venous or arterial thromboembolic event occurs
• Endometrial malignancy develops
• Severe visual toxicity occurs
• Pregnancy is confirmed

 

https://pi-pil-repository.sahpra.org.za/wp-content/uploads/2021/09/pil-clean-tamoplex-post-reg-cl-20201207.pdf

 

**Usually discontinued after 5 years - can be given upto 10 years

Trade Name
Drug Class Selective Estrogen Receptor Modulators (SERMs)
Cost
Email
Company
Drug Rep Admin
Indications Breast Cancer
Dosage

Indications (Detailed)

Breast Cancer: Hormone Receptor Positive (HR+) [Non-metastatic]
Websites:
Breast Cancer: Hormone Receptor Positive (HR+) [Metastatic]
Websites:
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