🔹 1. Basic Information
Generic name: Anastrozole
Brand name: Mylan Anastrozole
Drug class: Aromatase inhibitor (non-steroidal)
Formulation: Film-coated oral tablets
Strength: 1 mg
Mechanism of Action:
Selectively inhibits the aromatase enzyme, preventing the conversion of androgens to oestrogens in peripheral tissues → reduces circulating oestrogen levels (>80%) in postmenopausal women → suppresses growth of oestrogen-dependent breast tumours.
🔹 2. Indications
Early breast cancer in postmenopausal women.
Advanced or metastatic breast cancer in postmenopausal women.
Not effective in oestrogen receptor–negative tumours unless previously responsive to tamoxifen.
🔹 3. Dosing & Administration
Dose: 1 mg orally once daily.
Route: Oral (tablet swallowed whole).
Duration: Continue until disease progression or as clinically indicated.
Usually, Endocrine Therapy is given for 5-10 years
Renal impairment: No adjustment for mild–moderate impairment.
Hepatic impairment: No adjustment for mild hepatic disease.
Children: Not recommended (safety and efficacy not established).
🔹 4. Contraindications
Hypersensitivity to anastrozole or excipients.
Premenopausal women.
Pregnancy and lactation.
Severe renal impairment (CrCl < 20 mL/min).
Moderate or severe hepatic impairment.
Patients with hereditary galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption (due to lactose content).
🔹 5. Warnings & Precautions
Bone health: Causes bone mineral density loss due to oestrogen suppression → increased fracture risk. Manage per postmenopausal bone health guidelines (e.g. DEXA scans, bisphosphonates).
Lactose content: Avoid in patients with lactose intolerance or galactosaemia.
Menopausal status: Confirm biochemically before initiating therapy.
Use in children/premenopausal women: Not recommended (ineffective and unsafe).
🔹 6. Drug Interactions
Minimal CYP450-mediated interactions expected.
No significant interactions with bisphosphonates or commonly prescribed medicines.
Avoid co-administration with:
Tamoxifen or oestrogen-containing therapies (reduces efficacy).
Other anticancer drugs: Limited safety data available.
🔹 7. Side Effects & Management
Very common / Common:
Hot flushes, headache, dizziness, asthenia, arthralgia, joint stiffness, arthritis, rash, sweating, nausea, fatigue
→ Usually mild; manage symptomatically.
Less common:
Depression, carpal tunnel syndrome, hair thinning, weight gain, hypercholesterolaemia, bone pain, vaginal dryness, oedema.
→ Monitor lipid and bone profile; treat supportively.
Rare / Serious:
Osteoporosis, fractures, cutaneous vasculitis, Stevens-Johnson syndrome, anaphylaxis, thromboembolism.
→ Discontinue and manage accordingly.
🔹 8. Overdose
No specific antidote.
Treatment is symptomatic and supportive — consider gastric lavage, monitoring of vital signs, and dialysis (as anastrozole is not highly protein bound).
🔹 9. Pharmacology
Pharmacodynamics:
Selective, potent, non-steroidal aromatase inhibitor → decreases oestrogen production by >80% without affecting cortisol or aldosterone.
Pharmacokinetics:
Rapid absorption (Tmax ≈ 2 h)
Half-life: 40–50 h
40% protein bound
Extensively metabolised (N-dealkylation, hydroxylation, glucuronidation); metabolites excreted in urine.
Steady-state reached within 7 days of daily dosing.
🔹 10. Use in Special Populations
Elderly: No dose adjustment.
Renal impairment: Avoid if CrCl < 20 mL/min.
Hepatic impairment: Avoid if moderate or severe.
Pregnancy/Lactation: Contraindicated.
Paediatrics: Not indicated.
| Trade Name | |
|---|---|
| Drug Class | Aromatase Inhibitor |
| Cost | |
| Company | |
|---|---|
| Drug Rep | Admin |
| Indications | Breast Cancer |
| Dosage |