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Megestrol is indicated for:
Advanced/metastatic breast cancer: 160 mg/day
Recurrent/inoperable endometrial carcinoma: 40–320 mg/day (divided doses)
Requires ≥2 months of continuous therapy for efficacy assessment
Treatment of AIDS-related cachexia (unexplained weight loss >10%)
Cancer-associated anorexia-cachexia syndrome
Progestational Agent: Synthetic antineoplastic with dual action:
Suppresses pituitary gonadotropins → reduces estrogen-driven tumor growth
Direct cytotoxic effect on hormone-sensitive cancer cells
Pharmacokinetics:
Peak plasma concentration: 2–3 hours post-dose
Half-life: 33–38 hours
Excretion: Urine (66%), Feces (20%)
| Formulation | Indication | Dosage |
|---|---|---|
| Tablets | Breast Cancer | 160 mg once daily |
| Tablets | Endometrial Carcinoma | 40–320 mg/day (divided) |
| Oral Suspension | AIDS/Cancer Cachexia | 800 mg (20 mL) once daily |
*Minimum 8-week trial recommended for cachexia response*
❌ Absolute Contraindications:
Pregnancy (Category X - Fetal abnormalities risk)
Hypersensitivity to megestrol acetate
History of thromboembolism (DVT/PE)
⚠️ Critical Precautions:
Fluid retention: Exacerbates CHF, hypertension, or renal disease
Adrenal suppression: Monitor for Cushingoid symptoms with long-term use
Hepatic impairment: Requires dose reduction (primary metabolism route)
Elderly patients: Increased risk of renal/toxicity (adjust for CrCl <30 mL/min)
| Common (>10%) | Serious (Monitor Closely) |
|---|---|
| • Weight gain (appetite stimulation) | • Thromboembolism (DVT/PE) |
| • Peripheral edema | • Hyperglycemia / New-onset diabetes |
| • Mild nausea/vomiting | • Adrenal insufficiency |
| • Breakthrough uterine bleeding | • Tumor flare (with hypercalcemia) |
Pregnancy/Lactation:
Contraindicated - Virilization of female fetuses
Discontinue breastfeeding (excretion unknown)
Pediatrics: Safety/efficacy not established
Renal Impairment: Reduce dose if CrCl <30 mL/min
Hepatic Impairment: Avoid in severe disease
Fluid Retention Risk: Avoid concurrent NSAIDs/corticosteroids
Diabetic Patients: Monitor glucose (progestins reduce insulin sensitivity)
No Known Pharmacokinetic Interactions - Limited interaction data available
Symptoms: Severe nausea, dyspnea, lethargy
Treatment: Supportive care (no specific antidote)
*Maximum tested dose: 1600 mg/day for 6+ months*
Store below 30°C in original packaging
Protect from light/humidity
Keep out of children’s reach
Medical Notice: Use only under specialist supervision. Not a substitute for surgery/chemotherapy.
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