1. Definition & Composition
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Generic Name: Deferasirox
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Dosage Form: Dispersible tablet (oral suspension preparation)
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Strength: 250 mg per tablet
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Class: Oral iron chelator (tridentate ligand)
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Mechanism: Selectively binds ferric iron (Fe³⁺) forming stable complexes excreted in feces
2. Importance & Clinical Use
Primary Indications
✅ Chronic Iron Overload in:
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Transfusion-dependent thalassemia (≥6 transfusions/year)
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Sickle cell disease (≥8 transfusions/year)
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Myelodysplastic syndromes (MDS)
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Other transfusion-dependent anemias
✅ Non-Transfusion Iron Overload (e.g., hereditary hemochromatosis if intolerant to phlebotomy)
Key Benefits
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Once-daily oral dosing (vs. subcutaneous/infusional chelators)
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Effective iron excretion (up to 30 mg Fe/day at optimal doses)
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Reduces liver/cardiac iron (T2* MRI improvement in 6-12 months)
3. Dosage & Administration
Dosing Guidelines
Patient Population | Initial Dose | Maintenance Adjustment |
---|---|---|
Transfusion-dependent | 20 mg/kg/day | ↑ by 5-10 mg/kg every 3-6 months (max 40 mg/kg/day) |
Non-transfusion overload | 10 mg/kg/day | Adjust based on serum ferritin |
Administration Protocol
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Take on empty stomach (30 min before breakfast)
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Disperse tablet in water/orange juice (NOT milk or antacids)
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Stir until fine suspension → drink immediately
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Avoid aluminum-containing antacids (separate by 4 hrs)
4. Side Effects & Toxicity
Common (≥10%)
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Gastrointestinal: Nausea (35%), diarrhea (25%), abdominal pain (20%)
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Skin Rash (15%)
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Mild proteinuria (12%)
Serious (Require Monitoring)
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Renal Toxicity: ↑ serum creatinine (30%), acute kidney injury
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Hepatotoxicity: ↑ ALT/AST (10%), rare hepatic failure
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GI Ulceration/hemorrhage (especially in elderly)
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Auditory/Visual disturbances (high-frequency hearing loss, cataracts)
5. Storage & Handling
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Store below 30°C in original blister packaging
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Protect from moisture (desiccant in bottle)
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Reconstituted suspension: Use within 30 minutes
6. Contraindications & Warnings
❌ Absolute Contraindications:
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Severe renal impairment (CrCl <40 mL/min)
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Advanced hepatic cirrhosis (Child-Pugh C)
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History of GI perforation/hemorrhage
⚠️ Boxed Warnings (FDA):
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Renal/hepatic failure (monitor creatinine/ALT weekly initially)
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Fatal GI hemorrhage (higher risk in elderly)
7. Drug Interactions
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Antacids/Al supplements: ↓ Deferasirox absorption
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CYP3A4 inducers (rifampin): ↓ Efficacy
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CYP1A2 substrates (theophylline): ↑ Toxicity risk
8. Monitoring Protocol
Parameter | Frequency | Action Threshold |
---|---|---|
Serum ferritin | Monthly | Maintain 500-1000 ng/mL |
Serum creatinine | Weekly ×1 month, then monthly | ↑ >33% baseline → dose reduction |
Liver function | Monthly | ALT >5× ULN → interrupt |
Auditory/visual | Annual exams | New-onset changes → reassess |
9. Cost & Alternatives
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Price: ~$250/30 tablets (generic available)
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Comparators:
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Deferoxamine (IV): More potent but requires infusion
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Deferiprone (oral): Better cardiac iron removal but ↑ agranulocytosis risk
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10. Conclusion
DESIROX 250 mg is a first-line oral chelator for chronic iron overload, offering:
✔ Convenient dosing vs. parenteral alternatives
✔ Proven efficacy in reducing organ iron
✔ Flexible dose adjustments based on ferritin trends
Critical Practice Points:
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Strict adherence to monitoring protocols (renal/hepatic)
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Avoid use with NSAIDs/anticoagulants (↑ bleeding risk)
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Consider switching to IV chelation if poor GI tolerance
Reviews
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