Exjade Deferasirox Dispersible Tablets

1. Indications and Usage
Chronic Iron Overload:
Treatment of chronic iron overload in patients aged 2 years and older due to frequent blood transfusions (e.g., transfusion-dependent anemias such as beta-thalassemia, myelodysplastic syndromes, or other rare anemias).
2. Dosage and Administration
Route of Administration:
Oral administration.
Recommended Dosage:
Initial Dose: 20 mg/kg of body weight once daily.
Dose Adjustment: Dosage may be adjusted or maintained at 10 mg/kg or 30 mg/kg based on serum ferritin trends and patient response.
Maximum Dose: Generally should not exceed 30 mg/kg daily (up to 40 mg/kg may be considered if clinically necessary but with caution).
Critical Administration Instructions:
Fasting: Must be taken on an empty stomach, at least 30 minutes before a meal, once daily at the same time each day.
Dissolution: The tablet must be completely dissolved in a glass of water, orange juice, or apple juice (approx. 100–200 mL, or more for higher doses). Stir until a uniform suspension is formed and drink immediately. Any residue must be re-suspended in a little more liquid and swallowed.
Contraindicated Vehicles: Do not dissolve in milk or carbonated beverages.
Do Not Swallow Whole: The tablet is not designed to be swallowed whole.
3. Mechanism of Action
Iron Chelation:
Deferasirox is a selective, tridentate, oral iron chelator.
Binding:
It binds with high affinity to ferric iron (Fe³⁺) in a 2:1 ratio.
Therapeutic Result: It removes excess iron from the body primarily through fecal excretion (biliary excretion), reducing iron load in the liver and other tissues.
4. Safety and Warnings
Renal Impairment:
Increases in serum creatinine are common.
Action: Monitor renal function (serum creatinine and creatinine clearance) before initiation, every 2 weeks during the first month, and monthly thereafter.
Contraindication: Not recommended for patients with severe renal impairment (e.g., creatinine clearance < 30 mL/min).
Hepatic Impairment:
Monitor liver function tests (ALT, AST) before initiation and monthly thereafter.
Gastrointestinal Hemorrhage:
Gastrointestinal bleeding has been reported, particularly in elderly patients or those with advanced malignancies.
Hypersensitivity:
Serious skin reactions (e.g., Stevens-Johnson Syndrome) have been reported.
5.Adverse Reactions
Most Common:
Nausea, vomiting, diarrhea, abdominal pain, rash, headache, and increased serum creatinine (non-progressive in most cases).
6.Drug Interactions
Antacids:
Do not administer concomitantly with aluminum-containing antacids (may reduce efficacy).
UGT Inducers:
Avoid concomitant use with strong inducers of UDP-glucuronosyltransferase (e.g., Rifampicin, Phenytoin, Carbamazepine) as they may decrease Deferasirox exposure.
NSAIDs:
Use with caution with non-steroidal anti-inflammatory drugs (NSAIDs) due to potential additive nephrotoxicity.
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Deferasirox.
Appearance: White to pale yellow, round, biconvex tablets with “510” or “520” debossed on one side.
Packaging: Blister packs (e.g., 125 mg, 250 mg, 500 mg).
Storage: Store below 30°C in a dry place. Protect from moisture.