Deferasirox
Mechanism :
Two molecules of deferasirox are capable of binding to 1 atom of iron. Deferasirox works in treating iron toxicity by binding trivalent (ferric) iron (for which it has a strong affinity), forming a stable complex which is eliminated via the kidneys.
Indication :
- Transfusional Hemosiderosis
- Non-transfusion-dependent thalassemia
Contraindications :
Hypersensitivity, Renal OR liver failure, Thrombocytopenia.
Dosing :
Oral
Transfusional iron overload:
2 years of age or older:
Initial dose: 20 mg/kg once a day.
Maintenance dose: 20 to 40 mg/kg/day.
Maximum dose: 40 mg/kg/day.
Thalassemia:
10 mg/kg orally once daily.
Adverse Effect :
Renal toxicity, proteinuria, hepatic toxicity, GI hemorrhage, bone marrow suppression, hypersensitivity, auditory and ocular abnormalities.
Interaction :
Aluminium: Possible physicochemical interaction.
Anticoagulants: Increase the risk for gastrointestinal ulceration/irritation and/or GI bleeding. If these two agents must be used, patients need to be closely monitored for signs and symptoms of GI toxicity.
Etravirine, Tofacitinib (and other CYP3A4 substrates): When administered concomitantly with deferasirox, may experience a decrease in serum concentration. It is recommended to monitor therapy.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Avoid. |
| 10-20 | Avoid. |
| <10 | Avoid. |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unlikely to be dialysed. Avoid |
| HD | Dialysed. Avoid |
| HDF/High flux | Dialysed. Avoid |
| CAV/VVHD | Unlikely to be dialysed. Avoid |
Hepatic Dose :
Child-Pugh A: No dosage adjustment necessary.
Child-Pugh B: Reduce the starting dose by 50%.
Child-Pugh C: Avoid use.