Deferasirox is indicated for the treatment of chronic iron overload due to blood transfusions in adult and paediatric patients (aged 2 years and over).
Deferasirox is an orally active chelator that is highly selective for iron, It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Deferasirox promotes excretion of iron, primarily in the faeces. Deferasirox has low affinity for zinc and copper, and does not cause constant low serum levels of these metals. In an iron balance metabolic study in iron overloaded adult thalassaemia patients, Deferasirox at daily doses of 10, 20 and 40 mg/kg induced the mean net excretion of 0.119, 0.329, and 0,445 mg Fe/kg body weight/day, respectively.
2 years children & Adult Dose: Chronic Iron overload: Initially, 20 mg/kg daily. Adjust dosage every 3-6 months as needed based on trends in serum ferritin concentrations (monitor monthly). Adjust dosage in increments of 5 or 10 mg/kg daily (up to maximum dosage of 30 mg/kg daily) according to the patient$#$#$#$s clinical response and therapeutic goals. Consider temporarily interrupting therapy if serum ferritin concentrations are consistently <500 mcg/L.
Should not be taken with aluminium-containing antacids, Caution to be taken when combined with drugs metabolized through CYP3A4 (e.g. cyclosporine, simvastatin, hormonal contraceptive, midazolam). Dose increase should be considered when concomitantly used with rifampicin, phenytoin, phenobarbital, ritonavir etc. Interaction with other CYP2C8 substrates like paclitaxel cannot be excluded. Caution to be taken when combined with drugs with ulcerogenic potential (e.g. NSAIDS, corticosteroids, oral bisphosphonates) or with anticoagulants.
Creatinine clearance <40 mL/min or serum creatinine >2 times the age-appropriate upper limit of normal. High risk myelodysplastic syndrome (MDS) patients and patients with other hematological and non-hematological malignancies who are not expected to benefit from chelation therapy due to the rapid progression of their disease. Hypersensitivity to the active substance or to any of the excipients. Moderate hepatic impairment. Children. Pregnancy and lactation.
Serum creatinine increase, Abdominal pain, Nausea, Vomiting, Diarrhea, Proteinuria, Pyrexia, Headache, Cough , Nasopharyngitis, Pharyngolaryngeal pain, Influenza, Rash, Respiratory tract infection, Bronchitis, ALT increased, Arthralgia, back pain, Acute tonsillitis, Rhinitis, Fatigue, Ear infection, Transaminitis, Urticaria, Anaphylaxis, Angioedema, Cytopenias, including agranulocytosis, neutropenia and thrombocytopenia; leukocytoclastic vasculitis.
Pregnancy: No clinical data on exposed pregnancies are available for deferasirox. Studies in animals have shown some reproductive toxicity at maternally toxic doses. The potential risk for humans is unknown. As a precaution, it is recommended that Deferasirox not be used during pregnancy unless clearly necessary. Breast-feeding: In animal studies, Deferasirox was found to be rapidly and extensively secreted into maternal milk. No effect on the offspring was noted. It is not known if Deferasirox is secreted into human milk. Breast-feeding while taking Deferasirox is not recommended.
The maximal dose of Deferasirox is 40 mg/kg body weight. There is no information about overdose of Deferasirox.
Store in a dry place below 25°C, and protect from light. Keep out of the reach of children.
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