Chelova

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 selective for iron (as Fe3+ ). It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Although deferasirox has very low affinity for zinc and copper there are variable decreases in the serum concentration of these trace metals after the administration of deferasirox. The clinical significance of these decreases is uncertain.

May chelate Al when used with Al-containing antacids. Decreased exposure with colestyramine and potent inducers of UGT enzymes (e.g. carbamazepine, rifampicin, phenytoin). May increase serum concentration of CYP1A2 (e.g. duloxetine, theophylline) and CYP2C8 (e.g. repaglinide, paclitaxel) substrates, and decrease serum concentrations of CYP3A4 substrates (e.g. ciclosporin, hormonal contraceptives, simvastatin).

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.

Moderate hepatic impairment. Children. Pregnancy and lactation.

Dosage Modification for Adverse Renal Effects: Interrupt therapy if a progressive increase in SCR (Serum Creatinine Concentration) beyond the ULN occurs. Once SCR returns to within normal limits, reinitiate therapy at a lower dosage followed by gradual dosage escalation if clinical beneht is expected to outweigh potential risks. Reduce dosage by 10 mg/kg daily if SCR at 2 consecutive visits increases to a level >33% above the average pretreatment value and the increase cannot be attributed to other causes.

Dosage Modifcation for Adverse Hepatic Effects: Consider dosage adjustment or interruption of therapy in patients with severe, persistent, progressive, or unexplained elevations of liver function test results.

Antidote preparations

Single doses up to 40 mg/kg in normal subjects have been well tolerated. Acute signs of overdose may include nausea, vomiting, headache, and diarrhea. Overdose may be treated by induction of emesis or by gastric lavage, and by symptomatic treatment.

Store at 25° C. Protect from moisture.