Trade Names:Exjade- Tablets for oral suspension 125 mg- Tablets for oral suspension 250 mg- Tablets for oral suspension 500 mg
Active chelating agent that has a high affinity for binding with iron.
Bioavailability is 70%. Median time to T max is approximately 1.5 to 4 h. C max and AUC increase approximately linearly.
Protein binding is approximately 99% and almost exclusively to serum albumin. Vd is approximately 14 L.
Major metabolic pathway is glucuronidation, with subsequent biliary excretion. Deferasirox is deconjugated in the intestine and undergoes enterohepatic recirculation.
Primarily excreted in feces (84%) with minimal renal excretion (8%). Elimination t ½ ranges from 8 to 16 h.
In children younger than 6 yr of age, systemic exposure was approximately 50% lower than in adults.Gender
Cl appears to be moderately lower (17.5%) in women than in men.Renal/Hepatic Function Impairment
Has not been studied in patients with renal or hepatic function impairment.
Treatment of chronic iron overload caused by blood transfusions (transfusional hemosiderosis) in patients 2 yr of age and older.
PO Start when patient has evidence of chronic iron overload and a serum ferritin consistently greater than 1,000 mcg/L. Initial dose is 20 mg/kg.Maintenance dose
PO Adjust the dose as needed every 3 to 6 mo based on serum ferritin trends. Make dose adjustments in steps of 5 or 10 mg/kg based on patient's response and therapeutic goals. Consider interrupting therapy if serum ferritin consistently falls below 500 mcg/L. Dosage should not exceed 30 mg/kg/day.Dosage adjustment for renal function impairment
Dose reduction, interruption, or discontinuation should be considered for increases in serum creatinine. If there is a progressive increase in serum creatinine beyond the age-appropriate ULN, interrupt deferasirox therapy. Once creatinine has returned to within the normal range, therapy may be restarted at a lower dose followed by gradual dose escalation. For adult patients, reduce the daily dose by 10 mg/kg if serum creatinine increases to more than 33% above the average of the pretreatment measurements at 2 consecutive visits, and if the increase cannot be attributed to other causes. For children, reduce the dose by 10 mg/kg if serum creatinine levels rise above the age-appropriated ULN at 2 consecutive visits.
Store between 59° to 86°F. Protect from moisture.
Avoid coadministration.Other iron chelator therapy
Do not coadminister because safety has not been established.
None well documented.
Pyrexia (19%); headache (16%); fatigue (6%).
Rash (8%); urticaria (4%); leukocytoclastic vasculitis (postmarketing).
Nasopharyngitis (13%); pharyngolaryngeal pain (11%); pharyngitis (8%); acute tonsillitis, rhinitis (6%); ear infection (5%).
Abdominal pain (14%); diarrhea (12%); nausea (11%); vomiting (10%); upper abdominal pain (8%).
Acute renal failure (postmarketing).
Cytopenias including agranulocytosis, neutropenia, and thrombocytopenia (postmarketing).
Hepatic failure, some with fatal outcome (postmarketing).
Anaphylaxis and angioedema (postmarketing).
Increased creatinine (38%); increased ALT (8%).
Arthralgia (7%); back pain (6%).
Increased creatinine (11%).
Cough (14%); respiratory tract infection (10%); bronchitis (9%).
Closely monitor proteinuria. Monitor serum ferritin monthly. Monitor serum creatinine before initiating therapy and monthly thereafter. Monitor liver and renal function monthly during treatment. Auditory and ophthalmic testing are recommended before the start of treatment and every 12 mo thereafter.
Category B .
Safety and efficacy not established in children younger than 2 yr of age.
Use with caution, usually starting at the low end of the dosage range because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Serious hypersensitivity reactions (eg, anaphylaxis, angioedema) have been reported, with the onset of the reaction occurring in the majority of cases within the first month of treatment.
Dose-dependent increases in serum creatinine have been reported.
There have been postmarketing reports of hepatic failure, some with fatal outcome.
Auditory disturbances (eg, decreased hearing, high-frequency hearing loss) and ocular disturbances (eg, cataract, elevations in IOP, lens opacities, retinal disorders) have been reported.
Diarrhea, hepatitis, nausea.
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