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Administration
- Type: Antidote
- Dosage Forms: 125, 250, 500 mg disperse tab
- Routes of Administration: Oral
- Common Trade Names: Exjade
Adult Dosing
- 20-30 mg/kg PO QD
- Start: 20 mg/kg PO QD
- Max: 40 mg/kg/day
- Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin
- Decrease dose 10 mg/kg/day if Cr >33% above baseline x2 weeks
- Hold: Ferritin <500 mcg/L
- 10-20 mg/kg PO QD
- Start: 10 mg/kg PO QD
- Max: 20 mg/kg/day
- Decrease dose 50% if Cr >33% above baseline x2 weeks
- Interrupt treatment if already at 5 mg/kg/day
- Hold: Ferritin <300 mcg/L or liver iron <3 mg Fe/g
Pediatric Dosing
- 2-15 yo
- 20-30 mg/kg PO QD
- Start: 20 mg/kg PO QD
- Max: 40 mg/kg/day
- Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin
- Decrease dose 10 mg/kg/day if Cr >33% above baseline and >ULN
- 16+ yo
- 20-30 mg/kg PO QD
- Start: 20 mg/kg PO QD
- Max: 40 mg/kg/day
- Adjust dose by 5-10 mg/kg/day q3-6mo based on serum ferritin
- Decrease dose 10 mg/kg/day if Cr >33% above baseline x2 weeks
- 10-15 yo
- 10-20 mg/kg PO QD
- Start: 10 mg/kg PO QD
- Max: 20 mg/kg/day
- Adjust dose based on serum ferritin trends and liver iron concentration
- Decrease dose 5 mg/kg/day if Cr >33% above baseline and >ULN
- 16+ yo
- 10-20 mg/kg PO QD
- Start: 10 mg/kg PO QD
- Max: 20 mg/kg/day
- Adjust dose based on serum ferritin trends and liver iron concentration
- Decrease dose 50% if Cr >33% above baseline x2 weeks
- Interrupt treatment if already at 5 mg/kg/day
Special Populations
- Pregnancy Rating: C; Caution during pregnancy
- Lactation risk: L3; Safety unknown
Renal Dosing
- Adult:
- CrCl 40-60: Decrease start dose 50%
- Cr >2x ULN or CrCL <40: Contraindicated
- Pediatric:
- CrCl 40-60: Decrease start dose 50%
- Cr >2x ULN or CrCL <40: Contraindicated
Hepatic Dosing
- Adult:
- Child-Pugh Class B: Decrease start dose 50%
- Child-Pugh Class C: Avoid use
- Pediatric:
- Child-Pugh Class B: Decrease start dose 50%
- Child-Pugh Class C: Avoid use
Contraindications
- Allergy to class/drug
- Cr >2x ULN or CrCl <40
- Poor performance status
- High risk myelodysplastic syndrome
- Advanced malignancy
- Thrombocytopenia <50,000
- Hepatic impairment, Child-Pugh Class C
- Caution if hepatic impairment, Child-Pugh Class A or B
- Caution if renal impairment
- Caution if concurrent nephrotoxic agent
- Caution if hematologic disorder
- Caution in patients >55yo
Adverse Reactions
Serious
Common
Pharmacology
- Half-life: 8-16h
- Metabolism: Liver; CYP450: minimal (8%); UGT: 1A1 (primary), 1A3 substrate
- Excretion: Feces 84%, Urine 8%
Mechanism of Action
- Chelates iron, promoting fecal iron excretion
- Black Box Warning
- Risk for renal failure in pts with comorbidities or advanced hematological disorder
- Risk for hepatic failure in pts with Child-Pugh Class A, B, C disease
- Risk for gastrointestinal Hemorrhage in elderly pts with advanced hematologic malignancies or low platelets
See Also
References