DEFERIPRONE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DEFERIPRONE (DEFERIPRONE).

How it works

Deferiprone is an iron chelator that binds to ferric iron (Fe3+) to form a stable complex, promoting iron excretion in urine. It reduces iron overload in tissues and prevents iron-induced free radical damage.

What the body does with it

Metabolism	Primarily metabolized via glucuronidation by UGT1A6 and UGT2B7; also undergoes N-methylation by TPMT; limited CYP450 involvement.
Excretion	Primarily renal excretion as iron complex (ferrioxamine) and unchanged drug; 70-90% of a dose is recovered in urine within 24 hours, predominantly as the iron chelate. Less than 10% is eliminated in feces via biliary excretion.
Half-life	2-3 hours (terminal elimination half-life). Due to its short half-life, multiple daily doses are required to maintain therapeutic chelation; levels decline rapidly after dose cessation.
Protein binding	Minimal (<10%), primarily to albumin; binding is negligible due to high water solubility.
Volume of Distribution	1-2 L/kg. Indicates extensive distribution into total body water; penetrates into cells and tissues, including liver and heart, to chelate iron.
Bioavailability	75-90% after oral administration; well absorbed from the gastrointestinal tract.
Onset of Action	Oral: Urinary iron excretion begins within 1-2 hours after a single dose, reflecting rapid absorption and chelation of iron.
Duration of Action	Approximately 8-12 hours after an oral dose (based on urinary iron excretion returning to baseline). Clinical effect requires thrice-daily dosing for continuous chelation.

Classification & Brands

Dosing & administration

75 mg/kg/day orally in three divided doses (maximum 3 g/day).

Dosage form	TABLET
Renal impairment	Contraindicated in patients with GFR < 60 mL/min/1.73 m². No dose adjustment for GFR ≥ 60.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use.
Pediatric use	25 mg/kg/dose orally three times daily (75 mg/kg/day), not to exceed 3 g/day. For children ≥ 6 years.
Geriatric use	Initiate at lower end of dosing range (50 mg/kg/day) and monitor for adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DEFERIPRONE (DEFERIPRONE).

Breastfeeding	Not recommended during breastfeeding. M/P ratio is unknown; deferiprone is excreted in human milk in low concentrations, but potential for iron chelation in the nursing infant exists.
Teratogenic Risk	Pregnancy Category D. In first trimester, there is evidence of fetal harm based on animal studies and human data; deferiprone crosses the placenta and may cause iron depletion in the fetus. In second and third trimesters, risk of fetal iron deficiency anemia and potential teratogenicity persists; use only if benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

WARNING: AGRANULOCYTOSIS AND NEUTROPENIA Deferiprone can cause agranulocytosis and neutropenia, which may be severe and life-threatening. Monitor neutrophil counts weekly. Discontinue drug if infection develops or neutrophil count is low.

Side Effect Profile

Serious Effects

Absolute Contraindications

History of agranulocytosis or recurrent neutropenia, hypersensitivity to deferiprone or any component, severe renal impairment (creatinine clearance < 30 mL/min), pregnancy (risk outweighs benefit), breastfeeding.

Clinical Precautions

Precautions

Agranulocytosis/neutropenia (monitor ANC weekly), gastrointestinal effects (nausea, vomiting, abdominal pain), zinc deficiency, hepatic enzyme elevations, arthropathy, and potential for fetal harm (pregnancy category D).

Clinical Tips & Counseling

Drug interactions

Loading safety data…

DEFERIPRONE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DEFERIPRONE (DEFERIPRONE).

How it works

What the body does with it

Metabolism	Primarily metabolized via glucuronidation by UGT1A6 and UGT2B7; also undergoes N-methylation by TPMT; limited CYP450 involvement.
Excretion	Primarily renal excretion as iron complex (ferrioxamine) and unchanged drug; 70-90% of a dose is recovered in urine within 24 hours, predominantly as the iron chelate. Less than 10% is eliminated in feces via biliary excretion.
Half-life	2-3 hours (terminal elimination half-life). Due to its short half-life, multiple daily doses are required to maintain therapeutic chelation; levels decline rapidly after dose cessation.
Protein binding	Minimal (<10%), primarily to albumin; binding is negligible due to high water solubility.
Volume of Distribution	1-2 L/kg. Indicates extensive distribution into total body water; penetrates into cells and tissues, including liver and heart, to chelate iron.
Bioavailability	75-90% after oral administration; well absorbed from the gastrointestinal tract.
Onset of Action	Oral: Urinary iron excretion begins within 1-2 hours after a single dose, reflecting rapid absorption and chelation of iron.
Duration of Action	Approximately 8-12 hours after an oral dose (based on urinary iron excretion returning to baseline). Clinical effect requires thrice-daily dosing for continuous chelation.

Classification & Brands

Dosing & administration

75 mg/kg/day orally in three divided doses (maximum 3 g/day).

Dosage form	TABLET
Renal impairment	Contraindicated in patients with GFR < 60 mL/min/1.73 m². No dose adjustment for GFR ≥ 60.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use.
Pediatric use	25 mg/kg/dose orally three times daily (75 mg/kg/day), not to exceed 3 g/day. For children ≥ 6 years.
Geriatric use	Initiate at lower end of dosing range (50 mg/kg/day) and monitor for adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DEFERIPRONE (DEFERIPRONE).

Breastfeeding	Not recommended during breastfeeding. M/P ratio is unknown; deferiprone is excreted in human milk in low concentrations, but potential for iron chelation in the nursing infant exists.
Teratogenic Risk	Pregnancy Category D. In first trimester, there is evidence of fetal harm based on animal studies and human data; deferiprone crosses the placenta and may cause iron depletion in the fetus. In second and third trimesters, risk of fetal iron deficiency anemia and potential teratogenicity persists; use only if benefit outweighs risk.