FERRIPROX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FERRIPROX (FERRIPROX).
Deferiprone is an iron chelator that forms a stable complex with ferric iron (Fe3+), promoting its excretion primarily in urine. It reduces iron overload in tissues and prevents organ damage from excess iron.
| Metabolism | Primarily metabolized via glucuronidation; major metabolite is 3-O-glucuronide. CYP450 involvement is minimal. |
| Excretion | Renal: approximately 85% as unchanged drug and metabolites (mainly glucuronide conjugate); fecal: <5% |
| Half-life | Terminal elimination half-life is approximately 2.5 to 4 hours; clinical context: requires thrice-daily dosing to maintain therapeutic chelation |
| Protein binding | Approximately 5-10% bound to plasma proteins (mainly albumin) |
| Volume of Distribution | Approximately 1.3 L/kg, indicating extensive distribution into tissues; reflects ability to chelate intracellular and extracellular iron |
| Bioavailability | Oral: ~75% (with moderate interindividual variability); not administered parenterally |
| Onset of Action | Oral: ~1-2 hours for serum iron reduction; clinical effect on iron mobilization observed within hours |
| Duration of Action | Chelation effect persists for 4-6 hours after an oral dose; necessitates t.i.d. dosing for continuous iron removal |
25 mg/kg orally three times daily, not to exceed 100 mg/kg/day.
| Dosage form | TABLET |
| Renal impairment | For GFR 50-90 mL/min: no adjustment. For GFR <50 mL/min: contraindicated. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B or C: contraindicated. |
| Pediatric use | For children ≥2 years: 25 mg/kg orally three times daily; for children <2 years: safety not established. |
| Geriatric use | No specific adjustment recommended; monitor renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FERRIPROX (FERRIPROX).
| Breastfeeding | It is not known whether deferiprone is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from FERRIPROX, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. M/P ratio not available. |
| Teratogenic Risk | Pregnancy Category D. There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans. In animal studies, deferiprone was teratogenic in rats and rabbits. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. First trimester: Avoid if possible. Second and third trimesters: Use only if clearly needed. |
■ FDA Black Box Warning
FERRIPROX can cause agranulocytosis, which may be life-threatening. Neutrophil counts must be monitored weekly during therapy. Interrupt therapy if infection develops or neutrophil count falls below 1500/µL.
| Serious Effects |
["Hypersensitivity to deferiprone or any ingredient","History of agranulocytosis due to deferiprone","Current neutropenia (absolute neutrophil count <1500/µL)"]
| Precautions | ["Agranulocytosis/neutropenia: Monitor neutrophil count weekly; withhold if infection develops.","Increased liver enzymes: Monitor ALT/AST monthly; consider dose reduction if elevations persist.","Zinc deficiency: Monitor zinc levels periodically; supplement if necessary.","Arthropathy: Joint pain/swelling may occur; discontinue if severe.","Carcinogenicity: Long-term carcinogenic risk unknown."] |
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| Fetal Monitoring | Monitor serum ferritin levels every 2-3 months to assess iron burden. Monitor absolute neutrophil count (ANC) weekly due to risk of agranulocytosis. Monitor liver function tests and serum iron levels. In pregnant women, additional obstetric monitoring including fetal growth ultrasound may be warranted. Monitor for signs of infection. |
| Fertility Effects | In animal studies, deferiprone caused decreased fertility in male rats at doses comparable to human exposure. In humans, no specific studies on fertility have been conducted; however, cases of oligospermia and azoospermia have been reported with deferiprone use. Reversible upon discontinuation. |