DESFERAL
Clinical safety rating
cautionComprehensive clinical and safety monograph for DESFERAL (DESFERAL).
Deferoxamine is an iron-chelating agent that binds ferric iron forming ferrioxamine, a stable complex that is excreted renally, reducing iron accumulation in tissues.
| Metabolism | Deferoxamine is metabolized primarily in the liver via oxidative deamination to two major metabolites: an acid-degradation product and a neutral compound. The exact enzymes are not well-defined but likely involve hepatic oxidases. |
| Excretion | Renal: approximately 40-60% of absorbed dose excreted in urine as unchanged drug and iron complex; biliary/fecal: minor route, <5%. |
| Half-life | Terminal elimination half-life: 6-12 hours (prolonged in iron overload, up to 20-30 hours with large doses; clinical context: supports subcutaneous infusion over 8-12 hours for chronic chelation). |
| Protein binding | ~10-20% bound to plasma proteins; primarily albumin and transferrin (minimal due to low affinity). |
| Volume of Distribution | Dry weight: 1.5-2.0 L/kg (indicates extensive distribution into extracellular fluid and tissues; increased in iron overload due to iron stores). |
| Bioavailability | Subcutaneous: ~80-90% (injectable only; oral bioavailability negligible, <5%). |
| Onset of Action | Subcutaneous/intramuscular: 30-60 minutes to peak serum iron chelation; intravenous: immediate (minutes) urinary iron excretion. |
| Duration of Action | Duration: 6-8 hours after single dose; continuous infusion (e.g., 8-24 hours) maintains chelation; clinical note: effect persists until drug is eliminated and iron complex excreted. |
| Molecular Weight | 656.79 |
| Action Class | Iron chelating agents |
Acute iron poisoning: 1 g IM, then 0.5 g IM every 4-12 hours; max 6 g/day. Chronic iron overload: 0.5-1 g IM daily; also IV/SC 20-40 mg/kg/day over 8-24 hours.
| Dosage form | INJECTABLE |
| Renal impairment | GFR >60 mL/min: no adjustment; GFR 10-60: reduce dose by 50%; GFR <10: avoid use or use with extreme caution. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25-50%; Child-Pugh C: avoid use. |
| Pediatric use | Acute poisoning: 15 mg/kg/h IV initially, max 6 g/24h; acute chronic overload: 20-40 mg/kg/day SC/IV over 8-24h. |
| Geriatric use | Start at lower end of dosing range due to potential renal impairment; monitor renal function and iron levels. |
| 1st trimester | Deferoxamine is teratogenic in animals; limited human data. Use only if clearly needed and no safer alternative. |
| 2nd trimester | May be used if benefit outweighs risk. Monitor iron levels. |
| 3rd trimester | May be used if benefit outweighs risk. Avoid near term due to potential maternal hypotension. |
Clinical note
Comprehensive clinical and safety monograph for DESFERAL (DESFERAL).
| Placental transfer | Crosses placenta; limited data on degree. |
| Breastfeeding | Excreted into breast milk in low amounts; unlikely to harm infant due to poor oral absorption. However, consider deferring breastfeeding if maternal iron overload is severe. |
| Lactation Rating | L3 |
| Teratogenic Risk | FDA Category C. First trimester: Animal studies show fetal abnormalities, but no adequate human studies. Second/Third trimesters: Avoid unless essential; deferoxamine crosses placenta and may cause fetal skeletal anomalies, anemia, and growth restriction at high doses. |
| Fetal Monitoring | Maternal: renal function, audiometry, ophthalmic exams, serum ferritin, iron levels, growth velocity in children. Fetal: ultrasound for growth restriction and skeletal anomalies, amniotic fluid assessment. |
| Fertility Effects | May cause reversible ovarian and testicular dysfunction; associated with delayed puberty and reduced fertility in chronic use. Discontinuation may restore fertility. |
■ FDA Black Box Warning
None
| Serious Effects |
Severe renal impairment (anuria)History of hypersensitivity to deferoxamine
| Precautions | Hypersensitivity reactions including anaphylaxis, urticaria, and angioedema, Ocular toxicity (cataracts, decreased visual acuity, retinal damage) with high doses or prolonged therapy, Auditory toxicity (tinnitus, sensorineural hearing loss) especially at high doses, Renal impairment may reduce drug clearance; monitor renal function, Growth retardation in children with long-term use, Increased risk of infections, particularly Yersinia enterocolitica and Mucorales fungi, Severe neurotoxicity including seizures, coma, and encephalopathy, especially with rapid intravenous administration, Acute respiratory distress syndrome (ARDS) reported with rapid IV infusion |
| Food/Dietary | Avoid high-iron foods (e.g., red meat, liver, fortified cereals) during therapy. Do not take with vitamin C supplements as they may increase iron absorption and toxicity. No significant food interaction except iron-containing foods/supplements. |
| Clinical Pearls | Administer IM or IV, but avoid rapid IV infusion to prevent hypotension. Monitor urine color for reddish hue indicating iron excretion. For acute iron poisoning, check serum iron and total iron-binding capacity (TIBC); chelation is indicated if serum iron exceeds TIBC or >350 mcg/dL. Use test dose (50 mg/kg) if uncertain of iron overload. Avoid in severe renal failure unless dialysis is available due to desferrioxamine-iron complex excretion. Can cause Yersinia enterocolitica infection; discontinue if fever or diarrhea develops. |
| Patient Advice | Take this medication exactly as prescribed; it is given by injection under the skin, into a muscle, or into a vein. · Your urine may turn a reddish-brown color during treatment; this is normal and indicates iron excretion. · Report any signs of infection such as fever, sore throat, or diarrhea immediately. · Avoid alcohol and large amounts of vitamin C unless approved by your doctor, as they can affect iron removal. · Stay hydrated; drink plenty of fluids unless instructed otherwise. · Do not take any iron supplements or multivitamins containing iron without consulting your healthcare provider. · If you miss a dose, contact your doctor for instructions; do not double the dose. |
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