DESFERAL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DESFERAL (DESFERAL).

How it works

Deferoxamine is an iron-chelating agent that binds ferric iron forming ferrioxamine, a stable complex that is excreted renally, reducing iron accumulation in tissues.

What the body does with it

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.

Classification & Brands

Action Class

Iron chelating agents

Dosing & administration

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.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DESFERAL (DESFERAL).

Breastfeeding	Excreted into breast milk in low levels; M/P ratio unknown. Use with caution, especially in infants with iron overload; consider risk of maternal iron deficiency. Monitor infant for gastrointestinal effects.
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

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Severe renal disease or anuria (as drug is excreted renally)","Hypersensitivity to deferoxamine or any component of the formulation","Primary hemochromatosis with mild iron overload (prefer phlebotomy)"]

Clinical Precautions

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"]

Clinical Tips & Counseling

Drug interactions

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DESFERAL

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DESFERAL (DESFERAL).

How it works

Deferoxamine is an iron-chelating agent that binds ferric iron forming ferrioxamine, a stable complex that is excreted renally, reducing iron accumulation in tissues.

What the body does with it

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.

Classification & Brands

Action Class

Iron chelating agents

Dosing & administration

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.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DESFERAL (DESFERAL).

Breastfeeding	Excreted into breast milk in low levels; M/P ratio unknown. Use with caution, especially in infants with iron overload; consider risk of maternal iron deficiency. Monitor infant for gastrointestinal effects.
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

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

Clinical Precautions

Precautions

Clinical Tips & Counseling

Drug interactions

Loading safety data…