DEFEROXAMINE MESYLATE

Clinical safety rating: safe

Animal studies have demonstrated safety

How it works

Deferoxamine chelates iron by forming a stable complex (ferrioxamine) that is excreted renally, preventing iron from catalyzing free radical formation and reducing tissue damage.

What the body does with it

Metabolism	Primarily metabolized via enzymatic pathways (oxidation and glucuronidation) in the liver; undergoes enterohepatic recirculation.
Excretion	Primarily renal; within 24 hours, approximately 50% of an intramuscular dose is excreted as unchanged drug and 20% as ferrioxamine (the iron chelate). Biliary excretion is minor (<10%).
Half-life	Terminal elimination half-life is approximately 5-6 hours for the parent drug after IM or IV administration. The half-life of ferrioxamine is about 6 hours. Clinical context: repeated dosing may be needed for sustained chelation.
Protein binding	Minimal (<10%); weakly bound to plasma proteins, mainly albumin.
Volume of Distribution	Approximately 0.4-0.6 L/kg; indicates distribution primarily into extracellular fluid.
Bioavailability	Subcutaneous: approximately 80-90% relative to IM; Oral: negligible (<5% absorbed).
Onset of Action	IM: within 30 minutes; IV: immediate; Subcutaneous: 1-2 hours.
Duration of Action	IM/IV: 6-8 hours; Subcutaneous: 8-12 hours with continuous infusion. Clinical note: continuous infusion provides sustained chelation.

Classification & Brands

Dosing & administration

For acute iron intoxication: 1 g intramuscularly initially, then 0.5 g every 4 hours for 2 doses, then 0.5 g every 4-12 hours up to a maximum of 6 g/day. For chronic iron overload: 20-40 mg/kg/day subcutaneously over 8-12 hours via infusion pump, or 1-2 g intravenously over 8-24 hours.

Dosage form	INJECTABLE
Renal impairment	No specific GFR-based dosing guidelines; caution advised in severe renal impairment due to potential accumulation.
Liver impairment	No Child-Pugh based dose adjustments defined; use with caution in severe hepatic impairment.
Pediatric use	Same as adult dosing based on body weight. For acute iron poisoning: 15 mg/kg/hour intravenously, maximum 6 g/day. For chronic overload: 20-40 mg/kg/day subcutaneously.
Geriatric use	No specific adjustments; start at lower end of dosing range due to potential renal function decline.

Use during pregnancy

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

Clinical note

Prochlorperazine may cause loss of consciousness Can cause ocular and auditory toxicity with prolonged use.

Breastfeeding	Deferoxamine is excreted into breast milk in small amounts; M/P ratio unknown. Due to potential for adverse effects in the nursing infant (e.g., iron deficiency), caution is advised. Manufacturer recommends discontinuing breastfeeding or drug based on importance.
Teratogenic Risk	Animal studies have shown embryotoxicity and skeletal abnormalities at high doses. Limited human data in first trimester; iron chelation during pregnancy is generally avoided due to potential fetal harm. In second and third trimesters, deferoxamine may be used for acute iron poisoning or severe iron overload, with caution. Risk cannot be excluded.

Warnings & precautions

■ FDA Black Box Warning

Risk of serious allergic reactions (including anaphylaxis), hypotension, and pulmonary toxicity (including adult respiratory distress syndrome) have been reported. Use with caution in patients with impaired renal function.

Side Effect Profile

Common Effects	Hypotension
Serious Effects

Absolute Contraindications

Hypersensitivity to deferoxamine, severe renal failure, anuria.

Clinical Precautions

Precautions

Monitor for ocular and auditory toxicity (high frequency hearing loss, visual disturbances), growth retardation in children, acute respiratory distress syndrome (especially with high doses), infections (Yersinia, Mucor), and renal impairment.

Clinical Tips & Counseling

Drug interactions

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