Desferal, deferoxamine mesylate USP, is an iron-chelating agent, available in vials for intramuscular, subcutaneous, and intravenous administration. Desferal is supplied as vials containing 500 mg and 2 g of deferoxamine mesylate USP in sterile, lyophilized form. Deferoxamine mesylate is N-[5-[3-[(5-aminopentyl)hydroxycarbamoyl]propionamido]pentyl]-3-[[5-(N hydroxyacetamido)pentyl]carbamoyl]propionohydroxamic acid monomethanesul-fonate (salt)
deferoxamine mesilate; deferoxamine methanesulfonate; desferal; desferal mesylate; desferal methanesulfonate; desferrioxamine B mesylate; desferrioxamine B methane sulfonate; desferrioxamine methanesulfonate
Molecular formula: C25H48N6O8•CH4O3S Molecular weight: 656.8 Melting point: 148-149 °C The log of the formation constant (K) of deferoxamine complexed with ferric ion (Fe+3) is 30.6
Pharmacologic: heavy metal antagonists
Deferoxamine Mesylate for Injection is indicated for:
• Acute iron intoxication.
• Chronic iron overload due to transfusion-dependent anemias.
• Diagnosis of aluminum overload (deferoxamine infusion test).
• Chronic aluminum overload in patients with End-Stage Renal Failure (ESRF) under maintenance dialysis.
In cases of acute iron intoxication, Deferoxamine Mesylate for Injection is an adjunct to, and not a substitute for, standard therapeutic measures which may include:
• Induction of emesis.
• Gastric lavage.
• Maintenance of clear airways.
• Control of peripheral vascular failure.
• Correction of acidosis.
Warning and precautions
Therapy with Deferoxamine Mesylate for Injection should be initiated and maintained by physicians experienced in the treatment of chronic iron overload due to blood transfusions. It should be noted that some of the signs and symptoms reported as adverse effects may in fact be manifestations of the underlying disease (iron and/or aluminum overload).
Concomitant use of Prochlorperazine Concurrent treatment with Deferoxamine Mesylate for Injection and prochlorperazine, a phenothiazine derivative, may lead to temporary impairment of consciousness.
As with all medicines, Deferoxamine Mesylate for Injection should be kept out of reach of children. Rapid intravenous injection of Deferoxamine Mesylate for Injection exceeding 15 mg/kg/h has produced flushing of the skin, urticaria, hypotension and shock Vitamin C supplements should not be given to patients with cardiac failure because impairment of cardiac function may be experienced in patients with severe chronic iron overload receiving combined treatment of Deferoxamine Mesylate for Injection with high doses of vitamin C (more than 500 mg daily)
There are no adequate and well-controlled studies in pregnant women. Studies in animals (rabbits) have shown reproductive toxicity/teratogenicity. The risk to the fetus/mother is unknown.
Women of childbearing potential with chronic iron and/or aluminum overload should not receive Deferoxamine Mesylate for Injection unless the use of an effective form of contraception, established before treatment, is continued throughout treatment and for at least the first month after treatment.
During pregnancy, particularly in the first trimester, Deferoxamine Mesylate for Injection should only be used if the hazard of acute iron intoxication is considered to be greater than the potential teratogenic hazard of Deferoxamine Mesylate for Injection.
It is not known whether deferoxamine mesylate passes into the breast milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse drug reactions in breast-fed newborns/infants, a decision should be made whether to abstain from breast-feeding or to abstain from using the medicinal product, taking into account the importance of the medicinal product to the mother.
Acute Iron Ingestion IM, IV (Adults and Children 3 years and above): 1 g, then 500 mg q 4 hr for 2 doses. Additional doses of 500 mg q 4–12 hr may be needed (not to exceed 6 g/24 hr).
Chronic Iron Overload IM, IV (Adults and Children 3 years and above): 500 mg–1 g daily IM; additional doses of 2 g should be given IV for each unit of blood transfused (not to exceed 1 g/day in absence of transfusions; 6 g/day if patient receives transfusions). Subcut (Adults and Children 3 years and above): 1–2 g/day (20–40 mg/kg/day) infused over 8–24 hr.