DEFEROXAMINE MESYLATE- deferoxamine mesylate injection, powder, lyophilized, for solution
Hospira, Inc.
Fliptop Vials
For subcutaneous, intramuscular or intravenous administration.
DESCRIPTION
Deferoxamine Mesylate for Injection, USP, is an iron-chelating agent, available in vials for intramuscular, subcutaneous, and intravenous administration. Deferoxamine mesylate 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 monomethanesulfonate (salt), and its structural formula is:
structural formula deferoxamine mesylate
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Deferoxamine mesylate USP is a white to off-white powder. It is freely soluble in water and slightly soluble in methanol. Its molecular weight is 656.79. The molecular formula is C25 H48 N6 O8 � CH4 O3 S.
CLINICAL PHARMACOLOGY
Deferoxamine mesylate chelates iron by forming a stable complex that prevents the iron from entering into further chemical reactions. It readily chelates iron from ferritin and hemosiderin but not readily from transferrin; it does not combine with the iron from cytochromes and hemoglobin. Deferoxamine mesylate does not cause any demonstrable increase in the excretion of electrolytes or trace metals. Theoretically, 100 parts by weight of deferoxamine mesylate is capable of binding approximately 8.5 parts by weight of ferric iron.
Deferoxamine mesylate is metabolized principally by plasma enzymes, but the pathways have not yet been defined. The chelate is readily soluble in water and passes easily through the kidney, giving the urine a characteristic reddish color. Some is also excreted in the feces via the bile.
INDICATIONS AND USAGE
Deferoxamine Mesylate for Injection, USP is indicated for the treatment of acute iron intoxication and of chronic iron overload due to transfusion-dependent anemias.
Acute Iron Intoxication
Deferoxamine mesylate is an adjunct to, and not a substitute for, standard measures used in treating acute iron intoxication, which may include the following: induction of emesis with syrup of ipecac; gastric lavage; suction and maintenance of a clear airway; control of shock with intravenous fluids, blood, oxygen, and vasopressors; and correction of acidosis.
Chronic Iron Overload
Deferoxamine mesylate can promote iron excretion in patients with secondary iron overload from multiple transfusions (as may occur in the treatment of some chronic anemias, including thalassemia). Long-term therapy with deferoxamine mesylate slows accumulation of hepatic iron and retards or eliminates progression of hepatic fibrosis.
Iron mobilization with deferoxamine mesylate is relatively poor in patients under the age of 3 years with relatively little iron overload. The drug should ordinarily not be given to such patients unless significant iron mobilization (e.g., 1 mg or more of iron per day) can be demonstrated.
Deferoxamine mesylate is not indicated for the treatment of primary hemochromatosis, since phlebotomy is the method of choice for removing excess iron in this disorder.
