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Deferoxamine (Deferoxamine Mesylate) - Description and Clinical Pharmacology

 
 



Fliptop Vials

For subcutaneous, intramuscular or intravenous administration.

Rx only

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:

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 C25H48N6O8 • CH4O3S.

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.

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