Deferoxamine Mesylate

Deferoxamine Mesylate is indicated for:

• Acute iron intoxication.
• Chronic iron overload due to transfusion-dependent anemias.
• Diagnosis of aluminum overload (deferoxamine mesylate) infusion test.
• Chronic aluminum overload in patients with End-Stage Renal Failure (ESRF) under maintenance dialysis.

Deferoxamine works in treating iron toxicity by binding trivalent (ferric) iron (for which it has a strong affinity), forming ferrioxamine, a stable complex which is eliminated via the kidneys. 100 mg of deferoxamine is capable of binding approximately 8.5 mg of trivalent (ferric) iron. Deferoxamine works in treating aluminum toxicity by binding to tissue-bound aluminum to form aluminoxamine, a stable, water-soluble complex. The formation of aluminoxamine increases blood concentrations of aluminum, resulting in an increased concentration gradient between the blood and dialysate, boosting the removal of aluminum during dialysis. 100 mg of deferoxamine is capable of binding approximately 4.1 mg of aluminum.

Deferoxamine mesylate should only be given parenterally. The dose should not exceed 6.0 grams in a twenty-four hour period. Although Deferoxamine can be given by intramuscular injection, in most cases it exerts a considerably greater effect when administered by continuous infusion either intravenously (especially in cases of acute iron intoxication) or subcutaneously (especially in patients with chronic iron overload).

Rapid intravenous injection of Deferoxamine exceeding 15 mg/kg/h has produced flushing of the skin, urticaria, hypotension and shock

Concomitant use of Prochlorperazine: Concurrent treatment with Deferoxamine and prochlorperazine, a phenothiazine derivative, may lead to temporary impairment of consciousness.

Concomitant use of Vitamin C: Where an iron-overload is associated with ascorbic acid deficiency, oral administration of Vitamin C in the standard dosage (150 - 250 mg daily) may serve to enhance excretion of the iron complex in response to Deferoxamine. Larger doses of Vitamin C fail to produce an additional effect.

Concomitant use of Erythropoietin: There is evidence that aluminum intoxication causes reduced erythropoiesis. In dialysis patients with iron and/or aluminum overload receiving Deferoxamine and erythropoietin, it is important to adjust the dosage of the latter when necessary. Regular monitoring of iron stores should also be conducted.

Patients who are hypersensitive to deferoxamine mesylate or component of the container, except where desensitization is successful.

Pregnant Women: There are no adequate and well-controlled studies conducted in pregnant women.Studies in animals (rabbits) have shown reproductive toxicity. The risk to the fetus/mother is unknown. Women of childbearing potential with chronic iron and/or aluminum overload should not receive deferoxamine 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 should only be used if the hazard of acute iron intoxication is considered to be greater than the potential teratogenic hazard of deferoxamine.

Nursing Women: 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.

Therapy with Deferoxamine should be initiated and maintained by physician 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). As with all medicines, Deferoxamine should be kept out of reach of children. Rapid intravenous injection of Deferoxamine 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 with high doses of vitamin C (more than 500 mg daily)

Since Ddeferoxamine mesylate is available only for parenteral administration, acute intoxication is unlikely to occur.

Carboxylic acids and derivatives

Store between 15-25 °C. Do not store above 25°C.