Deferoxamine

It is indicated for the treatment of acute iron intoxication and of chronic iron overload due to transfusion-dependent anemias.

Iron-chelating agent

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.

Acute Iron Intoxication Intramuscular Administration This route is preferred and should be used for ALL PATIENTS NOT IN SHOCK. A dose of 1000 mg should be administered initially. This may be followed by 500 mg every 4 hours for two doses. Depending upon the clinical response, subsequent doses of 500 mg may be administered every 4-12 hours. The total amount administered should not exceed 6000 mg in 24 hours. For reconstitution instructions for intramuscular administration see Table 1. Intravenous Administration THIS ROUTE SHOULD BE USED ONLY FOR PATIENTS IN A STATE OF CARDIOVASCULAR COLLAPSE AND THEN ONLY BY SLOW INFUSION. THE RATE OF INFUSION SHOULD NOT EXCEED 15 MG/KG/HR FOR THE FIRST 1000 MG ADMINISTERED. SUBSEQUENT IV DOSING, IF NEEDED, MUST BE AT A SLOWER RATE, NOT TO EXCEED 125 MG/HR. For reconstitution instructions for intravenous administration see Table 2. The reconstituted solution is added to physiologic saline, (e.g., 0.9% sodium chloride, 0.45% sodium chloride), glucose in water, or Ringer?s lactate solution. An initial dose of 1000 mg should be administered at a rate NOT TO EXCEED 15 mg/kg/hr. This may be followed by 500 mg over 4 hours for two doses. Depending upon the clinical response, subsequent doses of 500 mg may be administered over 4-12 hours. The total amount administered should not exceed 6000 mg in 24 hours. As soon as the clinical condition of the patient permits, intravenous administration should be discontinued and the drug should be administered intramuscularly. Chronic Iron Overload Subcutaneous Administration A daily dose of 1000-2000 mg (20-40 mg/kg/day) should be administered over 8-24 hours, utilizing a small portable pump capable of providing continuous mini-infusion. The duration of infusion must be individualized. In some patients, as much iron will be excreted after a short infusion of 8-12 hours as with the same dose given over 24 hours. For reconstitution instructions for subcutaneous administration see Table 3. Intravenous Administration The standard recommended method of it administration is via slow subcutaneous infusion over 8-12 hours. In patients with intravenous access, the daily dose of it can be administered intravenously. The standard dose is 20-40 mg/kg/day for children and 40-50 mg/kg/day over 8-12 hours in adults for 5-7 days per week. In children, average doses should not exceed 40 mg/kg/day until growth has ceased. In adults, average doses should not exceed 60 mg/kg/day. The intravenous infusion rate should not exceed 15 mg/kg/hour. For reconstitution instructions for intravenous administration see Table 2. In patients who are poorly compliant, it may be administered prior to or following same day blood transfusion (for example 1 gram over 4 hours on the day of transfusion); however, the contribution of this mode of administration to iron balance is limited. it should not be administered concurrently with the blood transfusion as this can lead to errors in interpreting side effects such as rash, anaphylaxis and hypotension. Intramuscular Administration A daily dose of 500-1000 mg may be administered intramuscularly. The total daily dose should not exceed 1000 mg

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.

Known hypersensitivity to the active substance. it is contraindicated in patients with severe renal disease or anuria, since the drug and the iron chelate are excreted primarily by the kidney

At the Injection Site: Localized irritation, pain, burning, swelling, induration, infiltration, pruritus, erythema, wheal formation, eschar, crust, vesicles, local edema. Injection site reactions may be associated with systemic allergic reactions (see Body as a Whole, below). Hypersensitivity Reactions and Systemic Allergic Reactions: Generalized rash, urticaria, anaphylactic reaction with or without shock, angioedema Body as a Whole: Local injection site reactions may be accompanied by systemic reactions like arthralgia, fever, headache, myalgia, nausea, vomiting, abdominal pain, or asthma.

There are no adequate and well-controlled studies in pregnant women. it should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Nursing Mothers It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when it is administered to a nursing woman.

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

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

Deferoxamine mesylate (500 mg vials): Each 7.5 ml vial of white to practically white sterile lyophilized powder contains the medicinal ingredient deferoxamine mesylate (500 mg) for injection without non-medicinal ingredients. Available in cartons of 10 vials.