Transfusion-Induced Iron Overload Medication

Updated: May 07, 2021
  • Author: Geneva E Guarin, MD, MBA; Chief Editor: Emmanuel C Besa, MD  more...
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Medication

Medication Summary

The goals of pharmacotherapy in cases of transfusion-induced iron overload are to protect tissues from damage caused by iron, decrease plasma and cytosolic levels of reactive labile iron to normal, and rid the body of all excess iron, thereby preserving organ function. [13]  Three iron-chelating agents are available: deferoxamine, deferasirox, and deferiprone.

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Chelating Agents

Class Summary

Chelating agents help reduce iron levels in the body by promoting the excretion of chelated iron.

Deferoxamine (Desferal mesylate)

The drug is siderophore (iron-binder) derived from the bacterium Streptomyces pilosus.

It is usually administered as a slow SC infusion through a portable pump. It is freely soluble in water. Approximately 8 mg of iron is bound by 100 mg of deferoxamine, forming a 1:1 hexadentate complex. Its half-life is 20-30 minutes.

Promotes renal and hepatic excretion in urine and bile in feces. Gives urine a red discoloration. Readily chelates iron from ferritin and hemosiderin but not from transferrin. Does not affect iron in the cytochromes or hemoglobin. Most effective when provided to the circulation continuously by infusion. Helps prevent damage to the liver and bone marrow from iron deposition.

May be administered either by IM injection or by slow IV infusion. 

The starting dose in individuals without iron-induced cardiac dysfunction is 30 mg/kg daily infused over 8 to 12 hours, five days per week. Dosing an be changed by 5 to 10 mg every three to six months depending on transfusion burden and iron status of the patient.

Does not effectively chelate other trace metals of nutritional importance. Provided in vials containing 500 mg of lyophilized sterile drug. Two mL of sterile water for injection should be added to each vial, bringing the concentration to 250 mg/mL. For IV use, this may be diluted in 0.9% sterile saline, 5% dextrose solution, or Ringer solution.

Deferasirox (Exjade tablets)

Tablets for oral suspension. Oral iron chelation agent that is demonstrated to reduce the liver iron concentration in adults and children who receive repeated RBC transfusions. Binds iron with high affinity in a 2:1 ratio (tridentate complex). Approved to treat chronic iron overload due to multiple blood transfusions.

Treatment initiation is recommended with evidence of chronic iron overload (ie, transfusion of about 100 mL/kg packed RBCs [about 20 U for a 40-kg person] and a serum ferritin level consistently >1000 mcg/L). 

The dose for deferasirox is 20 mg/kg/day orally once daily, and then increased by 5 to 10 mg every three to six months based on levels of iron stores. 

 

Deferiprone (Ferriprox)

1,2 dimethyl-3-hydroxypyridine-4-one is a member of a family of hydroxypyridine-4-one (HPO) chelators that requires 3 molecules to fully bind iron (III), each molecule providing 2 coordination sites (bidentate chelation). Half-life is approximately 2 hours. Inactive metabolite is predominantly excreted in urine. It is indicated for adults and children aged 3 years and older with iron overload from transfusion for thalassemia syndromes, sickle cell disease, or other anemias. Available as tablets and oral solution.  

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