An oral iron chelating agent.
Trade name Ferripox.
With up to 100 mg daily, divided into three doses iron excretion of up to 0.6 mg per kilogram of body weight per day can be achieved, compared with an estimated mean daily iron intake of 0.3 to 0.5 mg per kilogram per day from blood transfusions in patients with thalassemia major.
Rapidly absorbed, with the peak blood level at about 45 minutes after ingestion.
Food slows absorption but does not reduce the amount of drug absorbed.
The drug is cleared for the blood with 85% conversion to a glucoronide which is capable of binding iron.
The amount of iron chelated is related mainly to the speed of glucoronidation.
Non-transferrin bound Iron is taken up inappropriately by highly vascular organs such as the liver, heart, pancreas, leading to elevated levels of intracellular iron, with non–transf2242ing-bound iron gaining intracellular access through iron permeases.
Deferiprone rapidly scavenges iron from non-transf2242in-bound iron.
Removes iron from the reticuloendothelial system.
The deferiprone-iron complex is excreted in the urine.
Approximately 4% of the single-dose is excreted as the complex in patients with a heavy iron load.
Side effects include: nausea, abdominal pain, vomiting, transit rise in liver enzymes, arthropathy, neutropenia, agranulocytosis, and zinc deficiency in patients with diabetes.
About 5-10% of patients discontinue the drug prematurely because of side effects.
Agranulocytosis is the most serious side effect and is seen in three times as frequent in females as in males (2.4% versus 0.8%).
Neutropenia occurs four times as frequently as agranulocytosis.
Available as 0.5 g or 1 g tablets, and the liquid formulation of 100 mg/mL.
Treatment is usually initiated at 75 mg per kilogram per day divided into three doses given at 8 hour intervals.
Doses can be increased to a maximum total dose of 100 mg per kilogram per day to achieve greater efficacy.
Studies have shown its superiority as compared with subcutaneous desferoxamine 5 to 7 days a week reducing cardiac iron levels and improving cardiac function.
A metaanalysis of 15 randomized controlled trials showed that deferiprone is more efficacious than deferoxamine for improving cardiac ejection fraction and also endocrine dysfunction
Compared to desferoxamine it is more efficacious improving cardiac ejection fraction and endocrine dysfunction.
Cardiac morbidity and mortality are substantially lower among patients treated with deferiprone than those receiving different desferoxamine.
Intermittent administration of desferoxamine extracts about 1-2% of cardiac iron each month, whereas desferoxamine with daily deferiprone increases the extraction to 3 to 4%, the drug combination can reverse in the endocrine complications, including diabetes.
Combination therapy with deferiprone and deferoxamine is effective in reversing cardiac iron overload and impaired ventricular cardiac function.