Products
Deferiprone is commercially available in the form of film-coated tablets (Ferriprox, generic). It was approved in many countries in 2001.
Structure and properties
Deferiprone, or 3-hydroxy-1,2-dimethylpyridin-4-one (C7H9NO2, Mr = 139.2 g/mol) is a methylated and hydroxylated pyridinone derivative. It belongs to the α-ketohydroxypyridones. Deferiprone exists as a white to pink crystalline powder that is sparingly soluble in water.
Effects
Deferiprone (ATC V03AC02) is a bidentate ligand that binds iron (Fe3+) in a 3:1 ratio. It promotes the excretion of iron primarily through the urine, thus counteracting iron overload. It binds other metal ions such as copper, aluminum, and zinc to a lesser extent. Unlike deferoxamine, deferiprone can be administered perorally and no infusion is necessary.
Indications
As a second-line agent for the treatment of iron overload in patients with thalassemia major (thalassemia, a disease of red blood cells).
Dosage
According to the SmPC. Tablets are usually taken three times daily and preferably fasting. Dosage is based on body weight.
Contraindications
- Hypersensitivity
- Recurrent neutropenia episodes or agranulocytosis in patient history.
- Concurrent administration of drugs that may cause neutropenia or agranulocytosis.
- Pregnancy and lactation, women of childbearing age without safe contraceptive measures.
Full precautions can be found in the drug label.
Interactions
Deferiprone is conjugated by UGT1A6. Drug-drug interactions have been described with antacids, sucralfate, polyvalent cations, and vitamin C. Deferiprone should not be administered with drugs that may cause neutropenia or agranulocytosis.
Adverse Effects
The most common possible adverse effects include nausea, vomiting, and abdominal pain. The iron-deferiprone complex discolors urine to a reddish brown. Deferiprone may cause neutropenia and agranulocytosis in rare cases, posing a risk for the development of life-threatening infectious diseases.
