Class: Chelating agent
- Tablets, oral 500 mg
Orally active chelating agent that has a high affinity for binding with iron.
Rapidly absorbed. T max is approximately 1 to 2 h. Mean C max is 20 mcg/mL, and mean AUC is 53 mcg•h/mL. Administration with food decreases C max by 38% and AUC by 10%.
Protein binding is less than 10%. Vd is approximately 1 to 1.6 L/kg.
Majority of deferiprone is metabolized by UGT1A6. Major metabolite is the 3-O-glucuronide, which lacks iron binding capability.
More than 90% is eliminated from plasma 5 to 6 h after administration; 75% to 90% is excreted in the urine as the metabolite. Elimination half-life is 1.9 h.
Special PopulationsRenal Function Impairment
Not evaluated.Hepatic Function Impairment
Not conclusively evaluated.Elderly
Pharmacokinetics have not been studied in elderly patients.Children
Pharmacokinetics have not been studied in pediatric patients.Gender
Influence of gender has not been established.Race
Influence of race has not been established.Weight
Influence of obesity has not been established.
Indications and Usage
Treatment of transfusional iron overload due to thalassemia syndromes when current chelation therapy is inadequate.
Hypersensitivity to deferiprone or to any of the components of the product.
Dosage and AdministrationAdults
PO Initial dosage is 25 mg/kg 3 times daily. Adjust dose based on patient response and therapeutic goals (maintenance or reduction of body iron burden) up to a max dosage of 33 mg/kg 3 times daily.
- Administer 3 times daily; may take with meals to reduce nausea.
- Round the dose to the nearest 250 mg (half-tablet).
- If the serum ferritin consistently falls below 500 mcg/L, consider temporary interruption of therapy.
- Allow at least a 4 h interval between administration of deferiprone and other medications or supplements containing polyvalent cations (eg, aluminum, iron, zinc).
Store between 59° and 86°F.
Drug InteractionsDrugs associated with neutropenia or agranulocytosis
Avoid concomitant use. However, if this is not possible, closely monitor the absolute neutrophil count (ANC).Polyvalent cations (eg, aluminum, cation-containing antacids, iron, zinc)
Deferiprone has the potential to bind polyvalent cations (eg, iron). Allow at least a 4-hour interval between deferiprone and other medications (eg, antacids) or supplements containing these polyvalent cations.UGT1A6 inhibitors (eg, silymarin [milk thistle])
Coadministration has not been evaluated. Closely monitor for adverse reactions that may require downward dose titration or interruption.
Atrial fibrillation, cardiac failure, hypertension, hypotension (postmarketing).
Headache (3%); bruxism, cerebellar syndrome, cerebral hemorrhage, convulsion, depression, enteroviral encephalitis, gait disturbance, intracranial pressure increased, obsessive-compulsive disorder, psychomotor skills impaired, pyramidal tract syndrome, somnolence (postmarketing).
Cryptococcal cutaneous infection, furuncle, Henoch-Schönlein purpura, hyperhidrosis, photosensitivity reaction, pruritus, pustular rash, rash, subcutaneous abscess, urticaria (postmarketing).
Diplopia, papilledema, periorbital edema, pharyngitis, retinal toxicity (postmarketing).
Nausea (13%); abdominal pain or discomfort, vomiting (10%); diarrhea (3%); dyspepsia (2%); enterocolitis, gastric ulcer, pancreatitis, parotid gland enlargement, rectal hemorrhage (postmarketing).
Chromaturia (15%); glycosuria, hemoglobinuria (postmarketing).
Neutropenia (6%); agranulocytosis (2%); pancytopenia, thrombocytosis (postmarketing).
Hepatomegaly, infectious hepatitis, jaundice (postmarketing).
Anaphylactic shock, hypersensitivity (postmarketing).
Increased ALT (8%); decreased neutrophils (7%); increased AST (1%); increased blood bilirubin, increased blood CPK (postmarketing).
Increased appetite (4%); increased weight (2%); decreased appetite (1%); dehydration, metabolic acidosis, peripheral edema (postmarketing).
Arthralgia (10%); back pain, pain in extremity (2%); arthropathy (1%); chondropathy, myositis, trismus (postmarketing).
Acute respiratory distress syndrome, epistaxis, hemoptysis, pneumonia, pulmonary embolism (postmarketing).
Chills, hypospadias, multiorgan failure, pyrexia, sepsis (postmarketing).
Deferiprone can cause agranulocytosis that can lead to serious infections and death. Neutropenia may precede the development of agranulocytosis. Interrupt therapy if neutropenia or infection develops, and monitor the ANC more frequently. Advise patients to immediately report any symptoms indicative of infection.
Measure serum ferritin concentration every 2 to 3 mo. Measure ANC before starting therapy and weekly during therapy. For ANC less than 1.5 × 10 9 /L and more than 0.5 × 10 9 /L, discontinue therapy and all other medications with a potential to cause neutropenia, and obtain a CBC, including a WBC corrected for the presence of nucleated RBCs, ANC, and platelet count daily until ANC returns to at least 1.5 × 10 9 /L. Monitor serum ALT monthly. Monitor plasma zinc.
Category D . Can cause fetal harm.
Safety and efficacy not established.
Use with caution, usually starting at the low end of the dosage range because of the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.
Henoch-Schönlein purpura, periorbital edema with skin rash, and urticaria have been reported.
Laboratory Test Abnormalities
Elevations in ALT and AST and decreases in zinc concentrations may occur. Consider interruption of therapy if increased serum transaminase levels persist.
A thorough QT study has not been conducted, but 1 patient with a history of QT prolongation experienced torsades de pointes during therapy. Use with caution in patients at increased risk of QT prolongation.
With long-term overdose, axial hypotonia, cerebellar symptoms, diplopia, hand movements, lateral nystagmus, and psychomotor slowdown may occur.
- Advise patient to read the Medication Guide prior to first use and to reread it with each refill.
- Inform patients of the risks of developing agranulocytosis and instruct them to immediately interrupt therapy and report to their health care provider if they experience symptoms of infection (eg, fever, flu-like symptoms, sore throat).
- Advise patients that the amount of deferiprone prescribed is based on body weight and on the therapeutic goal (reduction or stabilization of body iron load).
- Advise patients to take the first dose in the morning, the second dose at midday, and the third dose in the evening. Inform patients that taking deferiprone with meals may reduce nausea.
- Instruct patients that if a dose is missed, they should take it as soon as possible. If it is almost time for the next dose, advise the patient to skip the missed dose and resume their regular dosing schedule. Inform patients not to double doses.
- Inform patients that their urine may show a reddish/brown discoloration. Advise patients that this is a very common sign of the desired effect and is not harmful.
- Counsel women of reproductive potential to avoid pregnancy while taking deferiprone and to immediately notify their health care provider if they become pregnant or plan to become pregnant.
- Inform patients that they should not breast-feed during therapy.
- Inform patients to immediately seek medical attention if they experience dizziness, light-headedness, palpitations, seizures, or syncope.
Copyright © 2009 Wolters Kluwer Health.
More about deferiprone
- Other brands: Ferriprox