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Deferiprone

Pronunciation

(de FER i prone)

Index Terms

  • APO-066

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Oral:

Ferriprox: 100 mg/mL (500 mL) [contains fd&c yellow #6 (sunset yellow); cherry-peppermint flavor]

Tablet, Oral:

Ferriprox: 500 mg [scored]

Brand Names: U.S.

  • Ferriprox

Pharmacologic Category

  • Chelating Agent

Pharmacology

Iron-chelating agent with affinity for ferric ion (iron III); binds to ferric ion and forms a 3:1 (deferiprone:iron) complex which is excreted in the urine. Has a lower affinity for other metals such as copper, aluminum, and zinc.

Absorption

Rapid

Distribution

1.6 L/kg (in thalassemia patients)

Metabolism

Primarily by UGT 1A6; major metabolite (3-O-glucuronide) lacks iron-binding capacity

Excretion

Urine (75% to 90%; primarily as metabolite)

Time to Peak

~1-2 hours

Half-Life Elimination

~2 hours

Protein Binding

<10%

Use: Labeled Indications

Transfusional iron overload: Treatment of transfusional iron overload due to thalassemia syndromes with inadequate response to other chelation therapy.

Limitation of use: Safety and effectiveness have not been established for the treatment of transfusional iron overload in patients with other chronic anemias.

Contraindications

Hypersensitivity to deferiprone or any component of the formulation

Dosage

Oral: Note: Round dose to the nearest 250 mg (or 1/2 tablet) or 2.5 mL (solution). If serum ferritin falls consistently below 500 mcg/L, consider temporary treatment interruption.

Adults: Transfusional iron overload: Initial: 25 mg/kg 3 times/day (75 mg/kg/day); individualize dose based on response and therapeutic goal; maximum dose: 33 mg/kg 3 times/day (99 mg/kg/day)

Elderly: Begin at the low end of dosing range

Dosage adjustment for toxicity:

ANC <1,500/mm3 and >500/mm3: Interrupt treatment immediately and monitor until recovery; do not rechallenge unless the potential benefit outweighs the risk

ANC <500/mm3: In addition to immediate treatment interruption, consider hospitalization (and other clinically-appropriate management); do not resume unless the potential benefits outweigh potential risks

Infection: Interrupt treatment; monitor ANC more frequently

Dosage adjustment in renal impairment: There are no dosage adjustments provided in the manufacturer’s labeling.

Dosage adjustment in hepatic impairment: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied in patients with severe impairment).

Administration

Administer in the morning, at midday and in the evening. Administration with food may decrease nausea. Administer after at least a 4-hour interval with medications or supplements containing polyvalent cations (iron, aluminum, zinc).

Hazardous agent - use appropriate precautions for handling and disposal (NIOSH 2014 [group 2]).

Dietary Considerations

May be taken with food to decrease nausea. Allow at least a 4-hour interval with foods containing iron, aluminum, and zinc.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Store oral solution in original carton to protect from light; use contents within 35 days after first opening bottle; discard any remaining solution after 35 days.

Drug Interactions

Antacids: May decrease the serum concentration of Deferiprone. Management: Separate administration of deferiprone and oral medications or supplements that contain polyvalent cations by at least 4 hours. Exceptions: Sodium Bicarbonate. Consider therapy modification

Calcium Salts: May decrease the serum concentration of Deferiprone. Management: Separate administration of deferiprone and oral medications or supplements that contain polyvalent cations by at least 4 hours. Consider therapy modification

Iron Salts: May decrease the serum concentration of Deferiprone. Management: Separate administration of deferiprone and oral medications or supplements that contain polyvalent cations by at least 4 hours. Exceptions: Ferric Carboxymaltose; Ferric Gluconate; Ferric Pyrophosphate Citrate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Consider therapy modification

Magnesium Salts: May decrease the serum concentration of Deferiprone. Management: Separate administration of deferiprone and oral medications or supplements that contain polyvalent cations by at least 4 hours. Consider therapy modification

Multivitamins/Minerals (with ADEK, Folate, Iron): May decrease the serum concentration of Deferiprone. Management: Separate administration of deferiprone and oral medications or supplements that contain polyvalent cations by at least 4 hours. Consider therapy modification

Multivitamins/Minerals (with AE, No Iron): May decrease the serum concentration of Deferiprone. Management: Separate administration of deferiprone and oral medications or supplements that contain polyvalent cations by at least 4 hours. Consider therapy modification

Myelosuppressive Agents: May enhance the neutropenic effect of Deferiprone. Avoid combination

UGT1A6 Inhibitors: May increase the serum concentration of Deferiprone. Monitor therapy

Zinc Salts: May decrease the serum concentration of Deferiprone. Management: Separate administration of deferiprone and oral medications or supplements that contain polyvalent cations by at least 4 hours. Exceptions: Zinc Chloride. Consider therapy modification

Adverse Reactions

>10%:

Gastrointestinal: Nausea (13%)

Genitourinary: Chromaturia (15%)

1% to 10%:

Central nervous system: Headache (3%)

Gastrointestinal: Abdominal pain/discomfort (10%), vomiting (10%), appetite increased (4%), diarrhea (3%), dyspepsia (2%), weight gain (2%), appetite decreased (1%)

Hematologic: Neutropenia (6% to 7%), agranulocytosis (2%)

Hepatic: ALT increased (8%), AST increased (1%)

Neuromuscular and skeletal: Arthralgia (10%), back pain (2%), limb pain (2%), arthropathy (1%)

<1% (Limited to important or life-threatening): Acute respiratory distress syndrome, anaphylactic shock, atrial fibrillation, bilirubin increased, bruxism, cardiac failure, cerebellar syndrome, cerebral hemorrhage, chills, chondropathy, CPK increased, cryptococcal cutaneous infection, dehydration, depression, diplopia, enterocolitis, enteroviral encephalitis, epistaxis, fever, furuncle, gait disturbance, gastric ulcer, glycosuria, hemoglobinuria, hemoptysis, Henoch-Schönlein purpura (IgA vasculitis), hepatitis (infectious), hepatomegaly, hyperhydrosis, hyper-/hypotension, hypersensitivity, hypospadias, intracranial pressure increased, jaundice, metabolic acidosis, multiorgan failure, myositis, obsessive compulsive disorder, pancreatitis, pancytopenia, papilledema, parotid gland enlargement, periorbital edema, peripheral edema, pharyngitis, photosensitivity, pneumonia, pruritus, psychomotor skills impaired, pulmonary embolism, pustular rash, pyramidal tract syndrome, rash, rectal hemorrhage, retinal toxicity, seizure, sepsis, somnolence, subcutaneous abscess, thrombocytosis, torsade de pointes, trismus, urticaria, zinc levels decreased

ALERT: U.S. Boxed Warning

Agranulocytosis/Neutropenia:

Deferiprone can cause agranulocytosis that can lead to serious infections and death. Neutropenia may precede the development of agranulocytosis. Measure the absolute neutrophil count (ANC) before starting deferiprone therapy and monitor the ANC weekly during therapy. Interrupt deferiprone therapy if neutropenia develops. If infection develops, interrupt deferiprone and monitor the ANC more frequently. Advise patients taking deferiprone to report immediately any symptoms indicative of infection.

Warnings/Precautions

Concerns related to adverse effects:

• Agranulocytosis//Neutropenia: [US Boxed Warning]: May cause agranulocytosis, which could lead to serious infections (some fatal). Agranulocytosis may be preceded by neutropenia; monitor absolute neutrophil count (ANC) prior to treatment initiation and weekly during therapy. If infection develops, interrupt treatment and monitor ANC more frequently. Patients should promptly report any symptoms which may indicate infection. Interrupt treatment if neutropenia (ANC <1,500/mm3) develops; withhold any other medications which may also be associated with neutropenia; monitor CBC, corrected WBC, ANC, and platelets daily until ANC recovery. If ANC <500/mm3, consider hospitalization (and other clinically appropriate management); do not resume or rechallenge unless the potential benefits outweigh potential risks. Neutropenia and agranulocytosis were generally reversible upon discontinuation. The mechanism for deferiprone-induced agranulocytosis is not known. Avoid concurrent use with other agents associated with neutropenia (or agranulocytosis).

• Hepatotoxicity: Elevations in ALT values have been observed; monitor ALT and consider treatment interruption for persistent elevations.

• Hypersensitivity: Hypersensitivity reactions have been reported (eg, Henoch-Schonlein purpura, urticaria, and periorbital edema with skin rash).

• Zinc deficiency: Lower plasma zinc concentrations have been observed; monitor zinc levels and supplement if necessary.

Special handling:

• Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 2]).

Monitoring Parameters

Serum ferritin (every 2-3 months); ANC (at baseline and weekly during treatment); if ANC <1,500/mm3, monitor CBC, WBC (corrected for nucleated RBCs), ANC, and platelets daily until ANC recovery; ALT (monthly); zinc levels; signs or symptoms of infection

Pregnancy Risk Factor

D

Pregnancy Considerations

Adverse effects have been observed in animal reproduction studies. Although there is limited data in humans, deferiprone may cause fetal harm if administered during pregnancy. During treatment with deferiprone in women of reproductive potential, pregnancy should be avoided.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience joint pain, abdominal pain, nausea, vomiting, or urine discoloration. Have patient report immediately to prescriber signs of infection (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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