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Deferiprone

Medically reviewed by Drugs.com. Last updated on Oct 2, 2020.

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, 1000 mg [scored]

Ferriprox Twice-A-Day: 1000 mg [scored]

Generic: 500 mg

Brand Names: U.S.

  • Ferriprox
  • Ferriprox Twice-A-Day

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

500 mg tablet: 1.6 L/kg.

1,000 mg tablet (twice-a-day formulation): 97 ± 28 L.

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 to 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

Canadian labeling: Additional contraindications (not in US labeling): Severe neutropenia (ANC <500/mm3); pregnancy; breastfeeding

Dosing: Adult

Note: Round dose to the nearest 250 mg (or ½ of 500 mg tablet), 500 mg (or ½ of 1,000 mg tablet), or 2.5 mL (oral solution). If serum ferritin falls consistently below 500 mcg/L, consider temporary treatment interruption until serum ferritin rises above 500 mcg/L. Use actual body weight for dose calculation.

Transfusional iron overload: Oral: Note: Deferiprone is available as an oral solution, a 500 mg tablet, and as 2 different 1,000 mg tablet formulations (a twice-a-day formulation and a 3-times-a-day formulation); verify formulation prior to ordering/dispensing to avoid medication errors.

Initial: 75 mg/kg/day in 2 divided doses (using 1,000 mg twice-a-day tablet formulation only) or in 3 divided doses (using oral solution, 500 mg tablet, or 1,000 mg 3-times-a-day tablet formulation); individualize dose based on response and therapeutic goal.

Maximum dose: 99 mg/kg/day.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing. Begin at the low end of dosing range.

Dosing: 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 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

Administration

Note: Deferiprone is available as an oral solution, a 500 mg tablet, and as 2 different 1,000 mg tablet formulations (a twice-a-day formulation and a 3-times-a-day formulation); verify formulation prior to administration to avoid medication errors.

Oral:

Allow at least a 4-hour interval between deferiprone and medications or supplements containing polyvalent cations (eg, iron, aluminum, zinc).

Oral solution, 500 mg tablet, or 1,000 mg 3-times-a-day tablet formulation: Administer in the morning, at midday, and in the evening. Administration with food may decrease nausea.

1,000 mg twice-a-day tablet formulation: Administer approximately every 12 hours (in the morning and evening) with food to decrease nausea/vomiting.

Dietary Considerations

Take with food to decrease nausea/vomiting. 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

Myelosuppressive Agents: May enhance the neutropenic effect of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. Consider therapy modification

Polyvalent Cation Containing Products: 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

UGT1A6 Inhibitors: May increase the serum concentration of Deferiprone. Avoid combination

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Gastrointestinal: Nausea (13%)

Genitourinary: Urine discoloration (15%)

1% to 10%:

Central nervous system: Headache (2% to 3%)

Gastrointestinal: Vomiting (10%), abdominal distress (≤10%), abdominal pain (≤10%), increased appetite (4%), diarrhea (3%), dyspepsia (2%), weight gain (2%), decreased appetite (1%)

Hematologic & oncologic: Neutropenia (6%), agranulocytosis (2%)

Hepatic: Increased serum alanine aminotransferase (7% to 8%), increased serum aspartate aminotransferase (1%)

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

<1%, postmarketing, and/or case reports: Abnormal gait, acute respiratory distress syndrome, anaphylactic shock, atrial fibrillation, bruxism, cardiac failure, cerebellar syndrome, cerebral hemorrhage, chills, chondrolysis of articular cartilage, cryptococcosis (cutaneous infection), decreased serum zinc, dehydration, depression, diaphoresis, diplopia, drowsiness, encephalitis (enteroviral), enterocolitis, epistaxis, fever, furuncle, gastric ulcer, glycosuria, hemoglobinuria, hemoptysis, Henoch-Schönlein purpura, hepatitis A, hepatomegaly, hypersensitivity reaction, hypertension, male hypospadias, hypotension, increased creatine phosphokinase in blood specimen, increased intracranial pressure, increased serum bilirubin, jaundice, metabolic acidosis, motor dysfunction (pyramidal tract syndrome), multi-organ failure, myositis, obsessive compulsive disorder, pancreatitis, pancytopenia, papilledema, parotid gland enlargement, periorbital edema, peripheral edema, pharyngitis, pneumonia, pruritus, psychomotor impairment, pulmonary embolism, pustular rash, rectal hemorrhage, retinal toxicity, seizure, sepsis, skin photosensitivity, skin rash, subcutaneous abscess, thrombocythemia, trismus, urticaria

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 ANC before starting deferiprone therapy and monitor the ANC weekly during therapy. Interrupt deferiprone therapy if neutropenia develops. Interrupt deferiprone therapy if infection develops 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-Schönlein purpura [immunoglobulin A vasculitis], urticaria, and periorbital edema with skin rash).

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

Dosage form specific issues:

• Tablets: Available in 2 different 1,000 mg formulations (a twice-a-day formulation and a 3-times-a-day formulation); each has different identifying characteristics. Ensure the tablet formulation is correct for the dosing regimen prior to prescribing and dispensing to prevent medication errors.

Monitoring Parameters

Serum ferritin (every 2 to 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 status (prior to initiation and as clinically indicated).

Reproductive Considerations

Verify pregnancy status prior to initiation of deferiprone treatment. Females of reproductive potential should use contraception during treatment and for 6 months after the last deferiprone dose. Males with female partners of reproductive potential should use effective contraception during therapy and for 3 months after the last deferiprone dose.

Pregnancy Considerations

Based on data from animal reproduction studies, in utero exposure to deferiprone may cause fetal harm. Outcome information following deferiprone use in pregnancy is limited. Deferiprone should be discontinued if pregnancy occurs. When iron chelation therapy is needed in a pregnant woman, agents other than deferiprone are preferred (Diamantidis 2016; Origa 2019).

Patient Education

What is this drug used for?

• It is used to get rid of iron when too much is in the body.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Joint pain

• Abdominal pain

• Nausea

• Vomiting

• Urine discoloration

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Purple spots or redness of the skin

• Infection

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.