deferiprone (Rx)

Brand and Other Names:Ferriprox
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 500mg

oral solution

  • 80 mg/mL

Transfusional Iron Overload

Iron chelator indicated for treatment of transfusional iron overload caused by thalassemia syndromes when current chelation therapy is inadequate

Approval based on serum ferritin level reduction; no controlled trials demonstrating a direct treatment benefit (eg, improvement in disease-related symptoms, functioning, or increased survival)

Initial dose: 25 mg/kg PO TID  

Dosage range: 25-33 mg/kg PO TID (ie, total daily dosage range 75-99 mg/kg/day)

Round dose to nearest 250 mg (half-tablet) or nearest 2.5 mL (oral solution)

Monitoring and dose adjustments

  • Monitor serum ferritin concentration every 2-3 months to assess the effects on body iron stores
  • Dose adjustments should be tailored to the individual patient’s response and therapeutic goals (maintenance or reduction of body iron burden)
  • If the serum ferritin falls consistently <500 mcg/L, consider temporarily interrupting therapy

Siderosis (Orphan)

Orphan designation for treatment of superficial siderosis

Orphan sponsor

  • ApoPharma, Inc; 200 Barmac Drive; Canada

Dosage Modifications

Renal impairment: Based on a clinical study, no adjustment required in patients with impaired renal function

Hepatic impairment: Based on a clinical study, no adjustment required in patients mildly or moderately impaired hepatic function

Dosing Consideration

Limitation of use

  • Safety and efficacy not established for treatment of transfusional iron overload in patients with other chronic anemias

Safety and efficacy not established

Neurodegeneration With Brain Iron Accumulation (Orphan)

Orphan designation treatment of neurodegeneration with brain iron accumulation (NBIA)

Sponsor

  • ApoPharma, Inc; 200 Barmac Drive, M9L 2Z7; Canada

Safety and effectiveness in elderly individuals have not been established

In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy

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Interactions

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            Adverse Effects

            >10%

            Nausea (13%)

            1-10%

            Abdominal pain/discomfort (10%)

            Vomiting (10%)

            Arthralgia (10%)

            Increased alanine aminotransferase (7%)

            Neutropenia (6%) Diarrhea (3%)

            Dyspepsia (2%)

            Back pain (2%)

            Pain in extremity (2%)

            Headache (2%)

            Agranulocytosis (2%)

            Increased aspartate aminotransferase (1%)

            Decrease appetite (1%)

            Arthropathy (1%)

            Postmarketing Reports

            Blood and lymphatic system disorders: Thrombocytosis, pancytopenia

            Cardiac disorders: Atrial fibrillation, cardiac failure

            Congenital, familial and genetic disorders: Hypospadias

            Eye disorders: Diplopia, papilledema, retinal toxicity

            Gastrointestinal disorders: Enterocolitis, rectal hemorrhage, gastric ulcer, pancreatitis, parotid gland enlargement

            General disorders and administration site conditions: Chills, pyrexia, edema peripheral, multi-organ failure

            Hepatobiliary disorders: Jaundice, hepatomegaly. Immune system disorders: anaphylactic shock, hypersensitivity

            Infections and infestations: Cryptococcal cutaneous infection, enteroviral encephalitis, pharyngitis, pneumonia, sepsis, furuncle, infectious hepatitis, rash pustular, subcutaneous abscess

            Investigations: Blood bilirubin increased, blood creatinine phosphokinase increased

            Metabolism and nutrition disorders: Metabolic acidosis, dehydration

            Musculoskeletal and connective tissue disorders: Myositis, chondropathy, trismus

            Nervous system disorders: Cerebellar syndrome, cerebral hemorrhage, convulsion, gait disturbance, intracranial pressure increased, psychomotor skills impaired, pyramidal tract syndrome, somnolence

            Psychiatric disorders: Bruxism, depression, obsessive-compulsive disorder

            Renal disorders: Glycosuria, hemoglobinuria

            Respiratory, thoracic and mediastinal disorders: Acute respiratory distress syndrome, epistaxis, hemoptysis, pulmonary embolism

            Skin, subcutaneous tissue disorders: Hyperhidrosis, periorbital edema, photosensitivity reaction, pruritus, urticaria, rash, Henoch-SchÖnlein purpura

            Vascular disorders: Hypotension, hypertension

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            Warnings

            Black Box Warnings

            Can cause agranulocytosis that can lead to serious infections and death; neutropenia may precede agranulocytosis

            Measure absolute neutrophil count (ANC) before initiating and monitor weekly while on therapy

            Interrupt treatment if infection develops and monitor ANC more frequently

            Advise patients taking to report immediately any symptoms indicative of infection

            Contraindications

            Hypersensitivity; Henoch-SchÖnlein purpura, urticaria, and periorbital edema with skin rash have been reported

            Cautions

            Fatal agranulocytosis can occur; interrupt therapy if neutropenia develops (ANC <1.5 x 10^9/L)

            If infection occurs, interrupt therapy and monitor the ANC more frequently

            Pregnancy; can cause fetal harm; women should be advised of the potential hazard to the fetus and to avoid pregnancy while on this drug

            Monitor serum ferritin concentration every 2-3 months to assess the effects on body iron stores

            Thorough QT interval studies have not been conducted

            In clinical studies, 7.5% of subjects treated developed increased ALT values; monitor

            Decreased plasma zinc concentrations; monitor plasma zinc, and supplement in the event of a deficiency

            Drug interactions overview

            • Avoid coadministration with other drugs known to cause neutropenia or agranulocytosis; however, if this is not possible, closely monitor the absolute neutrophil count
            • Allow at least a 4-hour interval between deferiprone and mineral supplements, and antacids that contain polyvalent cations (eg, iron, aluminum, zinc) to avoid binding and malabsorption of supplements
            • Avoid use of UGT1A6 inhibitors (eg, diclofenac, probenecid, or silymarin [milk thistle]) with deferiprone
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            Pregnancy & Lactation

            Pregnancy

            Limited available data with use in pregnant women are insufficient to inform a drug-associated risk of major birth defects and miscarriage

            Verify the pregnancy status of females of reproductive potential prior to initiating therapy

            Animal data

            • May cause fetal harm when administered to a pregnant woman based on genotoxicity and developmental toxicity in animal studies
            • In animal reproduction studies, administration of deferiprone to pregnant animals during the period of organogenesis resulted in adverse developmental outcomes including embryofetal death and malformations in rats and rabbits at doses much lower than the MRHD (maximum recommended human dose) based on body surface area

            Contraception

            • Females: Advise females of reproductive potential to avoid pregnancy during treatment and 6 months of contraception is recommended after cessation of therapy; advise females to immediately report pregnancy
            • Males: Advise males with female sexual partners of reproductive potential to use effective contraception during treatment and 3 months of contraception is recommended after cessation of therapy

            Lactation

            There is no information regarding the presence of deferiprone in human milk, the effects on the breastfed child, or the effects on milk production

            Because of the potential for serious adverse reactions, including the potential for tumorigenicity shown for deferiprone in animal studies, advise not to breastfeed during treatment and for 2 weeks after last dose

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Chelating agent with an affinity for ferric ion (iron III); binds with ferric ions to form neutral 3:1 (deferiprone:iron) complexes that are stable over a wide range of pH values

            Has a lower binding affinity for other metals (eg, copper, aluminum, zinc) than for iron

            Absorption

            Absorption: Rapidly absorbed from upper GI within 5-10 minutes of PO administration

            Peak plasma time: 1 hr (fasting); 2 hr (with food)

            Peak plasma concentration: 20 mcg/mL

            AUC: 53 mcg•hr/mL

            Food decreases Cmax by 38% and AUC by 10%, but magnitude of exposure change does not warrant dose adjustment

            Metabolism

            Primarily eliminated via metabolism to the 3-O-glucuronide (lacks iron binding capability)

            UGT 1A6 is primarily responsible for glucuronidation

            Distribution

            Protein bound: <10%

            Vd: 1.6 L/kg (in patients with thalassemia); 1 L/kg (in healthy subjects)

            Elimination

            Half-life: 1.9 hr

            Excretion: 75-90% excreted within 24 hr in urine as metabolite

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            Administration

            Oral Administration

            Tablets and oral solution: Take 3 times a day, with or without food

            Oral solution

            • Pour prescribed dose of oral solution into the measuring cup
            • Swallow dose; add ~10-15 mL of water to the measuring cup; gently swirl the measuring cup to mix the water and any remaining drug in the measuring cup

            Storage

            Tablet: Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F)

            Oral solution

            • Unused bottle: Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F)
            • Store in the original bottle and carton to protect from light
            • After first opening of the bottle, discard any unused portion after 8 weeks
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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.