deferiprone


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deferiprone

(de-fer-ip-rone) ,

Ferriprox

(trade name)

Classification

Therapeutic: antidotes
Pharmacologic: chelating agents
Pregnancy Category: D

Indications

Treatment of transfusional iron overload due to thalassemia when other chelation regimens are inadequate.

Action

Bonds with ferric ions to form neutral complexes which are then eliminated.

Therapeutic effects

Decrease in iron overload as reflected in decreased ferritin levels.

Pharmacokinetics

Absorption: Well absorbed following oral administration.
Distribution: Unk.
Metabolism and Excretion: Mostly metabolized (by UGT 1A6 enzyme system), 75–90% excreted in urine as metabolites.
Half-life: 1.9 hr.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
POwithin 5–10 min1–2 hr8–12 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Obstetric: Pregnancy should be avoided; Lactation: Breast feeding not recommended.
Use Cautiously in: Renal/hepatic impairment (safety and effectiveness not established); Any risk/history of QT prolongation including HF, bradycardia, diuretic use, cardiac hypertrophy, hypokalemia, hypomagnesemia; Pediatric: Safe and effective use in children has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • headache

Cardiovascular

  • Torsades de Pointes (life-threatening)

Gastrointestinal

  • abdominal pain (most frequent)
  • nausea (most frequent)
  • change in appetite
  • vomiting
  • ↑ liver enzymes

Genitourinary

  • chromaturia (most frequent)

Hematologic

  • agranulocytosis (life-threatening)
  • neutropenia

Musculoskeletal

  • arthralgia
  • arthropathy
  • back pain
  • extremity pain

Miscellaneous

  • ↓ zinc levels

Interactions

Drug-Drug interaction

Concurrent use of other drugs that cause neutropenia/agranulocytosis may ↑ risk of neutropenia/agranulocytosis. May also chelate other concurrently administered polyvalent cations in mineral supplements and antacids, including iron, aluminum and zinc ; wait 4 hr between administration.

Route/Dosage

Oral (Adults) 25 mg/kg three times daily, may be adjusted up to 33 mg/kg three times daily (range 75–99 mg/kg/day in divided doses). Dose should be rounded to the nearest 250 mg (1/2 tablet).

Availability

Tablets: 500 mg

Nursing implications

Nursing assessment

  • .
  • Lab Test Considerations: Monitor serum ferritin every 2–3 mo to assess efficacy. If serum ferritin falls consistently below 500 mcg/L, consider temporarily interripting deferiprone therapy.
    • Measure ANC before starting and weekly during therapy. Interrupt deferiprone if neutropenia (ANC <1.5 X 109/L) or if infection develops. If ANC <1.5 X 109/L and >0.5 X 109/L, obtain CBC with WBC corrected for presence of nucleated red blood cells, ANC, and platelet count daily until recovery (ANC ≥1.5 X 109/L. For agranulocytosis (ANC <0.5 X 109/L), Consider hospitalization and manage as clinically appropriate. Do not resume deferiprone in patients who develop agranulocytosis or rechallenge patients who develop neutropenia, unless benefits outweigh risks.
    • Monitor serum AST and ALT monthly during therapy. Interrupt therapy if persistent ↑ in serum transaminases occurs.
    • Monitor plasma zinc levels. ↓ may occur and may require supplementation.

Potential Nursing Diagnoses

Risk for infection (Adverse Reactions)

Implementation

  • Oral: Administer first dose in the morning, second dose midday, and third dose in the evening. May be taken with meals to decrease nausea.

Patient/Family Teaching

  • Instruct patient to take deferiprone 3 times/day. Take missed doses as soon as remembered, but not just before next dose. Do not double doses.
  • Advise patient to stop therapy and notify health care professional immediately if signs and symptoms of infection (fever, sore throat) or if palpitations, dizziness, syncope, or seizures occur.
  • Inform patient that reddish/brown urine may occur; common and not harmful.
  • Advise female patients to use contraception and avoid breastfeeding during therapy. If pregnancy is planned or suspected, notify health care professional promptly.

Evaluation/Desired Outcomes

  • Decrease in serum ferritin levels.
References in periodicals archive ?
The patients were receiving regular erythrocyte transfusions and insufficient iron-chelating agents (deferoxamine or deferiprone or deferasirox).
His family spends at least P46,800 for the procedure, including blood transfusion (P10,800 for three bags of blood) and the intake of three types of medication (desferal, deferiprone and exjade).
Additional oral iron chelators such as deferiprone and deferasirox have been used in the past five years.
He is trialling the drug Deferiprone (Ferriprox) in an attempt to remove the iron deposits from the surface of the brain.
He is trialling the drug deferiprone in an attempt to remove the iron deposits from the surface of the brain.
Christou et al., "Improved survival in thalassemia major patients on switching from desferrioxamine to combined chelation therapy with desferrioxamine and deferiprone," Haematologica, vol.
Kolnagou, "Benefits and risks of deferiprone in iron overload in thalassaemia and other conditions: Comparison of epidemiological and therapeutic aspects with deferoxamine," Drug Safety, vol.
Chen et al., "Deferiprone inhibits iron overload-induced tissue factor bearing endothelial microparticle generation by inhibition oxidative stress induced mitochondrial injury, and apoptosis," Toxicology and Applied Pharmacology, vol.
The development of iron chelators, namely, deferoxamine, deferiprone, and deferasirox (the three chelators currently available in Oman) have led to a marked reduction in the risk of iron-related complications and improved the survival of these patients.
Improvement of erythropoiesis during treatment with deferiprone in a patient with myelofibrosis and transfusional hemosiderosis.
However, its obstruction of the blood–brain barrier has restricted its use in neurodegenerative disorders.[sup][136] The chelator deferiprone has an advantage over desferrioxamine, a 12-month study in patients with early-stage PD revealed a meaningful reduction in iron levels and improvement in motor symptoms,[sup][137] and several Phase II clinical trials evaluating deferiprone are ongoing [Table 1].[sup][50],[51]
Pineda, "Combined Therapy with Idebenone and Deferiprone in Patients with Friedreich's Ataxia," Cerebellum, vol.