Deferiprone

Oral
Iron overload in patients with thalassaemia

May be taken with or without food.

Neutropenia (including history of recurrent cases), history of agranulocytosis. Pregnancy and lactation.

Immunocompromised patients. Hepatic and renal impairment.

Reddish-brown urine discolouration, abdominal pain, arthralgia, neutropenia, nausea, vomiting, diarrhoea, dyspepsia, increased ALT concentrations, headache, appetite change, asthenia, musculoskeletal pain, peripheral oedema, dizziness, somnolence, pruritus, urticaria.
Potentially Fatal: Agranulocytosis.

PO: D

This drug may cause reddish-brown discolouration of urine.

Monitor serum ferritin every 2-3 mth, absolute neutrophil count (ANC) at baseline and wkly during treatment (if ANC <1500/mm³, monitor CBC, WBC and platelets daily until ANC recovery); ALT mthly, Zn level, signs/symptoms of infection.

Serum concentration may be increased by UGT1A6 inhibitors (e.g. phenylbutazone). May chelate polyvalent cations, allow at least 4-hr interval w/ antacids and mineral supplements containing Al, Fe or Zn. Risk of additive toxicity w/ drugs that may cause neutropenia or agranulocytosis.

Absorption may be decreased when taken w/ foods containing Fe, Al and Zn.

Description:
Mechanism of Action: Deferiprone is a chelating agent w/ high affinity to ferric ion (iron III). It binds w/ ferric ions to form neutral 3:1 (deferiprone:iron) complexes. It also has low affinity to other metals including copper, Al and Zn.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Time to peak plasma concentration: Approx 1-2 hr.
Distribution: Volume of distribution: 1.6 L/kg. Plasma protein binding: <10%.
Metabolism: Metabolised by uridine diphosphate-glucuronosyltransferases (UGT)1A6 to the inactive metabolite, 3-O-glucuronide.
Excretion: Via urine (75-90%, as metabolite and Fe-deferiprone complex). Elimination half-life: Approx 2-3 hr.

Source: National Center for Biotechnology Information. PubChem Database. Deferiprone, CID=2972, https://pubchem.ncbi.nlm.nih.gov/compound/Deferiprone (accessed on Jan. 20, 2020)

Store between 20-25°C. Protect from light. Any unused portions should be disposed of in accordance w/ local requirements.

Antidotes & Detoxifying Agents

V03AC02 - deferiprone ; Belongs to the class of iron chelating agents. Used in iron overload.

Anon. Deferiprone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/10/2016.

Buckingham R (ed). Deferiprone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com . Accessed 11/10/2016.

Ferriprox Solution (ApoPharma USA, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 11/10/2016.

Ferriprox Tablet, Film-coated (ApoPharma USA, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 11/10/2016.

Joint Formulary Committee. Deferiprone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/10/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Deferiprone. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 11/10/2016.