Adult: In patients with thalassaemia major when deferoxamine is ineffective or contraindicated: As oral solution and 500 mg or 1,000 mg conventional tab: 75 mg/kg daily given in 3 divided doses, may be adjusted according to response and treatment goals. Max: 100 mg/kg daily. As 1,000 mg delayed-release tab: 75 mg/kg daily given in 2 divided doses, may be adjusted according to response and treatment goals. Max: 99 mg/kg daily. The calculated dosage (per kg body weight) must be rounded to the nearest half tab (250 mg or 500 mg) or the nearest 2.5 mL. Dosing interruption may be required based on the individual serum ferritin levels, ANC, and presence of infection or hepatotoxicity. Dosage and treatment recommendations may vary among individual products and between countries (refer to detailed product guidelines).
Administration
May be taken with or without food.
Contraindications
Hypersensitivity. Neutropenia, including history of recurrent episodes of neutropenia; history of agranulocytosis. Pregnancy and lactation.
Special Precautions
Patient with hepatitis C. Immunocompromised patients (e.g. HIV positive patients). Concomitant use with agents known to cause neutropenia or agranulocytosis. Hepatic and renal impairment.
Adverse Reactions
Significant: Hepatotoxicity (e.g. increased serum ALT levels), hypersensitivity reactions (e.g. Henoch-Schonlein purpura, urticaria, periorbital oedema with skin rash); Zn deficiency, reddish-brown urine discolouration. Gastrointestinal disorders: Nausea, vomiting, abdominal pain or discomfort, diarrhoea, dyspepsia. General disorders and administration site conditions: Fatigue, fever. Infections and infestations: Flu syndrome. Investigations: Increased serum AST levels, weight gain. Metabolism and nutrition disorders: Increased or decreased appetite. Musculoskeletal and connective tissue disorders: Arthralgia, back pain. Nervous system disorders: Headache. Skin and subcutaneous tissue disorders: Pruritus. Potentially Fatal: Neutropenia and agranulocytosis which may result in serious infections.
Women of childbearing potential must use proven birth control methods during therapy and for 6 months after stopping the treatment. Men with female partners of childbearing potential must also use proven birth control methods during treatment and for 3 months after the last dose.
Monitoring Parameters
Evaluate pregnancy status in women of childbearing potential before treatment initiation. Monitor ANC at baseline, weekly during the 1st 6 months, every 2 weeks for the next 6 months of treatment, and then every 2-4 weeks thereafter; serum ferritin every 2-3 months; ALT at baseline and every month; Zn levels at baseline and regularly during therapy. Assess for signs and symptoms of infection (e.g. fever, sore throat, flu-like symptoms).
Drug Interactions
Serum concentrations may be increased with UGT1A6 inhibitors (e.g. phenylbutazone, diclofenac, probenecid). Serum levels of deferiprone may be reduced when given with polyvalent cation-containing agents (e.g. Al-based antacids, drugs or supplements containing Fe, Al or Zn). Potentially Fatal: May result in enhanced neutropenic effect when taken with other agents that may cause neutropenia or agranulocytosis.
Food Interaction
May increase serum concentration with silymarin. Serum concentration may be increased by alcohol.
Action
Description: Mechanism of Action: Deferiprone is an orally active Fe chelating agent with a high binding affinity to ferric ion. It binds to ferric ions to form a neutral, stable, and water-soluble 3:1 ratio (deferiprone:Fe) complex. Deferiprone also has a low affinity to metals such as copper, Al, and Zn. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 1-2 hours. Distribution: Volume of distribution: 1.6 L/kg (conventional tab, oral solution); 97 ± 28 L (delayed-release tab). Plasma protein binding: <10%. Metabolism: Metabolised predominantly by UGT1A6 into 3-O-glucuronide (major metabolite that lacks Fe-binding capacity). Excretion: Mainly via urine (75-90%, primarily as glucuronide metabolite and Fe-deferiprone complex). Elimination half-life: Approx 2-3 hours.
Chemical Structure
Deferiprone Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2972, Deferiprone. https://pubchem.ncbi.nlm.nih.gov/compound/Deferiprone. Accessed May 29, 2024.
Storage
Conventional/delayed-release tab: Store between 15-30°C. Oral solution: Store below 30°C. Protect from light.
V03AC02 - deferiprone ; Belongs to the class of iron chelating agents. Used in iron overload.
References
Anon. Deferiprone. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 16/03/2024.Anon. Deferiprone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 16/03/2024.Buckingham R (ed). Deferiprone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/03/2024.Chiesi New Zealand Ltd. Ferriprox 500 mg Tablet, 1,000 mg Tablet, and 100 mg/mL Oral Solution data sheet 08 November 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 16/03/2024.Deferiprone 1,000 mg Film-coated Tablets (Mercury Pharmaceuticals Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 16/03/2024.Ferriprox 1,000 mg Delayed-release Tablets (Pharmaforte [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 16/03/2024.Ferriprox 100 mg/mL Oral Solution (Chiesi Limited). MHRA. https://products.mhra.gov.uk. Accessed 16/03/2024.Ferriprox 100 mg/mL Oral Solution (Pharmaforte [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 16/03/2024.Ferriprox Solution (Chiesi USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 16/03/2024.Ferriprox Tablet, Film Coated (Chiesi USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 14/05/2024.Joint Formulary Committee. Deferiprone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/03/2024.
Sign Out
