Febuxostat


Generic Medicine Info
Indications and Dosage
Oral
Hyperuricaemia
Adult: In patients with chronic gout: Initially, 40 mg once daily, may increase dose to 80 mg once daily if serum uric acid is >6 mg/dL after 2 weeks. Alternatively, 80 mg once daily, may increase dose to 120 mg once daily if serum uric acid is >6 mg/dL after 2-4 weeks.

Oral
Cancer therapy-induced hyperuricaemia
Adult: For prophylaxis and treatment of patients with intermediate to high risk for tumour lysis syndrome: 120 mg once daily, starting 2 days before chemotherapy and continued for 7-9 days, depending on chemotherapy duration.
Renal Impairment
Hyperuricaemia:
CrCl (mL/min) Dosage
<30 Max: 40 mg once daily. Dosage recommendations may vary among countries and individual products (refer to specific country or product guidelines).
Hepatic Impairment
Hyperuricaemia:
Mild: 80 mg daily. Dosage recommendations may vary among countries and individual products (refer to specific country or product guidelines).
Administration
May be taken with or without food. May be taken w/o regard to antacid use.
Contraindications
Concomitant use with azathioprine, mercaptopurine.
Special Precautions
Patient with history of hypersensitivity reaction to allopurinol; major CV disease (e.g. MI, stroke, unstable angina), thyroid disorders; increased risk for urate formation (e.g. Lesch-Nyhan syndrome, malignant disease and its treatment). Organ transplant recipients. Not recommended to be started during an acute attack of gout. Use of febuxostat is restricted to patients who are intolerant to allopurinol or for whom allopurinol is contraindicated or ineffective. Not recommended for the treatment of asymptomatic or secondary hyperuricaemia. Hepatic and renal impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Gout flares, xanthine deposition, LFT abnormalities, increased TSH.
Eye disorders: Blurred vision.
Gastrointestinal disorders: Diarrhoea, nausea.
General disorders and administration site conditions: Oedema, fatigue.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia, pain in extremity.
Nervous system disorders: Headache, dizziness, paraesthesia.
Psychiatric disorders: Somnolence.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Potentially Fatal: CV death, hepatic failure. Rarely, hypersensitivity, including Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms, and acute anaphylactic reaction/shock.
Patient Counseling Information
This drug may cause dizziness, somnolence, paraesthesia and blurred vision; if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor LFTs at baseline and periodically thereafter; serum uric acid levels 2 weeks after initiation of treatment, after each dosage titration, then every 6 months (symptomatic patients or tophi) or every 12 months (patients on urate-lowering therapy, regardless of symptoms); renal function. Assess for gout flares and signs or symptoms of CV events and hypersensitivity or severe skin reactions.
Drug Interactions
Decreased efficacy with potent UGT enzyme inducers.
Potentially Fatal: Increased plasma concentrations resulting in severe toxicity of mercaptopurine and azathioprine.
Action
Description:
Mechanism of Action: Febuxostat is a potent, non-purine, selective inhibitor of xanthine oxidase, the enzyme that catalyses the conversion of hypoxanthine to xanthine to uric acid. The inhibition of xanthine oxidase decreases the serum concentrations of uric acid.
Pharmacokinetics:
Absorption: Rapidly and well absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1-1.5 hours.
Distribution: Volume of distribution: Approx 50 L. Plasma protein binding: Approx 99%, mainly to albumin.
Metabolism: Extensively metabolised via conjugation by UGT enzyme system and via oxidation by the CYP450 isoenzyme system into active hydroxyl metabolites.
Excretion: Via urine (approx 49% as metabolites, 3% as unchanged drug); faeces (approx 45% as metabolites, 12% as unchanged drug). Elimination half-life: Approx 5-8 hours.
Chemical Structure

Chemical Structure Image
Febuxostat

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 134018, Febuxostat. https://pubchem.ncbi.nlm.nih.gov/compound/Febuxostat. Accessed Apr. 27, 2023.

Storage
Store between 15-30°C. Protect from light.
MIMS Class
Hyperuricemia & Gout Preparations
ATC Classification
M04AA03 - febuxostat ; Belongs to the class of preparations inhibiting uric acid production. Used in the treatment of gout.
References
A. Menarini New Zealand Pty Ltd. Adenuric 80 mg Film Coated Tablets data sheet 30 September 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 03/04/2023.

Adenuric 80 mg Film-coated Tablets (Menarini International Operations Luxembourg S.A.). MHRA. https://products.mhra.gov.uk. Accessed 03/04/2023.

Anon. Febuxostat. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 03/04/2023.

Anon. Febuxostat. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/04/2023.

Buckingham R (ed). Febuxostat. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/04/2023.

Goutric 40 mg Film Coated Tablets (Novugen Pharma [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 03/04/2023.

Joint Formulary Committee. Febuxostat. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/04/2023.

Uloric Tablets (Takeda Pharmaceuticals America, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 03/04/2023.

Disclaimer: This information is independently developed by MIMS based on Febuxostat from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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