Febuxostat


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Suy thận
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).
Suy gan
Hyperuricaemia:
Mild: 80 mg daily. Dosage recommendations may vary among countries and individual products (refer to specific country or product guidelines).
Cách dùng
May be taken with or without food. May be taken w/o regard to antacid use.
Chống chỉ định
Concomitant use with azathioprine, mercaptopurine.
Thận trọng
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.
Tác dụng không mong muốn
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.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, somnolence, paraesthesia and blurred vision; if affected, do not drive or operate machinery.
Chỉ số theo dõi
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.
Tương tác
Decreased efficacy with potent UGT enzyme inducers.
Potentially Fatal: Increased plasma concentrations resulting in severe toxicity of mercaptopurine and azathioprine.
Tác dụng
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.
Đặc tính

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.

Bảo quản
Store between 15-30°C. Protect from light.
Phân loại MIMS
Thuốc trị tăng acid uric máu & bệnh gout
Phân loại ATC
M04AA03 - febuxostat ; Belongs to the class of preparations inhibiting uric acid production. Used in the treatment of gout.
Tài liệu tham khảo
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.

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