Description
Indications |
Listed in Dosage. | ||||
Dosage |
Adult : PO Chronic hyperuricaemia with gout Initial: 40 mg/day. If serum uric acid >6 mg/dL after 2 weeks, increase dose to 80 mg/day; may be further increased to 120 mg/day. Cancer therapy-induced hyperuricaemia in patients with intermediate to high risk of tumour lysis syndrome 120 mg/day starting 2 days before the beginning of cytotoxic therapy and continued for 7-9 days based on chemotherapy duration. | ||||
Dosage Details |
Oral Hyperuricaemia with gout Adult: For chronic cases: Initially, 40 mg once daily. If serum uric acid >6 mg/dL after 2 weeks, increase dose to 80 mg once daily; may be further increased to 120 mg once daily if necessary.
Oral Adult: In patients with intermediate to high risk of tumour lysis syndrome: 120 mg once daily. Start 2 days before the beginning of cytotoxic therapy and continue for 7-9 days based on chemotherapy duration. |
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Renal Impairment |
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Administration |
May be taken with or without food. May be taken w/o regard to antacid use. | ||||
Contraindications |
Hypersensitivity. Concomitant use of azathioprine or mercaptopurine. | ||||
Special Precautions |
Patient with ischaemic heart disease, CHF, gout flares, Lesch-Nyhan syndrome, organ transplant, altered thyroid function, history of hypersensitivity reaction to allopurinol. Hepatic and severe renal impairment. Pregnancy and lactation. | ||||
Adverse Drug Reactions |
Significant: Gout flares, xanthine deposition, LFT abnormalities, increased TSH. Cardiac disorders: Chest pain and discomfort, atrial fibrillation, palpitations, left bundle branch block, sinus tachycardia. Gastrointestinal disorders: Diarrhoea, nausea, vomiting, constipation, dry mouth, abdominal pain and distension, GERD, dyspepsia, flatulence, altered taste. General disorders and administration site conditions: Fatigue, oedema. Hepatobiliary disorders: Cholelithiasis. Investigations: ECG abnormalities, weight gain. Metabolism and nutrition disorders: Diabetes mellitus, hyperlipidaemia, decreased appetite. Musculoskeletal and connective tissue disorders: Arthralgia, myalgia, arthritis, musculoskeletal pain, muscle weakness, muscle spasm, muscle tightness, bursitis. Nervous system disorders: Headache, dizziness, paraesthesia, hypoaesthesia, hemiparesis. Psychiatric disorders: Somnolence, insomnia. Renal and urinary disorders: Renal failure, nephrolithiasis, haematuria, proteinuria, pollakiuria. Reproductive system and breast disorders: Decreased libido, erectile dysfunction. Respiratory, thoracic and mediastinal disorders: Hyposmia, bronchitis, upper respiratory tract infection, cough, dyspnoea. Skin and subcutaneous tissue disorders: Rash, dermatitis, urticaria, pruritus, skin discolouration, skin lesion, petechiae. Vascular disorders: Flushing, hypertension, haemorrhage, hot flush. Potentially Fatal: MI, stroke, CV death, hepatic failure; rarely, hypersensitivity reactions (e.g. Stevens-Johnson Syndrome, toxic epidermal necrolysis, acute anaphylactic shock, drug reaction with eosinophilia and systemic symptoms). |
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Patient Counselling |
This drug may cause somnolence, dizziness, paraesthesia and blurred vision, if affected, do not drive or operate machinery. | ||||
Monitoring Parameters |
Monitor LFT before initiation and regularly during therapy; serum uric acid level as early as 2 weeks after initiating therapy; signs and symptoms of MI and stroke and of hypersensitivity reactions. | ||||
Drug Interactions |
Decreased efficacy with potent UGT enzyme inducers. Potentially Fatal: Reduces the metabolism of azathioprine and mercaptopurine, resulting to bone marrow toxicity. |
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Mechanism of Action |
Description: Febuxostat is a non-purine selective inhibitor of xanthine oxidase, the enzyme that catalyses the conversion of hypoxanthine to xanthine to uric acid, thereby decreasing serum concentration of uric acid. Pharmacokinetics: Absorption: Rapidly and well absorbed from the gastrointestinal tract. Time to peak plasma concentration: 1-1.5 hours. Distribution: Plasma protein binding: Approx 99%, mainly to albumin. Metabolism: Extensively metabolised via conjugation by uridine diphosphate glucuronosyltransferase (UGT) enzyme system and via oxidation by CYP enzyme system. Excretion: Via urine (approx 49%, mainly as metabolites and 3% as unchanged drug) and faeces (approx 45%, mainly as metabolites and 12% as unchanged drug). Terminal elimination half-life: 5-8 hours. |
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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. |
