Febuxostat is a xanthine oxidase inhibitor used for treating gout caused by excessive levels of uric acid in the blood (hyperuricemia). Uric acid is formed from the breakdown of certain chemicals (purines) in the body.
Xanthine oxidase inhibitor
Febuxostat is a non-purine, selective xanthine oxidase (XO) inhibitor. It decreases serum uric acid level by inhibiting xanthine oxidase, which is responsible for uric acid production. Xanthine oxidase breaks down hypoxanthine to xanthine and thus to uric acid. Febuxostat is not expected to inhibit other enzymes involved in purine and pyrimidine synthesis and metabolism at therapeutic concentrations.
Treatment of chronic hyperuricaemia in gout BY MOUTH Adult: Initially 80 mg once daily, if after 2-4 weeks of initial dose, serum uric acid greater than 6 mg/100mL then increase dose; increased if necessary to 120 mg once daily Prophylaxis and treatment of acute hyperuricaemia with initial chemotherapy for haematologic malignancies BY MOUTH Adult: 120 mg once daily, to be started 2 days before start of cytotoxic therapy and continued for 7-9 days, according to chemotherapy duration
Mercaptopurine/Azathioprine: On the basis of the mechanism of action of Febuxostat on XO inhibition concomitant use is not recommended. Inhibition of XO by Febuxostat may cause increased plasma concentrations of these drugs leading to toxicity.
Rosiglitazone/CYP2C8 substrates: Co-administration of Febuxostat with rosiglitazone or other CYP2C8 substrates is not expected to require any dose adjustment for those compounds.
Naproxen and other inhibitors of glucuronidation: Febuxostat metabolism depends on Uridine Glucuronosyl Transferase (UGT) enzymes. Medicinal products that inhibit glucuronidation, such as NSAIDs and probenecid, could in theory affect the elimination of Febuxostat. Febuxostat can be co-administered with naproxen with no dose adjustment of Febuxostat or naproxen being necessary.
Inducers of glucuronidation: Potent inducers of UGT enzymes might possibly lead to increased metabolism and decreased efficacy of Febuxostat. Monitoring of serum uric acid is therefore recommended 1-2 weeks after start of treatment with a potent inducer of glucuronidation. Conversely, cessation of treatment of an inducer might lead to increased plasma levels of Febuxostat.
Colchicine/ Indometacin/ Hydrochlorothiazide/ Warfarin: Febuxostat can be co-administered with colchicine or indomethacin with no dose adjustment of Febuxostat. No dose adjustment is necessary for hydrochlorothiazide or warfarin when administered with Febuxostat .
Antacids: Concomitant ingestion of an antacid containing magnesium hydroxide and aluminium hydroxide has been shown to delay absorption of Febuxostat (approximately 1 hour) and to cause a 32% decrease in Cmax, but no significant change in AUC was observed. Therefore, Febuxostat may be taken without regard to antacid use.
Not a treatment for acute gout but continue if attack develops when already receiving febuxostat, and treat attack separately Congestive heart failure . ischaemic heart disease . thyroid disorders . transplant recipients
Common or very common Abnormal liver function tests . gastro-intestinal disturbances . headache . oedema . rash Uncommon Renal failure . appetite change . arthralgia . arthritis . atrial fibrillation . bronchitis . bursitis . chest pain . cholelithiasis . cough . decreased libido . dermatitis . diabetes mellitus . dizziness . drowsiness . dyspnoea . ECG abnormalities . erectile dysfunction . flushing . haematuria . hemiparesis . hyperlipidaemia . hypertension . hypoaesthesia . increased thyroid stimulating hormone . increased urinary frequency . insomnia . muscle spasm . muscle weakness . myalgia . nephrolithiasis . palpitation . paraesthesia . proteinuria . smell disturbances . taste disturbances . upper respiratory tract infection . weight change Rare Asthenia . blurred vision . hepatitis . jaundice . mouth ulceration . nervousness . pancreatitis . pancytopenia . rhabdomyolysis . thirst . thrombocytopenia . tinnitus . tubulointerstitial nephritis
PREGNANCY Manufacturer advises avoid?limited information available. BREAST FEEDING Manufacturer advises avoid?present in milk in animal studies.
Febustat was studied in healthy subjects in doses up to 300 mg daily for seven days without evidence of dose-limiting toxicities.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
.png&w=384&q=75)