Urimin

Generic composition: Febuxostat

General Introduction:

Urimin is Febuxostat, a selective xanthine oxidase inhibitor. Hyperuricemia is a condition where there is elevated level of uric acid in blood and occurs when the body produces more uric acid than it can eliminate. The uric acid forms crystals in joints (gouty arthritis) and tissues, causing inflammation and pain. Elevated blood uric acid levels also can cause kidney disease and kidney stones.

Therapeutic category

• Anti-gout

Dosage forms available

• URIMIN 40mg Tablets
• URIMIN 80mg Tablets

Mechanism of action

Febuxostat is a non-purine selective inhibitor of xanthine oxidase. It works by non-competitively blocking the molybdenum-pterin center which is the active site on xanthine oxidase. Xanthine oxidase is needed to successively oxidize both hypoxanthine and xanthine to uric acid. Febuxostat prevents the production of uric acid by blocking the activity of the enzyme (xanthine oxidase) that converts purines to uric acid.

 Pharmacokinetics

Absorption: about 49%, 99.2% protein bound,

Distribution: apparent volume of distribution (Vss/F) of febuxostat was approximately 50L

Metabolism: metabolized by both conjugations via uridine diphosphate glucuronosyltransferase (UGT) enzymes including UGT1A1, UGT1A3, UGT1A9, and UGT2B7 and oxidation via cytochrome P450 (CYP) enzymes including CYP1A2, 2C8 and 2C9 and non-P450 enzymes.

Elimination: eliminated primarily through both hepatic and renal pathways.

Half-life: about 5-8 hours.

 Uses

• Chronicgout
• Hyperuricemia

Dosage

• 40 mg daily without regard of food; increased to 80mg per day if the target serum level of <6mg/dL is not achieved after 2 weeks, maximum dose upto 120mg.
• No dose adjustment in elderly and mild-to-moderate hepatic and renal impairment.

 Side effects

Common s/e include: Nausea, Rash, Joint pain, Gout flares, Liver problems

Less common include: stroke, heart attack, anemia, hepatitis, hypersensitivity, weight loss

 Contraindications

• Hypersensitivity to febuxostat or any other excipient
• Co-administration of theophylline, azathioprine, didanosine and mercaptopurine

 Precautions

• High blood uric acid levels caused by a condition other than gout (eg, Lesch-Nyhan syndrome, cancer or treatment of cancer, organ transplant)
• Caution in use for children under 18 yrs; safety and efficacy not established in children
• Pregnancy and lactation

Advantages

• More effective than allopurinol in treating hyperuricemia as it is selective of xanthine oxidase thus does not interfere with other purine metabolism
• Faster inhibition of uric acid synthesis than allopurinol