Pharmacology · NSAIDs and Autocoids (Histamine, Serotonin, Eicosanoids, Gout Drugs)

Febuxostat is preferred over allopurinol in a patient with chronic kidney disease and gout. The pharmacological basis is:

  • A Febuxostat is a non-purine selective inhibitor of xanthine oxidase requiring no renal dose adjustment unlike allopurinol
  • B Febuxostat inhibits uricase and reduces urinary urate excretion protecting tubules
  • C Febuxostat acts on URAT1 transporter reducing renal urate reabsorption
  • D Febuxostat is renally excreted unchanged and avoids the hepatic first-pass effect seen with allopurinol
Correct answer: A. Febuxostat is a non-purine selective inhibitor of xanthine oxidase requiring no renal dose adjustment unlike allopurinol

Explanation

Febuxostat is a non-purine selective xanthine oxidase inhibitor metabolised predominantly by hepatic glucuronidation and CYP-mediated oxidation; it does NOT require dose adjustment in mild-moderate CKD. In contrast, allopurinol and its active metabolite oxypurinol are renally cleared, and dose reduction is mandatory in CKD to avoid severe toxicity (DRESS syndrome). Option B is incorrect — febuxostat inhibits xanthine oxidase, not uricase; option C describes URAT1 blockers (probenecid, lesinurad).

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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