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

A 50-year-old man with recurrent gout attacks is started on probenecid for urate-lowering therapy. Which statement about probenecid is correct?

  • A It should be initiated during an acute gout flare for faster relief
  • B It is effective even when creatinine clearance falls below 30 mL/min
  • C It reduces urate formation by inhibiting xanthine oxidase
  • D It inhibits URAT1 and OAT transporters in the proximal tubule, increasing urinary urate excretion
Correct answer: D. It inhibits URAT1 and OAT transporters in the proximal tubule, increasing urinary urate excretion

Explanation

Probenecid blocks reabsorption of urate in the proximal convoluted tubule by inhibiting the URAT1 anion exchanger and organic anion transporters, making it uricosuric. It must be avoided during an acute attack and until the flare settles, since shifting urate stores can worsen the attack. Its uricosuric action requires adequate renal function and becomes ineffective at low creatinine clearance, which rules out options A and B.

Reference: Katzung's Basic and Clinical Pharmacology, 16th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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