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  • Developed in 1951 to decr. penicillin excretion but also decr. excretion of a no. other drugs (eg. indocid, methotrexate, sulphonamides, cephalosporins, active metab. of clofibrate) but uric acid is the only important endogenous compound whose excretion is incr. by probenecid;
  • It also inhibits:
    • transport of 5-HIAA & other acid metab.(& penG) from CSF to plasma;
    • biliary secretion of: indocyanine green/BSP/rifampicin;


  • peak 2-4hrs orally; T½ dose depend. = 5-8hrs; 85-95% albumin bound;
  • actively secreted in renal tubule & some unbound is filtered;
  • as high lipid soluble, almost complete reabs. by back diffus. unless lumen pH incr..
  • dose: 250mg bd 1wk → 500mg bd/qid (gout) with liberal fluid intake;

Adverse effects:

  • uncommon: GIT/HS rash; rare: GN;


  • PU; acute gout; blood dyscrasias; uric acid kidney stones; child.<2yrs old;

Huge OD:

  • CNS stim. → convulsions, resp. failure → death;
probenecid.txt · Last modified: 2008/09/30 11:42 by

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