see uricosuric agents, gout

• 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;

• uncommon: GIT/HS rash; rare: GN;

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

• CNS stim. → convulsions, resp. failure → death;