probenecid
Table of Contents
Probenecid
see uricosuric agents, gout
Summary
- 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;
P/K:
- 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;
C/I:
- 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 127.0.0.1