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Pharmacology: Probenecid is a uricosuric agent. It promotes excretion of urates and inhibits tubular reabsorption, which results in a lowering of the elevated concentration of uric acid in the plasma and in slow depletion of urate tophi and deposits in the tissues.
It inhibits the tubular secretion of penicillin and usually increases penicillin plasma level by any route the antibiotic is given. A 2 fold to 4 fold elevation has been demonstrated for various penicillins. It also enhances the plasma concentration of cephalexin and cephalothin.
Probenecid also has been reported to inhibit the renal transport of many other compounds including aminohippuric acid, aminosalicylic acid, indomethacin, sodium iodomethamate and related iodinated organic acids, 17-ketosteroids, pantothenic acid, phenolsulfonphthalein, sulphonamides, and sulphonylureas.
It decreases both hepatic and renal excretion of sulfobromophthalein. The tubular reabsorption of phosphorous is inhibited in hypoparathyroid but not in euparathyroid individuals. It does not influence plasma concentration of salicylates nor the excretion of streptomycin, chloramphenicol, chlortetracycline, oxytetracycline or neomycin.
Probenecid is rapidly absorbed from the gastrointestinal tract and is extensively bound to plasma proteins.
It is metabolized by the liver and excreted in the urine mainly as metabolites. Excretion is increased in alkaline urine.
