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This problem was overcome Post Date: Sun, 12 Oct 2008 4:59:52 +0000 The first compound to receive clini-cal trial was CARINAMIDE. It proved to be effective, but the drug was secreted by the renal tubules fairly rapidly so that it was necessary to give large and frequent doses. This problem was overcome with the discovery of probenecid (Beyer et al, 1951). Autor of the post: Undefined Increasing the size Post Date: Sun, 12 Oct 2008 4:46:14 +0000 Chemistry. Various congeners of probenecid have been studied. Increasing the size of the N-alkyl substitution results in more efficient compounds. Autor of the post: Undefined Pharmacological Actions Post Date: Sun, 12 Oct 2008 4:30:51 +0000 Optimal activity ap-pears in probenecid, the N-dipropyl derivative. Gutman (1966) has reviewed the structure-activity relationship of probenecid congeners and that of other uricosuric drugs.Pharmacological Actions. Autor of the post: Undefined In higher doses than Post Date: Sun, 12 Oct 2008 4:14:13 +0000 The pharmaco-logical actions of probenecid are largely con-fined to the inhibition of the renal tubular transport of organic acids. It has been widely used in the laboratory and clinical investi-gation of the excretion of a number of sub-stances. In higher doses than are required for a uricosuric effect, probenecid also inhibits the transport of organic acids at other sites, for example, the transport system that re-moves organic acids from cerebrospinal fluid (Spector and Lorenzo, 1974). Autor of the post: Undefined Penicillin Post Date: Sun, 12 Oct 2008 3:58:59 +0000 It is a potent inhibitor of certain glycine conjugases. How-ever, its therapeutic applications have been limited principally to the modification of the renal excretion of penicillin and uric acid.Penicillin. Autor of the post: Undefined Uric Acid Post Date: Sun, 12 Oct 2008 3:47:00 +0000 In adequate concentration, probenecid completely blocks the renal tu-bular secretory transport of penicillin (see Chapter 57). This does not mean that the renal excretion of penicillin falls to zero; theantibiotic present in the glomerular filtrate is not reabsorbed by the tubules and con-tinues to be excreted in the urine.Uric Acid. Autor of the post: Undefined It is now clear Post Date: Sun, 12 Oct 2008 3:27:53 +0000 Normally a high percentage of the uric acid filtered by the glomerulus is reabsorbed by the proximal tubule; this is true even when plasma values are very much elevated. Reabsorption is due to active trans-port (see Berliner et al, 1950). It is now clear that the human proximal tubule also secretes uric acid, as does the proximal tubule of many lower animals (Gutman et al, 1959). Autor of the post: Undefined In support of this, it Post Date: Sun, 12 Oct 2008 3:15:10 +0000 Small doses of probenecid and other uri-cosuric agents, such as phenylbutazone and salicylates, actually depress the excretion of uric acid. This has been attributed to inhibi-tion of secretion (Gutman and Yii, 1958). In support of this, it has been found that pyra-zinamide, a tuberculostatic drug that reduces urate excretion in man, also blocks secretion in those species in which secretion is un-equivocally demonstrable (Yu et al, 1961). Autor of the post: Undefined Miscellaneous Substances Post Date: Sun, 12 Oct 2008 3:03:20 +0000 Large doses of probenecid, however, by de-pressing the more capacious system for re-absorption of uric acid, cause greatly en-hanced excretion (Sirota et al, 1952; for further details, see Mudge et al, 1973). This uricosuric action of probenecid is of value in the treatment of chronic tophaceous gout.Miscellaneous Substances. Autor of the post: Undefined Following intravenous administration Post Date: Sun, 12 Oct 2008 2:52:49 +0000 The renal tubular transport of certain diagnostic agents, such as iodo-pyracet and related iodinated organic acids, and of PAH and PSP is markedly depressed. In fact, the adequacy of the dose level of probenecid can be tested easily by measuring PSP excretion. Following intravenous administration of the dye, the urinary excretion in the first 15 minutes is only 20% of nor-mal because of tubular blockade by probenecid. 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