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Some degree of gastrointestinal irritation Post Date: Sat, 11 Oct 2008 23:51:58 +0000 Untoward Reactions and Precautions.Probenecid is well tolerated by most patients.Some degree of gastrointestinal irritation is experienced by at least 2% of patients; the incidence is considerably higher after large doses. Autor of the post: Undefined More serious hypersensitiv-ity reactions occur Post Date: Sat, 11 Oct 2008 23:39:16 +0000 Cautious administration is advised in patients with a history of peptic ulcer. Most reports place the incidence of hypersensitiv-ity reactions, usually mild skin rashes, be-tween 2 and 4%. More serious hypersensitiv-ity reactions occur, but they are rare. Autor of the post: Undefined The compound also increases Post Date: Sat, 11 Oct 2008 23:26:32 +0000 The appearance of a rash during the concurrent administration of probenecid and penicillin G or a congener presents the physician with an awkward diagnostic dilemma. The hazard of intrarenal precipitation of uric acid during uricosuric therapy is discussed below. The compound also increases to some degree the concentration of sulfonamide in the blood. Autor of the post: Undefined Despite its therapeutic efficacy Post Date: Sat, 11 Oct 2008 23:15:12 +0000 Huge overdosage of probenecid results in stimulation of the central nervous system, convulsions, and death from respiratory fail-ure (McKinney et al, 1951).SULFINPYRAZONEHistory. Despite its therapeutic efficacy as an anti-inflammatory and uricosuric agent, phenylbuta-zone (see Chapter 17) has undesirable side effects severe enough to preclude its continuous use in the treatment of chronic gout. Autor of the post: Undefined Since active metabolites of phenylbutazone Post Date: Sat, 11 Oct 2008 23:04:20 +0000 For this reason, a number of chemical congeners were evaluated for uricosuric and anti-inflammatory activity. One of these, in which a phenyl-thioethyl configuration replaces the butyl side chain of the parent compound, displayed promising activity. Since active metabolites of phenylbutazone were known to be formed, the metabolites of the new compound were also isolated and studied. Autor of the post: Undefined The chemical structure of sulfin-pyrazone Post Date: Sat, 11 Oct 2008 22:49:30 +0000 It was found that side chain oxidation in vivo led to the formation of the sulfoxide, sulfin-pyrazone, a potent uricosuric agent (Burns et al, 1957; Ytt et al, 1958).Chemistry. The chemical structure of sulfin-pyrazone is as follows: SulfinpyrazoneIt is a strong organic acid (pKa 2,8) that readily forms soluble salts. Autor of the post: Undefined Sulfinpyrazone in sufficient dosage Post Date: Sat, 11 Oct 2008 22:37:59 +0000 Burns and coworkers (1958) studied a number of congeners; they found that a low pKa and polar side chain substitutions favor uricosuric activ-ity (see also Gutman, 1966).Pharmacological Actions. Sulfinpyrazone in sufficient dosage is a potent inhibitor of the renal tubular reabsorption of uric acid. Autor of the post: Undefined Its uricosuric action is additive Post Date: Sat, 11 Oct 2008 22:18:39 +0000 As with other uricosuric agents, small doses may reduce the excretion of uric acid, pre-sumably by inhibiting secretory but not re-absorptive transport. By competitive inhibi-tion, sulfinpyrazone reduces the renal tubular secretion of other organic anions such as PAH and salicylic acid. Its uricosuric action is additive to that of probenecid and phenylbutazone but is mutually antagonistic to that of the salicylates (Yu et al, 1963). Autor of the post: Undefined Sulfinpyrazone lacks the clinically striking anti-inflammatory Post Date: Sat, 11 Oct 2008 22:07:04 +0000 Sulfinpyrazone possesses to an unusual de-gree the ability to displace other organic anions that are bound extensively to plasma proteins (e g, sulfonamides, salicylates), thus altering their distribution to tissues and their renal excretion (Anton, 1961). The extent to which this property may be a clinical asset or liability depends on concomitant medica-tion.Sulfinpyrazone lacks the clinically striking anti-inflammatory and analgesic properties of its congener, phenylbutazone. Autor of the post: Undefined Absorption, Fate, and Excretion Post Date: Sat, 11 Oct 2008 21:53:24 +0000 Platelet Aggregation. The effect of sulfin-pyrazone on platelet function is discussed in Chapter 65.Absorption, Fate, and Excretion. 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