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The half-life of the drug Post Date: Sat, 11 Oct 2008 21:41:48 +0000 Sulfin-pyrazone is well absorbed after oral adminis-tration. It is bound to plasma proteins to the extent of 98 to 99%. The half-life of the drug in plasma after its intravenous injection is about 3 hours. Autor of the post: Undefined Approxi-mately half of the orally Post Date: Sat, 11 Oct 2008 21:27:55 +0000 After oral administration, however, its uricosuric effect may persist for as long as 10 hours. Although little sulfin-pyrazone is available for filtration at the glomerulus, it is secreted by the proximal tubule and undergoes little passive back diffusion because of its low pA"a. Approxi-mately half of the orally administered dose appears in the urine within 24 hours. Autor of the post: Undefined Sulfinpyrazone, USP (ANTURANE), is available Post Date: Sat, 11 Oct 2008 21:13:54 +0000 Most of the drug (90%) in the urine is unchanged; the remainder is eliminated as the N1-/?-hydroxyphenyl metabolite, which also is a potent uricosuric substance. (For details, see Burns et al, 1957, 1958; Gutman et al, 1960; Dayton et al, 1961,)Preparations and Dosage. Sulfinpyrazone, USP (ANTURANE), is available as official 100-mg tablets and 200-mg capsules. Autor of the post: Undefined This may require from 100 Post Date: Sat, 11 Oct 2008 20:54:55 +0000 For the treatment of chronic gout, the initial dosage is 100 to 200 mg per day. After the first week, the dose may be gradually in-creased until a satisfactory lowering of plasma uric acid is achieved and maintained. This may require from 100 to 400 mg per day, divided in two to four doses and preferably given with meals. Autor of the post: Undefined In responsive patients not requiring Post Date: Sat, 11 Oct 2008 20:35:55 +0000 Occasional resistant patients have been treated successfully with doses as high as 800 mg per day. Larger doses are poorly tolerated and unlikely to produce a further uricosuric effect in the resistant patient. In responsive patients not requiring high dosage, a single daily dose of 100 mg is sometimes satisfactory for mainte-nance. Autor of the post: Undefined Its frequency and severity increase Post Date: Sat, 11 Oct 2008 20:21:59 +0000 Untoward Reactions and Precautions.Gastrointestinal irritation occurs in 10 to 15% of all patients receiving sulfinpyrazone, and an occasional patient may require discon-tinuance of its use. Its frequency and severity increase with dosage. Autor of the post: Undefined Hypersensitivity reac-tions, usually a rash Post Date: Sat, 11 Oct 2008 20:03:59 +0000 Gastric distress is lessened when the drug is taken in divided doses with meals. Sulfinpyrazone should be given to patients with a history of peptic ulcer only with the greatest caution and careful observation. Hypersensitivity reac-tions, usually a rash with fever, do occur, but less frequently than with probenecid. Autor of the post: Undefined Adequate precautions must also Post Date: Sat, 11 Oct 2008 19:44:58 +0000 The severe blood dyscrasias and salt and water retention, hazards of phenylbutazone ther-apy (see Chapter 17), have not been observed during sulfinpyrazone therapy. However, the ability of the drug to depress hematopoiesis has been demonstrated experimentally, and periodic blood-cell counts are therefore ad-vised during prolonged therapy. Adequate precautions must also be taken to prevent intrarenal precipitation of urates (see below). Autor of the post: Undefined The drug also resembles probenecid Post Date: Sat, 11 Oct 2008 19:30:41 +0000 Diagnostic procedures depending on the renal tubular secretion of PAH, PSP, and other organic acids are invalidated by sulfin-pyrazone therapy. The effects of sulfinpyra-zone on the renal elimination of other drugs are very similar to those of probenecid. The drug also resembles probenecid in that its uricosuric action is antagonized by salicy-lates. Autor of the post: Undefined However, their use as uricosuric Post Date: Sat, 11 Oct 2008 19:16:06 +0000 OTHER DRUGSA number of drugs having primary pharmaco-logical actions completely unrelated to uric acid metabolism or renal function show moderate-to-marked uricosuric activity. Notable among these are certain anticoagulant coumarins and indandiones and oral hypoglycemic drugs of the sulfonylurea group. However, their use as uricosuric agents is precluded because of the inappropriateness of their primary effects. 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