Plasma Levels and Effects of Sulfinpyrazone in Patients Requiring Chronic Hemodialysis

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Abstract
Sulfinpyrazone (Anturane), which inhibits platelet synthesis of prostaglandins and platelet release of serotonin, was given to patients with chronic renal failure requiring hemodialysis. Patients were matched in double-blind fashion to receive placebo or sulfinpyrazone at 200 mg orally 3 times a day. Peak plasma levels of sulfinpyrazone after the 1st 200/mg dose ranged from 6.7-11.4 .mu.g/ml (mean: 8.7 .mu.g/ml). The plasma concentration showed a monoexponential disappearance pattern with an apparent half-life of 4 h. At steady state, sulfinpyrazone peak plasma levels were 10.7-30.1 .mu.g/ml. Residual plasma levels 12 h after a final dose while in steady state were 3.7 and 4.3 .mu.g/ml. Sulfinpyrazone protected against falls of platelet counts normally encountered during hemodialysis. Sulfinpyrazone blocked the increased platelet aggregability, and the platelet uptake and release of serotonin normally seen after dialysis. Sulfinpyrazone prevented the consumption of antithrombin III, which is normally seen with hemodialysis, without changing the anticoagulant efficacy of heparin. Sulfinpyrazone can be given to patients with chronic renal failure. It prevents platelet consumption during hemodialysis and protects against the decrement of antithrombin III normally seen during hemodialysis.