Bern M M, Cavaliere B M, Lukas G
J Clin Pharmacol. 1980 Feb-Mar;20(2-3):107-16. doi: 10.1002/j.1552-4604.1980.tb02532.x.
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 mateched in double-blind fashion to receive either placebo or sulfinpyrazone at 200 mg orally three times a day. Peak plasma levels of sulfinpyrazone after the first 200-mg dose ranged from 6.7 to 11.4 micrograms/ml (mean : 8.7 micrograms/ml). The plasma concentration showed a monoexponential disappearance pattern with an apparent half-life of 4 hours. At steady state, sulfinpyrazone peak plasma levels were 10.7 to 30.1 micrograms/ml. Residual plasma levels 12 hours after a final dose while in steady state were 3.7 and 4.3 micrograms/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 following dialysis. Sulfinpyrazone prevented the consumption of antithyrombin III which is normally seen with hemodialysis, without having changed 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 antithyrombin III normally seen during hemodialysis.
磺吡酮（安妥明）可抑制血小板合成前列腺素及释放血清素，被给予需要血液透析的慢性肾衰竭患者。患者以双盲方式配对，分别接受安慰剂或每日口服3次、每次200毫克的磺吡酮。首次服用200毫克剂量后，磺吡酮的血浆峰值水平在6.7至11.4微克/毫升之间（平均：8.7微克/毫升）。血浆浓度呈单指数衰减模式，表观半衰期为4小时。在稳态时，磺吡酮的血浆峰值水平为10.7至30.1微克/毫升。在稳态下最后一剂后12小时的残留血浆水平为3.7和4.3微克/毫升。磺吡酮可防止血液透析期间通常出现的血小板计数下降。磺吡酮可阻止透析后通常出现的血小板聚集性增加以及血小板对血清素的摄取和释放。磺吡酮可防止血液透析时通常出现的抗凝血酶III的消耗，而不改变肝素的抗凝效果。磺吡酮可给予慢性肾衰竭患者。它可防止血液透析期间血小板的消耗，并防止血液透析时通常出现的抗凝血酶III的减少。
