Plasma levels and effects of sulfinpyrazone in patients requiring chronic hemodialysis.
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.
D001777:Blood Coagulation / Q000187:drug effects; D005342:Fibrinolysis / Q000187:drug effects; D006801:Humans; D010973:Platelet Adhesiveness / Q000187:drug effects; D010976:Platelet Count; D006435:Renal Dialysis; D012701:Serotonin / Q000097:blood; D013442:Sulfinpyrazone / Q000097:blood* / Q000494:pharmacology; D014511:Uremia / Q000097:blood
D012701:Serotonin; D013442:Sulfinpyrazone