Serlin M J, Mossman S, Sibeon R G, Tempero K F, Breckenridge A M
Clin Pharmacol Ther. 1980 Oct;28(4):493-8. doi: 10.1038/clpt.1980.193.
The effect of diflunisal on steady-state warfarin dynamics and kinetics was studied in five healthy men taking daily subtherapeutic doses of warfarin. Diflunisal 500 mg twice daily for 2 wk increased the percentage unbound warfarin from 1.02% to 1.24% and lowered total warfarin from 741 to 533 ng/ml, but did not alter the anticoagulant response (prothrombin complex activity, PCA). When diflunisal was discontinued but warfarin continued, there was a loss of anticoagulant effect and a difference in the rates at which percentage unbound warfarin and total warfarin concentration returned to prediflunisal levels. There was a correlation between plasma diflunisal and percentage unbound warfarin. Diflunisal reduced both the maximum plasma protein-binding capacity for warfarin and the apparent association constant.
在五名每日服用低于治疗剂量华法林的健康男性中,研究了双氯芬酸对稳态华法林动力学和药代动力学的影响。双氯芬酸500毫克,每日两次,服用2周,使游离华法林百分比从1.02%增至1.24%,总华法林浓度从741降至533纳克/毫升,但未改变抗凝反应(凝血酶原复合物活性,PCA)。当停用双氯芬酸但继续服用华法林时,抗凝作用丧失,游离华法林百分比和总华法林浓度恢复至双氯芬酸治疗前水平的速率存在差异。血浆双氯芬酸与游离华法林百分比之间存在相关性。双氯芬酸降低了华法林的最大血浆蛋白结合能力和表观缔合常数。