Green David, Davies Richard O, Holmes Geoffrey I, Kohl Helga, Lee Robyn B, Reynolds Nancy, Schmid Frank R, Ts'ao Chung-Hsin
Atherosclerosis Program, Rehabilitation Institute of Chicago, the Section of Arthritis-Connective Tissue Diseases, Department of Medicine and Department of Pathology, Northwestern University Medical School, Chicago, and Merck Sharp & Dohme Research Laboratories, West Point, Pennsylvania.
Pharmacotherapy. 1983 Mar;3(2 Pt 2):65S-69S. doi: 10.1002/phar.1983.3.2p2.65.
The effects of diflunisal, a nonacetylated difluorinated salicylate, on platelet function were compared with those of aspirin and placebo. In a randomized, double-blind trial, normal subjects were given diflunisal, 250, 500, or 1,000 mg twice daily; aspirin, 650 or 1,300 mg twice daily; or placebo for 8-day periods. Diflunisal, 250 mg, had no effect on platelet function, whereas 500 mg induced minimal inhibition of collagen-induced release of platelet serotonin, and 1,000 mg inhibited platelet malondialdehyde production, moderately prolonged template bleeding times (p = NS), and increased fecal blood loss (p < 0.05). In contrast, aspirin, 650 mg, markedly inhibited collagen-induced platelet aggregation and serotonin release, and 1,300 mg prolonged bleeding time (p < 0.01) and increased fecal blood loss (p < 0.01). The effects of aspirin lasted for up to 5 days, whereas changes induced by diflunisal had returned to baseline 24 hours after the drug was discontinued. We conclude that in doses in the same range as those of aspirin diflunisal inhibits platelet function less.
将一种非乙酰化二氟水杨酸(双氟尼酸)对血小板功能的影响与阿司匹林和安慰剂进行了比较。在一项随机双盲试验中,正常受试者分别每日两次给予250、500或1000毫克双氟尼酸;650或1300毫克阿司匹林;或安慰剂,为期8天。250毫克双氟尼酸对血小板功能无影响,而500毫克可引起对胶原诱导的血小板5-羟色胺释放的最小抑制,1000毫克可抑制血小板丙二醛生成,适度延长模板出血时间(p=无显著性差异),并增加粪便失血量(p<0.05)。相比之下,650毫克阿司匹林可显著抑制胶原诱导的血小板聚集和5-羟色胺释放,1300毫克可延长出血时间(p<0.01)并增加粪便失血量(p<0.01)。阿司匹林的作用可持续长达5天,而双氟尼酸引起的变化在停药后24小时已恢复至基线水平。我们得出结论,在与阿司匹林相同剂量范围内,双氟尼酸对血小板功能的抑制作用较小。