Vinge E, Corell T, Andersson K E
Eur J Clin Pharmacol. 1984;26(6):711-7. doi: 10.1007/BF00541930.
Fenflumizole (2-(2,4-difluorophenyl)-4,5-bis(4-methoxyphenyl)imidazole), a new non-steroidal anti-inflammatory drug, was given to healthy subjects in single oral doses of 0.1, 1 and 2 mg/kg. The effect of the drug was followed for up to 8 h by repeated tests of arachidonic acid-induced platelet aggregation and was related to its concomitant plasma concentration. Fenflumizole reversibly inhibited platelet aggregation and the degree of inhibition was found to be linearly correlated with the log plasma concentration. There was depression of the formation of thromboxane B2 and 6-keto-prostaglandin F1 alpha (the stable metabolites of thromboxane A2 and prostacyclin) in clotted whole blood measured by radioimmunoassay after fenflumizole 1 mg/kg. This effect was directly related to the concentration of the drug in plasma, the maximum effect being reached at fenflumizole concentrations greater than 200 ng/ml. EC50-values for inhibition of the formation of thromboxane B2 and 6-keto-prostaglandin F1 alpha were approximately 20 and 40 ng/ml, respectively. The results suggest that orally administered fenflumizole is a potent inhibitor of platelet aggregation and prostanoid formation.
芬氟咪唑（2-(2,4-二氟苯基)-4,5-双(4-甲氧基苯基)咪唑）是一种新型非甾体抗炎药，以0.1、1和2mg/kg的单次口服剂量给予健康受试者。通过对花生四烯酸诱导的血小板聚集进行重复测试，对该药物的效果进行了长达8小时的跟踪，并将其与同时测定的血浆浓度相关联。芬氟咪唑可逆性抑制血小板聚集，发现抑制程度与血浆浓度的对数呈线性相关。在给予1mg/kg芬氟咪唑后，通过放射免疫测定法测定的凝血全血中血栓素B2和6-酮-前列腺素F1α（血栓素A2和前列环素的稳定代谢产物）的生成受到抑制。这种作用与血浆中药物的浓度直接相关，在芬氟咪唑浓度大于200ng/ml时达到最大作用。抑制血栓素B2和6-酮-前列腺素F1α生成的EC50值分别约为20和40ng/ml。结果表明，口服芬氟咪唑是血小板聚集和类前列腺素生成的有效抑制剂。
