Rossi E C, Levin N W
J Clin Invest. 1973 Oct;52(10):2457-67. doi: 10.1172/JCI107437.
The evidence indicating that platelets may play a role in the occurrence of certain thromboembolic phenomena has stimulated a search for inhibitors of platelet function. This report presents data to indicate that nitrofurantoin is a potent inhibitor of primary ADP-induced platelet aggregation. The addition of 10 muM nitrofurantoin to citrated platelet-rich plasma obtained from 12 normal subjects produced a 29+/-6% (2 SD) inhibition of the velocity of platelet aggregation induced by 2 muM ADP. The inhibitory effect of nitrofurantoin demonstrated competitive kinetics in respect to ADP. The intravenous (180 mg) or oral (200 mg) administration of nitrofurantoin produced a serum nitrofurantoin concentration ranging from 2.7 to 23 muM in 28 normal subjects. Platelet-rich plasma obtained from these subjects demonstrated inhibition of the velocity of ADP-induced platelet aggregation that correlated with the log of the serum nitrofurantoin concentration (P < 0.001). Collagen-induced platelet aggregation was also inhibited in a dose-related manner, and the bleeding time was significantly prolonged in the two subjects with the highest serum nitrofurantoin concentration. These studies indicate that nitrofurantoin in vivo inhibits platelet function to a degree that is proportional to the serum nitrofurantoin concentration.
有证据表明血小板可能在某些血栓栓塞现象的发生中起作用，这激发了人们对血小板功能抑制剂的探索。本报告提供的数据表明，呋喃妥因是原发性ADP诱导的血小板聚集的有效抑制剂。向从12名正常受试者获得的枸橼酸化富血小板血浆中加入10μM呋喃妥因，可使2μM ADP诱导的血小板聚集速度受到29±6%（2个标准差）的抑制。呋喃妥因的抑制作用在ADP方面表现出竞争性动力学。在28名正常受试者中，静脉注射（180mg）或口服（200mg）呋喃妥因后，血清呋喃妥因浓度范围为2.7至23μM。从这些受试者获得的富血小板血浆显示，ADP诱导的血小板聚集速度受到抑制，且与血清呋喃妥因浓度的对数相关（P<0.001）。胶原诱导的血小板聚集也呈剂量依赖性抑制，在血清呋喃妥因浓度最高的两名受试者中，出血时间显著延长。这些研究表明，体内呋喃妥因抑制血小板功能的程度与血清呋喃妥因浓度成正比。
