de Boer A, Danhof M, Cohen A F, Magnani H N, Breimer D D
Centre for Human Drug Research, Leiden, The Netherlands.
Thromb Haemost. 1991 Aug 1;66(2):202-7.
Potential interactions between Org 10172 (Lomoparan, i.v. bolus injection of 3,250 anti-Xa units followed by 750 units twice daily s.c. for 8 days) and acetylsalicylic acid (ASA) (500 mg orally 14 and 2 h before i.v. Org 10172 administration) were studied in eight healthy male volunteers using an open, randomised three-way cross-over design. Except for moderate bruising at venepuncture and s.c. injection sites which were equally distributed over all three treatments (Org 10172 alone, ASA alone, Org 10172 and ASA combined), no side effects were observed. The effects of the separate drugs on several haemostatic parameters were as expected, although the prolongations in bleeding time after ASA were highly variable and tended to be somewhat more pronounced after the combination (p greater than 0.05). Org 10172 did not influence the inhibiting effects of ASA on platelet function nor the functional recovery afterwards, as evaluated by thromboxane A2 (TXA2) generation and collagen-induced platelet aggregation. Furthermore, no important interactions were observed with regard to the coagulation tests and plasma anti-Xa activity. Although this study did not entirely exclude small interactions between Org 10172 and ASA in this relatively small group of subjects, these effects are probably without clinical significance.
在8名健康男性志愿者中，采用开放、随机、三交叉设计，研究了Org 10172（洛莫帕兰，静脉推注3250抗Xa单位，随后每天皮下注射750单位，共8天）与乙酰水杨酸（ASA）（在静脉注射Org 10172前14小时和2小时口服500毫克）之间的潜在相互作用。除了在静脉穿刺和皮下注射部位出现的中度瘀伤，且在所有三种治疗（单独使用Org 10172、单独使用ASA、联合使用Org 10172和ASA）中分布均匀外，未观察到其他副作用。尽管单独使用药物对几个止血参数的影响符合预期，尽管ASA后出血时间的延长差异很大，且联合用药后往往更明显（p大于0.05）。通过血栓素A2（TXA2）生成和胶原诱导的血小板聚集评估，Org 10172既不影响ASA对血小板功能的抑制作用，也不影响其后的功能恢复。此外，在凝血试验和血浆抗Xa活性方面未观察到重要的相互作用。尽管该研究并未完全排除在这一相对较小的受试者群体中Org 10172与ASA之间存在微小相互作用，但这些影响可能无临床意义。
