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恶丙嗪单独或与阿司匹林联合使用对止血和血浆蛋白结合的影响。

Effects of oxaprozin alone or in combination with aspirin on hemostasis and plasma protein binding.

作者信息

Kahn S B, Hubsher J A

出版信息

J Clin Pharmacol. 1983 Apr;23(4):139-46. doi: 10.1002/j.1552-4604.1983.tb02717.x.

Abstract

Oxaprozin, a new nonsteroidal antiinflammatory agent, was studied alone and in combination with aspirin for its effects on hemostasis and protein binding in 10 healthy adults. When both oxaprozin and aspirin were given separately for seven days and in combination for five days, both drugs prolonged bleeding time and inhibited collagen- and epinephrine-induced platelet aggregation to a similar degree. The effects of the combination of oxaprozin and aspirin were not additive. The data from the protein binding study showed that oxaprozin was more than 99 per cent bound to plasma proteins. Aspirin displaced oxaprozin from its binding sites. As a result, the rate of plasma clearance of oxaprozin significantly increased from 20 to 26 ml/min/kg (P less than 0.05), and the plasma half-life decreased from 45 to 40 hours. Platelet count and the humoral clotting mechanism were not affected by either drug alone or in combination. There was no clinical evidence of bleeding. One subject who received oxaprozin for 12 days and, in addition, aspirin for the last five days developed a rash that subsided after both drugs were discontinued; one subject treated with aspirin experienced tinnitus. These data suggest that oxaprozin, like aspirin and other nonsteroidal antiinflammatory drugs, should be used with caution when administered to patients who have suffered trauma, who undergo surgery, or who have known defects in hemostasis.

摘要

奥沙普秦是一种新型非甾体抗炎药,对10名健康成年人单独使用及与阿司匹林联合使用时对止血和蛋白结合的影响进行了研究。当奥沙普秦和阿司匹林分别给药7天以及联合给药5天时,两种药物均使出血时间延长,并以相似程度抑制胶原和肾上腺素诱导的血小板聚集。奥沙普秦与阿司匹林联合使用的效果并非相加性。蛋白结合研究的数据表明,奥沙普秦与血浆蛋白的结合率超过99%。阿司匹林将奥沙普秦从其结合位点上置换下来。结果,奥沙普秦的血浆清除率显著从20 ml/min/kg增至26 ml/min/kg(P<0.05),血浆半衰期从45小时降至40小时。单独或联合使用两种药物均未影响血小板计数及体液凝血机制。无出血的临床证据。一名接受奥沙普秦治疗12天且在最后5天加用阿司匹林的受试者出现皮疹,在两种药物停用后皮疹消退;一名接受阿司匹林治疗的受试者出现耳鸣。这些数据提示,奥沙普秦与阿司匹林及其他非甾体抗炎药一样,在给予创伤患者、接受手术患者或已知有止血缺陷的患者时应谨慎使用。

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