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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.

DOI:10.1002/j.1552-4604.1983.tb02717.x
PMID:6863578
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。

相似文献

1
Effects of oxaprozin alone or in combination with aspirin on hemostasis and plasma protein binding.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。
J Clin Pharmacol. 1983 Apr;23(4):139-46. doi: 10.1002/j.1552-4604.1983.tb02717.x.
2
[The inhibitory effect of oxaprozin, a new non-steroidal anti-inflammatory drug, on platelet aggregation].[新型非甾体抗炎药奥沙普秦对血小板聚集的抑制作用]
Nihon Yakurigaku Zasshi. 1984 May;83(5):395-400.
3
Effects of oral aspirin and oxaprozin on the development of lupus-like disease in MRL/1 mice.口服阿司匹林和恶丙嗪对MRL/1小鼠狼疮样疾病发展的影响。
J Immunopharmacol. 1984;6(1-2):69-78. doi: 10.3109/08923978409026459.
4
Gastroscopic evaluation of the effect of aspirin and oxaprozin on the gastric mucosa.阿司匹林和奥沙普秦对胃黏膜影响的胃镜评估。
J Clin Pharmacol. 1981 Apr;21(4):157-61. doi: 10.1002/j.1552-4604.1981.tb05694.x.
5
[The analgesic and antipyretic effects of a non-steroidal anti-inflammatory drug, oxaprozin, in experimental animals].
Nihon Yakurigaku Zasshi. 1984 Apr;83(4):345-54.
6
Naproxen-aspirin interactions in man.萘普生与阿司匹林在人体中的相互作用。
Clin Pharmacol Ther. 1974 Apr;15(4):374-9. doi: 10.1002/cpt1974154374.
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Oxaprozin disposition in renal disease.肾病中恶丙嗪的处置
Clin Pharmacol Ther. 1982 Apr;31(4):509-15. doi: 10.1038/clpt.1982.68.
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Double-blind comparison of single oral doses of oxaprozin, aspirin, and placebo for relief of post-operative oral surgery pain.单次口服奥沙普秦、阿司匹林及安慰剂缓解口腔外科术后疼痛的双盲对照研究
J Int Med Res. 1983;11(5):308-14. doi: 10.1177/030006058301100511.
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Oxaprozin dose proportionality.
J Clin Pharmacol. 1984 Nov-Dec;24(11-12):515-22. doi: 10.1002/j.1552-4604.1984.tb02761.x.
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Effects of zomepirac on hemostasis in healthy adults and on platelet function in vitro.佐美酸对健康成年人止血及体外血小板功能的影响。
J Clin Pharmacol. 1980 May-Jun;20(5-6 Pt 2):409-17.

引用本文的文献

1
Clinical pharmacokinetics of oxaprozin.奥沙普秦的临床药代动力学
Clin Pharmacokinet. 1998 Dec;35(6):425-36. doi: 10.2165/00003088-199835060-00002.
2
Oxaprozin. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy.奥沙普秦。对其药效学、药代动力学特性及治疗效果的初步综述。
Drugs. 1986 Oct;32(4):291-312. doi: 10.2165/00003495-198632040-00001.
3
Pharmacokinetic drug interactions with nonsteroidal anti-inflammatory drugs.非甾体抗炎药的药代动力学药物相互作用。
Clin Pharmacokinet. 1990 Jul;19(1):44-66. doi: 10.2165/00003088-199019010-00004.