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奥沙美辛对人体香豆素抗凝作用及血小板功能的影响。

Effects of oxametacin on coumarin anticoagulation and on platelet function in humans.

作者信息

Baele G, Rasquin K, Barbier F

出版信息

Arzneimittelforschung. 1983;33(1):149-52.

PMID:6681967
Abstract

In 12 chronically anticoagulated patients the administration of 1-p-chlorobenzoyl-5-methoxy-2-methyl-3-indoacetohydroxamic acid (oxametacin, Flogar), three times 100 mg a day, decreased the thrombotest percentage from a mean of 11.2% to a mean of 8.3% after one week and of 7.8% after two weeks of treatment. A potentiating effect of oxametacin was also found when the prothrombin time or the activated partial thromboplastin time were used as parameters. In one third of our patients an adaptation of the coumarin dose or even an interruption in the warfarin administration was necessary. Although no severe bleedings occurred, care should be taken in prescribing oxametacin to anticoagulated patients. In a second part of this study we compared the ex vivo effects of a single oral dose of 1 g of acetylsalicylic acid, 50 mg of indometacin and 100 mg of oxametacin in human volunteers. Platelet aggregation and 5HT--14C release induced by collagen. Thrombofax, ADP, adrenaline (epinephrine), bovine plasma and ristocetin were measured before, 1 and 24 h after drug administration. A clear-cut inhibitory effect as induced by acetylsalicylic acid was not found for oxametacin.

摘要

在12名长期接受抗凝治疗的患者中,给予1-对氯苯甲酰基-5-甲氧基-2-甲基-3-吲哚乙酰异羟肟酸(奥沙美辛,Flogar),每日3次,每次100mg,治疗1周后血栓试验百分比从平均11.2%降至平均8.3%,治疗2周后降至7.8%。当以凝血酶原时间或活化部分凝血活酶时间作为参数时,也发现奥沙美辛有增强作用。在我们三分之一的患者中,需要调整香豆素剂量,甚至中断华法林治疗。虽然未发生严重出血,但给抗凝患者开奥沙美辛时仍应谨慎。在本研究的第二部分中,我们比较了在人类志愿者中单次口服1g乙酰水杨酸、50mg吲哚美辛和100mg奥沙美辛的体外效应。在给药前、给药后1小时和24小时测量由胶原、血栓形成素、ADP、肾上腺素(epinephrine)、牛血浆和瑞斯托菌素诱导的血小板聚集和5HT--14C释放。未发现奥沙美辛有乙酰水杨酸所诱导的那种明显抑制作用。

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