Avouac Bernard, Combe Bernard, Darné Bernadette
Service de rhumatologie, Hôpital Henri Mondor, Cretei.
Presse Med. 2003 Nov 22;32(37 Pt 2):S38-43.
Conventional NSAIDs and aspirin have platelet-inhibiting properties via platelet cyclo-oxygenase-1 (Cox-1) isoenzyme inhibition. Among the NSAIDs which induce reversible inhibition of Cox-1, naproxen seems to have a potent platelet-inhibiting action associated with a decrease in cardiovascular clinical events in secondary prevention. Flurbiprofen is indicated in the secondary prevention after myocardial infarction. Conversely, no conventional NSAID is indicated and none have demonstrated efficacy in primary prevention. GI BLEEDING: The platelet-inhibiting action of conventional NSAIDs and aspirin is a key factor in explaining the increased risk of bleeding reported with these medicinal products. Digestive system bleeding is the main risk. Few data are available regarding bleeding other than gastro-intestinal. COX-2 SPECIFIC INHIBITION PROPERTIES: Conversely, Cox-2 specific inhibitors have no platelet-inhibiting properties: the pharmacological profile of Cox-2 SI is therefore different from that of conventional NSAIDs. These medicinal products are anti-inflammatory, analgesic, platelet-inhibiting agents which are not harmful to the GI mucosa and which probably induce less bronchospasms. In patients with cardiovascular risks, Cox-2 SI can and should be used in combination with platelet-inhibiting agents, in particular aspirin, because they do not alter the aspirin effect on platelets, contrary to what is observed with conventional NSAIDs. PRESCRIPTION WITH ANTI-COAGULANTS: The concomitant prescription of conventional NSAIDs with anti-coagulants is not recommended because, in addition to the possible potentiation of oral anti-coagulants, NSAIDs increase the risk of serious bleeding adverse events due to their irritative effect on the GI mucosa and their platelet-inhibiting effect. This risk might be lower with Cox-2 specific inhibitors.
传统非甾体抗炎药(NSAIDs)和阿司匹林通过抑制血小板环氧化酶-1(Cox-1)同工酶而具有血小板抑制特性。在诱导Cox-1可逆性抑制的NSAIDs中,萘普生似乎具有强大的血小板抑制作用,且与二级预防中心血管临床事件的减少有关。氟比洛芬适用于心肌梗死后的二级预防。相反,没有传统NSAID被批准用于一级预防,也没有证据表明其在一级预防中有效。胃肠道出血:传统NSAIDs和阿司匹林的血小板抑制作用是解释这些药物出血风险增加的关键因素。消化系统出血是主要风险。关于胃肠道以外部位出血的数据很少。Cox-2特异性抑制特性:相反,Cox-2特异性抑制剂没有血小板抑制特性:因此Cox-2 SI的药理特性与传统NSAIDs不同。这些药物是抗炎、止痛、不损害胃肠道黏膜且可能诱发较少支气管痉挛的血小板抑制药物。对于有心血管风险的患者,Cox-2 SI可以且应该与血小板抑制药物,特别是阿司匹林联合使用,因为与传统NSAIDs不同,它们不会改变阿司匹林对血小板的作用。与抗凝剂联合处方:不建议将传统NSAIDs与抗凝剂同时处方,因为除了可能增强口服抗凝剂的作用外,NSAIDs因其对胃肠道黏膜的刺激作用和血小板抑制作用而增加严重出血不良事件的风险。使用Cox-2特异性抑制剂时这种风险可能较低。