College of Pharmacy, Gulf Medical University, Post Box: 4184, Ajman, United Arab Emirates.
Medical University of South Carolina Drug Information Center, Charleston, SC, USA.
Am J Cardiovasc Drugs. 2017 Oct;17(5):343-346. doi: 10.1007/s40256-017-0223-6.
Non-steroidal anti-inflammatory drugs (NSAIDs) were differentiated from steroidal anti-inflammatory medicines to help clinicians who needed to use anti-inflammatory agents that were safer than steroids. With market entry of rofecoxib in 1999, NSAIDs were then further classified into traditional NSAIDs and cyclooxygenase (COX)-2 inhibitors (coxibs), the latter posing potentially fewer gastrointestinal risks. In 2005, rofecoxib was withdrawn from the market because of concerns about the risk of heart attack and stroke with long-term use, and clinical practice began focusing more on the cardiovascular versus gastrointestinal safety of coxibs. Since then, many coxibs have remained unapproved by the US FDA or have been removed from the market. This article explains how coxibs refocused attention on the cardiovascular safety of NSAIDs and the general implications of that. COX-2 activity/specificity is one factor associated with increased cardiovascular risks; however, these risks cannot be attributed to coxibs alone. The traditional NSAIDs (i.e., meloxicam, etodolac, and nabumetone) have significant COX-2 specificity, but naproxen and ibuprofen have less specificity. All NSAIDs, whether traditional or a coxib, pose some cardiovascular risks. It is possible that clinicians continue to focus more on decreasing the immediate gastric risks than preventing the later cardiovascular risks. The cardiovascular risks posed by NSAIDs should not be disregarded for the sake of achieving gastrointestinal benefits. Current recommendations suggest NSAIDs should be considered a single class of non-aspirin NSAIDs. Preferred NSAIDs are ibuprofen and naproxen. Coxibs are preferred in patients with low cardiovascular risk and high gastrointestinal risk who are intolerant to anti-dyspepsia therapy.
非甾体抗炎药（NSAIDs）与甾体抗炎药区分开来，是为了帮助临床医生使用比类固醇更安全的抗炎药物。1999 年罗非昔布上市后，NSAIDs 进一步分为传统 NSAIDs 和环氧化酶（COX）-2 抑制剂（coxibs），后者胃肠道风险较低。2005 年，由于担心长期使用罗非昔布会增加心脏病发作和中风的风险，该药物被撤出市场，临床实践开始更加关注 coxibs 的心血管安全性与胃肠道安全性。此后，许多 coxibs 未获美国 FDA 批准或已退出市场。本文解释了 coxibs 如何重新引起人们对 NSAIDs 心血管安全性的关注，以及这一情况的普遍影响。COX-2 活性/特异性是与心血管风险增加相关的一个因素；然而，这些风险不能仅仅归因于 coxibs。传统 NSAIDs（如美洛昔康、依托度酸和萘丁美酮）具有显著的 COX-2 特异性，但萘普生和布洛芬特异性较低。所有 NSAIDs，无论是传统 NSAIDs 还是 coxibs，都存在一定的心血管风险。临床医生可能会继续更加关注降低即时胃风险，而不是预防后期心血管风险。为了获得胃肠道益处而忽视 NSAIDs 带来的心血管风险是不妥的。目前的建议表明，应将 NSAIDs 视为非阿司匹林 NSAIDs 单一类别。首选 NSAIDs 为布洛芬和萘普生。对于不耐受抗消化不良治疗且心血管风险低但胃肠道风险高的患者，coxibs 是首选。
