浅谈非甾体抗炎药的合理使用

非甾体抗炎药是临床上常用的抗炎解热镇痛药,现已发展到结构不同种类繁多的一大类药物,广泛应用于风湿性疾病和慢性炎性关节炎、各种原因导致的发热、痛性疾病、预防心肌梗死和缺血性脑血管意外发生等。近年来由于滥用非甾体抗炎药而导致的不良反应事件不断增多,药物的安全性得到人们的广泛关注。非甾体抗炎药的合理用药具有重要的临床意义,有利于提高药物疗效,减少或规避药品不良反应。     

非甾体抗炎药物的进展

目的：对非甾体抗炎药物的发展进行介绍。方法：通过对国内外文献的分析，概述了非甾体抗炎药作用机制及主要的研究进展。结果：新型非甾体抗炎药和传统相比，具有疗效好、不良反应小的特点。结论：新型非甾体抗炎药通过结构的改变，降低药物的不良反应，为临床应用提供了更好的选择，同时也为此类药物的发展提供了一个良好的研究方向。     

我院1998～1999年非甾体抗炎药用药分析

非甾体抗炎药是治疗风湿和类风湿性关节炎的常用药,近些年来,该类药物发展很快,新的剂型不断出现,此类药物的临床适应症基本相同,但作用特点和价格各有差异,因此,如何根据患者的实际情况合理使用非甾体抗炎药,以期达到最佳疗效和最少费用,提高病人的耐受性,从而降低不良反应,这无疑是摆在我们医药工作者面前的一个值得注意的问题.本文就几种常用的非甾体抗炎药的疗效、金额排序以及我院1998-1999年此类药品的消耗情况进行分析,从加强医院药品经济管理,控制药品费用过快增长角度进行探讨,以供临床用药参考.     

非甾体抗炎药的心血管不良反应及其预防

［摘要］参考国内外相关文献，探讨非甾体抗炎药的心血管不良反应产生原因和相关因素。非甾体抗炎药的心血管不良反应产生原因与其作用机制有关；药物及患者因素可产生不同影响。应重视非甾体抗炎药的心血管不良反应，严格按药品说明书限定的适应证，合理用药。     

非甾体抗炎药的临床研究新进展

非甾体抗炎药(NSAIDs)是临床上广泛应用的一类具有解热镇痛,大部分还有抗炎、抗风湿作用的药物.非甾体抗炎药的不良反应如消化道损害,肝肾损害发生率较高,针对这些不良发应开发了许多新的药物,如非甾体缓(控)释剂、非甾体和胃肠道保护剂的复方制剂、NO型非甾体药物等.近期研究还发现,非甾体抗炎药除了传统的治疗作用外,对阿尔茨海默病、早产、癌症等疾病均有预防或治疗作用,其临床应用不断扩展.本文就非甾体抗炎药的临床研究新进展作一综述.     

几种常用非甾体抗炎药的药物经济学分析

非甾体抗炎药是治疗风湿和类风湿性关节炎的常用药，此类药物的临床适应证基本相同，但作用特点和价格各有差异。如何根据患者的情况选择和鉴别药物，使之用药更加有效、安全方便、经济，提高病人的耐受性而降低不良反应，是值得关注的问题。本文就几种常用非甾体抗炎药的...     

某院2010-2013年非甾体抗炎药物临床利用情况分析

目的：为有效反映非甾体抗炎药在某院的临床应用情况,分析其临床应用趋势,提高非甾体抗炎药应用的安全性、合理性和经济性,从经济学的角度对某院2010-2013年非甾体抗炎药物临床使用情况进行药物利用研究（DUR）。方法：采用回顾性调查方法,结合用药金额排序法、用药频度分析法、日均费用分析法和药物利用指数分析法等研究方法,对某院2010-2013年非甾体抗炎药的临床使用情况进行统计分析。结果：该院非甾体抗炎药销售金额每年小幅度增长,阿司匹林、美洛昔康等用药频度较高,除部分特异性 COX-2抑制剂外,各类常用非甾体抗炎药日均费用较低但部分药物的药物利用度不高。结论：具有选择性的非甾体抗炎药成为新的用药趋势,提高非甾体抗炎药的利用度是今后医院改革的工作重点。     

痛风的药物治疗

目前用于预防和治疗痛风的药物有：秋水仙碱，非甾体抗炎药，皮质类固醇，促尿酸排泄药和黄嘌呤氧化酶抑制剂，这些药物的作用机理不同，疗效及不良反应也有差异，需合理选用，权衡利弊。     

我院1999～2000年非甾体抗炎药用药情况分析

目的：了解本院非甾体抗炎药的产品结构和使用情况，进行临床利用评价。方法：采用用药频度(DDDs)排序、金额排序、金额排序／DDDs排序比较。结果：2年中频度排序和金额排序前10位的药品基本类同，个别品种的异军突起，正体现了此类药物的创新、发展。结论：我院非甾体抗炎药的临床应用较为合理，传统的非甾体抗炎药在临床发挥了重要作用，但其缺点也是显而易见的，随着医学的发展和病人对生活质量的高要求，开发高效、长效、低毒性的非甾体抗炎药巳势在必行。     

环氧化酶抑制药的临床应用进展

［摘要］传统非甾体抗炎药对环氧化酶（COX）的选择性较差，不良反应明显，临床应用受限。近年来，一些疗效好、不良反应低的新型非甾体抗炎药相继问世，应用于临床。该文主要综述了COX 1特异性抑制药、COX非特异性抑制药、COX 2倾向性抑制药、COX 2特异性抑制药、选择性5 LOX/COX 2双重抑制药、COX 3倾向性抑制药等6类非甾体抗炎药中的代表药物的临床应用进展。     

非甾体消炎药在术后急性疼痛治疗中的合理应用

非甾体消炎药是临床常用的解热镇痛药。它在术后多模式镇痛治疗中发挥着重要作用,但其在缓解疼痛、降低炎症反应的同时,可引起胃肠道、心血管等的不良反应。因此,只有合理应用NSAIDs,才能提高疗效,保证安全。     

Oral versus topical NSAIDs in rheumatic diseases: a comparison

Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most commonly prescribed drugs worldwide and are responsible for approximately one-quarter of all adverse drug reaction reports. NSAIDs are widely prescribed for patients with rheumatic disease--a population at increased risk for serious gastrointestinal (GI) complications. Topical administration of NSAIDs offers the advantage of local, enhanced drug delivery to affected tissues with a reduced incidence of systemic adverse effects, such as peptic ulcer disease and GI haemorrhage. NSAIDs administered topically penetrate slowly and in small quantities into the systemic circulation; bioavailability and maximal plasma NSAID concentration after topical application are generally less than 5 and 15%, respectively, compared with equivalent oral administration. Product formulation may have a dramatic impact, not only on absorption rates but also on penetration depth. Compared with oral administration, topical application leads to relatively high NSAID concentrations in the dermis. Concentrations achieved in the muscle tissue below the site of application are variable, but are at least equivalent to that obtained with oral administration. NSAIDs applied topically do reach the synovial fluid, but the extent and mechanism (topical penetration versus distribution via the systemic circulation) remain to be determined. In addition, marked interindividual variability was noted in all studies; percutaneous absorption may be strongly influenced by individual skin properties. In general, interpretation of clinical studies measuring efficacy of topical NSAIDs in rheumatic disease states is difficult because of a remarkably high placebo response rate, use of rescue paracetamol (acetaminophen), and significant variability in percutaneous absorption and response rates between patients. Overall efficacy rates attributable to topical NSAIDs in patients with rheumatic disorders ranged from 18 to 92% of treated patients. Topically applied NSAIDs have a superior safety profile to oral formulations. Adverse effects secondary to topical NSAID application occur in approximately 10 to 15% of patients and are primarily cutaneous in nature (rash and pruritus at site of application). GI adverse drug reactions are rare with topically applied NSAIDs, compared with a 15% incidence reported for oral NSAIDs. Available clinical studies suggest, but do not document, equivalent efficacy of topical over oral NSAIDs in rheumatic diseases.     

Cyclooxygenase-2 selective inhibitors

The identification of two cyclooxygenase (COX) enzymes has been a tremendous advance in understanding the role of prostaglandins in inflammation and the actions of nonsteroidal antiinflammatory drugs (NSAIDs). COX-1 activity appears to be related to "constitutive" or "housekeeping" functions in the gastric mucosa, kidney and platelets. COX-2 activity is "inducible" and generally occurs in response to a specific stimulus to enhance inflammatory actions. Current NSAIDs inhibit both COX-1 and COX-2, although the clinical benefit of NSAIDs appears to be associated with inhibition of COX-2 activity. The inhibition of COX-1 activity by NSAIDs is related to adverse side effects in general, particularly gastrointestinal toxicity. Recently, COX-2 selective inhibitors have been developed. Current data would suggest that by inhibiting COX-2 action, these agents may have efficacy similar to that of standard NSAIDs and that by not inhibiting COX-1 activity, they may have less toxicity than standard NSAIDs. Thus, these actions indicate that COX-2 selective inhibitors will have similar clinical efficacy to the traditional NSAIDs with fewer adverse side effects.     

Building a better aspirin: gaseous solutions to a century-old problem

The gastrointestinal adverse effects of nonsteroidal anti-inflammatory drugs (NSAIDs) have been recognized since shortly after the introduction of aspirin to the marketplace over a century ago. However, the underlying pathogenesis of NSAID-induced gastropathy remains incompletely understood. Advances in understanding some of the factors that contribute to the mucosal injury have provided clues for the development of safer NSAIDs. The inhibitory effects of nitric oxide (NO) on NSAID-induced leukocyte adherence were exploited in the development of NO-releasing NSAIDs. As well as eliciting less gastrointestinal damage than conventional NSAIDs, these drugs do not elevate blood pressure and show anti-inflammatory effects, additional to those of the parent drugs. Modification of other drugs in a similar manner (i.e., NO-releasing derivatives) has similarly resulted in more effective drugs. More recently, hydrogen sulphide-releasing derivatives of NSAIDs and of other drugs, have been developed, based on the observed ability of H(2)S to reduce inflammation and pain in experimental models. H(2)S-releasing NSAIDs produce negligible gastric damage and exhibit enhanced anti-inflammatory potency as compared to the parent drugs. The NO-NSAIDs and H(2)S-releasing NSAIDs represent examples of new anti-inflammatory drugs with greatly reduced toxicity and improved therapeutic activity, both created through the concept of exploiting the beneficial effects of endogenous gaseous mediators.     

Antipyretic analgesics: nonsteroidal antiinflammatory drugs, selective COX-2 inhibitors, paracetamol and pyrazolinones

Antipyretic analgesics are a group of heterogeneous substances including acidic (nonsteroidal antiinflammatory drugs, NSAIDs) and nonacidic (paracetamol, pyrazolinones) drugs. Moreover, various selective cyclooxygenase-2 (COX-2) inhibitors with improved gastrointestinal tolerability as compared with conventional NSAIDs have been established for symptomatic pain treatment in recent years. The present review summarizes the pharmacology of all of these drugs with particular emphasis on their rational use based on the diverse pharmacokinetic characteristics and adverse drug reaction profiles. Referring to the current debate, potential mechanisms underlying cardiovascular side effects associated with long-term use of COX inhibitors are discussed.     

我省部分医院解热镇痛药的产品结构调查分析

抽取有代表性的3家医院为研究单位，调查分析这些医院1993～1995年消耗的NSAIDS品种及消耗量。以了解临床上使用的NSAIDs的产品结构、预测其发展趋势。为NSAIDs新产品的开发利用和临床合理有效地选择NSAIDs提供依据。调查表明，这3家医院中NSAIDs的应用有些新的发展，某些疗效好、不良反应少的药物逐渐引入临床，但毒性大的老品种仍占一定的比例，品种结构单调，复方制剂组方雷同化，剂型以普通片剂或肠溶衣片为多见（70％）。面对这些问题，尚需加强新制剂、新品种及多种规格的制剂的开发与引进，使临床使用NSAIDS类药物品种结构更趋于合理。     

The role of COX-2 in acute pain and the use of selective COX-2 inhibitors for acute pain relief

Nonsteroidal anti-inflammatory drugs (NSAIDs) are the mainstay of therapy for the management of acute pain. Cyclooxygenase (COX) enzyme is of particular interest because it is the major target of NSAIDs. Although NSAIDs are remarkably effective in the management of pain and inflammation, their use is limited by several adverse effects including gastrointestinal bleeding and ulceration, impaired renal function, and inhibition of platelet aggregation. Discovery of a second cyclooxygenase, COX-2, led to the hypothesis that NSAID side effects could be decreased, as the inhibition of COX-2 is more directly implicated in ameliorating inflammation while the inhibition of COX-1 is related to adverse effects in the GI tract. This stimulated the development of selective COX-2 inhibitors (coxibs) that are better tolerated than nonselective NSAIDs but comparable in analgesic efficacy. This article provides an overview on the therapeutic use of selective COX-2 inhibitors for relief of acute pain, largely based on clinical trials in patients undergoing the surgical removal of impacted third molars, with focus on analgesic efficacy and the potential safety associated with their use compared to dual COX-1/COX-2 inhibitors.     

Combined lipoxygenase/cyclo-oxygenase inhibition in the elderly: the example of licofelone

One of the categories of drugs most frequently used by the elderly, and probably the most commonly self-prescribed class of drug in this age group, is NSAIDs. However, NSAIDs are one of the primary causes of adverse drug reactions and are notorious for their gastric toxicity. They also inhibit renal function and reduce the efficacy of diuretics and ACE inhibitors, drugs that are commonly used by elderly patients. Recent studies have shown that cyclo-oxygenase (COX)-2 is important in renal physiology. This means that selective COX-2 inhibitors, while undoubtedly safer than NSAIDs in terms of gastric toxicity, are not devoid of renal toxicity (in addition to their now clearly established adverse effects on coronary heart disease risk). Both the gastric and renal toxicities induced by traditional NSAIDs and selective COX-2 inhibitors seem to be related to inhibition of prostaglandin, but not leukotriene, synthesis. Maintaining the correct balance between prostaglandins and leukotrienes is essential for continuing good health, but both classes of mediators also play an important role in the pathogenesis of several diseases.Recently, a new class of anti-inflammatory drugs, the lipoxygenase (LOX)/COX inhibitors, has been developed as a means of simultaneously inhibiting the synthesis of prostaglandins, thromboxanes and leukotrienes. Inhibition of leukotriene synthesis increases anti-inflammatory efficacy, particularly in rheumatic diseases, while reducing the risk of gastric damage. The LOX/COX inhibitor licofelone, which is currently in phase III trials, is the first of this new class and in the most advanced stage of development. Preliminary data with this drug seem promising, but further well designed clinical trials of this agent in the elderly will be necessary before a final evaluation is possible.