非甾体抗炎药的胃肠损害及其防治

非甾体抗炎药(NSAIDs)是一大类不含皮质激素而具有抗炎、镇痛、解热作用的药物,其临床应用极为广泛,是仅次于抗感染药的第二大类药.NSAIDs的不良反应也相当常见,主要是胃肠道和肾的损害.NSAIDs对正常肾脏的影响较少,即在没有肾脏危险因素时,NSAIDs对肾脏的副作用很小,而在有肾脏危险因素存在时,几乎所有NSAIDs的肾脏副作用都相似.因此提高NSAIDs安全性的重点主要是针对NSAIDs的胃肠损害.     

术后急性疼痛药物治疗的不良反应及其防治

控制术后急性疼痛的一线药物主要包括麻醉性镇痛药、非甾体消炎药(NSAIDs)及用于神经阻滞的局部麻醉药。临床医生在关注镇痛效果的同时,还应当注意可能发生的不良反应,并及时处理。     

非甾体抗炎药临床作用及副作用研究新进展

非甾体抗炎药(non-steroid anti-inflammtory drugs,NSAIDs)是众所周知的急、慢性风湿性疾病的治疗一线药,据估计全球大约有5亿人在使用NSAIDs,是仅次于抗生素、维生素的第三大类药.     

非甾体抗炎药在某院临床的应用分析

目的分析我院非甾体抗炎药(NSAIDs)的应用状况,为临床合理用药提供参考。方法对我院2005年至2007年NSAIDs的用药频度(DDDs)、每日药费(DDDc)、购药金额等进行统计、分析。结果NSAIDs的品种、数量及金额等逐年增长;DDDs排序前2位的药品为阿司匹林肠溶片和尼美舒利胶囊;购药金额排序较前的药品为尼美舒利胶囊、醋氯芬酸胶囊和复方锌布颗粒,消耗金额增幅最大的是醋氯芬酸胶囊。结论传统的NSAIDs依然占主导地位,特异性COX2抑制剂应用广泛,发展前景好;我院NSAIDs的应用基本合理。     

非甾体类抗炎药致胃溃疡药学分析

目的：探讨非甾体类药（NSAIDs）相关性溃疡的发病机理、相关因素、预防治疗。方法：从NSAIDs致溃疡临床表现、分析发病机理、相关因素和预防治疗。结果：根据患者情况，合理选用NSAIDs药物和其它药物可减少NsAIDs致胃溃疡的风险，防止胃溃疡发生。结论：NSAIDs是诱发消化性溃疡的重要病因，需长期服用NSAIDs的高危患者，要同时服用两种以上NSAIDs或与糖皮质激素同服者应给予预防性治疗，可减少NSAIDs致胃溃疡的风险，防止胃溃疡发生。     

麻醉药的不良反应与相互作用

全身麻醉药分为吸入麻醉药和静脉麻醉药。吸入麻醉药有两种：一种是挥发性液体,如乙醚、异氟烷等;另一种是气体,如氧化亚氮。静脉麻醉药为非挥发性的全麻药,主要由静脉给药。局部麻醉药：在临床上应用第一个局麻药是可卡因（1884年）,由于吸收生毒性较大,使用上受到很大限制。     

非甾体抗炎药的合理应用

非甾体抗炎药(NSAIDs)在临床中一直是治疗类风湿性关节炎的一线药NSAIDs,通过抑制环氧化酶(COX)的活性以减少花生四烯酸代谢为前列腺素,达到控制关节肿痛的目的,临床特点是起效快,可迅速减轻炎症肿胀,缓解疼痛和改善功能。但此药引起不良反应等毒副作用发生。所以NSAIDs在临床应进行系统分析,合理选择使用,掌握用药原则,注意剂量与疗程,提高NSAIDs的疗效与用药安全。     

麻醉药不是麻醉药品抗精神病药不是精神药品

麻醉药不是麻醉药品抗精神病药不是精神药品汪学胜（湖北省长阳县药品检验所４４３５００）我们在对医疗单位药品检查时发现，有一些医疗单位和个人不能正确区别麻醉药与麻醉药品，抗精神病药与精神药品。将不需要实行特殊管理的麻醉药、抗精神病药当作麻醉药品、精神药品...     

双氯灭痛引起昏迷1例临床分析

双氯灭痛为非甾体类抗感染药（NSAIDs）,抑制机体内前列腺素（PG）的生物合成,有解热、镇痛的作用。应用NSAIDs时,在使用时应选用毒性最小的NSAIDs,用最低的有效剂量和尽可能短的持续时间。尤其老年人及小儿用药应加强观察以确保用药安全。     

非甾体抗炎药的不良反应及预防

非甾体抗炎药（NSAIDs）是一类具有抗炎、解热和镇痛作用的药物，在临床上广泛用于骨关节炎、类风湿关节炎和多种免疫功能紊乱的炎症性疾病（如牙痛、头痛、痛经及肌肉痛）症状的缓解，是全世界范围内使用最广泛的药物种类之一。据统计，全球大约每天有3000万人在使用NSAIDs。同样，在国内NSAIDs的销量仅次于抗感染药。位居第二。随着NSAIDs使用的增多，其不良反应病例也在增加。有关统计表明。使用NSAIDs的人群中，有20％～25％出现了不同程度的不良反应，在所有药物不良反应报道中，NSAIDs占25％。所以，这类药的安全使用问题也越来越受到临床医师、药师、患、社会的关注。特别是默沙东制药公司于2004年9月30日宣布了主动从全球市场撤回罗非昔布（万络），2005年4月7日，美国食品药品监督管理局（rDA）公布关于NSAIDs的新安全措施．宣布了上市的NSAIDs都必须在其说明书上注明“具有增加心血管事件和胃肠道出血危险”的警告，这使NSAIDs安全用药成为目前医药界的热点问题。     

Novel treatments for pain

At present, the principal treatments for pain are non-steroidal anti-inflammatory drugs (NSAIDs) and opioids, but both of these classes suffer from drawbacks in clinical use. Some of the NSAIDs are associated with gastric damage as well as kidney and liver toxicity, and an increase in blood clotting time, while the opioids can produce tolerance and dependence, along with constipation, nausea, respiratory depression and sedation. In certain cases, both NSAID and opioid use are ineffective. There are some other less commonly used treatments including local anesthetics, anticonvulsants and tricyclic antidepressants, but, many recent strategies have involved the search for other NSAIDs and opioids which lack the unwanted side-effects present in both classes of drug. More recently, in addition to the classical strategies, some novel approaches have started to produce compounds which have entered the clinic, including cyclooxygenase-2 (COX-2) inhibitors and modulators of the alpha2delta subunit of L-type calcium channels.     

Postoperative pain control in children: a guide to drug choice

Postoperative pain in children can usually be well controlled with a combination of analgesics, including acetaminophen (paracetamol), NSAIDs, opioids, and local/regional anesthesia. Recent research has shown that the dosage of acetaminophen required to provide analgesia is higher than the traditional dosages used for the regulation of elevated body temperature. Rectal administration of acetaminophen gives a lower and more variable bioavailability compared with oral administration. There is growing experience with the use of NSAIDs in children and several studies have demonstrated the relatively strong analgesic potential of these drugs. Titration of opioids to analgesic effect, and the use of nurse- and patient-controlled continuous opioid infusions in children have gained widespread use and, with proper education and supervision, are considered excellent methods of pain control. Local peripheral and central blocks decrease the need for anesthetics during surgery and provide effective postoperative pain relief.     

Drug interaction considerations in the therapeutic use of carbonic anhydrase inhibitors

Introduction: Carbonic anhydrase inhibitors (CAIs) of the sulfonamide and sulfamate type are clinically used drugs as diuretics, antiglaucoma, antiepileptic, antiobesity and anti-high altitude disease agents. Anticancer agents based on CAIs are also in clinical development for the management of hypoxic, metastatic tumors. Acetazolamide, methazolamide, dichlorophenamide, dorzolamide and brinzolamide are mainly used as antiglaucoma drugs, sulthiame, topiramate and zonisamide as antiepileptic/antiobesity agents, celecoxib and polmacoxib are dual carbonic anhydrase/cycloxygenase inhibitors. Girentuximab, a monoclonal antibody and SLC-0111, a sulfonamide inhibitor, are in clinical trials as anticancer agents.

Areas covered: The drug interactions with many classes of pharmacological agents are reviewed. Some of these drugs, such as acetazolamide, topiramate and celecoxib show a large number of interactions with non-steroidal anti-inflammatory drugs (NSAIDs), diuretics, antiepileptics, immunosupressants, anticholinesterase drugs, β-blockers, anesthetics, oral contraceptives, anticancer agents, antifungals, anti-mycobacterials, lithium, metformin and clopidogrel.

Expert opinion: The multiple drug interactions in which CAIs are involved should be carefully considered when such drugs are used in combination with the drug classes mentioned above, as the risks of developing toxicity and serious side effects if the dosages are not adjusted are high. There are also synergistic effects between CAIs and some NSAIDs, anticancer agents and benzodiazepines for the management of cystoid macular edema, some tumor types and neuropathic pain, respectively.     

Strategy for development of NSAIDs with lower risk for side effects

Nonsteroidal antiinflammatory drugs (NSAIDs) are one of the most frequently used classes of medicines worldwide. The major clinical problem encountered with the use of NSAIDs is gastrointestinal complications. In the USA, about 16,500 people per year die as a result of NSAID-associated gastrointestinal complications. COX-2-specific NSAIDs have been developed as safer for the gastrointestinal tract, although the risk of cardiovascular thrombotic disease has recently been noted with the use of COX-2-specific NSAIDs. To find the strategy for the development of gastrointestinally safe NSAIDs other than COX-2-specific NSAIDs, we examined the molecular mechanism for NSAID-induced gastric ulcer formation. We found that NSAIDs induce gastric mucosal cell death in a manner independent of COX inhibition and that this cytotoxic effect is due to their membrane permeabilization activity, which is not required for the antiinflammatory activity of NSAIDs. Furthermore, we showed that in addition to COX inhibition by NSAIDs, direct cytotoxicity of NSAIDs is required for NSAID-induced gastric ulcer formation. These results suggest that NSAIDs that have neither membrane permeabilization activity nor COX-2 specificity would be safe for both the gastrointestinal tract and cardiovascular system and we are now chemically synthesizing such NSAIDs.     

Use and costs of anti-secretory and cardiovascular co-medication in osteoarthritis patients treated with selective or non-selective NSAIDS

Objective This study aims to compare use and costs of anti-secretory and cardiovascular co-medication in osteoarthritis patients treated with selective or non-selective NSAIDs.Method A retrospective study examined Belgian patients aged 65 years or more who suffer from osteoarthritis and are chronic users of selective NSAIDs (n = 1,376) or non-selective NSAIDs (n = 8,482). A before-and-after analysis compared drug use and costs between period 1 (first 6 months of 2002) and period 2 (several 1-year periods stretching over 2003–2004). A cohort analysis contrasted patients taking selective NSAIDs with patients taking non-selective NSAIDs.Main outcome measures Anti-secretory co-medication included histamine H2-receptor antagonists and proton pump inhibitors. Cardiovascular co-medication referred to cardiac glycosides, anti-arrhythmics, anti-thrombotics, anti-angina drugs, anti-hypertensive drugs and serum-lipid-reducing drugs. Volume of drug use was expressed as number of packages and costs were computed in Euro.Results The volume of anti-secretory co-medication increased by 36% with selective NSAIDs and by 55% with non-selective NSAIDs between periods 1 and 2. Cardiovascular co-medication rose by 18% with selective NSAIDs and by 12% for non-selective NSAIDs. Focusing on patients who did not take anti-secretory co-medication in period 1, patients taking selective NSAIDs were just as likely to start anti-secretory co-medication in period 2 as patients taking non-selective NSAIDs (odds ratio: 1.05; 95% confidence interval: 0.90–1.23). Patients taking selective NSAIDs were just as likely to start cardiovascular co-medication as patients taking non-selective NSAIDs (odds ratio: 1.03; 95% confidence interval: 0.78–1.36). Annual costs of treating osteoarthritis in ambulatory care amounted to 756 € with selective NSAIDs and 416 € with non-selective NSAIDs. This originated from higher acquisition costs (278 € vs. 24 €) and higher costs of co-medication (477 € vs. 392 €) with selective NSAIDs.Conclusions The use of selective and non-selective NSAIDs is accompanied by a higher use of co-medication over time. The increase in anti-secretory co-medication was more prominent with non-selective NSAIDs. The rise in cardiovascular co-medication was more pronounced with selective NSAIDs. Treatment of osteoarthritis with selective NSAIDs is more expensive than with non-selective NSAIDs in terms of acquisition costs and costs of co-medication.     

麻醉药临床研究与应用新进展

目的:探讨麻醉药的临床应用情况及发展趋势。方法:结合临床实践,介绍在当代麻醉学发展中具有里程碑意义的几类新型麻醉药:水溶性异丙酚、静脉注射用乳化吸入麻醉药、氙气和新型肌松药拮抗药Sugammadex。结果:与传统麻醉药相比,新型麻醉药或通过剂型改造或通过新型机制,不仅增加了药效,降低了不良反应,还扩大了应用范围。有些药物更适合于门诊手术麻醉,为实施安全舒适的临床麻醉提供了保证。结论:作为新型药物,其潜在的不良反应还需深入观察;新型麻醉药的使用也对临床麻醉监测和管理理念的更新提出了更高要求。     

吸入麻醉药“浓度效应”的定量分析

目的:对吸入麻醉药的浓度效应做出定量分析。方法:利用热力学的宏观理论和高等数学的思维方法,分三个层面讨论浓度效应:肺泡内麻醉药的浓度与吸入浓度的关系;肺泡内麻醉药的分压与吸入浓度的关系;血液中麻醉药的分压与吸入浓度的关系。结果:吸入浓度越高,肺泡内麻醉药的浓度升高越快,肺泡内麻醉药的分压和血中麻醉药的分压也上升的越快。结论:浓度效应的存在能用数学物理的方法给予证明。     

非甾体类抗炎药致上消化道出血的临床分析

目的探讨非甾体类抗炎药(NSAIDs)致上消化道出血的临床特点。方法对182例上消化道出血患者的临床资料进行回顾性分析,根据出血前1周内是否服用过NSAIDs,将患者分为NSAIDs组(43例)和非NSAIDs组(139例)。对比分析两组患者的临床资料。结果两组比较,NSAIDs组与非NSAIDs组在年龄、溃疡类型等方面差异有统计学意义。结论应加强对NSAIDs相关性上消化道出血临床特点的认识,以减少NSAIDs的不良反应。     

Risks versus benefits of cyclooxygenase-2-selective nonsteroidal antiinflammatory drugs.

PURPOSE: A summary of the basic science underlying the current controversies regarding cyclooxygenase-2 (COX-2)-selective nonsteroidal antiinflammatory drugs (NSAIDs), including data on their cardiovascular safety, their gastrointestinal (GI) benefits, cost-effectiveness, physician-prescribing trends, and recommendations for prescribing these agents is presented. SUMMARY: A number of randomized controlled trials (RCTs) have reported that COX-2-selective NSAIDs increase cardiovascular events, although there appear to be gradations of risks among the COX-2-selective NSAIDs. In addition, traditional NSAIDs may increase the risk for cardiovascular events, complicating the interpretation of RCTs that use traditional NSAIDs as comparators. Selective inhibitors of COX-2-selective NSAIDs are effective antiinflammatory and analgesic drugs with improved upper-GI safety compared to traditional NSAIDs. Data on the cost-effectiveness of COX-2-selective NSAIDs indicate that they should be limited to patients at high risk for upper-GI adverse effects. However, they had been increasingly used in patients with lower GI risks until recent events reversed that trend. Circumstances under which COX-2-selective NSAIDs may be appropriate are in patients at high GI risk and in patients who did not respond to multiple traditional NSAIDs. The national spotlight in the United States on NSAID-related adverse events and recent lawsuits against health care providers prescribing COX-2-selective NSAIDs further highlights the need for provider-patient communication and risk disclosure. The relative cardiovascular risks of NSAIDs are similar in magnitude to other currently prescribed therapies. CONCLUSION: Health care providers must consider the efficacy, GI and cardiovascular risks, concomitant medications, and costs when determining the appropriateness of COX-2-selective NSAID therapy.