手性非甾体抗炎药物

非甾体抗炎药物是一种具有重要临床应用价值的药物，其化学结构类型多样化，多数结构是手性分子。ＮＳＡＩＤ对映异构体在药效，毒性和动力学性质上存在差别，而除了少数药物外，临床应用的手性ＮＳＡＩＤ是其外消旋体。因此在手性ＮＳＡＩＤ产品中是不中应该有Ｒ－构型是一值得讨论的问题。     

酮洛芬及其手性对映体的研究进展

<正> 自1898年人们成功合成阿司匹林以来,已经发展出一类结构不同,作用及机理相似,效果可靠,并具有广泛的非特异性抗炎、适度镇痛和解热作用的非甾体抗炎药(NSAIDs)。非甾体抗炎药中,大多数是手性药物,而手性药物在目前临床应用的药物中占有很大的比例,常用的700多种药物有一半至少含有1个手性中心,其中90％使用外消旋体。很多内源性大分     

手性药物的药动学、药效学及不良反应

本文探讨手性药物的代谢动力学及药效学特征,阐明其药理活性和不良反应实质。结果表明有些手性药物在临床上的应用是有益的,有些则会造成不良后果。因此,通过对手性药物的深入研究,对临床合理应用手性药物具有重要的意义。     

芳基丙酸类非甾体抗炎药的研究进展

六十年代初问世的新型非甾体抗炎药——芳基丙酸类,具有疗效强,毒性低,患者易于耐受等特点,是一类高效、完全的抗炎、解热、镇痛药。本文就这类药物的研究进展作一简介:1.苯氧布洛芬钙(Fenoprofen Calcium)本品消炎作用相当于阿司匹林50倍,消炎痛10倍,与中枢镇痛药吗啡、美沙酮、可待因、达尔丰有协同作用,增加镇痛效果,口服吸收85%以上,半衰期2.5～3h,与蛋白结合率99%以上。主要经肾摊泄,疗效比布洛芬好,副作用少。适用于急     

抗真菌药物的药动学和药效学研究进展

目的:介绍临床常用抗真菌药物的药动学和药效学研究进展,旨在为临床合理用药提供相关依据。方法:查阅国内、外相关文献,进行系统的阅读复习,并进行综合分析。结果:真菌感染发病复杂,诊断困难,预后较差,但是抗真菌药物研发的不断进步,为临床医生用药提供了更多选择,真菌感染的治疗和预后将逐步得到改善。结论:临床常用抗真菌药物的药动学和药效学研究,对于临床合理用药具有重要的指导意义。     

非甾体抗炎药酮洛芬及其手性对映体

非甾体抗炎药(NSAIDs)具有解热、镇痛、抗炎和抗风湿等作用.大多数NSAIDs都具有手性,它的两个对映体在体内的药理活性、代谢过程及毒性反应存在显著的差异,故以传统的消旋体给药方式带来的一些问题引起越来越广泛的关注.开发不良反应少、对环氧化酶有特异性选择作用的新一代NSAIDs已成为研究热点.该文对酮洛芬及其手性对映体在药物代谢动力学、药效学、临床应用及制剂开发的研究进行了介绍.     

Monitoring of nonsteroidal antiinflammatory drugs

Until now, little or no attention has been paid to the monitoring of therapy with nonsteroidal antiinflammatory drugs (NSAIDs). The authors discuss reasons for that situation. They emphasize that lack of monitoring of unwanted side-effects of the widely used NSAIDs is no doubt due to the overuse of these drugs. The expedience and a protocol concerning the efficacy and toxicity monitoring of such drugs are critically discussed. The authors stress that toxicity monitoring should be performed in selected patient groups that to only in those patients at risk.     

2-芳基丙酸类药物的立体选择性药效学及药动学

2 芳基丙酸类衍生物或称为洛芬类 ,包括布洛芬、萘普生、氟比洛芬和依托度酸等 ,是非甾体类抗炎药物中十分重要的一类药物。这类药物几乎全部是以消旋体形式上市的 ,而两个对映体间的药理活性、作用机制及毒理又存在很大不同。正是由于洛芬类药物所表现的丰富生物特性以及这些特性对于临床用药的指导作用 ,从而使得这类药物倍受关注。该文主要阐述以氟比洛芬为代表的洛芬类药物在药理学上的立体选择性     

Pseudoporphyria from nonsteroidal antiinflammatory drugs

Pseudoporphyria is a condition in which skin fragility and blistering typical of cutaneous porphyria are associated with normal porphyrin metabolism. Naproxen has recently been described as a cause for drug-induced pseudoporphyria and eight examples of this are reported. We also report instances from ketoprofen and diflunisal.     

Combination use of nonsteroidal antiinflammatory drugs

Polypharmacy with nonsteroidal antiinflammatory drugs (NSAIDs) is widely practiced despite being condemned by many rheumatologist. Combination use of aspirin with other NSAIDs might be discouraged for three well-documented reasons. First, aspirin reduces the blood levels of many NSAIDs. Second, multiple drugs are antagonistic or at least less than additive in animal models of inflammation. Third, there is no good clinical data to suggest that combination use of NSAIDs is beneficial. Unless new studies become available, NSAIDs should be used one at a time, with supplementary analgesics added on a prn basis.     

非甾体类抗炎药与心血管疾病的研究进展

非甾体类抗炎药（NSAIDs）是当今广泛应用的一类药物。目前许多证据表明选择性的环氧化酶-2（COX-2）抑制剂具有不良心血管作用，包括增加心肌梗死、中风、心衰和高血压的危险，对有心血管病史或高心血管疾病危险者上述不良作用可能最为明显。对上述病人，仅在没有可替代的药物时使用COX-2抑制剂，并使用最小的剂量和必需的最短的时间。普通的非选择性的环氧化酶（COX）抑制剂其心血管安全性也有待更多的证据。因此，使用NSAIDs时要注意权衡利弊。     

Update on sensitivity to nonsteroidal antiinflammatory drugs

Non steroidal antiinflammatory drugs (NSAIDs) are among the most frequently prescribed medications worldwide. These drugs are effective for the treatment of a wide spectrum of diseases: musculoskeletal disorders, headhache, fever, pain, and others. Their widespread use explains the very high incidence of intolerance; reactions range from asthma, rhinitis, to urticaria/angioedema, various skin eruptions and anaphylactic shock. The pathogenesis of intolerance is still unclear: immune-mediated reactions have been reported following the use of pyrazolone derivatives and, less commonly aspirin, anthranilic-acid derivatives and diclofenac. It has been suggested that NSAIDs may induce pseudoallergic reactions, while in case of bronchial asthma the inhibition of cyclooxigenase by NSAIDs has been proposed as a pathogenetic mechanism. The diagnosis of NSAIDs sensitivity can usually be established by history; in fact skin prick tests with NSAIDs have not been successful and no reliable in vitro tests are available. The only definitive diagnostic test is oral test dosing. To identify an alternative NSAIDs in a sensitive patient a tolerance test is performed. Here we review the current state of knowledge concerning NSAIDs sensitivity, including personal data to increase awareness on this issue.     

Induction of hemolytic anemia by nonsteroidal antiinflammatory drugs

The incidence of immune hemolytic anemia (IHA) is increasing. The proliferation of pharmaceuticals is a contributing factor to this increase. IHA is an uncommon, though significant, adverse effect of a wide variety of drugs. Several recent case reports have implicated the nonsteroidal antiinflammatory drugs (NSAIDs). Because of the extensive use of this class of drugs, a review of case reports, clinical studies, and in vitro research was conducted on NSAID-induced IHA. Mefenamic acid, ibuprofen, sulindac, naproxen, tolmetin, feprazone, and aspirin are reported to cause IHA, with mefenamic acid most frequently implicated. Mefenamic acid appears to cause hemolytic anemia by an autoimmune mechanism similar to methyldopa and aspirin by an immune complex mechanism. However, there is insufficient information concerning ibuprofen, sulindac, naproxen, tolmetin, and feprazone to assign specific mechanisms of immune hemolysis. In individuals with glucose-6-phosphate dehydrogenase (G-6-PD) deficiency, aspirin at usual therapeutic doses is not a predisposing factor to hemolysis unless other risk factors are present. Although individuals with G-6-PD deficiency are at increased risk of developing hemolytic anemia when exposed to oxidizing stresses, the use of NSAIDs does not appear to increase this risk significantly. Because NSAID-induced IHA occurs infrequently and the sensitivity of currently used tests to detect drug-dependent antibodies is limited, routine serologic testing in patients receiving NSAIDs is not justified. If hemolytic anemia occurs in a NSAID-treated patient and the history is consistent with a drug-induced etiology, the NSAID should be discontinued. With discontinuation of the offending agent, the prognosis is good. There is a rapid hematologic recovery, with a slow resolution of abnormal serologic findings.     

非甾体抗炎药在妊娠期与哺乳期应用的安全性评价

为妊娠妇女及乳母处方非甾体抗炎药时,应谨慎权衡利弊.非甾体抗炎药作为前列腺素合成抑制剂可致凝血功能异常、子宫动脉导管收缩并延长产程.水杨酸盐对动物可致畸,但沿缺乏使人致畸的依据.孕妇使用阿司匹林可致分娩时及产前、产后出血,并致新生儿患出血性疾病.一般认为吲哚美辛对胎儿的循环有影响并能致畸,但也尚有争议.而蔡普生对胎儿的循环、凝血以及肾脏功能均有影响.布洛芬、保泰松也可引起先天性缺损.因此,该类药物一般应避免使用于妊娠妇女.从物理、化学性质,药动学方面看,虽然大部分非甾体抗炎药在乳汁中的排泌率低,对乳儿的影响不大,但吲哚美辛由于半衰期长、代谢物仍有活性,乳母阿司匹林用量的21%又可通过乳汁被乳儿摄入,水杨酸盐应为乳母的禁忌药物.