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The topical NSAID felbinac versus oral NSAIDS: a critical review. 局部非甾体抗炎药felbinac与口服非甾体抗炎药:一个重要的回顾。
G Hosie, H Bird

Musculoskeletal disorders such as soft tissue injuries have traditionally been treated with oral NSAIDs, despite the significant side-effects associated with their clinical use. However, four separate multicentre, double-blind, double-dummy clinical trials have shown that the efficacy of the topical NSAID, felbinac, is equivalent to that of the oral NSAID, ibuprofen, in the treatment of soft tissue injuries, and to that of oral ibuprofen or fenbufen in mild to moderate osteoarthritis. In general practice the incidence of side-effects with felbinac is low, while oral NSAIDs have been associated with significant problems, particularly in the gastrointestinal system. Consequently, the cost of treating side-effects is reduced with felbinac treatment compared with oral NSAIDs, making it a logical treatment alternative from an economic view point as well as for reasons of efficacy and safety.

肌肉骨骼疾病,如软组织损伤,传统上用口服非甾体抗炎药治疗,尽管与临床使用相关的显著副作用。然而,四项独立的多中心、双盲、双虚拟临床试验表明,外用非甾体抗炎药felbinac治疗软组织损伤的疗效与口服非甾体抗炎药布洛芬相当,与口服布洛芬或芬布芬治疗轻中度骨关节炎的疗效相当。一般来说,服用非甾体抗炎药的副作用发生率很低,而口服非甾体抗炎药则会引起严重的问题,特别是在胃肠道系统。因此,与口服非甾体抗炎药相比,非比那克治疗副作用的成本降低了,从经济角度以及疗效和安全性的原因来看,它是一种合乎逻辑的治疗选择。
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引用次数: 0
NSAIDs and the gut--where are we now? 非甾体抗炎药和肠道,我们现在在哪里?
M Shield
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引用次数: 0
Arthrotec in general practice. Proceedings from the clinical investigator meeting held May 1994, Leeds, UK. 在一般实践中。1994年5月在英国利兹举行的临床研究者会议记录。
A G Mowat
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引用次数: 0
Double-blind, randomised, multi-centre clinical study evaluating the efficacy and tolerability of nimesulide in comparison with etodalac in patients suffering from osteoarthritis of the knee. 双盲、随机、多中心临床研究评估尼美舒利与依托达拉在膝关节骨性关节炎患者中的疗效和耐受性。
P W Lücker, C Pawlowski, I Friedrich, F Faiella, E Magni

In a double-blind study, the efficacy and tolerability of nimesulide 200mg/day, administered orally, was compared with etodolac 600mg/day in the treatment, for 3 months, of 200 patients suffering from osteoarthritis of the knee. Although spontaneous pain showed a significant improvement during the course of the study, there was no difference in the efficacy of either compound. Similarly, there was a progressive and significant reduction in the Lequesne functional index although no statistical difference was found between nimesulide and etodolac. The physician's overall assessment of efficacy was significantly in favour of nimesulide but the same assessment for patients who completed all 12 weeks showed no such bias. Adverse events (AEs) were generally mild or moderate and were commonly gastrointestinal in origin. There was no difference in the rate of incidence of AEs and, with the exception of week 8 where etodolac was apparently better tolerated, there were no statistical differences in tolerability between the two therapies.

在一项双盲研究中,比较了尼美舒利200mg/天口服与依托度酸600mg/天口服治疗200例膝关节骨关节炎患者3个月的疗效和耐受性。虽然自发性疼痛在研究过程中表现出明显的改善,但两种化合物的疗效没有差异。同样,尽管尼美舒利和乙妥酸之间没有统计学差异,但Lequesne功能指数也有渐进式的显著降低。医生对尼美舒利疗效的总体评估明显支持尼美舒利,但对完成所有12周的患者的相同评估没有显示出这种偏倚。不良事件(ae)一般为轻度或中度,通常起源于胃肠道。ae的发生率没有差异,除了第8周依托酸的耐受性明显更好外,两种治疗的耐受性没有统计学差异。
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引用次数: 0
Double-blind comparison of the efficacy of diclofenac/misoprostol and diclofenac in the treatment of rheumatoid arthritis. 双氯芬酸/米索前列醇与双氯芬酸治疗类风湿性关节炎疗效的双盲比较。
M V de Queiroz, A Beaulieu, K Kruger, E Woods, H Stead, S Geis

A double-blind, randomised, parallel-group study was conducted in eight countries to compare the efficacy of a fixed combination of diclofenac sodium (50 mg) and misoprostol (200 mcg) with a fixed combination of diclofenac sodium (50 mg) and placebo in treating the signs and symptoms of rheumatoid arthritis (RA). A total of 346 patients with RA who had been stabilised on diclofenac for at least 30 days were randomly assigned to receive either diclofenac/misoprostol BID or TID (n = 177) or diclofenac/placebo BID or TID (n = 169) for 12 weeks. Primary analyses of efficacy, made upon admission and at 4-week intervals, consisted of physician's global assessment of the arthritic condition, patient's global assessment of the arthritic condition, patient's global assessment of joint tenderness/pain, and physician's assessment of joint swelling. In this study, the fixed combination tablet of diclofenac sodium 50 mg/misoprostol 200 mcg administered BID or TID demonstrated no statistically significant difference in efficacy in the treatment of the signs and symptoms of RA compared with diclofenac sodium 50 mg/placebo administered BID or TID.

在8个国家进行了一项双盲、随机、平行组研究,比较双氯芬酸钠(50 mg)和米索前列醇(200 mcg)固定组合与双氯芬酸钠(50 mg)和安慰剂固定组合治疗类风湿性关节炎(RA)症状和体征的疗效。共有346例双氯芬酸稳定至少30天的RA患者被随机分配到双氯芬酸/米索前列醇BID或TID组(n = 177)或双氯芬酸/安慰剂BID或TID组(n = 169),为期12周。入院时和每隔4周进行一次疗效的初步分析,包括医生对关节炎状况的总体评估,患者对关节炎状况的总体评估,患者对关节压痛/疼痛的总体评估,以及医生对关节肿胀的总体评估。在本研究中,双氯芬酸钠50 mg/米索前列醇200 mcg固定联合片剂给药BID或TID与双氯芬酸钠50 mg/安慰剂给药BID或TID在治疗RA症状和体征方面的疗效无统计学差异。
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引用次数: 0
Clinical efficacy and safety profile of etodolac: focus on the elderly. 依托度酸的临床疗效和安全性:以老年人为重点。
P A Bacon
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引用次数: 0
Nabumetone, an effective anti-inflammatory agent, lacks gastrointestinal irritancy in the rat when dosed orally for one month: comparison with tiaprofenic acid and etodolac. 纳布美酮是一种有效的抗炎剂,与硫丙酸和依托度酸相比,口服一个月对大鼠没有胃肠道刺激。
R Melarange, C Gentry, P R Blower, C D Toseland, R Spangler

Objective: To determine the effects of nabumetone, compared with tiaprofenic acid and etodolac, on anti-inflammatory efficacy and gastrointestinal irritancy in the rat when dosed orally for one month at a high anti-inflammatory dose.

Methods: Carrageenan paw edema was used as a model of inflammation. Gastrointestinal mucosal integrity was assessed by concurrently measuring ulcer formation. mucosal and tissue prostanoid production and plasma haptoglobin. Haemoglobin, present in the cecal contents, was used as a measure of blood loss.

Results: Nabumetone, tiaprofenic acid and etodolac inhibited inflammation. Etodolac induced marked gastrointestinal damage and blood loss whereas tiaprofenic acid caused only gastric damage. Nabumetone was found not to alter mucosal integrity.

Conclusion: Nabumetone proved to be an effective anti-inflammatory agent that was devoid of gastrointestinal irritancy.

目的:比较纳布美酮在高抗炎剂量下口服1个月对大鼠的抗炎疗效和胃肠道刺激的影响,并与tiaprofenic acid和依托度酸进行比较。方法:以卡拉胶足跖水肿作为炎症模型。通过同时测量溃疡形成来评估胃肠道粘膜完整性。粘膜和组织前列腺素的产生和血浆触珠蛋白。盲肠内容物中的血红蛋白被用来衡量出血量。结果:纳布美酮、硫丙酸、依托多拉酸对炎症有抑制作用。依托度酸引起明显的胃肠损伤和失血,而硫丙酸仅引起胃损伤。纳布美酮不改变粘膜完整性。结论:那布美酮是一种无胃肠道刺激性的有效抗炎药。
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引用次数: 0
Historical overview of NSAIDs. 非甾体抗炎药的历史概述。
V Wright

Nonsteroidal anti-inflammatory drugs (NSAIDs) have become valuable therapeutic agents in the treatment of arthritic conditions. In 1971, Vane demonstrated that the primary mechanism of action of aspirin and related drugs was inhibition of synthesis of prostaglandins from arachidonic acid. Although Vane's prostaglandin hypothesis has been generally accepted, various studies have suggested that additional mechanisms may have a role in the effects of NSAIDs. With the increasing number of NSAIDs available and with recent information on the side effects associated with NSAID therapy, it becomes important to examine whether these drugs are being used in the most appropriate manner.

非甾体类抗炎药(NSAIDs)已成为治疗关节炎的重要药物。Vane在1971年证实阿司匹林及相关药物的主要作用机制是抑制花生四烯酸合成前列腺素。虽然Vane的前列腺素假说已被普遍接受,但各种研究表明,其他机制可能在非甾体抗炎药的作用中起作用。随着可获得的非甾体抗炎药数量的增加以及有关非甾体抗炎药治疗相关副作用的最新信息,检查这些药物是否以最适当的方式使用变得很重要。
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引用次数: 0
Piroxicam-beta-cyclodextrin in the treatment of acute pain of rheumatic disease. 吡罗昔康- β -环糊精治疗风湿性疾病急性疼痛。
J Y Reginster, P Franchimont

Analgesics continue to be the mainstay of therapy in osteoarthritis. Non-steroidal anti-inflammatory drugs (NSAIDs) play an important role, particularly where there is a significant inflammatory component to the osteoarthritis. Piroxicam-beta-cyclodextrin (PBC) is a new formulation in which piroxicam has been complexed with beta-cyclodextrin, a cyclic oligosaccharide. This results in an increase in the rate of absorption of the active compound and, consequently, in an earlier onset of analgesic action. PBC, like piroxicam, is administered once daily. PBC has been used in the treatment of osteoarthritis. In comparison with piroxicam, PBC showed a more rapid analgesic-anti-inflammatory action after the first administration in patients with active osteoarthritis. Subsequent evaluations at the second, fifth and last day of treatment demonstrated a comparable efficacy of the two drugs. The efficacy and tolerability of PBC was compared with other NSAIDs given intramuscularly, such as diclofenac and ketoprofen. The three compounds provided marked pain relief within thirty minutes and this increased progressively until the third to fourth hour. The efficacy of oral PBC was comparable to that of intramuscular diclofenac or ketoprofen. In comparison with metamisole PBC achieved a more rapid and sustained reduction in pain intensity during the first twelve hours of treatment. This rapid and marked reduction in pain intensity with PBC was also observed in patients with low-back pain when compared with etodolac. In view of its efficacy, tolerability and rapid onset of action, piroxicam-beta-cyclodextrin appears to be an useful analgesic and a prominent progress in the treatment of acute rheumatic pain.

止痛剂仍然是治疗骨关节炎的主要药物。非甾体抗炎药(NSAIDs)起着重要的作用,特别是在骨关节炎中有明显的炎症成分。吡罗昔康- β -环糊精(PBC)是吡罗昔康与环低聚糖- β -环糊精络合而成的新制剂。这导致活性化合物的吸收率增加,因此,在镇痛作用的早期发作。PBC和吡罗西康一样,每天给药一次。PBC已被用于治疗骨关节炎。与吡罗西康相比,PBC在活动性骨关节炎患者首次给药后表现出更快速的镇痛-抗炎作用。随后在治疗的第2天、第5天和最后一天进行的评估表明,两种药物的疗效相当。将PBC与肌注双氯芬酸、酮洛芬等非甾体抗炎药的疗效和耐受性进行比较。这三种化合物在30分钟内显著缓解疼痛,并逐渐增加,直到第三至第四小时。口服PBC的疗效与肌注双氯芬酸或酮洛芬相当。与metamisole相比,PBC在治疗的前12小时内实现了更快速和持续的疼痛强度减轻。与依托dolac相比,PBC在腰痛患者中也观察到疼痛强度的快速和显着降低。鉴于其疗效、耐受性和快速起效,吡罗昔康-环糊精似乎是一种有用的镇痛药,在治疗急性风湿痛方面取得了显著进展。
{"title":"Piroxicam-beta-cyclodextrin in the treatment of acute pain of rheumatic disease.","authors":"J Y Reginster,&nbsp;P Franchimont","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Analgesics continue to be the mainstay of therapy in osteoarthritis. Non-steroidal anti-inflammatory drugs (NSAIDs) play an important role, particularly where there is a significant inflammatory component to the osteoarthritis. Piroxicam-beta-cyclodextrin (PBC) is a new formulation in which piroxicam has been complexed with beta-cyclodextrin, a cyclic oligosaccharide. This results in an increase in the rate of absorption of the active compound and, consequently, in an earlier onset of analgesic action. PBC, like piroxicam, is administered once daily. PBC has been used in the treatment of osteoarthritis. In comparison with piroxicam, PBC showed a more rapid analgesic-anti-inflammatory action after the first administration in patients with active osteoarthritis. Subsequent evaluations at the second, fifth and last day of treatment demonstrated a comparable efficacy of the two drugs. The efficacy and tolerability of PBC was compared with other NSAIDs given intramuscularly, such as diclofenac and ketoprofen. The three compounds provided marked pain relief within thirty minutes and this increased progressively until the third to fourth hour. The efficacy of oral PBC was comparable to that of intramuscular diclofenac or ketoprofen. In comparison with metamisole PBC achieved a more rapid and sustained reduction in pain intensity during the first twelve hours of treatment. This rapid and marked reduction in pain intensity with PBC was also observed in patients with low-back pain when compared with etodolac. In view of its efficacy, tolerability and rapid onset of action, piroxicam-beta-cyclodextrin appears to be an useful analgesic and a prominent progress in the treatment of acute rheumatic pain.</p>","PeriodicalId":12056,"journal":{"name":"European journal of rheumatology and inflammation","volume":"12 4","pages":"38-46"},"PeriodicalIF":0.0,"publicationDate":"1993-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"18806134","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Macrocyclic molecules and their pharmacological applications. 大环分子及其药理应用。
L Lasagna
{"title":"Macrocyclic molecules and their pharmacological applications.","authors":"L Lasagna","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":12056,"journal":{"name":"European journal of rheumatology and inflammation","volume":"12 4","pages":"3-5"},"PeriodicalIF":0.0,"publicationDate":"1993-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"18806133","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
期刊
European journal of rheumatology and inflammation
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