喹诺酮类药物常见不良反应的调查与分析

目的:分析喹诺酮类药物在临床治疗中发生的各种药物不良反应(ADR)类型和原因,为临床合理用药提供参考。方法:采用回顾性分析,对2008年—2009年间喹诺酮类药物不良反应进行分析。结果:159例ADR中涉及7种喹诺酮类药物,其中左氧氟沙星的不良反应发生率最高,主要ADR临床表现为皮肤及附件损害,其次为消化系统症状。各年龄段ADR的临床表现各有不同,静脉给药发生率大于口服给药。结论:喹诺酮类药物引起的ADR症状多,严重者可危及生命,临床医师应引起足够的重视,加强此类药物的用药监测,合理使用喹诺酮类药物。     

喹诺酮类药物的研究进展

目的：主要介绍喹诺酮类药的的近期研究发展状况,供同行参考。方法：分别介绍喹 物的抗菌活性和药代动力学特点、研究中的新品种以及当前研究的主要趋势。结果和结论：随着喹诺酮类的构效关系机制、耐药机制的研究深入,必将出现闻效了的新药物。     

喹诺酮类药物研究进展

自1962年美国Sterling-winthrop研究所Lesher等发现第一个喹诺酮类抗菌药萘啶酸以来许多学者致力于研究开发此类药物,特别是近十余年来取得了飞跃进展,从发展速度来看,喹诺酮合成抗菌药已超过生物合成及半合成抗生素。某些新     

喹诺酮类药物的不良反应

根据喹诺酮类抗菌药物对常见致病菌的抗菌活性和抗菌谱，将喹诺酮类抗菌药物分为4代：第1代代表药物有萘啶酸、吡哌酸等，主要用于泌尿系感染；第2代有诺氟沙星．环丙沙星、氧氟沙星等，适用于多种临床感染性疾病；第3代有左氧氟沙星、司帕沙星、格帕沙星等；第4代曲伐沙星、西他沙星、莫西沙星、加替沙星等，以西他沙星为代表，可称是超广谱抗菌药物。随着临床使用的不断增加，对其不良反应及药物相互作用的报道也逐渐增多，现将其常见的不良反应作一概述。     

氟喹诺酮类药物的临床应用分析

目的 探讨分析临床治疗中氟喹诺酮类药物的应用状况.方法 从2010年7月至2011年6月在我院住院治疗并归档的病例中随机抽取实施抗菌治疗的患者资料1013例,统计分析抗菌治疗中氟喹诺酮类药物的使用状况及作用特点.结果 46%抗菌治疗的患者使用了氟喹诺酮类药物,左氧氟沙星的使用频率最高(占39.48%),联合用药占91.20%,不合理用药占8.80%;52例出现不良反应且多表现为呕吐、恶心、头晕、头痛、静脉炎、皮疹、瘙痒等临床症状.结论 临床应用中应注意适应证的掌握及药物剂量、疗程、药物配伍禁忌等,避免不良反应的发生     

氟喹诺酮类药物研究概况

氟喹诺酮类抗菌素是20世纪70年代初发展起来的一类新型抗感染药物,杀菌谱广、毒副作用小、结构简单、给药方便、价格适中,成为近年来发展较快的一类抗菌素和国内外竞相开发与应用的热点药物。     

浅析喹诺酮类药物的研究进展

喹诺酮类药为人工合成的抗菌药.该类药物发展迅速成为目前抗菌药物的研究热点.本文从抗菌作用机制,各种喹诺酮类药特点及共性,注意事项,研究展望等方面对该类药物做一综述,以便读者对其发展有更全面的了解.     

氟喹诺酮类药物的不良反应

随着80年代氟喹诺酮类(fluoroquinolones)药物的发展,目前在临床已成为广泛应用的一类抗生素,较为多见的为：诺氟沙星、环丙沙星、氧氟沙星、左氧氟沙星、依诺沙星、司帕沙星等,主要用于治疗消化、呼吸、泌尿和生殖等系统的感染性疾病。随着临床的广泛使用,对这类药物引起的不良反应也时有报道。本文对Inter网上“药物不良反应信息网”中有关氟喹诺酮类药物的不良反应进行统计、分析、归纳,目的是希望减少这类药物的不良反应。1资料来源与方法“药物不良反应信息网”(http：//www．badrin．com/)中“ADR个案”项下有关氟喹诺酮类药物的所有报道。2结果共搜索到药品不良反应(ADR)67例,其中,男性27例,女性32例,另有8例性别不详。老年患者19例,中青年患者38例,其中9例不详,另有1例年龄为8个月。结果见表1。     

喹诺酮类药物对豚鼠心电图的影响

目的　观察比较环丙沙星、左氧氟沙星和司帕沙星的心脏毒性。方法　记录腹腔给药后豚鼠心电图 ,探讨对心电图各项指标的影响。结果　环丙沙星、左氧氟沙星及司帕沙星均能引起豚鼠心电图异常 ,出现 QT间期显著延长、室性早搏、房室传导阻滞等 ,而其他指标未见显著改变。在同等剂量下 ,左氧氟沙星对心电图影响最小 ,环丙沙星与左氧氟沙星接近 ,而司帕沙星而对心电图影响最大。结论　环丙沙星、左氧氟沙星及司帕沙星均可引起豚鼠心电图改变 ,但左氧氟沙星及环丙沙星的作用低于司帕沙星。     

喹诺酮类抗菌药物发展历程与临床应用

喹诺酮类(quinolones)药物是一类人工合成的抗菌药,在世界范围内广泛应用于细菌感染所引起的感染性疾病的治疗。该类药物具有抗菌、抗结核、抗疟疾、抗病毒等多种活性,一直是药物研究与开发的一大热点。然而,随着查诺酮类药物的广泛临床应用,其所引起的不良反应和耐药性也在快速增长。本文就喹诺酮类药物的发展历程、作用机制、药动学、不良反应及耐药性等方面信息作一综述,以期为临床用药提供指导。     

Fluorinated quinolones

Quinolones, chemically related to nalidixic acid, have a strong and rapid bactericidal action against Gram-negative bacteria, includingPs. aeruginosa, someMycobacteria, Legionella andStaphylococci. Streptococci and anaerobic bacteria are usually less sensitive. The quinolones exert their bactericidal action through inhibition of the enzyme DNA gyrase. Quinolones are absorbed for 50–100% from the gastro-intestinal tract, their volume of distribution is generally high (2 l/kg) and high concentrations are reached in almost all organs. The elimination half-lives range from 4 to 14 h. The efficacy of quinolones in urinary tract infections has been shown in many studies. They also seem to be effective in many serious infections. In animal studies their efficacy was generally equal or superior to aminoglycosides. Until now only mild and infrequent side effects have been reported.     

Fluorinated quinolones

Quinolones, chemically related to nalidixic acid, have a strong and rapid bactericidal action against Gram-negative bacteria, includingPs. aeruginosa, someMycobacteria, Legionella andStaphylococci. Streptococci and anaerobic bacteria are usually less sensitive. The quinolones exert their bactericidal action through inhibition of the enzyme DNA gyrase. Quinolones are absorbed for 50–100% from the gastro-intestinal tract, their volume of distribution is generally high (2 l/kg) and high concentrations are reached in almost all organs. The elimination half-lives range from 4 to 14 h. The efficacy of quinolones in urinary tract infections has been shown in many studies. They also seem to be effective in many serious infections. In animal studies their efficacy was generally equal or superior to aminoglycosides. Until now only mild and infrequent side effects have been reported.     

喹诺酮类药物的临床应用

1 临床应用1.1 泌尿生殖道感染 喹诺酮类药物具有广谱的革兰阴性菌抗菌活性,故此类抗感染药物最初即被用来治疗泌尿生殖道感染。尤其是经肾排泄喹诺酮类药物因其泌尿生殖道药物浓度更高,所以它们治疗泌尿生殖道感染更为有效。绝大多数喹诺酮类药物给药3～10天治疗敏感大肠杆菌所致非并发性泌尿道感染的疗效均与甲氧苄啶-磺胺甲嗯唑相当。 并发性泌尿道感染包括结石或阻塞性尿路病和导管相     

新氟喹诺酮类药物的心脏毒性

本文着重介绍喹诺酮类药物的心脏毒性,以引起医务人员的警觉。喹诺酮类药物的心脏毒性主要表现为心律紊乱和QT间期延长,其发生频率随药物品种不同而异,司帕沙星和格帕沙星对心脏毒性大于其他同类药物,并有剂量依赖性。喹诺酮类药物引起心脏毒性的机制尚不清楚。提醒医生须合理应用喹诺酮类药物,严重心血管疾病者、心律失常患者、老年患者、电解质失调者应慎用此类药物。     

Developments in quinolones

The properties of several new, investigational quinolones are reviewed. Desirable characteristics of new quinolones are improved activity against especially Gram-positive bacteria, longer elimination half-life, slower development of resistance, fewer side effectsetc. Fleroxacin and lomefloxacin have entered phase III trials: their main advantage lies in improved pharmacokinetics. AM-1091, AT-4140 and T-3262 are still in early phases of development and show improved activity against Gram-positive bacteria. They also show a reduced penetration of the blood-brain barrier, probably resulting in fewer side effects in the central nervous system. AM-1091 shows incomplete cross-resistance with ciprofloxacin.     

The new quinolones

The new quinolones are reviewed. These drugs are fluorinated derivatives of nalidixic acid, like ciprofloxacin, norfloxacin, ofloxacin, pefloxacin, and others. The following aspects are discussed: microbiology, modes of action and of resistance, the pharmacologic properties, the adverse reactions, the interactions with other drugs, and the principal clinical applications.     

Resistance to quinolones

Resistance to quinolones is only due to mutations. The mechanism and the range of quinolones involved, depend on the locus of the chromosomal mutation e.g. a mutation in the gyr A locus is associated with resistance due to changes in the gyrase. Using high inoculain vitro, varying, but relatively low mutation rates of resistance to fluoroquinolones have been found (10⁻⁶-10⁻¹²).In vitro transfers of bacterial strains in increasing concentrations of quinolones yield parallel increases of the MIC's of most quinolones; however, the MIC's of the most active quinolones like ciprofloxacin usually remain below concentrations achievablein vivo. Exceptions are MIC's forPseudomonas aeruginosa and staphylococci. Combined resistance to quinolones and other antibiotics was observed afterin vitro transfers as well as in mutants (10⁻⁶-10⁻⁸) isolated from a high inoculum. Changes in the outer membrane proteins have been found in these mutants. Clinical resistance to fluoroquinolones is rare except inPseudomonas aeruginosa and staphylococci.

     

Developments in quinolones

The properties of several new, investigational quinolones are reviewed. Desirable characteristics of new quinolones are improved activity against especially Gram-positive bacteria, longer elimination half-life, slower development of resistance, fewer side effectsetc. Fleroxacin and lomefloxacin have entered phase III trials: their main advantage lies in improved pharmacokinetics. AM-1091, AT-4140 and T-3262 are still in early phases of development and show improved activity against Gram-positive bacteria. They also show a reduced penetration of the blood-brain barrier, probably resulting in fewer side effects in the central nervous system. AM-1091 shows incomplete cross-resistance with ciprofloxacin.