Institute of Clinical Pharmacology and Toxicology, Charité-Universitätsmedizin Berlin, Berlin, Germany.
Drugs Aging. 2010 Mar 1;27(3):193-209. doi: 10.2165/11531490-000000000-00000.
The fluoroquinolones ciprofloxacin, levofloxacin, moxifloxacin and gemifloxacin are widely used for the treatment of various types of bacterial infections. Overall, these antibacterial agents can be considered safe and well tolerated drugs. Comparative studies have evaluated the use of quinolones in elderly and younger populations. Although age per se does not seem to decrease their tolerability, specific adverse effects of the quinolones must be considered when they are chosen for antibacterial treatment. Renal function declines consistently with age and doses of renally excreted quinolones (e.g. ofloxacin, levofloxacin, gatifloxacin) need to be adjusted if a clinically relevant reduction of creatinine clearance is identified. Reactions of the gastrointestinal tract, such as nausea, dyspepsia, vomiting or diarrhoea, are among the most often registered adverse drug reactions during therapy with fluoroquinolones. Treatment with a quinolone causes diarrhoea less frequently than treatment with other classes of antimicrobials. Conflicting data have been published with respect to the incidence of Clostridium difficile-associated diarrhoea in quinolone-treated patients. Hypersensitivity reactions, often manifested on the skin, occur less commonly during therapy with quinolones than, for example, during therapy with beta-lactam antibacterials. Adverse reactions of the CNS are of particular concern in the elderly population. Given the CNS excitatory effects of quinolones, elderly patients should be monitored carefully for such symptoms. It is likely that many signs of possible adverse reactions, such as confusion, weakness, loss of appetite, tremor or depression, are often mistakenly attributed to old age and remain unreported. Quinolones should be used with caution in patients with known or suspected CNS disorders that predispose to seizures (e.g. severe cerebral arteriosclerosis or epilepsy). Quinolones can cause QT interval prolongation. They should be avoided in patients with known prolongation of the QT interval, patients with uncorrected hypokalaemia or hypomagnesaemia and patients receiving class IA (e.g. quinidine, procainamide) or class III (e.g. amiodarone, sotalol) antiarrhythmic agents. Tendinitis and tendon ruptures are recognized as quinolone-induced adverse effects that can occur during treatment or as late as several months after treatment. Chronic renal diseases, concomitant use of corticosteroids and age >60 years are known risk factors for quinolone-induced tendopathies. Overall, the specific adverse-effect profile of quinolones must be considered when they are chosen for treatment of bacterial infections. Because of physiological changes in renal function and when certain co-morbidities are present, some special considerations are necessary when elderly patients are treated with these drugs.
氟喹诺酮类药物环丙沙星、左氧氟沙星、莫西沙星和加替沙星被广泛用于治疗各种类型的细菌感染。总的来说，这些抗菌药物被认为是安全且耐受良好的药物。比较研究已经评估了喹诺酮类药物在老年和年轻人群中的应用。尽管年龄本身似乎不会降低其耐受性，但在选择用于抗菌治疗时，必须考虑喹诺酮类药物的特定不良反应。肾功能随着年龄的增长而持续下降，如果发现肌酐清除率有临床相关的降低，则需要调整经肾脏排泄的喹诺酮类药物（如氧氟沙星、左氧氟沙星、加替沙星）的剂量。胃肠道反应，如恶心、消化不良、呕吐或腹泻，是氟喹诺酮类药物治疗期间最常报告的药物不良反应之一。与其他类别的抗菌药物相比，喹诺酮类药物引起腹泻的频率较低。关于接受喹诺酮类药物治疗的患者中艰难梭菌相关性腹泻的发生率，已有相互矛盾的数据发表。与β-内酰胺类抗菌药物相比，喹诺酮类药物治疗期间发生过敏反应的情况较少，过敏反应通常表现在皮肤上。在老年人群中，中枢神经系统（CNS）不良反应尤其值得关注。由于喹诺酮类药物具有 CNS 兴奋作用，因此应密切监测老年患者是否出现此类症状。许多可能的不良反应迹象，如意识混乱、虚弱、食欲不振、震颤或抑郁，很可能被误认为是衰老的正常现象而未被报告。已知或疑似 CNS 疾病（如严重脑动脉粥样硬化或癫痫）易导致癫痫发作的患者，应谨慎使用喹诺酮类药物。喹诺酮类药物可引起 QT 间期延长。已知 QT 间期延长、未纠正的低钾血症或低镁血症、以及使用 I 类（如奎尼丁、普鲁卡因胺）或 III 类（如胺碘酮、索他洛尔）抗心律失常药物的患者，应避免使用喹诺酮类药物。肌腱炎和肌腱断裂是喹诺酮类药物引起的不良反应，可在治疗期间或治疗后数月发生。慢性肾脏疾病、同时使用皮质类固醇和年龄 >60 岁是喹诺酮类药物引起的肌腱病的已知危险因素。总的来说，在选择治疗细菌感染时，必须考虑喹诺酮类药物的特定不良反应特征。由于肾功能的生理变化以及某些合并症的存在，在给老年患者使用这些药物时需要一些特殊考虑。
