Culley C M, Lacy M K, Klutman N, Edwards B
Drug Information and Pharmacoepidemiology Center, University of Pittsburgh Medical Center, 137 Victoria Building, 200 Lothrop Street, Pittsburgh, PA 15261, USA.
Am J Health Syst Pharm. 2001 Mar 1;58(5):379-88.
The activity, pharmacokinetics, pharmacodynamics, efficacy, safety, drug interactions, and dosage and administration of moxifloxacin are reviewed. Moxifloxacin is an oral 8-methoxyquinolone antimicrobial approved in December 1999 for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia. This fluoroquinolone is active against common community-acquired respiratory pathogens (Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis), atypical pathogens, and many anaerobes. Moxifloxacin has an absolute bioavailability of 90% after oral administration and a mean elimination half-life of 12 hours. The drug is not a substrate or inhibitor of the hepatic cytochrome P-450 isoenzyme system thereby avoiding many potential drug interactions. Moxifloxacin has limited phototoxic potential. In clinical trials, moxifloxacin had clinical success rates of 88-97% and bacteriologic eradication rates of 90-97%. Reported adverse effects were primarily gastrointestinal (nausea, diarrhea) and were mild to moderate in severity. Moxifloxacin prolongs the QT interval by a mean + S.D. of 6 +/- 26 milliseconds above baseline and should be used with caution in patients with proarrhythmic conditions and avoided in patients receiving antiarrhythmia agents, such as quinidine, procainamide, amiodarone, and sotalol. The standard oral dosage is 400 mg once a day. Dosage adjustment is unnecessary in patients with renal dysfunction or mild to moderate hepatic dysfunction. Moxifloxacin is a safe and effective antimicrobial that will be useful for treating acute sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
本文综述了莫西沙星的活性、药代动力学、药效学、疗效、安全性、药物相互作用以及剂量和用法。莫西沙星是一种口服的8-甲氧基喹诺酮类抗菌药物，于1999年12月被批准用于治疗急性细菌性鼻窦炎、慢性支气管炎急性细菌性加重以及社区获得性肺炎。这种氟喹诺酮类药物对常见的社区获得性呼吸道病原体（肺炎链球菌、流感嗜血杆菌、卡他莫拉菌）、非典型病原体以及许多厌氧菌具有活性。莫西沙星口服后的绝对生物利用度为90%，平均消除半衰期为12小时。该药物不是肝细胞色素P-450同工酶系统的底物或抑制剂，因此避免了许多潜在的药物相互作用。莫西沙星的光毒性潜力有限。在临床试验中，莫西沙星的临床成功率为88%-97%，细菌清除率为90%-97%。报告的不良反应主要为胃肠道反应（恶心、腹泻），严重程度为轻至中度。莫西沙星使QT间期较基线平均延长+标准差6±26毫秒，对于有心律失常倾向的患者应谨慎使用，对于正在接受抗心律失常药物（如奎尼丁、普鲁卡因胺、胺碘酮和索他洛尔）治疗的患者应避免使用。标准口服剂量为每日400毫克。肾功能不全或轻度至中度肝功能不全的患者无需调整剂量。莫西沙星是一种安全有效的抗菌药物，可用于治疗急性鼻窦炎、慢性支气管炎急性细菌性加重以及社区获得性肺炎。
