Gemifloxacin for the Treatment of Respiratory Tract Infections: In Vitro Susceptibility, Pharmacokinetics and Pharmacodynamics, Clinical Efficacy, and Safety

摘要: Gemifloxacin is a synthetic fluoroquinolone antimicrobial agent exhibiting potent activity against most gram-negative and gram-positive organisms, such as the important community-acquired respiratory pathogens Streptococcus pneumoniae (including multidrug-resistant S. pneumoniae), Haemophilus influenzae, Moraxella catarrhalis. The agent's mechanism of action involves dual targeting two essential bacterial enzymes: DNA gyrase topoisomerase IV. was approved by Food Drug Administration in April 2003 for treatment pneumonia acute exacerbation chronic bronchitis. drug has an oral bioavailability approximately 71%. Approximately 20-35% gemifloxacin excreted unchanged urine after 24 hours. elimination half-life 6-8 hours patients with normal renal function, supporting once-daily dosing. 24-hour free-drug area under plasma concentration-time curve:minimum inhibitory concentration ratio (JAUC 0 - 2 4 :MIC) associated efficacy, based on results from vitro animal models infection, 30. With mean fAUC 3 μg.hour/ml (35% total AUC 8.4) median MIC 90% tested strains 0.03, :MIC 100 would be expected standard dosing (320 mg once/day). In clinical studies involving both hospitalized outpatient populations, been highly effective Clinical success rates ranged 93.9-95.9% 96.1-97.5% those well tolerated; frequency adverse events this low. Most are mild-to-moderate severity, diarrhea (< 4%), nausea rash 3%), headache 2%) commonly reported. interactions not common, although absorption greatly reduced when given divalent trivalent cation-containing compounds, antacids. Due to its many common pathogens, proven favorable safety profile, empiric lower tract infections.