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Gemifloxacin
See also Fluoroquinolones
General information
Gemifloxacin is a fluoroquinolone that has enhanced affinity for topoisomerase. Compared with other fluoroquinolones, gemifloxacin was the most potent against penicillin-intermediate and penicillin-resistant pneumococci, methicillin-susceptible and methicillin-resistant Staphylococcus epidermidis isolates, and coagulase-negative staphylococci [ , ]. It has excellent activity against Haemophilus influenzae and Moraxella catarrhalis and is unaffected by beta-lactamases. It is generally two-fold less active than ciprofloxacin against most Enterobacteriaceae [ ]. Atypical respiratory pathogens (Legionella, Mycoplasma, and Chlamydia species) and Neisseria gonorrheae are highly susceptible [ ].
The pharmacokinetics of oral gemifloxacin have been characterized in healthy male volunteers [ ]. About 20–30% of the dose was excreted unchanged in the urine. The renal clearance was 160 ml/minute on average after single and multiple doses, which was slightly greater than the accepted glomerular filtration rate. There were no adverse effects.
Drug studies
Observational studies
In phase II trials oral gemifloxacin 320 mg/day produced bacteriological responses in 94% of patients with acute exacerbations of chronic bronchitis [ ] and in 95% of patients with uncomplicated urinary tract infections. Adverse events included nausea, abdominal pain, headache, and a mild rash in both patients and healthy volunteers.
After a single dose of 20–800 mg of gemifloxacin, there were no significant changes in clinical chemistry, hematology, or urinalysis, vital signs, or 12-lead electrocardiograms in healthy men, irrespective of dose [ ].
The effect of oral gemifloxacin 320 mg for 7 days on the human intestinal microflora has been investigated in 10 healthy subjects [ ]. The numbers of enterobacteria, enterococci, and streptococci were reduced. No other aerobic microorganisms were affected. The numbers of anerobic cocci and lactobacilli were reduced. The microflora normalized 49 days after withdrawal. There was no selection or overgrowth of resistant bacterial strains or yeasts.
Comparative studies
Gemifloxacin 320 mg od and trovafloxacin 200 mg od have been compared in 571 patients with community-acquired pneumonia in a multicenter, double-blind, parallel-group, randomized study [ ]. Gemifloxacin was slightly more effective (88%) than trovafloxacin (81%). Gemifloxacin was well tolerated and the incidence of transient liver function abnormalities was very low.
Organs and systems
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