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An update on fluoroquinolones
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1992
Year
Serratia SpEscherichia ColiPharmacotherapyAntimicrobial ChemotherapyAntibiotic ResistanceUnited StatesPharmaceutical ChemistryDrug ResistanceAntimicrobial TherapyInfection ControlAntimicrobial ResistanceHealth SciencesFluorous SynthesisDrug DevelopmentPharmacologyClinical MicrobiologyAntimicrobial SusceptibilityAntibioticsMicrobiologyAntimicrobial AgentsMedicineDrug Discovery
The use of fluoroquinolone antibacterial agents has increased remarkably over the past 5 years. The major new facts about fluoroquinolones center around resistance, use in the treatment of respiratory infections, and toxicity issues. There has been a continued increase in methicillin-resistant Staphylococcus aureus to the fluoroquinolones, and as a result commercially available fluoroquinolones can no longer be considered appropriate initial therapy for suspected methicillin-resistant S. aureus infections. Resistance of Pseudomonas aeruginosa has been slower to develop worldwide, except in the treatment of respiratory infections. There have been reports of resistance of Serratia sp, Enterobacter sp, and even some Escherichia coli and Salmonella sp. The use of fluoroquinolones for respiratory infections has continued, although greater caution has been advocated when pneumococcal infection is suspected. No major changes in the therapy for other infections has occurred with the exception of evidence that single-dose therapy for uncomplicated urinary tract infections in women is as effective as 3- or 5-day therapy when fluoroquinolones with a long half-life in urine are used. Temafloxacin was withdrawn from the market in all countries due to unexpected hematologic toxicity that resulted in hemolytic anemia and renal failure in one of 5000 to one of 10,000 individuals who received the drug in the first 4 months of its use in the United States. The cause of toxicity is unknown. The major difference between temafloxacin and other available fluoroquinolones is its difluorophenyl group at N-1. This group is present in tosufloxacin, the largest selling fluoroquinolone in Japan, but tosufloxacin at 150 mg twice daily yields a peak blood level of, at most, 0.5 µg/mL compared with blood levels as high as 9 µg/mL in elderly patients who receive 600 mg of temafloxacin every 12 hours. New fluoroquinolones are under study that improve the activity of the agents against gram-positive species or the pharmacokinetics of this class of antimicrobial agents.