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The levofloxacin thermo-sensitive gel prepared using 17% poloxamer 407 (P407) can successfully treat suppurative otitis media (SOM) through the well-controlled release of levofloxacin targeted against the inflammation.
Mean plasma concentrations of levofloxacin and ciprofloxacin were similar to those previously reported. For once-daily dosing of levofloxacin, 500 mg, the mean (+/- SD) steady-state concentrations at 4 h, 12 h, and 24 h in ELF were 9.9 +/- 2.7 microg/mL, 6.5 +/- 2.5 microg/mL, and 0.7 +/- 0.4 microg/mL, respectively; AM concentrations were 97.9 +/- 80.0 microg/mL, 36.7 +/- 23.4 microg/mL, and 13.8 +/- 16.0 microg/mL, respectively. For levofloxacin, 750 mg, the mean steady-state concentrations in ELF were 22.1 +/- 14.9 microg/mL, 9.2 +/- 5.3 microg/mL, and 1.5 +/- 0.8 microg/mL, respectively; AM concentrations were 105.1 +/- 65.5 microg/mL, 36.2 +/- 26.1 microg/mL, and 15.1 +/- 2.0 microg/mL, respectively. The concentrations of ciprofloxacin at 4 h and 12 h in ELF were 1.9 +/- 0.9 microg/mL and 0.4 +/- 0.1 microg/mL, respectively; AM concentrations were 34.9 +/- 23.2 microg/mL and 6.8 +/- 5.9 microg/mL, respectively. The differences in the ELF concentrations of the two levofloxacin groups vs those of the ciprofloxacin group were significant (p < 0.05) at each sampling time.
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The global resurgence of tuberculosis and the emergence of multidrug-resistant tuberculosis have emphasized an urgent need for new, effective antimycobacterial drugs. A new antimycobacterial drugs should have a different mechanism of action to the standard drugs and should not show cross-resistance with them. Favorable pharmacokinetic properties, low incidence of side effects and low cost are the characteristics that would make antimycobacterial drugs suitable for extensive use. The fluoroquinolones would appear to fulfill most of the criteria for an ideal class of antimycobacterial drugs. The fluoroquinolones have been proposed for the treatment of Mycobacterium tuberculosis (M. tuberculosis) infections, with the results of in vitro, animal model and clinical studies suggesting that ofloxacin, ciprofloxacin, sparfloxacin and levofloxacin are the most promising of these drugs. However, these fluoroquinolones should not be used as first-line drugs, but rather, they should be reserved for treatment of tuberculosis that is resistant to rifampicin and isoniazid. Recently, a new investigational fluoroquinolone derivative, AM-1155, DU-6859a and CS-940, have excellent in vitro activity against M. tuberculosis, further studies are required to assess its clinical activity. We discussed the future of view of development of fluoroquinolones for mycobacterial diseases on the basis of structure-activity and structure-side-effect relationship studies. The comparative analysis enabled us to elucidate the structural requirements for the antimycobacterial activity and side-effects of fluoroquinolones. In addition, we summarized the newer methods for high-throughput screening of compounds against M. tuberculosis and discussed the problem of development of fluoroquinolones for mycobacterial diseases.
There is little information on the use of levofloxacin, a new quinolone, in ICU patients.
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In respiratory tract infections, therapy is often empirical and there is a need for local data on the rate of resistance to available antimicrobials. In this multicentre study which is a part of the international e-BASKETT-II surveillance study, respiratory isolates of Streptococcus pneumoniae (n=260) and Streptococcus pyogenes (n=312) collected between September 2002 and June 2003 from 18 hospitals in Turkey were tested against penicillin G, amoxicillin, cefuroxime, ceftriaxone, erythromycin, clarithromycin, azithromycin, clindamycin, telithromycin, tetracycline, levofloxacin and vancomycin. Antibiotic susceptibilities were determined with disk diffusion method and confirmed with broth dilution method following the CLSI guidelines. Isolates which were resistant to erythromycin were genotyped by polymerase chain reaction. In S. pneumoniae 11.5% of the isolates were highly and 22.7% were intermediately resistant to penicillin. Rate of resistance to erythromycin, clarithromycin, azithromycin was 17.3%, and 21.5% of the isolates were resistant to tetracycline. Resistance to levofloxacin and vancomycin was not observed and only one isolate was found intermediately resistant (MIC=2 microg/mL) to telithromycin. Genotypes in erythromycin-resistant isolates were ermB (77.8%), mefA (17.8%) and ermB+mefA (2.2%). S. pyogenes isolates were uniformly susceptible to beta-lactams and vancomycin, and only one isolate was intermediately resistant to levofloxacin. Macrolide resistance was observed in 1.3% of the isolates and three out of these harboured the mefA gene. One isolate with an MIC of 4 microg/mL for telithromycin had ermB gene. Telithromycin has demonstrated a good in vitro activity against macrolide-resistant respiratory tract isolates. As a result, e-BASKETT-II surveillance study has been one of the most extensive in vitro studies comparing telithromycin to available antimicrobial agents for respiratory tract infections in Turkey.
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This study supports the efficacy of current intravenous antibiotics protocols but questions the efficacy of both clindamycin and levofloxacin in empirically treating periprosthetic infections and cephalexin in providing effective perioperative prophylaxis against skin flora. Because bacterial sensitivities vary by location and patient population, this study encourages other centers to develop their own antibiogram specifically tailored to periprosthetic infections to improve antimicrobial decision making and potentially improve implant salvage.
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A series of novel 7-(3-alkoxyimino-4-methyl-4-methylaminopiperidin-1-yl)fluoroquinolone derivatives were designed, synthesized, and characterized by 1H-NMR, MS, and HRMS. These fluoroquinolones were evaluated for their in-vitro antibacterial activity against representative Gram-positive and Gram-negative strains. Generally, all of the target compounds have considerable antibacterial activity against the tested forty strains, and exhibit exceptional potency in inhibiting the growth of methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant S. aureus (MRSA) ATCC33591 (MICs: 0.06 to 2 microg/mL). In particular, compounds 14, 19, 28, and 29 are fourfold more potent than ciprofloxacin against MSSA 08-49. Compounds 23, 26, and 27 are twofold more potent than ciprofloxacin against MRSA ATCC33591 and MSSA ATCC29213. In addition, compound 14 exhibits excellent activity (MIC: 0.06 microg/mL) against Acinetobactes calcoaceticus, which is two- to 16-fold more potent than the reference drugs gemifloxacin, levofloxacin, and ciprofloxacin.
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Linezolid desensitization can be a viable option in patients requiring antimicrobial therapy for complicated gram-positive skin infections.