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PubMed2002

In vitro activity of linezolid, quinupristin-dalfopristin, vancomycin, teicoplanin, moxifloxacin and mupirocin against methicillin-resistant Staphylococcus aureus: comparative evaluation by the E test and a broth microdilution method.

The E test and broth microdilution showed comparable accuracy for the susceptibility testing of methicillin-resistant S. aureus (MRSA). All of the 109 primary clinical MRSA isolates were fully susceptible to the glycopeptides vancomycin and teicoplanin, the oxazolidinone linezolid, and the streptogramin quinupristin-dalfopristin. Nine out of the 109 MRSA isolates (8.3 percent) demonstrated resistance to moxifloxacin and 5 out of the 109 strains (4.6 percent) were resistant to the topical agent mupirocin. Linezolid and quinupristin-dalfopristin may prove useful alternatives for the treatment of patients with MRSA infections. MRSA isolates should be screened for in vitro susceptibility against mupirocin prior to the topical application.

Acetamides↗
PubMed2003

In vitro antimicrobial activity of moxifloxacin compared to other quinolones against recent clinical bacterial isolates from hospitalized and community-based cancer patients.

The in vitro spectrum of moxifloxacin (a C-8-methoxyquinolone) was compared to that of ciprofloxacin and levofloxacin against 924 recent clinical isolates from cancer patients. Moxifloxacin was more active than the comparator agents against Gram-positive pathogens, with potent activity against Aerococcus spp., Listeria monocytogenes, Micrococcus spp., Rhodococcus equi, and Stomatococcus mucilaginous, methicillin-susceptible Staphylococcus spp., all beta hemolytic streptococci, viridans streptococci and Streptococcus pneumoniae. It also had good to moderate activity against Bacillus spp., Corynebacterium spp., Enterococcus faecalis, and methicillin-resistant staphylococci. Although ciprofloxacin was the most active agent tested against the Enterobacteriaceae, moxifloxacin inhibited the majority of these isolates at < or =2.0 microg/ml. Moxifloxacin was the least active of the three agents tested against Pseudomonas aeruginosa, but had significant activity against other non-fermentative Gram-negative bacilli including Acinetobacter spp., Flavobacterium spp., Pseudomonas spp. other than P. aeruginosa, and Stenotrophomonas maltophilia. The overall broad spectrum of moxifloxacin, and its availability for both oral and parenteral administration, warrants its evaluation for the prevention and treatment of infections in cancer patients.

Anti-Infective Agents↗
PubMed2003

In vitro pharmacodynamic activity of gatifloxacin, gemifloxacin, moxifloxacin and levofloxacin against Streptococcus pneumoniae containing specific mutations in DNA gyrase and topoisomerase IV.

An in vitro pharmacodynatnic modeling apparatus (PDMA) generated specific bacterial kill profiles for single-dose regimens of gatifloxacin (GT), gemifloxacin (GM), moxifloxacin (MX) and levofloxacin (LV) against isolates of Streptococcus pneumoniae with specific QRDR profiles: SP-WT (no modifications); SP-C (changes in parC); and SP-AC (changes in both parC and gyrA). No differences in 3-log reduction time or total log reduction were observed among the four agents for SP-WT; however, LV failed to achieve a 3-log reduction in SP-C and SP-AC, and total log reduction after 12 hrs was minimal compared to the other agents. GM and MX required less time for 3-log reduction of SP-AC compared to GT, but total log reductions in SP-AC were similar among the three newer quinolone agents (GM > MX > GT). The study isolates with QRDR modifications greatly reduced LV activity. GM and MX maintained the greatest degree of activity against all study isolates and their activity was not adversely influenced by the genetic modifications in SP-C and SP-AC. The dual targeting characteristic of GM was also assessed, but did not offer significant advantages relative to MX and GT.

Analysis of Variance↗
PubMed1998

In vitro activities of six fluoroquinolones against Canadian isolates of vancomycin-sensitive and vancomycin-resistant Enterococcus species.

The in vitro activities of six fluoroquinolones were determined against 1482 Enterococcus species isolates collected as part of a 1996 Canadian surveillance study. Clinafloxacin MIC90s were 4 or 8 microg/mL, trovafloxacin and BAY 12-8039 MIC90s were 8 or 16 microg/mL, sparfloxacin MIC90s were 32 microg/mL, and ciprofloxacin and ofloxacin MIC90s were >32 microg/mL for the vancomycin-sensitive Enterococcus faecalis, vancomycin-sensitive Enterococcus faecium, and vancomycin-resistant E. faecium isolates collected.

Anti-Bacterial Agents↗
PubMed1999

In vitro activity of the new quinolone moxifloxacin (Bay 12-8039) against resistant gram-positive clinical isolates.

The novel 8-methoxyquinolone, moxifloxacin (Bay 12-8039), was compared with ciprofloxacin and eight other antimicrobials for activity against 425 strains Gram-positive clinical isolates, including 73 methicillin-resistant staphylococci, 35 vancomycin-resistant enterococci, and 80 penicillin- or eythromycin-resistant streptococci. Overall, 82% of the strains were inhibited at < or = 2 micrograms/mL. Moxifloxacin was more active than ciprofloxacin against staphylococci (8- to 32-fold), enterococci (0- to 16-fold), pneumococci (16-fold) and other streptococci (4- to 16-fold) when MIC90 results were compared. Moxifloxacin demonstrated good activity against all Gram-positive isolates tested except for ciprofloxacin-resistant enterococci (MIC90, 32 micrograms/mL) and methicillin-resistant staphylococci (MIC90, 8 micrograms/mL). Clinical trials should be initiated to define the role of this new quinolone.

Anti-Infective Agents↗
PubMed2001

Human aqueous humor levels of oral ciprofloxacin, levofloxacin, and moxifloxacin.

PURPOSE: To evaluate the penetration of ciprofloxacin, levofloxacin, and moxifloxacin into the aqueous humor after oral administration. SETTING: Alcorcon Hospital, Madrid, Spain. METHODS: Forty-two patients having cataract surgery were randomly divided into 3 groups the day before surgery. The first group received 2 oral 500 mg doses of ciprofloxacin at 12-hour intervals. The second group received a single oral 500 mg dose of levofloxacin. The third group received a single oral 400 mg dose of moxifloxacin. At the time of surgery, 0.1 mL aqueous fluid was aspirated from the anterior chamber just before the operation and immediately stored at -80 degrees C. Drug concentrations were measured using a biological assay. RESULTS: The mean aqueous level of ciprofloxacin was 0.50 microg/mL +/- 0.25 (SD); of levofloxacin, 1.50 +/- 0.50 microg/mL; and of moxifloxacin, 2.33 +/- 0.85 microg/mL. The mean aqueous levels of levofloxacin and moxifloxacin were above the 90% minimum inhibitory concentration for most of the common microorganisms that cause endophthalmitis. CONCLUSIONS: Therapeutic concentrations of fluoroquinolones, mainly levofloxacin and moxifloxacin, were reached with oral administration. These antibiotics may be effective for prophylaxis and adjuvant therapy of bacterial endophthalmitis.

Administration, Oral↗
PubMed2002

C11-BODIPY(581/591), an oxidation-sensitive fluorescent lipid peroxidation probe: (micro)spectroscopic characterization and validation of methodology.

C11-BODIPY(581/591) is a fluorescent radio-probe for indexing lipid peroxidation and antioxidant efficacy in model membrane systems and living cells, with excellent characteristics: (i) emission in the visible range of the electromagnetic spectrum, with good spectral separation of the nonoxidized (595 nm) and oxidized (520 nm) forms; (ii) has a high quantum yield and because of this, low labeling concentrations can be used, ensuring minimal perturbation of the membrane whilst retaining favorable signal to noise ratios; (iii) has a good photo-stability and displays very few fluorescence artifacts; (iv) is virtually insensitive to environmental changes, i.e., pH or solvent polarity; (v) is lipophilic and as such easily enters membranes; (vi) once oxidized, C11-BODIPY(581/591) remains lipophilic and does not spontaneously leave the lipid bilayer; (vii) C11-BODIPY(581/591) localizes in two distinct pools within the lipid bilayer, a shallow pool at 18 A and a deep pool at < 7.5 A from the center of the bilayer; (viii) is not cytotoxic to rat-1 fibroblasts up to 50 microM; (ix) is sensitive to a variety of oxy-radicals and peroxynitrite, but not to superoxide, nitric oxide, transition metal ions, and hydroperoxides per se; (x) its sensitivity to oxidation is comparable to that of endogenous fatty acyl moieties.

Animals↗
PubMed2000

Microbiologic efficacy of moxifloxacin for the treatment of community-acquired pneumonia due to Chlamydia pneumoniae.

Nasopharyngeal specimens for culture of Chlamydia pneumoniae were obtained from patients participating in two pneumonia treatment studies: an open study of 400 mg moxifloxacin orally, qds for 10 days and a randomized, double-blind comparison of moxifloxacin, 400 mg orally, qds versus clarithromycin, 500 mg orally, bd, both for 10 days. C. pneumoniae was eradicated from the nasopharynx of seven of ten (70%) microbiologically evaluable patients who were treated with moxifloxacin and four of four who were treated with clarithromycin. Minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC) of 21 isolates of C. pneumoniae from 18 patients obtained before and after therapy were performed against moxifloxacin and clarithromycin. The MIC(90)s and MBC(90)s for moxifloxacin and clarithromycin were 1 and 0.06 mg/l, respectively. The MICs and MBCs against moxifloxacin of six isolates from three persistently infected patients who were treated with the drug were the same at baseline and follow-up. The persistence of C. pneumoniae after treatment with moxifloxacin was probably not due to the emergence of resistance.

Administration, Oral↗
PubMed2000

In vitro activity of gatifloxacin compared with gemifloxacin, moxifloxacin, trovafloxacin, ciprofloxacin and ofloxacin against uropathogens cultured from patients with complicated urinary tract infections.

Minimum inhibitory concentrations (MICs) of gatifloxacin were compared with those of gemifloxacin, moxifloxacin, trovafloxacin, ciprofloxacin and ofloxacin using an agar dilution method for 400 uropathogens cultured from the urine of urological patients with complicated and/or hospital-acquired urinary tract infections (UTI). The collection of strains was made up of Enterobacteriaceae (34.5%), enterococci (31.5%), staphylococci (21.2%) and non-fermenting bacteria (12.8%). The antibacterial activity of the three newer fluoroquinolones, gatifloxacin, gemifloxacin, and moxifloxacin, were similar, but showed some drug specific differences. Gemifloxacin was most active against Escherichia coli, but less so against Proteus mirabilis. In this series all isolates of E. coli were inhibited at a MIC of 0.25 mg/l gatifloxacin and moxifloxacin and by 0.125 mg/l gemifloxacin. The MIC distribution of all fluoroquinolones showed a bimodal distribution for staphylococci, enterococci and Pseudomonas aeruginosa. The two modes for P. aeruginosa were 1 and 64 mg/l for gemifloxacin and moxifloxacin and 0.5 and 64 mg/l for gatifloxacin. For staphylococci the two modes were 0.125 and 2 mg/l for gatifloxacin, 0.03 and 4 mg/l for gemifloxacin, and 0.03 and 2 mg/l for moxifloxacin; for enterococci, 0.25 and 16 mg/l for gatifloxacin, 0.06 and 2 mg/l for gemifloxacin, and 0.25 and 8 mg/l for moxifloxacin. Compared with trovafloxacin the MICs were similar, but the newer fluoroquinolones were more active than ciprofloxacin and ofloxacin against Gram-positive bacteria. Of the newer fluoroquinolones gatifloxacin had the highest rate of renal excretion and could be considered a promising alternative fluoroquinolone agent for the treatment of UTI.

Anti-Infective Agents↗
PubMed2001

Activity of moxifloxacin and other quinolones against pneumococci resistant to first-line agents, or with high-level ciprofloxacin resistance.

The activity of moxifloxacin and other quinolones was assessed against 288 epidemiologically diverse isolates of Streptococcus pneumoniae, many of them resistant to one or more first-line agents and/or with increased ciprofloxacin resistance (minimum inhibitory concentrations, MICs 16- > 64 mg/l compared with 1-2 mg/l for most isolates). Moxifloxacin and grepafloxacin were the most active quinolone analogues, inhibiting about 90% of the isolates at < or = 1 mg/l, whereas levofloxacin inhibited 64% of isolates at < = 1 mg/l and ciprofloxacin inhibited 42%. Moxifloxacin also was the most active agent against isolates with elevated ciprofloxacin resistance (MIC 16- > 64 mg/l): moxifloxacin MICs of around 4 mg/l were seen for most such isolates, compared with 16-32 mg for levofloxacin and grepafloxacin. The activity of moxifloxacin against pneumococci resistant to one or more first-line agent suggests it will have a useful therapeutic role, although its activity against highly ciprofloxacin resistant isolates seems marginal.

Anti-Bacterial Agents↗
PubMed2001

Comparative in vitro bacteriostatic and bactericidal activity of trovafloxacin, levofloxacin and moxifloxacin against clinical and environmental isolates of Legionella spp.

The susceptibility of 140 Legionella spp isolates (106 clinical and 34 environmental isolates) to trovafloxacin (TRFX), levofloxacin (LEVX), moxifloxacin (MOFX), ciprofloxacin (CIPX), ofloxacin (OFLX), erythromycin (ERY), azithromycin (AZI) and rifampicin (RIF) was studied using a standard microdilution method and buffered yeast extract broth (BYE) supplemented with 0.1% alpha-ketoglutarate. The post-antibiotic effects (PAEs) of the study drugs against 10 clinical isolates of Legionella pneumophila sg.1 were compared. The MIC inhibiting 90% of strains tested on BYEalpha broth were 0.008, 0.016, 0.016, 0.06, 0.125, 0.5, 0.5, and 0.004 mg/l for TRFX, LEVX, MOXX, CIP, OFLX, ERY, AZI, and RIF, respectively. The MBC/MIC ratios ranged from one to eight depending on the antibiotic tested: TRFX [1x-2 x MIC], LEVX, MOFX, CIPX and OFLX [1x-4 x MIC], RIF [2x-4 x MIC], ERY and AZI [2x-8 x MIC]. TRFX, RIF, LEVX, MOFX, CIPX, OFLX, ERY and AZI showed similar activity against Legionella species other than L. pneumophila. One-hour exposures to the study antimicrobial agents at a concentration of 4 x MIC resulted in PAEs as follows (average in hours): TRFX: 2.68 h; RIF: 2.63 h; CIPX: 2.62 h; MOFX: 2.56 h; LEVX: 2.41 h; OFLX: 2.25 h; AZI: 1.65 h; and ERY: 1.54 h. In conclusion, our in vitro data confirm that trovafloxacin, levofloxacin, moxifloxacin and rifampicin have excellent bacteriostatic and bactericidal activity against Legionella spp and show significant post-antibiotic effect.

Anti-Bacterial Agents↗
PubMed2001

Multicentre study of the in vitro evaluation of moxifloxacin and other quinolones against community acquired respiratory pathogens.

The in vitro activity of moxifloxacin was compared with that of ciprofloxacin, levofloxacin, ofloxacin and trovafloxacin against 710 strains (180 Streptococcus pneumoniae, 180 Haemophilus influenzae, 160 Moraxella catarrhalis and 190 Streptococcus pyogenes) isolated from patients with community-acquired respiratory tract infections. MIC values for moxifloxacin, trovafloxacin were 0.25/0.25, 0.03/0.03, 0.06/0.03 and 0.125/0.0125 mg/l for S. pneumoniae, H. influenzae, M. catharralis and S. pyogenes. Based upon the MIC(90) values and the MIC distributions, moxifloxacin and trovafloxacin were the most active of the quinolones tested. They showed enhanced activity against Gram-positive organisms including penicillin non susceptible S. pneumoniae strains. Moxifloxacin was also highly active against ciprofloxacin-resistant S. pneumoniae strains.

Anti-Infective Agents↗
PubMed2002

Susceptibility to moxifloxacin and other antimicrobial agents of major pathogens responsible for community acquired respiratory tract infection in Poland.

The in vitro activity of moxifloxacin was compared with that of other antimicrobial agents against 470 bacterial strains isolated from patients with respiratory tract infection. Bacteria studied included 110 penicillin susceptible and 110 penicillin non-susceptible Streptococcus pneumoniae, 50 strains of S. pyogenes, 120 strains of Haemophilus influenzae and 80 strains of Moraxella catarrhalis. Moxifloxacin was the most active of the antimicrobials tested.

Anti-Bacterial Agents↗
PubMed2002

Minimal inhibitory concentrations and time-kill determination of moxifloxacin against aerobic and anaerobic isolates.

Moxifloxacin is a new oral 8-methoxy-quinolone with a wide spectrum of activity against Gram-negative and anaerobic bacteria, atypical micro-organisms and multi-resistant Gram-positive bacteria. This study was designed to assess the in vitro activity of moxifloxacin against Gram-positive bacteria with different resistance patterns, anaerobes and atypical micro-organisms such as Chlamydia and Mycoplasma. Moxifloxacin had good activity against Streptococcus pneumoniae with all strains inhibited by < or =0.12 mg/l. The minimal inhibitory concentrations (MICs) of moxifloxacin for Streptococcus pyogenes and Streptococcus agalactiae ranged from 0.03 to 0.5 mg/l while those of ciprofloxacin were about two- to four-fold higher (MICs=0.12-1 mg/l). Moxifloxacin was poorly active against enterococci but its activity against Clostridium and Bacteroides spp. was in the same range as that of metronidazole and superior to that of clindamycin. Moxifloxacin was substantially more active than both ciprofloxacin and sparfloxacin against Chlamydia.

Aerobiosis↗
PubMed2002

Single and multi-step resistance selection study in Streptococcus pneumoniae comparing ceftriaxone with levofloxacin, gatifloxacin and moxifloxacin.

Attempts were made to select resistant pneumococcal mutants by sequential subculturing of 12 clinically isolated pneumococci, [four were penicillin sensitive (MIC) 0.03-0.06 mg/l, four penicillin intermediate (MIC 0.25-0.5 mg/l) and four penicillin resistant (MIC 2-4 mg/l)] in sub-inhibitory concentrations of ceftriaxone, levofloxacin, gatifloxacin and moxifloxacin. Subculturing in gatifloxacin, levofloxacin, moxifloxacin and ceftriaxone selected 12 mutants (12/12), 10 mutants (10/12), 10 mutants (10/12) and three mutants (3/12), respectively. DNA sequencing of the quinolone-resistant mutants showed that most strains had mutations in GyrA at E85 or S81. This in vitro mutation study demonstrates a clear distinction between the low frequency of development of resistance with ceftriaxone exposure as opposed to the high frequency with quinolone exposure.

Anti-Bacterial Agents↗
PubMed2002

In vitro activity of moxifloxacin against recent community-acquired respiratory tract pathogens isolated in France: a national survey.

Between February and June 2000, 2345 consecutive strains of Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Staphylococcus aureus and Klebsiella pneumoniae were isolated from 2088 adult patients suffering from community-acquired respiratory tract infections, in 97 hospital laboratories. Of the 1037 S. pneumoniae isolates, 48.3% were intermediately or highly penicillin resistant. For invasive isolates, the MIC90s of penicillin G, amoxycillin, cefuroxime, ceftriaxone, erythromycin, ofloxacin, ciprofloxacin and moxifloxacin were 2, 2, 4, 0.5, 1024, 2, 2 and 0.25 mg/l, respectively. All but one invasive strain were susceptible to moxifloxacin whereas 97.5% were susceptible to levofloxacin. The MIC90s of clinical isolates with intermediate susceptibility or high resistance to penicillin G, were 2, 2, 4, 1, 1024, 2, 2 and 0.25 mg/l. About 98.1, 97.0, and 83.1% of strains were inhibited by concentrations < or = 1 mg/l of moxifloxacin, levofloxacin and ciprofloxacin, respectively (E-test). Eight of the 1037 S. pneumoniae strains were not susceptible to moxifloxacin and had mutations in gyrA (eight strains), parC (four strains) or parE (three strains). Against H. influenzae (32.7% were beta-lactamase producers) and M. catarrhalis (96.3% were beta-lactamase producers), the MIC90s of moxifloxacin, amoxycillin and co-amoxiclav were 0.094 and 0.125 mg/l, 64 and 8 mg/l, and 1.5 and 0.25 mg/l, respectively. Against oxacillin-susceptible S. aureus and K. pneumoniae, the MIC90s of moxifloxacin were 0.125 and 0.84 mg/l respectively. Moxifloxacin had the highest in vitro activity of all antibiotics tested.

Adolescent↗
PubMed2002

Moxifloxacin activity against clinical isolates compared with the activity of ciprofloxacin.

The activity of moxifloxacin, a new 8-methoxyquinolone, was compared in vitro with the activity of ciprofloxacin against clinical strains isolated from various sites of infection. The mode MIC values of moxifloxacin were superior to those of ciprofloxacin against Streptococcus pneumoniae, methicillin-susceptible and -resistant Staphylococcus aureus, Enterococcus spp., Escherichia coli and Acinetobacter spp., while ciprofloxacin was more active against Klebsiella pneumoniae and Pseudomonas spp. Both antibiotics had similar activity against Haemophilus influenzae, Moraxella catarrhalis and Enterobacter spp.

Anti-Infective Agents↗
PubMed2002

Antibacterial activity of moxifloxacin against periodontal anaerobic pathogens involved in systemic infections.

The in vitro activity of moxifloxacin was compared with that of penicillin G, amoxycillin/clavulanate, cefoxitin, erythromycin, clindamycin and metronidazole against 158 isolates associated with periodontal infections. MIC(50)/MIC(90) values of moxifloxacin were respectively 0.06/0.5 mg/l for Porphyromonas gingivalis (35), for Prevotella spp. (28) and Actinomyces spp. (35), 0.12/0.25 mg/l for Fusobacterium nucleatum (20) and 0.06/0.12 mg/l for Peptostreptococcus spp. (30). The minimum inhibitory concentration (MIC) range of moxifloxacin for Bacteroides forsythus (6) and Campylobacter rectus (4) was 0.06-0.12 mg/l. The minimum bactericidal concentrations were equal to or 2-4 times the MIC values. Moxifloxacin produced a bactericidal effect at 8 h. Our results show that moxifloxacin has good antibacterial activity against periodontal pathogens comparable with that of cefoxitin and amoxycillin/clavulanate, and better than that of clindamycin, metronidazole and penicillin.

Anaerobiosis↗