Comparative Effects of Levofloxacin and Ofloxacin on the Normal Oral and Intestinal Microflora

Edlund, Charlotta; Sjöstedt, Svante; Nord, Carl Erik

doi:10.3109/00365549709011835

Cited by 50 publications

(28 citation statements)

References 10 publications

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“…The populations rapidly recovered to the predosing levels after antibiotic dosing ceased. These observations are consistent with those presented in previous reports, in which it was reported that levofloxacin elicited a selective reduction in the gut microbiota and predominantly affected gram-negative aerobic bacteria (18).…”

Section: Discussionsupporting

confidence: 93%

“…The levels of fluoroquinolones achieved in the gut model are presented in Table 2. Although there were some variations in the peak fluoroquinolone concentrations between the gut model experiments, the levels achieved were still within the ranges previously reported from in vivo studies (Table 2) (9,18,19). The ciprofloxacin concentrations were below the limits of detection (2 mg/liter) within 10 days of the cessation of dosing.…”

Section: Gut Bacterial Populations (I) Ciprofloxacin Administrationsupporting

confidence: 85%

“…Bacterial populations were enumerated daily, and no further interventions were performed for 7 days. On day 21 (period C), a second inoculum of C. difficile (ϳ10 7 CFU) spores was added to vessel 1, in addition to the commencement of antimicrobial instillation, with the dosing regimens determined from published data from studies with patients or volunteers (Table 1) to achieve a minimum of two-thirds of the published fecal levels (9,18,19). Ciprofloxacin was instilled every 12 h for 7 days, and levofloxacin and moxifloxacin were instilled once daily for 7 and 10 days, respectively.…”

Section: Methodsmentioning

confidence: 99%

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Effects of Exposure of Clostridium difficile PCR Ribotypes 027 and 001 to Fluoroquinolones in a Human Gut Model

Saxton

Baines

Freeman

et al. 2009

Antimicrob Agents Chemother

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The incidence of Clostridium difficile infection is increasing, with reports implicating fluoroquinolone use. A three-stage chemostat gut model was used to study the effects of three fluoroquinolones (ciprofloxacin, levofloxacin, and moxifloxacin) on the gut microbiota and two epidemic C. difficile strains, strains of PCR ribotypes 027 and 001, in separate experiments. C. difficile total viable counts, spore counts, and cytotoxin titers were determined. The emergence of C. difficile isolates with reduced antibiotic susceptibility was monitored with fluoroquinolone-containing medium, and molecular analysis of the quinolone resistance-determining region was performed. C. difficile spores were quiescent in the absence of fluoroquinolones. Instillation of each fluoroquinolone led to C. difficile spore germination and high-level cytotoxin production. High-level toxin production occurred after detectable spore germination in all experiments except those with C. difficile PCR ribotype 027 and moxifloxacin, in which marked cytotoxin production preceded detectable germination, which coincided with isolate recovery on fluoroquinolone-containing medium. Three C. difficile PCR ribotype 027 isolates and one C. difficile PCR ribotype 001 isolate from fluoroquinolone-containing medium exhibited elevated MICs (80 to >180 mg/liter) and possessed mutations in gyrA or gyrB. These in vitro results suggest that all fluoroquinolones have the propensity to induce C. difficile infection, regardless of their antianaerobe activities. Resistant mutants were seen only following moxifloxacin exposure.

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Section: Discussionsupporting

confidence: 93%

Section: Gut Bacterial Populations (I) Ciprofloxacin Administrationsupporting

confidence: 85%

Section: Methodsmentioning

confidence: 99%

See 1 more Smart Citation

Effects of Exposure of Clostridium difficile PCR Ribotypes 027 and 001 to Fluoroquinolones in a Human Gut Model

Saxton

Baines

Freeman

et al. 2009

Antimicrob Agents Chemother

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“…Although some fluoroquinolone antibiotics have enhanced in vitro activity against anaerobes (e.g., moxifloxacin and gatifloxacin) (1,13), studies with human volunteers have demonstrated that none of the currently available agents in this class cause a significant reduction in the density of intestinal anaerobes (2,(6)(7)(8)(9)14). Therefore, we examined the effect of fluoroquinolone antibiotics with various levels of antianaerobe activity on the persistence of VRE stool colonization in mice.…”

mentioning

confidence: 99%

Effect of Parenteral Fluoroquinolone Administration on Persistence of Vancomycin-Resistant Enterococcus faecium in the Mouse Gastrointestinal Tract

Donskey¹,

Helfand²,

Pultz³

et al. 2004

Antimicrob Agents Chemother

101

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We examined the effect of subcutaneous fluoroquinolone antibiotic administration on persistence and density of vancomycin-resistant Enterococcus faecium stool colonization in mice. Levofloxacin and ciprofloxacin did not promote colonization in comparison to saline controls, whereas moxifloxacin and gatifloxacin promoted persistent overgrowth in a dose-dependent fashion.In a mouse model and in colonized patients, we have demonstrated that antibiotics with potent in vitro activity against intestinal anaerobes promote persistent high-density colonization with vancomycin-resistant Enterococcus faecium (VRE), whereas antibiotics with minimal antianaerobe activity (including ciprofloxacin) do not (4, 5). Although some fluoroquinolone antibiotics have enhanced in vitro activity against anaerobes (e.g., moxifloxacin and gatifloxacin) (1, 13), studies with human volunteers have demonstrated that none of the currently available agents in this class cause a significant reduction in the density of intestinal anaerobes (2,(6)(7)(8)(9)14). Therefore, we examined the effect of fluoroquinolone antibiotics with various levels of antianaerobe activity on the persistence of VRE stool colonization in mice.The mouse model that we have previously utilized to study the effect of antibiotics on persistence of VRE stool colonization was used (4). Male CF1 mice (Harlan Sprague-Dawley, Indianapolis, Ind.) weighing 25 to 30 g were housed in individual cages and fed rodent chow and water ad libitum. VRE colonization with Enterococcus faecium strain C68 was established in all mice by administering oral vancomcyin (250 g/ liter) in drinking water for 2 days before and 5 days after esophageal instillation of 10 8 CFU of VRE in 0.5 ml (4). After discontinuation of oral vancomycin, mice were begun on twice-daily subcutaneous injections of saline (negative controls) or antibiotics for 15 days. Three different doses of the fluoroquinolone antibiotics were studied: a low dose equal to the usual human dose administered over a 24-h period (milligrams of antibiotic per gram of body weight); a medium dose of 5 times the low dose, and a human-equivalent dose of 12 times the usual human dose calculated by the technique of Freireich et al. (11). The dose of levofloxacin was based on the 750-mg-per-day human dose. Gatifloxacin and moxifloxacin were administered only at the lower two dosages because the highest dosage of these agents resulted in significant subcutaneous tissue irritation. The dosages included ciprofloxacin at 0.4, 2, and 4.8 mg/day; levofloxacin at 0.375, 1.875, and 4.7 mg/day; gatifloxacin at 0.2 and 1 mg/day; and moxifloxacin at 0.2 and 1 mg/day. Clindamycin at 1.4 mg/day promoted persistent high-density colonization in previous experiments and was included as a positive control (4).Four mice were included in each experimental group, and the experiments were performed twice (eight mice per group). Stool samples were collected prior to starting subcutaneous antibiotics and then on days 5, 10, and 15 of antibiotic therapy. To measure the de...

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“…50% of marketed drugs are chiral and out of that 50% are available as racemate (an equal mixture of both enantiomers) mixtures [10]. The most important thing here is that these two enantiomers may have same pharmacological action, for example, ofloxacin (R-enantiomer) and levofloxacin (S-enantiomer) which are both antimicrobials of quinolones [11]. One enantiomer may be active and the other may be inactive, the examples are (S)-albuterol, a β2-adrenergic receptor agonist for treatment of asthma, and (S)-omeprazole, a proton pump inhibitor for treatment of gastroesophageal reflux has been shown to be superior to their racemic formulations in clinical trials cause their R-enantiomers are inactive [9].…”

Section: Introductionmentioning

confidence: 99%

A Comparative Study of Stereochemical Effects of Anti-Prostate Agents by Molecular Docking

Osanyinpeju

Bashary

Mittal

et al. 2018

Asian J Pharm Clin Res

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Objective: A comparative study of anti-prostate agents to investigate the stereochemical influences on binding affinity by molecular docking. Methods:Structures of enantiomers (R and S stereoisomers) for known anti-prostate cancer (PCa) agents were drawn using ChemBioDraw 2D software. Thereafter, they were converted to 3D structures using the ChemBioDraw 3D software in which they were subjected to energy minimization using the MM2 method and then saved as PDB extension files which can be accessed using the ADT interface. AutoDock Vina (ADT) 1.5.6 software version was used for molecular docking study.Results: A total of 12 different anti-PCa agents were selected and drawn including well-known drug R-bicalutamide. All molecules showed the binding affinity with respect to the nature of stereochemistry. R-stereoisomers showed better interaction as well as binding affinity toward 1z95 (mutated androgen receptor protein involved in the progression of PCa) whereas their S-stereoisomers were found inferior in comparison. Conclusion:This study showed that CB1-R and R-bicalutamide (with R-stereochemistry) were better in binding affinity comparative to their counterpart CB1-S and S-Bicalutamide (with S-stereochemistry). All the selected anti-PCa agents were showing the effect of stereochemical center; therefore, we must choose the right kind of stereochemistry while planning to develop the newer anti-PCa agents.

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Comparative Effects of Levofloxacin and Ofloxacin on the Normal Oral and Intestinal Microflora

Cited by 50 publications

References 10 publications

Effects of Exposure of Clostridium difficile PCR Ribotypes 027 and 001 to Fluoroquinolones in a Human Gut Model

Effects of Exposure of Clostridium difficile PCR Ribotypes 027 and 001 to Fluoroquinolones in a Human Gut Model

Effect of Parenteral Fluoroquinolone Administration on Persistence of Vancomycin-Resistant Enterococcus faecium in the Mouse Gastrointestinal Tract

A Comparative Study of Stereochemical Effects of Anti-Prostate Agents by Molecular Docking

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