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Category: Bacterial Pathogenesis
Fluoroquinolones, Page 1 of 2
< Previous page | Next page > /docserver/preview/fulltext/10.1128/9781555815929/9781555812379_Chap26-1.gif /docserver/preview/fulltext/10.1128/9781555815929/9781555812379_Chap26-2.gifAbstract:
The majority of new fluoroquinolones have two ionizable functions: the 3-carboxyl group and a protonizable site at position 7, such as a 7-piperazinyl heterocycle. The majority of fluoroquinolones have good antistaphylococcal activity. Sitafloxacin, moxifloxacin, gatifloxacin, trovafloxacin, and gemifloxacin have excellent activity, while for grepafloxacin and gatifloxacin, the MIC50s are, respectively, 0.125 and 0.25 µg/ml. DC-756 is as active as sitafloxacin (DU-6859a), one of the most active fluoroquinolones against gram-positive cocci, against Staphylococcus aureus, Streptococcus pneumoniae, and Streptococcus pyogenes. KRQ 10099 is an analog of ofloxacin bearing a bicyclic nucleus instead of a piperazinyl moiety. KRQ 10018 is an 8-methyl-2-pyridone derivative. Against reference strains, KRQ 10018 is extremely active against gram-positive cocci, including ciprofloxacin-resistant S. aureus isolates and ofloxacin-resistant Staphylococcus epidermidis. The majority of fluoroquinolones are eliminated principally renally and/or biliarly. The major system is CYP1A2, the activity of which may be inhibited by the fluoroquinolones. In addition to its antiviral activity, zidovudine possesses a certain antibacterial activity against Enterobacteriaceae through its action on bacterial DNA. As a result of its activity on DNA, zidovudine might modify the activity of the fluoroquinolones. The currently available fluoroquinolones are not treatments for acute forms of malaria, but they may abolish a pauciparasitic form if administered simultaneously for another disease.
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Pyridone-β-carboxylic derivatives
Fluoroquinolones: N-1 substituents
Fluoroquinolones: C-5 substituents
Fluoroquinolones: C-8 substituents
7-Piperazinyl derivatives
7-Pyrrolidinyl derivatives
7-Bicyclic derivatives
FD501 and FD103
Garenoxacin
MF5137
Antibacterial activities of the fluoroquinolones in terms of the substituents
Levofloxacin (4-quinolone/l-isomer of ofloxacin)
Enantiomeric derivatives of sitafloxacin
Enantiomers of trovafloxacin
Fluoroquinolones: structure-activity relationships and mycobacteria
Cytochrome P450 methylamine dehydrogenase inactivation with N-1 cyclopropyl quinolones
Trovafloxacin (esterification)
Prulifloxacin dioxil (NAD 394)/(NAD 441A)
Ofloxacin: N-succinimyl ester
Ester of tosufloxacin
Prodrugs of norfloxacin
3β-Methyl quinolones
Aurachins
G1499-2
Quinolones of natural origin (Pyo III to XII)
Quinolinol derivatives
CL-38489 derivatives
YM-30059
E. rutaecarpa extract products
Chemical classification of fluoroquinolones
Pyridone β-carboxylic acid, monocyclic derivative: Ro-13-5478
Quinolones: bicyclic derivatives with a pentacycle
Chemical classification of fluoroquinolones (group IIA)
Chemical classification of fluoroquinolones (group IIA)
Tricyclic derivatives: 1,8 bond at the quinoline nucleus
Tetracyclic derivatives
Biological classification of fluoroquinolones
Microbiological classification of fluoroquinolones
Ionization of quinolones: pH effect
S. pneumoniae 2816 (cefotaxime resistant) (killing pharmacokinetics) (adapted from Baquero et al., 1996; HMR data on file)
Activity of Y-34867 against H. pylori
Distribution of the bacterial population of S. pneumoniae (654 strains)
Antitrypanosomal quinolones
DC-756
ABT-492 (WQ-3034)
WQ-3330 and WQ-2942
Des(6F) quinolones
NSFQ-105 and derivatives
7-Alkylamino, N-1 5′-amino-2′,4′-difluorophenyl quinolones
WQ-2756
YH-6
6-Nitroquinolone
DQ-113
DK-507k
DW-286
DW-224
DX-619
AM-1939
Pradofloxacin
Piperazinyl-linked fluoroquinolones
WQ-0835
Transmembrane passage of fluoroquinolones
Efflux pump of fluoroquinolones
Phylogenetic tree of the evolution of six transporter families (TMS, tansmembrane segments)
Model of the mode of action of DNA gyrase
Two-door model
DNA supercoiling: action of DNA gyrase
Fixation of quinolone to DNA strand
Model of DNA gyrase interaction in quinolones
SOS response
Bactericidal activity
Bactericidal activity
Survival of E. coli KL-16 in phosphate buffer
Biphasic killing curves in E. coli KL-16 at different concentrations of ofloxacin and nalidixic acid
Epidemiology of the activity of levofloxacin and other fluoroquinolones against S. pneumoniae in Europe
Epidemiology of the activity of levofloxacin and other fluoroquinolones against S. pneumoniae in the United States
Regulation of the mar and sox genes of MAR
Pharmacodynamics (murine model)
Elimination pathway of fluoroquinolones
Metabolism of the 7-piperazinyl nucleus
Metabolism of trovafloxacin
Metabolites (others) of trovafloxacin
Metabolism of pazufloxacin
Metabolism of fluoroquinolones
Interactions of cations, antacids, and antiulcer agents
Al2+, Mg2+, Ca2+, Fe2+, and other cations form complexes with fluoroquinolones
Metabolism of theophylline in humans and potential interaction with fluoroquinolones
Nosocomial infection: microbiology
Nadifloxacin and T-3912
Phototoxicity
Phototoxic potential of fluoroquinolones (murine model)
In vitro and in vivo activities of the enantiomers of temafloxacin
Tosufloxacin: pharmacokinetics of the enantiomers
In vitro activities of the diastereoisomers of sitafloxacin
Pharmacokinetics of the enantiomers of gatifloxacin
In vitro activities of some fluoroquinolones against M. ulcerans
Physicochemical properties of quinolones
Physicochemical properties of quinolones
Effects of cations on the activity of ofloxacin and levofloxacin in Mueller-Hinton broth a
In vitro activities of fluoroquinolones against Staphylococcus spp.
Activities of fluoroquinolones against strains of S. aureus of reduced susceptibility to vancomycin
Activities of fluoroquinolones against streptococci
In vitro activities of fluoroquinolones against Enterococcus spp.
In vitro activities of fluoroquinolones against gram-positive bacilli
Fluoroquinolones and L. monocytogenes a
In vitro activities of quinolones against B. anthracis
In vitro activities of quinolones and other antibacterials against B. anthracis a
In vitro activities of fluoroquinolones against Enterobacteriaceae
In vitro activities of fluoroquinolones against nonfermentative gram-negative bacilli
In vitro activities of fluoroquinolones against nonfermentative gram-negative rods a
In vitro activities of fluoroquinolones against B. pertussis a
In vitro activities of fluoroquinolones against Rickettsia spp. a
In vitro activities of fluoroquinolones against Bartonella a
Activities of fluoroquinolones against C. burnetii a
In vitro activities of fluoroquinolones against B. melitensis a
In vitro activities of quinolones against Borrelia spp.
In vitro activities of antibiotics against Y. pestis a
In vivo activities of fluoroquinolones against Y. pestis
In vitro activities of fluoroquinolones against N. meningitidis
In vitro activities of ABT-492 and comparators against microaerophilic microorganisms
In vitro activities of fluoroquinolones against anaerobic gram-negative bacteria
In vitro activities of fluoroquinolones against anaerobic gram-positive bacteria
In vitro activities of quinolones against the B. fragilis group
In vitro activities of fluoroquinolones against common pathogens responsible for lower respiratory tract infections
In vitro activities of fluoroquinolones against atypical and intracellular bacteria responsible for respiratory tract infections
In vitro activities of fluoroquinolones against C. pneumoniae a
In vitro activities of fluoroquinolones against C. psittaci a
In vitro activities of fluoroquinolones against L. pneumophil a
In vivo efficacies of fluoroquinolones in pneumonia of guinea pigs due to L. pneumophila a
In vitro activities of fluoroquinolones against Mycoplasma spp.
In vitro activities of fluoroquinolones against different resistance phenotypes of N. gonorrhoeae a
In vitro activities of fluoroquinolones against G. vaginalis
In vitro activities of fluoroquinolones against Mobiluncus spp.
In vitro activities of fluoroquinolones against P. bivia
In vitro activities of quinolones against C. trachomatis a
In vitro activities of fluoroquinolones against M. hominis and U. urealyticum a
In vitro activities of fluoroquinolones against Mycoplasma species a
In vitro activities of fluoroquinolones against agents responsible for infections from bites
In vitro activities of fluoroquinolones against T. brucei
In vivo activities of fluoroquinolones against L. donovani infection in mice (n = 6)
In vitro activities of fluoroquinolones against P. carinii
In vivo efficacies of fluoroquinolones in pneumocystosis in rats
In vitro activities of the new quinolones
Comparative in vitro activity of ABT-492
Phototoxicity potential of fluoroquinolones
In vitro activity of DQ-113
Comparative in vitro activity of DK-507k
Therapeutic efficacy of DK-507k in murine systemic infections
Pharmacokinetics of DK-507k in rats (5 mg/kg) a
Pharmacokinetics of DK-507k in male monkeys (5 mg/kg)
Protein binding of DK-507k
Single-dose toxicity in rats and mice
In vitro activity of DW-286
In vivo efficacies of DW-286
In vitro activity of DX-619
In vitro activity of AM-1939 against gram-positive cocci
In vitro activity of veterinary fluoroquinolone against gram-negative bacilli from Felidae
Pradofloxacin activity against anaerobes from cats and dogs
Pharmacokinetics of pradofloxacin in dogs after oral dosing
In vitro activity of WQ-0835
Breakpoints of fluoroquinolones (French Antibiotic Sensitivity Test Committee, 1998)
Intracellular concentration and efflux of fluoroquinolones a
Intracellular accumulation of fluoroquinolones in E. coli
Properties of bacterial topoisomerases
Molecular weights of the two DNA gyrase subunits of different bacterial species
Molecular weights of the topoisomerase IV subunits of different bacterial species
Genes involved in the activity of fluoroquinolones a
Frequency of selection of mutants from S. pneumoniae R 6 a
Frequency of selection of mutants from S. pneumoniae R 6 t LLR6P16 a
Elimination of fluoroquinolones in the sudoriferous glands
Epidemiology of resistance to fluoroquinolones in 1992 to 1993 a
Incidence of resistance of methicillin-resistant strains of S. aureus to ciprofloxacin a
Mechanisms of resistance of the fluoroquinolones a
Mutations responsible for a reduction in intracellular accumulation a
Mutations in gyrB in E. coli
Mutations in GyrA of different bacterial species
Activities of ciprofloxacin and nalidixic acid in terms of the mutation points in E. coli GyrA
Mutations in topoisomerase IV
Activity of ciprofloxacin against mutant strains of N. gonorrhoeae in cell targets
OBCs of quinolones (E. coli KL-16) a
Oral pharmacokinetics of fluoroquinolones
Intravenous pharmacokinetics of fluoroquinolones
Fluoroquinolones: repeated-dose oral pharmacokinetics
Pharmacokinetics of ciprofloxacin extended-release tablets
Bioavailability and protein binding of quinolones
Pharmacokinetics of fluoroquinolones: effect of food
Effects of dairy products on the pharmacokinetics of fluoroquinolones
Pharmacokinetics of fluoroquinolones in elderly subjects
Pharmacokinetics of fluoroquinolones in patients with renal insufficiency
Trovafloxacin pharmacokinetics in patients with hepatic insufficiency
Grepafloxacin (400 mg every 24 h for 7 days) pharmacokinetics in patients with hepatic insufficiency
Gemifloxacin pharmacokinetics in hepatically impaired patients (320 mg single dose once a day)
Pharmacokinetics of alatrofloxacin in obese patients a
Fluoroquinolones: metabolism
Fluoroquinolones: main metabolites a
Classes of esterases
Pharmacokinetics of pefloxacin in burn patients
Fluoroquinolones: concentrations in serum in pregnant women
Concentrations of fluoroquinolones in amniotic fluid
Pharmacokinetics of trovafloxacin in AIDS patients
Pharmacokinetics of levofloxacin in HIV-positive patients
Distribution of fluoroquinolones in the bronchial mucosa
Concentrations of fluoroquinolones in respiratory tissue
Distribution of ofloxacin in the ear bones
Distribution of fluoroquinolones in cutaneous and subcutaneous tissues
Concentrations of ofloxacin in cutaneous tissue and the colonic wall a
Distribution of fluoroquinolones in noninflammatory CSF
Distribution of fluoroquinolones in inflammatory CSF
Distribution of fluoroquinolones in hepatobiliary tissues
Concentrations of fluoroquinolones in the eye
Pharmacokinetics of fluoroquinolones in tears
Penetration of fluoroquinolones into saliva
Pharmacokinetics of fleroxacin and temafloxacin in plasma and colostrum
Concentrations of fluoroquinolones in colostrum
Concentrations of fluoroquinolones in skin blister fluid
Interactions of fluoroquinolones with other medicinal products
Quinolones and antiulcer agents
Modifications of the pharmacokinetic parameters of fluoroquinolones after ingestion of aluminum hydroxide [Al(OH)3] a
Interactions of Maalox and ciprofloxacin
Fluoroquinolones and pharmacokinetics of theophylline
Interference with the pharmacokinetics of theophylline
Fluoroquinolones and nonsteroidal anti-inflammatory drugs (NSAIDs)
Pharmacokinetics of warfarin alone or in combination with levofloxacin
Pharmacokinetics of ciprofloxacin and didanosine
Pharmacokinetics of caffeine with trovafloxacin
Pharmacokinetics of ethanol in the presence of ciprofloxacin
Pharmacokinetics of digoxin in the presence of levofloxacin
Pharmacokinetics of fluoroquinolones with clindamycin or metronidazole
Plasma pharmacokinetics of metronidazole and clindamycin alone or in combination with fluoroquinolones
In vitro activity of zidovudine
Pharmacokinetics of morphine in combination with trovafloxacin
Pharmacokinetics of cyclosporine in the presence of levofloxacin
Duration of bactericidal activity of fluoroquinolones in the urine
Fecal concentrations of fluoroquinolones
Activities of fluoroquinolones against bacterial species responsible for traveler’s diarrhea
In vitro activities of fluoroquinolones against V. cholerae
In vitro activities of fluoroquinolones against Salmonella serovar Typhi
Bacteriology of superinfections of chronic bronchitis
Causative agents of community-acquired pneumonia a
Fluoroquinolones and atypical pneumonia
Prevalence of nosocomial infections in Europe in 1992 a
Pharmacokinetics of fluoroquinolones in patients with cystic fibrosis
Moxifloxacin concentrations in sinus tissues
In vitro activity of nadifloxacin
In vitro comparative activity of T-3912
In vitro activities of fluoroquinolones against M. tuberculosis
In vitro activities of fluoroquinolones against atypical mycobacteria
In vitro comparative activities of ciprofloxacin and gatifloxacin against rapidly growing mycobacteria
Efficacies of fluoroquinolones in the prevention of infections in neutropenic patients
Recommended treatment duration according to Schaad
Pharmacokinetics of ciprofloxacin in pediatric subjects
Pharmacokinetics of norfloxacin in children
Pharmacokinetics of alatrofloxacin in pediatric subjects
Pharmacokinetics of levofloxacin in pediatric subjects
Pharmacokinetics of intravenous gatifloxacin in children
Adverse effects recorded during phase II and III clinical trials a
Incidence of phototoxicity in patients of fluoroquinolones
Photocarcinogenicity of quinolones
Neuropsychiatric disorders due to quinolones
Occurrence of adverse effects on the central nervous system with fluoroquinolones
Concentrations of fluoroquinolones required to inhibit binding to the GABA receptor by 50%
Increase in wave amplitude: excitatory potential of fluoroquinolones on the central nervous system
Incidence of cartilaginous toxicity in juvenile rats
Frequency of abnormal laboratory test results
Effect of fluoroquinolones on fecal flora
Toxicity of fluoroquinolones