Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new avelox research articles will be listed here shortly after becoming available to us.
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Medical research on avelox
Antimicrob Agents Chemother. 2008 Jul 14;
Black MT, Stachyra T, Platel D, Girard AM, Claudon M, Bruneau JM, Miossec C
NXL101 is one of a new class of quinoline antibacterial DNA gyrase and topoisomerase IV inhibitors, showing potent activity against gram-positive bacteria including methicillin- and fluoroquinolone-resistant strains. NXL101 inhibited topoisomerase IV more effectively than gyrase from Escherichia coli, whereas the converse is true of enzymes from Staphylococcus aureus. This apparent target preference is opposite to that which is associated with most fluoroquinolone antibiotics. In vitro isolation of S. aureus mutants resistant to NXL101 followed by cloning and sequencing of the genes encoding gyrase and topoisomerase IV led to the identification of several different point mutations within, or close to, the quinolone-resistance determining region (QRDR) of GyrA. However, the mutations were not those that are most frequently associated with decreased sensitivity to quinolones. A fluoroquinolone-resistant mutant variant of gyrase generated in vitro was highly resistant to inhibition by the fluoroquinolones ciprofloxacin and moxifloxacin but remained fully susceptible to inhibition by NXL101. Two mutant gyrases constructed in vitro, with mutations in gyrA engineered according to those most frequently found in S. aureus strains resistant to NXL101, were insensitive to inhibition by NXL101, and had a diminished sensitivity to ciprofloxacin and moxifloxacin. Certain combinations of mutations giving rise to NXL101 resistance, and those giving rise to fluoroquinolone resistance, may be mutually exclusive.
Antimicrob Agents Chemother. 2008 Jul 14;
Liu CY, Huang YT, Liao CH, Yen LC, Lin HY, Hsueh PR
This study reported on the data of susceptibility of five commonly used anti-anaerobic agents to five clinically frequently encountered anaerobes from 2000 to 2007 and to Bacteroides fragilis isolates causing nosocomial infections from 1990 to 2006. There was a trend of decreasing susceptibilities to ampicillin-sulbactam, cefmetazole, chloramphenicol. and clindamycin with time to these anaerobes during the study period. Rates of susceptibility to clindamycin and cefmetazole for all clinical isolates of Bacteroides fragilis isolates were higher than those of isolates associated with nosocomial infections. Minimum inhibitory concentrations (MICs) of 207 anaerobic blood isolates collected in 2006 to 14 antimicrobial agents were determined by the agar dilution method. The non-susceptibility rates to imipenem (meropenem) was 7% (12%) for B. fragilis (n=60), 7% (3%) for B. thetaiotamicron (n=30), 4% (4%) for Fusobacterium species (n=27), 6% (0%) for Prevotella species (n=16), 15% (0%) for Clostridium species (n=28), and 0% (0%) for Peptostreptococcus species (n=32). The susceptibility rate to moxifloxacin was 90% for B. fragilis, 87% for B. thetaiotaomicron, 81% for Fusobacterium species, 75% for Prevotella species, 93% for Clostridium species, and 78% for Peptostreptococcus species. Thirty-six percent of Clostridium species and 12% of Peptostreptococcus species were not susceptible to metronidazole. Comparison of data with a previous survey from the same institute in 2002 revealed the higher rates of nonsusceptibility to carbapenems especially for B. fragilis, Fusobacterium species, and Prevotella species isolates. The high rates of nonsusceptibility to commonly used anti-anaerobic agents mandate our attention and periodic monitoring the trend of the resistance is crucial.
Antimicrob Agents Chemother. 2008 Jul 7;
Pultz MJ, Nerandzic MM, Stiefel U, Donskey CJ
After orogastric administration of a fluoroquinolone-resistant Klebsiella pneumoniae strain, subcutaneous ciprofloxacin, levofloxacin, and moxifloxacin promoted persistent low-density colonization in 10% to 40% of treated mice, whereas clindamycin consistently promoted high-density colonization. No emergence of fluoroquinolone-resistant gram-negative bacilli was detected during or after treatment with the fluoroquinolone antimicrobial agents.
Effect of brivaracetam on cardiac repolarisation - a thorough QT study.
Curr Med Res Opin. 2008 Jul 3;
Rosillon D, Astruc B, Hulhoven R, Meeus MA, Troenaru MM, Watanabe S, Stockis A
OBJECTIVES: To assess the effect on cardiac repolarisation of the investigational synaptic vesicle protein 2A (SV2A) ligand brivaracetam.RESEARCH DESIGN AND METHODS: Subjects received double-blind, multiple bid doses of placebo (n = 53), brivaracetam 75 mg (n = 39) or brivaracetam 400 mg (n = 40), or open-label single-dose moxifloxacin 400 mg (positive control, n = 52). Continuous 12-lead ECG recordings were performed at baseline and after last dosing, using a Mortara Holter device. Plasma samples were obtained before and up to 12 h after last dosing for drug determination. Triplicate ECGs were extracted before each sample, and read centrally in a blinded manner. QT was corrected using a centre- and gender-specific correction (QTc(SS)).MAIN OUTCOME MEASURES: The primary endpoint was the largest time-matched mean difference of QTc(SS) change from baseline between drug and placebo (maximum DeltaDeltaQTc(SS)). The same approach was adopted using the Fridericia's correction (QTc(F)). The relationships between DeltaQTc(SS) and plasma concentration of brivaracetam and moxifloxacin were fitted to a straight line using linear least-squares regression.RESULTS: Mean maximum DeltaDeltaQTc(SS) for brivaracetam 75 and 400 mg bid, and moxifloxacin 400 mg was 0.2 ms, -1.1 ms and 12.4 ms, respectively. The one-sided 95% upper limit for 75 mg and 400 mg brivaracetam was 4.3 ms and 3.0 ms, respectively; the one-sided 95% lower limit for moxifloxacin was 8.6 ms. After brivaracetam no QTc(SS) intervals >480 ms or changes from baseline of >60 ms were observed. DeltaQTc(SS) did not increase with plasma concentration of brivaracetam, whereas there was a statistically significant rise with increasing moxifloxacin concentrations.CONCLUSIONS: The study was found to be valid in terms of assay sensitivity and the results demonstrated the absence of effects of brivaracetam on cardiac repolarisation. These results suggest that no intensive cardiac monitoring is required during the subsequent stages of brivaracetam development.
Levofloxacin-induced delirium with psychotic features.
Gen Hosp Psychiatry. 2008 Jul-Aug; 30(4): 381-3
Kiangkitiwan B, Doppalapudi A, Fonder M, Solberg K, Bohner B
OBJECTIVE: To raise awareness of a rare but serious adverse effect of a commonly used medication. METHOD: Report of a case. RESULTS: A previously healthy 42-year-old woman presented with acute-onset delirium with psychotic features as a consequence of levofloxacin therapy. Withdrawal of the medication was associated with return of the patient's normal mental status. CONCLUSION: The new quinolone derivatives (levofloxacin, sparfloxacin, grepafloxacin, trovafloxacin, gatifloxacin and moxifloxacin), also called gyrase inhibitors, are known for their potential to cause central nervous system-related adverse effects, including headache, dizziness and insomnia. Risk factors for neurotoxicity include renal insufficiency, underlying central nervous system (CNS) disease and increased CNS penetration of drug. Acute delirium resulting from levofloxacin therapy is an exceedingly rare complication that has been thought to occur more commonly in elderly patients. Here, we describe levofloxacin-induced delirium with psychotic features in a relatively young, otherwise healthy female.
Severe acute polyarthritis in a child after high doses of moxifloxacin.
Scand J Infect Dis. 2008; 40(6): 582-4
Torres JR, Bajares A
Clinically severe, acute polyarthritis, associated with high doses of oral moxifloxacin, has been documented for the first time in a 12-y-old child. MR studies revealed massive joint effusion, as well as moderate ligament and cartilage damage. On follow-up, neither long-term sequelae nor functional impairment of the involved joints was observed.
Mycobacterium peregrinum: bactericidal activity of antibiotics alone and in combination.
J Infect Chemother. 2008 Jun; 14(3): 262-3
Santos A, Cremades R, Rodriguez JC, Garcia-Pachon E, Ruiz M, Royo G
Mycobacterium peregrinum is a rapidly growing mycobacterium that is occasionally associated with disease at different locations. At present, little information is available on antibiotic activity against this microorganism. For this reason, we have carried out a study on the in vitro activity of 15 antibiotics, alone and in combination, against M. peregrinum. Our study shows that the new fluoroquinolones with a C8-methoxy group, especially moxifloxacin, exhibit greater activity against this species. These data should be evaluated in clinical assays or animal models in order to confirm their clinical significance.
POWERFUL BACTERICIDAL ACTIVITY OF MOXIFLOXACIN IN HUMAN LEPROSY.
Antimicrob Agents Chemother. 2008 Jun 23;
Pardillo FE, Burgos J, Fajardo TT, Cruz ED, Abalos RM, Paredes RM, Andaya CE, Gelber RH
In a clinical trial of moxifloxacin in 8 multibacillary (MB) leprosy patients, moxifloxacin proved highly effective. In all trial patients a single 400 mg dose of moxifloxacin resulted in significant killing (p
Antimicrob Agents Chemother. 2008 Jun 23;
Jones RN, Fritsche TR, Sader HS
DC-159a, a novel orally administered fluorinated quinolone, was evaluated by reference broth microdilution or agar dilution methods against 1,149 recent clinical isolates from five continents. Against pathogens associated with community-acquired respiratory infections (CA-RTI), the MIC90 values (microg/ml) were: Streptococcus pneumoniae (0.12), Haemophilus influenzae (0.015-0.03), Moraxella catarrhalis (0.03) and beta-haemolytic streptococci (0.12). Similarly, DC-159a was potent against various types of staphylococci (MIC90 range, 0.03-2 microg/ml), Enterococcus faecalis (MIC90, 4 microg/ml), wildtype Enterobacteriaceae (MIC90 range, 0.06-2 microg/ml), WILDTYPE Pseudomonas aeruginosa (MIC90, 2 microg/ml) or Acinetobacter spp. (MIC90, 0.12 microg/ml). Fluoroquinolone-non-susceptible (NS) organism subsets usually had elevated DC-159a MIC values, but MIC results were often two- to four-fold lower than levofloxacin or moxifloxacin. In conclusion, DC-159a appears to possess a balanced broad-spectrum of activity exceeding that of currently marketed fluoroquinolones, especially against CA-RTI pathogens.
Antimicrob Agents Chemother. 2008 Jun 23;
Lismond A, Tulkens PM, Mingeot-Leclercq MP, Courvalin P, Van Bambeke F
Antibiotic efflux is observed in both eukaryotic and prokaryotic cells, modulating accumulation and resistance. The present study examines whether eukaryotic and prokaryotic fluoroquinolone transporters can cooperate in the context of an intracellular infection. We have used (i) J774 macrophages (comparing a ciprofloxacin-resistant cell line overexpressing an MRP-like transporter with wild-type cells with basal expression); (ii) Listeria monocytogenes (comparing a clinical isolate [CLIP21369] displaying ciprofloxacin resistance associated with overexpression of the Lde efflux system with a wild-type strain [EGD]); (iii) ciprofloxacin (substrate of both Lde and MRP) and moxifloxacin (non-substrate); (iv) probenecid and reserpine (preferential inhibitors of MRP and Lde, respectively). The ciprofloxacin MICs for EGD were unaffected by reserpine while those for CLIP21369 were decreased approximately 4-fold (and made similar to those of EGD). Neither probenecid nor reserpine affected the moxifloxacin MICs against EGD or CLIP21369. In dose-response studies (0.01-100 x MIC) in broth, reserpine fully restored susceptibility of CLIP21369 to ciprofloxacin (no effect on EGD), but did not influence the activity of moxifloxacin. In dose-response studies against intracellular bacteria, reserpine, probenecid, and their combination increased the activity of ciprofloxacin in wild-type and ciprofloxacin-resistant macrophages in parallel to their increase in ciprofloxacin accumulation in macrophages for EGD, and (ii) increase in accumulation and decrease in MIC (in broth) for CLIP21369. Moxifloxacin accumulation and intracellular activity were not consistently affected by the inhibitors. A bacterial efflux pump may thus actively cooperate with a eukaryotic efflux transporter to reduce the activity of a common substrate (ciprofloxacin) towards an intracellular bacterial target.