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American Journal of Veterinary Research Oct 2019To determine the pharmacokinetics of levofloxacin following oral administration of a generic levofloxacin tablet and IV administration to dogs and whether the achieved...
OBJECTIVE
To determine the pharmacokinetics of levofloxacin following oral administration of a generic levofloxacin tablet and IV administration to dogs and whether the achieved plasma levofloxacin concentration would be sufficient to treat susceptible bacterial infections.
ANIMALS
6 healthy adult Beagles.
PROCEDURES
Levofloxacin was administered orally as a generic 250-mg tablet (mean dose, 23.7 mg/kg) or IV as a solution (15 mg/kg) to each dog in a crossover study design, with treatments separated by a minimum 2-day washout period. Blood samples were collected at various points for measurement of plasma levofloxacin concentration via high-pressure liquid chromatography. Pharmacokinetic analysis was performed with compartmental modeling.
RESULTS
After oral administration of the levofloxacin tablet, mean (coefficient of variation) peak plasma concentration was 15.5 μg/mL (23.8%), mean elimination half-life was 5.84 hours (20.0%), and mean bioavailability was 104% (29.0%). After IV administration, mean elimination half-life (coefficient of variation) was 6.23 hours (14.7%), systemic clearance was 145.0 mL/kg/h (22.2%), and volume of distribution was 1.19 L/kg (17.1%).
CONCLUSIONS AND CLINICAL RELEVANCE
In these dogs, levofloxacin was well absorbed when administered orally, and a dose of approximately 25 mg/kg was sufficient to reach pharmacokinetic-pharmacodynamic targets for treating infections with susceptible Enterobacteriaceae (ie, ≤ 0.5 μg/mL) or (ie, ≤ 1 μg/mL) according to clinical breakpoints established by the Clinical and Laboratory Standards Institute.
Topics: Administration, Intravenous; Administration, Oral; Animals; Anti-Bacterial Agents; Area Under Curve; Biological Availability; Chromatography, High Pressure Liquid; Cross-Over Studies; Dogs; Female; Half-Life; Levofloxacin; Male; Tablets
PubMed: 31556716
DOI: 10.2460/ajvr.80.10.957 -
PloS One 2023The negative consequences of Substandard and falsified (SF) medicines are widely documented nowadays and there is still an urgent need to find them in more efficient...
The negative consequences of Substandard and falsified (SF) medicines are widely documented nowadays and there is still an urgent need to find them in more efficient ways. Several screening tools have been developed for this purpose recently. In this study, three screening tools were used on 292 samples of ciprofloxacin and metronidazole collected in Cameroon. Each sample was then analyzed by HPLC and disintegration tests. Seven additional samples from the nitro-imidazole (secnidazole, ornidazole, tinidazole) and the fluoroquinolone (levofloxacin, ofloxacin, norfloxacin, moxifloxacin) families were analyzed to mimic falsified medicines. Placebo samples that contained only inert excipients were also tested to mimic falsified samples without active pharmaceutical ingredient (API). The three screening tools implemented were: a simplified visual inspection checklist, a low-cost handheld near infrared (NIR) spectrophotometer and paper analytical devices (PADs). Overall, 61.1% of the samples that failed disintegration and assay tests also failed the visual inspection checklist test. For the handheld NIR, one-class classifier models were built to detect the presence of ciprofloxacin and metronidazole, respectively. The APIs were correctly identified in all the samples with sensitivities and specificities of 100%. However, the importance of a representative and up-to-date spectral database was underlined by comparing models built with different calibration set spanning different variability spaces. The PADs were used only on ciprofloxacin samples and detected the API in all samples in which the presence of ciprofloxacin was confirmed by HPLC. However, these PADs were not specific to ciprofloxacin since they reacted like ciprofloxacin to other fluoroquinolone compounds. The advantages and drawbacks of each screening tool were highlighted. They are promising means in the frame of early detection of SF medicines and they can increase the speed of decision about SF medicines in the context of pharmaceutical post-marketing surveillance.
Topics: Humans; Metronidazole; Counterfeit Drugs; Substandard Drugs; Ciprofloxacin; Levofloxacin; Product Surveillance, Postmarketing
PubMed: 37566594
DOI: 10.1371/journal.pone.0289865 -
Antimicrobial Agents and Chemotherapy Jul 2015There is an urgent need to improve and shorten the treatment of tuberculosis (TB) and multidrug resistant tuberculosis (MDR-TB). Levofloxacin, a newer fluoroquinolone,...
There is an urgent need to improve and shorten the treatment of tuberculosis (TB) and multidrug resistant tuberculosis (MDR-TB). Levofloxacin, a newer fluoroquinolone, has potent activity against TB both in vitro and in vivo. Levofloxacin dosing can be optimized to improve the treatment of both TB and MDR-TB. Levofloxacin efficacy is linked primarily to the ratio of the area under the concentration-time curve for the free fraction of drug (fAUC) to the MIC. Since obtaining a full-time concentration profile is not feasible in the clinic, we developed a limited sampling strategy (LSS) to estimate the AUC. We also utilized Monte Carlo simulations to evaluate the dosing of levofloxacin. Pharmacokinetic data were obtained from 10 Brazilian TB patients. The pharmacokinetic data were fitted with a one-compartment model. LSSs were developed using two methods: linear regression and Bayesian approaches. Several LSSs predicted levofloxacin AUC with good accuracy and precision. The most accurate were the method using two samples collected at 4 and 6 h (R(2) = 0.91 using linear regression and 0.97 using Bayesian approaches) and that using samples collected at 2 and 6 h (R(2) = 0.90 using linear regression and 0.96 using Bayesian approaches). The 2-and-6-h approach also provides a good estimate of the maximum concentration of the drug in serum (Cmax). Our target attainment analysis showed that higher doses (17 to 20 mg/kg of body weight) of levofloxacin might be needed to improve its activity. Doses in the range of 17 to 20 mg/kg showed good target attainment for MICs from 0.25 to 0.50. At an MIC of 2, poor target attainment was observed across all doses. This LSS for levofloxacin can be used for therapeutic drug monitoring and for future pharmacokinetic/pharmacodynamic studies.
Topics: Adolescent; Adult; Aged; Antitubercular Agents; Area Under Curve; Brazil; Humans; Levofloxacin; Microbial Sensitivity Tests; Middle Aged; Models, Biological; Monte Carlo Method; Mycobacterium tuberculosis; Tuberculosis, Multidrug-Resistant; Tuberculosis, Pulmonary; Young Adult
PubMed: 25870068
DOI: 10.1128/AAC.00341-15 -
The Journal of Infection Jun 2023
Topics: Humans; Meropenem; Burkholderia pseudomallei; Levofloxacin; Taiwan; Anti-Bacterial Agents; Melioidosis
PubMed: 37003522
DOI: 10.1016/j.jinf.2023.03.022 -
Revista Espanola de Enfermedades... Jun 2020According to some series, 0.3-1.5% of all cases of acute pancreatitis are drug induced. Acute pancreatitis due to levofloxacin is included in its safety data sheet as an...
According to some series, 0.3-1.5% of all cases of acute pancreatitis are drug induced. Acute pancreatitis due to levofloxacin is included in its safety data sheet as an adverse effect.
Topics: Acute Disease; Humans; Levofloxacin; Pancreatitis
PubMed: 32496110
DOI: 10.17235/reed.2020.6652/2019 -
Clinical Experience of Using a Combination of Dexamethasone and Levofloxacin After Cataract Surgery.Medical Archives (Sarajevo, Bosnia and... 2024Where routine prophylactic antibiotics have been adopted following cataract surgery, rates of endophthalmitis have been decreasing. Intracameral and topical antibiotics...
BACKGROUND
Where routine prophylactic antibiotics have been adopted following cataract surgery, rates of endophthalmitis have been decreasing. Intracameral and topical antibiotics are currently used to prevent endophthalmitis after cataract surgery. When applying topical antibiotics, there are different recommendations on the frequency and duration of therapy. The development of bacterial resistance to the excessive and long-term use of antibiotics is a growing problem worldwide. The goal is to achieve a good antibiotic effect with the shortest possible use of antibiotics.
OBJECTIVE
The aim of this study was to compare the effectiveness of a new combination therapy of dexamethasone and levofloxacin for seven days after cataract surgery with the previous regimen of dexamethasone, neomycin sulfate, and polymyxin B, which was given for 21 days.
METHODS
A retrospective analysis of medical records and administered a questionnaire was conducted to assess the effectiveness of postoperative therapy in our cataract surgery patients. The study involved 52 patients who underwent surgery within the last year, performed by a single surgeon at our institution. The findings can help us improve the quality of care we provide and optimize our patients' overall quality of life.
RESULTS
We conducted an in-depth study on 52 individuals who underwent cataract surgery at our institution. The prescribed therapeutic regimen for the participants included administering Ducressa solution four times daily for the first seven days and Maxidex solution three times daily for the subsequent 14 days. The study found that none of the participants experienced complications after surgery, and all found it easy to instill the medication. The prescribed regimen effectively managed the postoperative recovery of the participants, and the medication was well-tolerated.
CONCLUSION
Our research found that a new combination of levofloxacin and dexamethasone, when used topically, may require a shorter treatment period, reducing the risk of antibiotic resistance and providing a safe alternative for endophthalmitis prevention.
Topics: Humans; Levofloxacin; Retrospective Studies; Quality of Life; Postoperative Complications; Anti-Bacterial Agents; Cataract Extraction; Dexamethasone; Endophthalmitis; Cataract
PubMed: 38566870
DOI: 10.5455/medarh.2024.78.127-130 -
Archives of Medical Research Oct 2020Since the beginning of the COVID-19 pandemic, researchers have focused on repurposing of existing antibiotics, antivirals and anti-inflammatory drugs to find an...
Since the beginning of the COVID-19 pandemic, researchers have focused on repurposing of existing antibiotics, antivirals and anti-inflammatory drugs to find an effective therapy. Fluoroquinolones are broad spectrum synthetic antimicrobial agents, being chemical derivatives of quinoline, the prodrome of chloroquine. Interestingly, fluoroquinolones may exert antiviral actions against vaccinia virus, papovavirus, CMV, VZV, HSV-1, HSV-2, HCV and HIV. A recent in silico study has shown that the fluoroquinolones, ciprofloxacin and moxifloxacin, may inhibit SARS-CoV-2 replication by exhibiting stronger capacity for binding to its main protease than chloroquine and nelfinavir, a protease inhibitor antiretroviral drug. Remarkably, fluoroquinolones have shown multiple immunomodulatory actions leading to an attenuation of the inflammatory response through the inhibition of pro-inflammatory cytokines. Noteworthy, respiratory fluoroquinolones, levofloxacin and moxifloxacin, constitute fist line therapeutic agents for the management of severe community-acquired pneumonia. They are characterized by advantageous pharmacokinetic properties; higher concentrations in the lungs; and an excellent safety profile comparable to other antibiotics used to treat respiratory infections, such as macrolides and b-lactams. Based on their potential antiviral activity and immunomodulatory properties, the favorable pharmacokinetics and safety profile, we propose the use of respiratory fluoroquinolones as adjuncts in the treatment of SARS-CoV-2 associated pneumonia.
Topics: Antiviral Agents; Humans; Levofloxacin; Moxifloxacin; SARS-CoV-2; COVID-19 Drug Treatment
PubMed: 32546446
DOI: 10.1016/j.arcmed.2020.06.004 -
Biomedica : Revista Del Instituto... May 2019Introduction: The main cause for Helicobacter pylori infection treatment failure is antibiotic resistance, where clarithromycin and metronidazole play the main role. In...
Introduction: The main cause for Helicobacter pylori infection treatment failure is antibiotic resistance, where clarithromycin and metronidazole play the main role. In Colombia, primary resistance as a consequence of the use of these two antibiotics and excessive levofloxacin use is above the accepted limit (13.6%, 83%, and 16%, respectively). Despite this fact, empirical therapies that include the combination of these antibiotics are used in patients with previous therapeutic failure. Objective: To determine antibiotic resistance in patients previously treated for H. pylori in Bogotá, Colombia. Materials and methods: We conducted a descriptive study that included ten isolates obtained from five patients with three or four previous failed treatments for H. pylori. Antibiotic resistance to amoxicillin, clarithromycin, levofloxacin, and metronidazole was investigated by agar dilution and confirmed by DNA sequencing (Magrogen, Korea). Results: Eight isolates were resistant to two or more antibiotics. All isolates were resistant to levofloxacin. Susceptibility patterns in isolates from the gastric antrum and the body of the stomach were different in three patients. Conclusion: As far as we know, this is the first evidence of multiple H. pylori resistance in Colombia in previously treated patients. Results demonstrated the consequences of using an ineffective antibiotic scheme and the need to assess antibiotic susceptibility in different anatomical sites of the stomach. The consequences of multiple resistance decrease possible antibiotic effectiveness to eradicate H. pylori in the future.
Topics: Adult; Aged; Amoxicillin; Anti-Bacterial Agents; Biopsy; Clarithromycin; Colombia; DNA, Bacterial; Drug Resistance, Multiple, Bacterial; Female; Gastritis; Gastroscopy; Genes, Bacterial; Helicobacter Infections; Helicobacter pylori; Humans; Levofloxacin; Male; Metronidazole; Microbial Sensitivity Tests; Middle Aged
PubMed: 31529855
DOI: 10.7705/biomedica.v39i3.4437 -
BMC Microbiology Jul 2016The emergence and spread of multidrug resistant methicillin-resistant Staphylococcus aureus (MDR-MRSA) has serious health consequences in the presence of sub-MIC...
BACKGROUND
The emergence and spread of multidrug resistant methicillin-resistant Staphylococcus aureus (MDR-MRSA) has serious health consequences in the presence of sub-MIC antibiotics. Therefore, this study was designed to evaluate β-lactamase activity, efflux activity, biofilm formation, and gene expression pattern in Staphylococcus aureus KACC 10778, S. aureus ATCC 15564, and S. aureus CCARM 3080 exposed to sublethal concentrations of levofloxacin and oxacillin.
RESULTS
The decreased MICs were observed in S. aureus KACC and S. aureus ATCC when exposed to levofloxacin and oxacillin, while and S. aureus CCARM remained resistance to streptomycin (512 μg/mL) in the presence of levofloxacin and imipenem (>512 μg/mL) in the presence of oxacillin. The considerable increase in extracellular and membrane-bound β-lactamase activities was observed in S. aureus ATCC exposed to oxacillin (>26 μmol/min/mL). The antibiotic susceptibility of all strains exposed to EPIs (CCCP and PAβN) varied depending on the classes of antibiotics. The relative expression levels of adhesion-related genes (clfA, clfB, fnbA, fnnB, and icaD), efflux-related genes (norB, norC, and qacA/B), and enterotoxin gene (sec) were increased more than 5-fold in S. aureus CCARM. The eno and qacA/B genes were highly overexpressed by more than 12- and 9-folds, respectively, in S. aureus CCARM exposed to levofloxacin. The antibiotic susceptibility, lactamase activity, biofilm-forming ability, efflux activity, and gene expression pattern varied with the intrinsic antibiotic resistance of S. aureus KACC, S. aureus ATCC, and S. aureus CCARM exposed to levofloxacin and oxacillin.
CONCLUSIONS
This study would provide useful information for better understating of combination therapy related to antibiotic resistance mechanisms and open the door for designing effective antibiotic treatment protocols to prevent excessive use of antibiotics in clinical practice.
Topics: Adhesins, Bacterial; Bacterial Adhesion; Bacterial Proteins; Biofilms; Carbonyl Cyanide m-Chlorophenyl Hydrazone; Coagulase; Dipeptides; Drug Resistance, Multiple, Bacterial; Gene Expression Regulation, Bacterial; Genes, Bacterial; Genotype; Imipenem; Levofloxacin; Membrane Transport Proteins; Methicillin-Resistant Staphylococcus aureus; Microbial Sensitivity Tests; Oxacillin; Phenotype; Polymerase Chain Reaction; Staphylococcus aureus; Streptomycin; beta-Lactamases
PubMed: 27473500
DOI: 10.1186/s12866-016-0791-7 -
Journal of Global Antimicrobial... Dec 2022This study presents 2016-2018 in vitro antimicrobial activity data and rates of resistant phenotypes for clinical isolates of Acinetobacter baumannii from Africa/Middle...
OBJECTIVES
This study presents 2016-2018 in vitro antimicrobial activity data and rates of resistant phenotypes for clinical isolates of Acinetobacter baumannii from Africa/Middle East, Asia/South Pacific, Europe, Latin America, and North America.
METHODS
A total of 4320 A. baumannii isolates were collected across all regions between 2016 and 2018. The in vitro antimicrobial activities of amikacin, colistin, levofloxacin, meropenem, and tigecycline were determined using the broth microdilution methodology of the Clinical and Laboratory Standards Institute. MICs were interpreted using the European Committee on Antimicrobial Susceptibility Testing (EUCAST) breakpoints (version 11.0). Rates of subsets that were resistant to amikacin, colistin, levofloxacin, and meropenem, according to EUCAST breakpoints, are also presented.
RESULTS
In each region, tigecycline and colistin were active against isolates of A. baumannii (MIC values, 1 or 2 mg/L) and the lowest rate of resistance was to colistin (1.2%-7.3%). The rates of resistance to the panel of agents were generally lower among A. baumannii from North America (1.3%-42.7%), compared with the other regions. Fewer than 11% of meropenem-resistant A. baumannii were also resistant to colistin. The rates of amikacin-, levofloxacin- and meropenem-resistant A. baumannii were lowest in North America and mostly higher in Africa/Middle East and Latin America.
CONCLUSION
In each geographical region, tigecycline and colistin maintained good in vitro antimicrobial activity against isolates of A. baumannii, including antimicrobial-resistant subsets. The higher rates of meropenem-resistant isolates, particularly in Africa/Middle East and Latin America, require continued monitoring because of the scarcity of effective treatment options.
Topics: Tigecycline; Acinetobacter baumannii; Amikacin; Colistin; Meropenem; Levofloxacin; Gram-Negative Bacteria; Anti-Bacterial Agents; Phenotype
PubMed: 35948242
DOI: 10.1016/j.jgar.2022.08.002