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Medicines (Basel, Switzerland) May 2023Fluoroquinolones (FQNs) are related to several central nervous system side effects. This review aims to evaluate the clinical-epidemiological profile, pathophysiological... (Review)
Review
BACKGROUND
Fluoroquinolones (FQNs) are related to several central nervous system side effects. This review aims to evaluate the clinical-epidemiological profile, pathophysiological mechanisms, and management of FQNs-associated movement disorders (MDs).
METHODS
Two reviewers identified and assessed relevant reports in six databases without language restriction between 1988 and 2022.
RESULTS
A total of 45 reports containing 51 cases who developed MDs secondary to FQNs were reported. The MDs included 25 myoclonus, 13 dyskinesias, 7 dystonias, 2 cerebellar syndromes, 1 ataxia, 1 tic, and 2 undefined cases. The FQNs reported were ciprofloxacin, ofloxacin, gatifloxacin, moxifloxacin, levofloxacin, gemifloxacin, and pefloxacin. The mean and median age were 64.54 (SD: 15.45) and 67 years (range: 25-87 years). The predominant sex was male (54.16%). The mean and median time of MD onset were 6.02 (SD: 10.87) and 3 days (range: 1-68 days). The mean and median recovery time after MD treatment was 5.71 (SD: 9.01) and 3 days (range: 1-56 days). A complete recovery was achieved within one week of drug withdrawal in 80.95% of the patients. Overall, 95.83% of the individuals fully recovered after management.
CONCLUSIONS
Future cases need to describe the long-term follow-up of the individuals. Additionally, FQN-induced myoclonus should include electrodiagnostic studies.
PubMed: 37367728
DOI: 10.3390/medicines10060033 -
Lipids in Health and Disease Feb 2015To investigate whether amoxillin and pefloxacin perturb lipid metabolism.
BACKGROUND
To investigate whether amoxillin and pefloxacin perturb lipid metabolism.
METHODS
Rats were treated with therapeutic doses of each antibiotic for 5 and 10 days respectively. Twenty four hours after the last antibiotic treatment and 5 days after antibiotic withdrawal, blood and other tissues (liver, kidney, brain, heart and spleen) were removed from the animals after an overnight fast and analysed for their lipid contents.
RESULTS
Both antibiotics produced various degrees of compartment-specific dyslipidemia in the animals. While plasma and erythrocyte dyslipidemia was characterised by up-regulation of the concentrations of the major lipids (cholesterol, triglycerides, phospholipids and free fatty acids), hepatic and renal dyslipidemia was characterised by cholesterogenesis and phospholipidosis. Splenic dyslipidemia was characterised by cholesterogenesis and decreased phospholipid levels. Cardiac and brain cholesterol contents were not affected by the antibiotics. A transient phospholipidosis was observed in the brain whereas cardiac phospholipids decreased significantly. Lipoprotein abnormalities were reflected as down-regulation of HDL cholesterol. Furthermore, the two antibiotics increased the activity of hepatic HMG-CoA reductase. Although erythrocyte phospholipidosis was resolved 5 days after withdrawing the antibiotics, dyslipidemia observed in other compartments was still not reversible.
CONCLUSION
Our findings suggest that induction of cholesterogenesis and phospholipidosis might represent additional adverse effects of amoxillin and pefloxacin.
Topics: Acyl Coenzyme A; Amoxicillin; Animals; Anti-Bacterial Agents; Brain Chemistry; Cholesterol; Erythrocytes; Kidney; Liver; Lung; Male; Myocardium; Pefloxacin; Phospholipids; Rats; Spleen
PubMed: 25879817
DOI: 10.1186/s12944-015-0011-8 -
Journal of Food Protection May 2018Lomefloxacin (LOM) and pefloxacin (PEF) are synthetic antibiotics that have been used in the treatment of infectious diseases in both human and animals. In the People's...
Lomefloxacin (LOM) and pefloxacin (PEF) are synthetic antibiotics that have been used in the treatment of infectious diseases in both human and animals. In the People's Republic of China, the use of LOM and PEF in livestock has been prohibited because of the concern that the residues of these drugs may pose a risk to public health. Despite this prohibition, these drugs are still being used in the poultry industry illegally, and so far there has been no systematic study of the persistence of LOM and PEF residues in chickens. In this study, laying hens were treated with a daily dose (10 mg/kg of body weight) of LOM or PEF for five consecutive days, and the drug residues in various tissues and eggs were determined over a 15-day period after the last drug administration. The highest LOM and PEF residual concentrations were found in the tissues 4 h after the last drug administration, and concentrations gradually decreased over time. Plasma had the lowest and liver had the highest residual concentrations throughout the 15-day study period. At the end of the 15 days, 3.64 ± 0.74 μg/kg LOM and 1.78 ± 0.28 μg/kg PEF were detected in the liver, with slightly lower residual concentrations in the kidney. No LOM or PEF residue was detected in the ovarian follicle, plasma, and muscle at the end of the 15 days. In eggs, the depletion rate of LOM was slower than that of PEF. LOM and PEF residues were detected in whole eggs for up to 10 and 8 days, respectively, after drug administration ceased. These findings suggest that the liver and, to a lesser extent, the kidney may be the sites where LOM or PEF residues would persist. This information can be a reliable reference for governmental agencies with respect to the screening of LOM and PEF residues in food products derived from laying hens.
Topics: Animals; Anti-Bacterial Agents; Chickens; China; Drug Residues; Eggs; Female; Fluoroquinolones; Organ Specificity; Pefloxacin
PubMed: 29637810
DOI: 10.4315/0362-028X.JFP-17-422 -
Frontiers in Veterinary Science 2017The pharmacokinetics of pefloxacin after single 10 mg/kg BW intravenous (IV) and oral doses were studied in healthy broiler chickens. For 24 h, serial blood samples...
The pharmacokinetics of pefloxacin after single 10 mg/kg BW intravenous (IV) and oral doses were studied in healthy broiler chickens. For 24 h, serial blood samples were obtained after IV and oral administration. Concentrations of pefloxacin and its major metabolite -demethyl pefloxacin (norfloxacin) were measured by use of high-performance liquid chromatography. The plasma concentrations-time data were found to fit a two-compartment open model. For pefloxacin, the elimination half-life () was 8.44 ± 0.48 and 13.18 ± 0.82 h after IV and oral administration, respectively. After single oral dose, pefloxacin was rapidly absorbed with an absorption half-life () and of 0.87 ± 0.07 and 2.01 ± 0.12 h, respectively. Maximum plasma concentration () was 4.02 ± 0.31 µg/mL. Oral bioavailability of pefloxacin was found to be 70 ± 2%. Pefloxacin was converted to -demethyl pefloxacin (norfloxacin). This metabolite represented 5% of the parent drug plasma concentrations. The maximal plasma concentration () of -demethyl pefloxacin (norfloxacin) was calculated as 0.19 ± 0.01 mg/mL. The of -demethyl pefloxacin after oral pefloxacin administration was 10.93 ± 0.80 h. The results indicate that an oral dose of 10 mg pefloxacin/kg BW, every 24 h, should be effective in treatment of the most systemic infections in poultry.
PubMed: 28596959
DOI: 10.3389/fvets.2017.00077 -
Pharmaceutics Jul 2019Quinolone antibiotics present an attractive oral treatment option in patients with cystic fibrosis (CF). Prior studies have reported comparable clearances and volumes of...
Quinolone antibiotics present an attractive oral treatment option in patients with cystic fibrosis (CF). Prior studies have reported comparable clearances and volumes of distribution in patients with CF and healthy volunteers for primarily renally cleared quinolones. We aimed to provide the first pharmacokinetic comparison for pefloxacin as a predominantly nonrenally cleared quinolone and its two metabolites between both subject groups. Eight patients with CF (fat-free mass [FFM]: 36.3 ± 6.9 kg, average ± SD) and ten healthy volunteers (FFM: 51.7 ± 9.9 kg) received 400 mg pefloxacin as a 30 min intravenous infusion and orally in a randomized, two-way crossover study. All plasma and urine data were simultaneously modelled. Bioavailability was complete in both subject groups. Pefloxacin excretion into urine was approximately 74% higher in patients with CF compared to that in healthy volunteers, whereas the urinary excretion of metabolites was only slightly higher in patients with CF. After accounting for body size and composition via allometric scaling by FFM, pharmacokinetic parameter estimates in patients with CF divided by those in healthy volunteers were 0.912 for total clearance, 0.861 for nonrenal clearance, 1.53 for renal clearance, and 0.916 for volume of distribution. Nonrenal clearance accounted for approximately 90% of total pefloxacin clearance. Overall, bioavailability and disposition were comparable between both subject groups.
PubMed: 31295857
DOI: 10.3390/pharmaceutics11070323 -
Journal of Laboratory Physicians Dec 2020Typhoid fever, caused by and , is a generalized infection with case fatality of about 10%. The symptoms may be severe, with life threatening sequelae of infection in...
Typhoid fever, caused by and , is a generalized infection with case fatality of about 10%. The symptoms may be severe, with life threatening sequelae of infection in a proportion of cases. Antimicrobial agents are the mainstay of therapy in enteric fever so as to prevent the complications associated with severe illness and mortality in the patients. Fluoroquinolones (e.g., ciprofloxacin) are very effective against completely susceptible bacteria. However, their efficacy is doubtful once any resistance is detected. Pefloxacin testing has ultimately helped in the accurate identification of quinolone susceptibility for a better therapeutic success rate. In the present study we have tried to evaluate the quinolone susceptibility in isolates based on minimum inhibitory concentration (MIC) determination. The method used in the study is quinolone susceptibility in isolates based on MIC determination. isolates show intermediate susceptibility to ciprofloxacin using disk diffusion. Both ciprofloxacin and pefloxacin MIC evaluation has been done to corroborate the results with pefloxacin disk diffusion testing. There was a positive correlation between the susceptibility to ciprofloxacin and pefloxacin. However, the isolates with intermediate susceptibility had variations in terms of susceptibility to pefloxacin. MIC values for pefloxacin and our findings suggested that pefloxacin susceptible on disk diffusion as per Clinical and Laboratory Standards Institute guidelines showed lower values for MIC using Pefloxacin HICOMB test and pefloxacin resistant isolates showed higher MIC values.
PubMed: 33390675
DOI: 10.1055/s-0040-1721163 -
ACS Chemical Neuroscience Jun 2022Quinolone antibiotics disrupt bacterial DNA synthesis by interacting with DNA gyrase and topoisomerase IV. However, in addition, they have been shown to act as...
Quinolone antibiotics disrupt bacterial DNA synthesis by interacting with DNA gyrase and topoisomerase IV. However, in addition, they have been shown to act as inhibitors of pentameric ligand-gated ion channels such as GABA receptors and the α7 nicotinic acetylcholine receptor (nAChR). In the present study, we have examined the effects of quinolone antibiotics on the human α4β2 nAChR, an important subtype that is widely expressed in the central nervous system. A key feature of α4β2 nAChRs is their ability to coassemble into two distinct stoichiometries, (α4)(β2) and (α4)(β2), which results in differing affinities for acetylcholine. The effects of nine quinolone antibiotics were examined on both stoichiometries of the α4β2 receptor by two-electrode voltage-clamp recording. All compounds exhibited significant inhibition of α4β2 nAChRs. However, all of the fluoroquinolone antibiotics examined (ciprofloxacin, enoxacin, enrofloxacin, difloxacin, norfloxacin, pefloxacin, and sparfloxacin) were significantly more potent inhibitors of (α4)(β2) nAChRs than of (α4)(β2) nAChRs. This stoichiometry-selective effect was most pronounced with pefloxacin, which inhibited (α4)(β2) nAChRs with an IC of 26.4 ± 3.4 μM but displayed no significant inhibition of (α4)(β2) nAChRs. In contrast, two nonfluorinated quinolone antibiotics (cinoxacin and oxolinic acid) exhibited no selectivity in their inhibition of the two stoichiometries of α4β2. Computational docking studies suggest that pefloxacin interacts selectively with an allosteric transmembrane site at the β2(+)/β2(-) subunit interface, which is consistent with its selective inhibition of (α4)(β2). These findings concerning the antagonist effects of fluoroquinolones provide further evidence that differences in the subunit stoichiometry of heteromeric nAChRs can result in substantial differences in pharmacological properties.
Topics: Anti-Bacterial Agents; Fluoroquinolones; Humans; Nicotinic Antagonists; Oocytes; Pefloxacin; Receptors, Nicotinic
PubMed: 35657695
DOI: 10.1021/acschemneuro.2c00200 -
MicrobiologyOpen Nov 2019Aeromonas is recognized as a human pathogen following ingestion of contaminated food and water. One major problem in Aeromonas identification is that certain species are...
Proteomic characterization and discrimination of Aeromonas species recovered from meat and water samples with a spotlight on the antimicrobial resistance of Aeromonas hydrophila.
Aeromonas is recognized as a human pathogen following ingestion of contaminated food and water. One major problem in Aeromonas identification is that certain species are phenotypically very similar. The antimicrobial resistance is another significant challenge worldwide. We therefore aimed to use mass spectrometry technology for identification and discrimination of Aeromonas species and to screen the antimicrobial resistance of Aeromonas hydrophila (A. hydrophila). A total of 150 chicken meat and water samples were cultured, and then, the isolates were identified biochemically by the Vitek 2 Compact system. Proteomic identification was performed by MALDI-TOF MS and confirmed by a microchannel fluidics electrophoresis assay. Principal component analysis (PCA) and single-peak analysis created by MALDI were also used to discriminate the Aeromonas species. The antimicrobial resistance of the A. hydrophila isolates was determined by Vitek 2 AST cards. In total, 43 samples were positive for Aeromonas and comprised 22 A. hydrophila, 12 Aeromonas caviae (A. caviae), and 9 Aeromonas sobria (A. sobria) isolates. Thirty-nine out of 43 (90.69%) Aeromonas isolates were identified by the Vitek 2 Compact system, whereas 100% of the Aeromonas isolates were correctly identified by MALDI-TOF MS with a score value ≥2.00. PCA successfully separated A. hydrophila, A. caviae and A. sobria isolates into two groups. Single-peak analysis revealed four discriminating peaks that separated A. hydrophila from A. caviae and A. sobria isolates. The resistance of A. hydrophila to antibiotics was 95.46% for ampicillin, 50% for cefotaxime, 45.45% for norfloxacin and pefloxacin, 36.36% for ceftazidime and ciprofloxacin, 31.81% for ofloxacin and 27.27% for nalidixic acid and tobramycin. In conclusion, chicken meat and water were tainted with Aeromonas spp., with a high occurrence of A. hydrophila. MALDI-TOF MS is a powerful technique for characterizing aeromonads at the genus and species levels. Future studies should investigate the resistance of A. hydrophila to various antimicrobial agents.
Topics: Aeromonas; Aeromonas caviae; Aeromonas hydrophila; Animals; Anti-Bacterial Agents; Bacterial Proteins; Bacterial Typing Techniques; Chickens; Drug Resistance, Bacterial; Humans; Meat; Microbial Sensitivity Tests; Proteome; Proteomics; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; Water Microbiology
PubMed: 30614207
DOI: 10.1002/mbo3.782 -
The Journal of Toxicological Sciences Jun 2011Four fluoroquinolones (pefloxacin, norfloxacin, ofloxacin and ciprofloxacin) were compared according to their biomechanical and histopathological effects on rat Achilles... (Comparative Study)
Comparative Study
Four fluoroquinolones (pefloxacin, norfloxacin, ofloxacin and ciprofloxacin) were compared according to their biomechanical and histopathological effects on rat Achilles tendon. Wistar rats were divided into one untreated control and four treatment groups in parallel. Pefloxacin mesylate dihydrate (40 mg/kg), norfloxacin (40 mg/kg), ofloxacin (20 mg/kg) and ciprofloxacin (50 mg/kg) were administered by gavage twice daily for three consecutive weeks. 6 weeks after treatment, the test animals were euthanised and Achilles tendon specimens were collected. A computer monitored tensile testing machine was utilised for biomechanical testing. The mean elastic modulus of the control group was significantly higher than that of the norfloxacin and pefloxacin groups (p<0.05 and p<0.01, respectively). The mean yield force (YF) of the control group was significantly higher than those of ciprofloxacin, norfloxacin and pefloxacin groups (p<0.001, p<0.05 and p<0.01, respectively). The mean ultimate tensile force (UTF) of the control group was significantly higher than of the ciprofloxacin, norfloxacin, and pefloxacin groups (p<0.001, p<0.05 and p<0.01, respectively). Hyaline degeneration and fibre disarrangement were observed in the tendons of the ciprofloxacin, pefloxacin, and ofloxacin treated-groups, whereas myxomatous degeneration was observed only in the ciprofloxacin and pefloxacin groups. In conclusion, these findings in our rat model reveal significant deterioration of biomechanical parameters following fluoroquinolone exposure, and indicate significantly higher biomechanical toxicity for ciprofloxacin and pefloxacin.
Topics: Achilles Tendon; Administration, Oral; Animals; Anti-Bacterial Agents; Ciprofloxacin; Elastic Modulus; Elasticity; Fluoroquinolones; Male; Norfloxacin; Ofloxacin; Pefloxacin; Rats; Rats, Wistar; Tensile Strength
PubMed: 21628961
DOI: 10.2131/jts.36.339 -
Micromachines Apr 2023g-CN and g-CN/TCNQ composites with different doping levels were prepared using the copolymerization thermal method with melamine as a precursor. XRD, FT-IR, SEM, TEM,...
g-CN and g-CN/TCNQ composites with different doping levels were prepared using the copolymerization thermal method with melamine as a precursor. XRD, FT-IR, SEM, TEM, DRS, PL, and I-T characterized them. The composites were successfully prepared in this study. The photocatalytic degradation of pefloxacin (PEF), enrofloxacin (ciprofloxacin), and ciprofloxacin (ciprofloxacin) under visible light (λ > 550 nm) showed that the composite material had the best degradation effect on PEF. When TCNQ doping is 20 mg and catalyst dosage is 50 mg, the catalytic effect is the best, and the degradation rate reaches 91.6%, k = 0.0111 min, which is four times that of g-CN. Repeated experiments found that the cyclic stability of the g-CN/TCNQ composite was good. The XRD images were almost unchanged after five reactions. The radical capture experiments revealed that ·O was the main active species in the g-CN/TCNQ catalytic system, and h also played a role in PEF degradation. And the possible mechanism for PEF degradation was speculated.
PubMed: 37241565
DOI: 10.3390/mi14050941