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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 -
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 -
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 -
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 -
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 -
The Cochrane Database of Systematic... Jul 2006Uncomplicated acute cystitis is one of the most common bacterial infections in adults. The percentage of women who have at least one episode of acute cystitis is... (Meta-Analysis)
Meta-Analysis Review
BACKGROUND
Uncomplicated acute cystitis is one of the most common bacterial infections in adults. The percentage of women who have at least one episode of acute cystitis is estimated to be between 40% to 50%. Quinolones are recommended for acute cystitis in regions where the level of resistance to other antimicrobials namely co-trimoxazole is high. However the efficacy, safety and tolerance of quinolones needs investigation.
OBJECTIVES
To compare the efficacy, safety and tolerance of different quinolones in women with uncomplicated acute cystitis.
SEARCH STRATEGY
We searched the Cochrane Central Register of Controlled Trials (CENTRAL, in The Cochrane Library Issue 3, 2003), MEDLINE (1966 - September 2003), EMBASE (1988 - September 2003), reference lists of articles and abstracts from conference proceedings without language restriction. Reference lists of urology, infectious diseases and nephrology textbooks, review articles and relevant studies.
SELECTION CRITERIA
Randomised and quasi-randomised controlled trials comparing two or more different quinolones in women (>/= 16 years) with uncomplicated acute cystitis were selected.
DATA COLLECTION AND ANALYSIS
Two reviewers independently assessed trial quality and extracted data. Statistical analyses were performed using the random effects model and the results expressed as relative risk (RR) for dichotomous outcomes with 95% confidence intervals (CI).
MAIN RESULTS
We identified 11 studies enrolling 7535 women. There were no significant differences in clinical or microbiological efficacy between quinolones. Photosensitivity reactions were more frequently observed for sparfloxacin when compared to ofloxacin. Any adverse event, adverse events causing withdrawal, skin adverse events, photosensitivity reactions were more common for lomefloxacin when compared to norfloxacin. Any adverse event, adverse drug reactions, CNS adverse events were more common for ofloxacin when compared to ciprofloxacin. CNS adverse events and insomnia were more often reported for rufloxacin when compared to pefloxacin. Adverse drug reactions occurred frequently for ofloxacin than levofloxacin. Insomnia was reported more frequently for enoxacin than ciprofloxacin.
AUTHORS' CONCLUSIONS
We found no significant differences in clinical or microbiological efficacy between quinolones but some differences in occurrence and spectrum of quinolone safety.
Topics: Acute Disease; Adult; Anti-Infective Agents, Urinary; Ciprofloxacin; Cystitis; Female; Fluoroquinolones; Humans; Levofloxacin; Norfloxacin; Ofloxacin; Pefloxacin; Quinolones; Randomized Controlled Trials as Topic
PubMed: 16856014
DOI: 10.1002/14651858.CD003597.pub2 -
Antimicrobial Agents and Chemotherapy Oct 1987MICs of pefloxacin and nine antistaphylococcal drugs were determined for 200 isolates of Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus,...
MICs of pefloxacin and nine antistaphylococcal drugs were determined for 200 isolates of Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, and Staphylococcus saprophyticus. All the strains were susceptible to pefloxacin, vancomycin, and rifampin. Oxacillin-resistant strains were uniformly resistant to cephalothin and were more likely to be resistant to gentamicin, erythromycin, clindamycin, doxycycline, and trimethoprim-sulfamethoxazole than were oxacillin-susceptible strains. Time-kill studies with 23 strains of S. aureus, S. epidermidis, and S. haemolyticus indicated that the relative order of bactericidal activities was gentamicin greater than or equal to pefloxacin greater than oxacillin greater than vancomycin greater than rifampin. Pefloxacin combined with oxacillin or vancomycin killed staphylococci more rapidly than oxacillin or vancomycin alone but less rapidly than pefloxacin alone. Gentamicin combined with oxacillin, vancomycin, or pefloxacin resulted in the most rapid killing of gentamicin-susceptible strains. Rifampin combined with oxacillin, vancomycin, or pefloxacin reduced the bactericidal activities of those drugs, but rifampin resistance was not observed as it was with rifampin alone. Pefloxacin is a potentially useful antistaphylococcal agent.
Topics: Anti-Bacterial Agents; Microbial Sensitivity Tests; Norfloxacin; Pefloxacin; Staphylococcus
PubMed: 3481244
DOI: 10.1128/AAC.31.10.1457