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1.
Environ Res ; 215(Pt 1): 114135, 2022 12.
Article in English | MEDLINE | ID: mdl-35998699

ABSTRACT

For investigating the spatial, temporal variations and assessing ecological risk of 10 antibiotics and 6 antimycotics, influent sewage water and treated effluent were collected during three different seasons in 19 waste water treatment plants of Tianjin. High performance liquid chromatography tandem mass spectrometry was used to analyze 16 substances. The concentration range of influent samples was not detected (nd) -547.94 ng/L and the concentration range of effluent samples was nd-52.97 ng/L. By calculating the removal efficiency, it was found that Ciprofloxacin (CIP), Ofloxacin (OFL) and Clotrimazole (CTR) were effectively removed. There were significant spatial and temporal differences, the concentration in the dry season was evidently higher than that in the wet and normal seasons, and the northeast was lower than that in the northwest and southeast. By establishing a data set of influent and effluent, the priority features were extracted by feature engineering, which were temperature and NH3-N. Under the condition of ensuring the best performance of the models, the influent model with 9 features and the effluent model with 4 features were established, and the quantitative relationship between the above features and concentration was obtained through partial dependence analysis. Except for Moxifloxacin (MOX), Norfloxacin (NOR) and OFL in the influent samples, the RQ values for other antibiotics and antimycotics were less than 0.1. Among the effluent samples, only NOR had an RQ value greater than 0.1, and OFL, MOX, and Pefloxacin (PEF) had RQ values between 0.01 and 0.1. Comparing the observations and predictions individual RQ values, the predictions were ideal and matched the observations. This work effectively assessed environmental impact and provided a valuable reference for evaluating antibiotics and antimycotics ecological toxicity.


Subject(s)
Water Pollutants, Chemical , Water Purification , Anti-Bacterial Agents/analysis , Ciprofloxacin , Clotrimazole/analysis , Environmental Monitoring , Moxifloxacin/analysis , Norfloxacin , Ofloxacin/analysis , Pefloxacin/analysis , Risk Assessment , Sewage/chemistry , Waste Disposal, Fluid , Wastewater/chemistry , Water Pollutants, Chemical/analysis
2.
Neuropharmacology ; 139: 194-204, 2018 09 01.
Article in English | MEDLINE | ID: mdl-30009834

ABSTRACT

Several previous studies have demonstrated that the activity of neurotransmitters acting on ligand-gated ion channels such as the nicotinic acetylcholine receptor (nAChR) can be altered by compounds binding to allosteric modulatory sites. In the case of α7 nAChRs, both positive and negative allosteric modulators (PAMs and NAMs) have been identified and have attracted considerable interest. A recent study, employing revised structural models of the transmembrane domain of the α7 nAChR in closed and open conformations, has provided support for an inter-subunit transmembrane allosteric binding site (Newcombe et al 2017). In the present study, we have performed virtual screening of the DrugBank database using pharmacophore queries that were based on the predicted binding mode of PAMs to α7 nAChR structural models. A total of 81 compounds were identified in the DrugBank database, of which the 25 highest-ranked hits corresponded to one of four previously-identified therapeutic compound groups (carbonic anhydrase inhibitors, cyclin-dependent kinase inhibitors, diuretics targeting the Na+-K+-Cl- cotransporter, and fluoroquinolone antibiotics targeting DNA gyrase). The top-ranked compound from each of these four groups (DB04763, DB08122, furosemide and pefloxacin, respectively) was tested for its effects on human α7 nAChR expressed in Xenopus oocytes using two-electrode voltage-clamp electrophysiology. These studies, conducted with wild-type, mutant and chimeric receptors, resulted in all four compounds exerting allosteric modulatory effects. While DB04763, DB08122 and pefloxacin were antagonists, furosemide potentiated ACh responses. Our findings, supported by docking studies, are consistent with these compounds acting as PAMs and NAMs of the α7 nAChR via interaction with a transmembrane site.


Subject(s)
Nicotinic Agonists/pharmacology , Nicotinic Antagonists/pharmacology , alpha7 Nicotinic Acetylcholine Receptor/agonists , alpha7 Nicotinic Acetylcholine Receptor/antagonists & inhibitors , Allosteric Regulation , Allosteric Site , Animals , Drug Evaluation, Preclinical/methods , Furosemide/chemistry , Furosemide/pharmacology , Humans , Membrane Potentials/drug effects , Molecular Docking Simulation , Molecular Structure , Mutagenesis, Site-Directed , Nicotinic Agonists/chemistry , Nicotinic Antagonists/chemistry , Oocytes , Pefloxacin/chemistry , Pefloxacin/pharmacology , Protein Conformation , Xenopus laevis , alpha7 Nicotinic Acetylcholine Receptor/metabolism
3.
Urologiia ; (2): 83-4, 86-7, 2013.
Article in Russian | MEDLINE | ID: mdl-23789370

ABSTRACT

An open prospective study aimed to assessment the efficacy of a new formulation--rectal suppository vitaprost plus--compared with the standard antibacterial prevention of infectious and inflammatory complications and irritative disorders after transurethral resection of the prostate (TURP) was performed. From January to November 2011, TURP for prostatic adenoma was performed in 73 patients. Patients were randomized into two groups. The study group received rectal suppositories vitaprost plus once a day as a prophylactic antibacterial therapy before and after surgery, control group--pefloxacin 400 mg 2 times a day. Both groups began taking the drug in the morning before surgery. Duration of antibiotic therapy was 10 days in both groups. In the study group, hyperthermia over 37.5 degrees C in the 1st postoperative day was observed in 13 (43%) patients, in the control group--in 16 patients (53%). Cancellation of antibacterial treatment was required in four patients of the study group. There was no discontinuation of treatment due to adverse reactions in any case. In all patients, cancellation of drug treatment has been associated with the development of febrile hyperthermia in the presence of clinical need for catheter deployment, which required a change of antibacterial therapy. In the study group this parameter was 13% versus 37% in control group (P < 0.05). No significant differences in objective parameters (maximum urinary flow rate, residual urine volume, prostate volume) were registered. However, a statistically significant reduction in subjective parametres (IPSS and QoL scores) in the study group (11.5 +/- 1.2 and 2.6 +/- 0.3 points, respectively) compared with controls (15.5 +/- 1.4 and 3.8 +/- 0.5 points, respectively) was observed.


Subject(s)
Fluoroquinolones/administration & dosage , Peptides/administration & dosage , Prostatic Hyperplasia/therapy , Transurethral Resection of Prostate , Aged , Humans , Male , Middle Aged , Prostatic Hyperplasia/pathology , Prostatic Hyperplasia/physiopathology , Suppositories , Pefloxacin
4.
J Vet Sci ; 9(1): 25-9, 2008 Mar.
Article in English | MEDLINE | ID: mdl-18296885

ABSTRACT

The pharmacokinetics of orally administered pefloxacin were studied to evaluate the bio-enhancing effect of the herbal bio-enhancer, trikatu, in mountain Gaddi goats (n = 6). The findings of the study revealed a decreased plasma concentration (p > 0.05) of pefloxacin following trikatu administration during the absorption phase (10, 15, 20 min post pefloxacin administration). In contrast, the plasma concentrations of pefloxacin were significantly higher at 4, 6, 8 and 12 h (during the elimination phase) of the pefloxacin administration. The findings of the investigation revealed higher values for the area under the curve, the area under the first moment of the plasma drug concentration time curve, the mean residential time, the total duration of pharmacological action and bioavailability. Trikatu treatment, however, significantly reduced the elimination half life (t 1/2 beta) and zero time intercept of the elimination phase. The apparent volume of distribution based on the total area under the plasma drug concentration curve [(Vd(area)] and the apparent volume of distribution based on the zero time plasma concentration intercept of the elimination phase [Vd(B)] were significantly higher in trikatu treated animals indicating a better penetration of the drug. Based on the MIC of 0.8 microg/ml of pefloxacin, a priming dose of 6.0 mg/kg and a maintenance dose of 2.21 mg/kg is required to be administered at 8 h intervals. For practical purposes in goats this would mean a priming dose of 6 mg/kg and a maintenance dose of 2 mg/kg given by the oral route, to be repeated at 8 h intervals.


Subject(s)
Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/pharmacokinetics , Goats/metabolism , Pefloxacin/administration & dosage , Pefloxacin/pharmacokinetics , Phytotherapy/veterinary , Plant Extracts/pharmacology , Administration, Oral , Animals , Anti-Bacterial Agents/blood , Biological Availability , Cross-Over Studies , Zingiber officinale , Herb-Drug Interactions , Pefloxacin/blood , Piper , Piper nigrum
5.
Article in English | WPRIM | ID: wpr-7148

ABSTRACT

The pharmacokinetics of orally administered pefloxacin were studied to evaluate the bio-enhancing effect of the herbal bio-enhancer, trikatu, in mountain Gaddi goats (n = 6). The findings of the study revealed a decreased plasma concentration (p > 0.05) of pefloxacin following trikatu administration during the absorption phase (10, 15, 20 min post pefloxacin administration). In contrast, the plasma concentrations of pefloxacin were significantly higher at 4, 6, 8 and 12 h (during the elimination phase) of the pefloxacin administration. The findings of the investigation revealed higher values for the area under the curve, the area under the first moment of the plasma drug concentration time curve, the mean residential time, the total duration of pharmacological action and bioavailability. Trikatu treatment, however, significantly reduced the elimination half life (t(1/2beta)) and zero time intercept of the elimination phase. The apparent volume of distribution based on the total area under the plasma drug concentration curve [(Vd((area))] and the apparent volume of distribution based on the zero time plasma concentration intercept of the elimination phase [Vd((B))] were significantly higher in trikatu treated animals indicating a better penetration of the drug. Based on the MIC of 0.8 microgram/ml of pefloxacin, a priming dose of 6.0 mg/kg and a maintenance dose of 2.21 mg/kg is required to be administered at 8 h intervals. For practical purposes in goats this would mean a priming dose of 6 mg/kg and a maintenance dose of 2 mg/kg given by the oral route, to be repeated at 8 h intervals.


Subject(s)
Animals , Administration, Oral , Anti-Bacterial Agents/administration & dosage , Biological Availability , Cross-Over Studies , Zingiber officinale , Goats/metabolism , Herb-Drug Interactions , Pefloxacin/administration & dosage , Phytotherapy/veterinary , Piper , Piper nigrum , Plant Extracts/pharmacology
6.
Pharm Dev Technol ; 11(3): 313-9, 2006.
Article in English | MEDLINE | ID: mdl-16895842

ABSTRACT

The major purpose of this study was to develop and characterize a series of carbopol- and methyl cellulose-based solutions as the in situ gelling vehicles for ophthalmic drug delivery. The rheological properties, in vitro release as well as in vivo pharmacological response of a combination of polymer solutions, including carbopol and methyl cellulose, were evaluated. It was found that the optimum concentration of carbopol solution for the in situ gel-forming delivery systems was 0.3% (w/w), and that for methyl cellulose solution was 1.5% (w/w). The mixture of 0.3% carbopol and 1.5% methyl cellulose solutions showed a significant enhancement in gel strength in the physiological condition; this gel mixture was also found to be free flowing at pH 4.0 and 25 degrees C. The rheological behaviors of carbopol/methyl cellulose solution were not affected by the incorporation of the drug. Drug levels in the aqueous humor of the rabbits were well above the MIC-values of relevant bacteria after 12 hours, the results of an optimized formulation containing 0.18% of pefloxacin mesylate compared well with the 0.3% marketed eye drop formulation, indicating our formulation to be significantly better considering that a similar effect was obtained at half the concentration. Both the in vitro release and in vivo pharmacological studies indicated that the carbopol/methyl cellulose solution had better ability to retain drug than did the carbopol or methyl cellulose solutions alone. The results demonstrated that the carbopol/methyl cellulose mixture can be used as an in situ gelling vehicle to enhance the ocular bioavailability of pefloxacin mesylate.


Subject(s)
Delayed-Action Preparations/administration & dosage , Drug Delivery Systems/methods , Fluoroquinolones/administration & dosage , Methylcellulose/chemistry , Ophthalmic Solutions/chemistry , Polyvinyls/chemistry , Acrylic Resins , Animals , Drug Carriers/chemistry , Drug Evaluation, Preclinical , Male , Models, Biological , Rabbits , Time Factors , Pefloxacin
7.
Cochrane Database Syst Rev ; (3): CD003597, 2006 Jul 19.
Article in English | MEDLINE | ID: mdl-16856014

ABSTRACT

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.


Subject(s)
Anti-Infective Agents, Urinary/therapeutic use , Cystitis/drug therapy , Acute Disease , Adult , Ciprofloxacin/therapeutic use , Female , Fluoroquinolones/therapeutic use , Humans , Levofloxacin , Norfloxacin/therapeutic use , Ofloxacin/therapeutic use , Pefloxacin/therapeutic use , Quinolones/therapeutic use , Randomized Controlled Trials as Topic
8.
Drugs ; 64(19): 2221-34; discussion 2235-6, 2004.
Article in English | MEDLINE | ID: mdl-15456336

ABSTRACT

Prulifloxacin, the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent. After absorption, prulifloxacin is metabolised by esterases to ulifloxacin. The drug has a long elimination half-life, allowing once-daily administration. Ulifloxacin is generally more active in vitro than other fluoroquinolones against a variety of clinical isolates of Gram-negative bacteria, including community and nosocomial isolates of Escherichia coli, Klebsiella spp., Proteus, Providencia and Morganella spp., Moraxella catarrhalis and Haemophilus spp. The activity of ulifloxacin against Pseudomonas aeruginosa varies between countries. Gram-positive organisms, including meticillin- or oxacillin-susceptible Staphylococcus aureus, Enterococcus spp. and Italian community isolates of Streptococcus pneumoniae are susceptible to ulifloxacin. Activity against Spanish strains of S. pneumoniae is moderate. In well designed clinical trials, good clinical and bacteriological efficacy (similar to that of ciprofloxacin, amoxicillin/clavulanic acid or pefloxacin) was seen with prulifloxacin 600 mg once daily for 10 days in patients with acute exacerbations of chronic bronchitis or complicated lower urinary tract infections (UTIs), and with single-dose prulifloxacin 600 mg in acute, uncomplicated lower UTIs. Prulifloxacin was generally well tolerated in clinical trials, with a similar tolerability profile to that of ciprofloxacin.


Subject(s)
Dioxolanes/metabolism , Dioxolanes/therapeutic use , Fluoroquinolones/metabolism , Fluoroquinolones/therapeutic use , Piperazines/metabolism , Piperazines/therapeutic use , Quinolones/metabolism , Quinolones/therapeutic use , Administration, Oral , Amoxicillin/pharmacology , Amoxicillin/therapeutic use , Animals , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/metabolism , Anti-Bacterial Agents/therapeutic use , Bronchitis, Chronic/complications , Bronchitis, Chronic/drug therapy , Ciprofloxacin/pharmacology , Ciprofloxacin/therapeutic use , Clavulanic Acid/pharmacology , Dioxolanes/pharmacology , Drug Evaluation, Preclinical/methods , Drug Therapy, Combination , Fluoroquinolones/chemistry , Fluoroquinolones/pharmacology , Gram-Negative Bacteria/classification , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/classification , Gram-Positive Bacteria/drug effects , Half-Life , Humans , Italy , Molecular Structure , New Zealand , Piperazines/pharmacology , Prodrugs/metabolism , Prodrugs/pharmacology , Prodrugs/therapeutic use , Quinolones/pharmacology , Urinary Tract Infections/complications , Urinary Tract Infections/drug therapy , Pefloxacin
9.
Article in Korean | WPRIM | ID: wpr-47343

ABSTRACT

BACKGROUND: At the neuromuscular junction, pefloxacin (P) may exacerbate myasthenia gravis and reduce the tau of MEPC. So here we investigated the effect of P on the neuromuscular blocking action of rocuronium (R). METHODS: Hemidiaphragm-phrenic nerve preparations were obtained from male Sprague-Dawley rats (150-250 g). Preparations were bathed in Kreb's solution (in (mM): NaCl 118, KCl 5, CaCl2 2.5, NaHCO3 30, KH2PO4 1, MgCl2 1 and glucose 11), maintained at 32oC and then aerated with a mixture of 95% O2 and 5% CO2. Isometric forces generated in response to 0.1 Hz, and, 50 Hz for 19 seconds with supramaximal electrical stimulation(0.2 msec, rectangular) to the phrenic nerve, were measured with a force transducer. Single twitch tension (ST) and peak tetanic tension (PTT) were calculated as % reduction versus the control, and tetanic fade (TF), as a % increase. Each preparation was exposed to one of 4 P concentrations of Krebs' solution (0, 0.25, 0.5, 1.0 mM), and enough R solution was added to the tissue bath to achieve the desired R concentration. The effects of P and R were allowed to stabilize before measuring tension parameters. EC5, EC25, EC50, EC75, and EC95 of R for ST, PTT and TF were calculated using a probit model. The interactions between the two drugs were drawn with Berenbaum's additive isobole at 25% isobole, 50% isobole, and 75% isobole. Differences between EC50's of R according to P concentrations were tested by one way ANOVA with Tamhane for post hoc; P <0.05 was regarded as significant. RESULTS: The cumulative concentration-effect curves shifted to the right in ST, and to the left in TF as the concentration of P was increased. The interactions between these two drugs varied from additive to antagonistic according to the magnitude of relaxation effect, drug concentration, and the frequency of stimulation. CONCLUSIONS: P augmented the TF of R. Our results suggest that simultaneous 0.1 Hz and 50 Hz stimulations allow the neuromuscular blocking action of a drug to be correctly evaluated.


Subject(s)
Animals , Humans , Male , Rats , Baths , Drug Interactions , Glucose , Magnesium Chloride , Myasthenia Gravis , Neuromuscular Blockade , Neuromuscular Junction , Pefloxacin , Phrenic Nerve , Rats, Sprague-Dawley , Refractory Period, Electrophysiological , Relaxation , Transducers
10.
Antibiot Khimioter ; 47(9): 14-7, 2002.
Article in Russian | MEDLINE | ID: mdl-12619515

ABSTRACT

Results of prospective comparative investigation of monofluoroquinolones (ciprofloxacin, ofloxacin, pefloxacin) arthropathy are presented. The trial was performed at 144 children with mucoviscidosis (aged 0.5-16) and at 37 children with aplastic anemia (aged 1.75-15). Two groups differ by necessary antibacterials regimes and hence by different abilities for arthropathy development: patients with mucoviscidosis were treated with fluoroquinolones followed by repeated short courses in combination with other antibacterials; patients with aplastic anemia--were treated permanently for a long time with low doses as monotherapy for autoinfection prophylaxis. Analysis was performed on the base of catamnesis, year growth rate, postmortal morphological investigation of the right knee joint. It was shown that quinolone arthropathy development didn't depend on treatment duration, as it developed during the first three weeks of the fluoroquinolone use, but depended on the drug, patient age and nosology. Arthropathy has favourable prognosis and was fully resolved at the period from 7 days to 3 month according to the arthropathy form (arthrologic, arthritic). Quinolones arthropathy at the children has specific features, the main one is absence of cartilage damage confirmed by morphological analysis.


Subject(s)
Fluoroquinolones/therapeutic use , Adolescent , Age Factors , Anemia, Aplastic/drug therapy , Anti-Infective Agents/therapeutic use , Body Height/drug effects , Cartilage/pathology , Child , Child, Preschool , Ciprofloxacin/therapeutic use , Cystic Fibrosis/drug therapy , Drug Administration Schedule , Female , Fluoroquinolones/administration & dosage , Fluoroquinolones/adverse effects , Humans , Infant , Joint Diseases/chemically induced , Knee Joint/drug effects , Knee Joint/pathology , Male , Ofloxacin/therapeutic use , Pefloxacin/therapeutic use , Prospective Studies , Treatment Outcome
11.
Antibiot Khimioter ; 46(3): 16-20, 2001.
Article in Russian | MEDLINE | ID: mdl-11548276

ABSTRACT

Data on comparative investigation of the clinical and bacteriological efficacy and tolerability of monofluoroquinolones ciprofloxacin, ofloxacin and pefloxacin are given. The results confirm good clinical efficacy of all three monofluoroquinolones and high antistaphylococcal activity of pefloxacin. Efficacy of monofluoroquinolones against P. aeruginosa and S. maltophilia was moderate--only isolation of bacteria from spetrum became lower. Tolerability of monofluoroquinolones was good. Only at 5 patients the drugs use was stopped (4 in the ciprofloxacin group and 1--in the pefloxacin group). At 2 patients it was caused by arthropathy which was drug- and age-dependent. Quinolone-arthropathy was more often in the pefloxacin group and was registered only at the children elder than 10 years old with arthrological anamnesis. This arthropathy differed from experimental one by positive outcome and full recovery in the period from 7 days to 3 months. Results of morphological investigation confirmed clinical data--no invalidizing cartilage damage was revealed.


Subject(s)
Anti-Infective Agents/therapeutic use , Ciprofloxacin/therapeutic use , Cystic Fibrosis/complications , Ofloxacin/therapeutic use , Pefloxacin/therapeutic use , Respiratory Tract Infections/drug therapy , Adolescent , Anti-Infective Agents/adverse effects , Arthritis/chemically induced , Arthritis/pathology , Child , Child, Preschool , Ciprofloxacin/adverse effects , Drug Resistance, Microbial , Female , Humans , Infant , Knee Joint/drug effects , Knee Joint/pathology , Male , Ofloxacin/adverse effects , Pefloxacin/adverse effects , Respiratory Tract Infections/microbiology
12.
Bratisl Lek Listy ; 102(8): 374-6, 2001.
Article in English | MEDLINE | ID: mdl-11763669

ABSTRACT

Opinions on antibiotic treatment of salmonella gastroenteritis are still different. Many authors support an opinion that antimicrobial treatment has no effect on salmonella elimination. The authors of the study have tried to prove that fluoroquinolones shorten the elimination of salmonellae and therefore they are useful not only for the treatment of salmonella gastroenteritis in immunocompromised patients to prevent sepsis and extraintestinal manifestations of the infection, but also for eradication of salmonellae in food industry workers, whose carrier state might exclude them from their work. (Tab. 3, Ref. 10.)


Subject(s)
Anti-Bacterial Agents/therapeutic use , Ofloxacin/therapeutic use , Pefloxacin/therapeutic use , Salmonella Infections/drug therapy , Trimethoprim, Sulfamethoxazole Drug Combination/therapeutic use , Female , Humans , Male , Microbial Sensitivity Tests , Retrospective Studies , Salmonella/drug effects , Salmonella Food Poisoning/drug therapy
13.
Antibiot Khimioter ; 45(7): 14-6, 2000.
Article in Russian | MEDLINE | ID: mdl-10987102

ABSTRACT

Sensitivity of 505 strains of gram-negative and gram-positive microorganisms to II generation fluoroquinolones (ciprofloxacin, pefloxacin) was determined. Strains of Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus with different level of sensitivity were selected. Pharmacokinetics of the drugs was investigated after their administration per os in one dose. The resulting indices were used for calculation of the following parameters--Cmax/MIC and AUC/MIC. These parameters may be used in evaluation of the drugs efficacy and for dosing corrections.


Subject(s)
Anti-Infective Agents/pharmacology , Anti-Infective Agents/pharmacokinetics , Ciprofloxacin/pharmacology , Ciprofloxacin/pharmacokinetics , Pefloxacin/pharmacology , Pefloxacin/pharmacokinetics , Anti-Infective Agents/blood , Anti-Infective Agents/therapeutic use , Chromatography, High Pressure Liquid , Ciprofloxacin/blood , Ciprofloxacin/therapeutic use , Escherichia coli/drug effects , Humans , Klebsiella pneumoniae/drug effects , Microbial Sensitivity Tests/statistics & numerical data , Pefloxacin/blood , Pefloxacin/therapeutic use , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effects
14.
APMIS ; 108(4): 261-6, 2000 Apr.
Article in English | MEDLINE | ID: mdl-10843412

ABSTRACT

Different methods have been described for determination of the post-antibiotic effects (PAEs) of antibiotics, from the conventional methods to the automatic measurement of bacterial regrowth. The PAEs of ciprofloxacin, ofloxacin and perfloxacin, as compared with those of amikacin, netilmicin and ceftazidime, have now been investigated for three clinical isolates of Pseudomonas species, using automated measurement of the growth with an Anthos microplate reader. It was found that, besides the well-known PAEs of aminoglycosides, quinolone antibiotics also exhibit drug- and concentration-dependent PAEs against clinical isolates of Pseudomonas when used in concentrations of 1/2x, 1 x or 5 x MIC. Of the three quinolones tested, pefloxacin showed the greatest PAE, independently of its MICs against the different strains. Ofloxacin had no or only an insignificant PAE, while ciprofloxacin had a marked PAE for all strains, including the reference strains.


Subject(s)
4-Quinolones , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/therapeutic use , Anti-Infective Agents/pharmacology , Fluoroquinolones , Microbial Sensitivity Tests/methods , Pseudomonas Infections/drug therapy , Pseudomonas/drug effects , Amikacin/pharmacology , Automation , Ceftazidime/pharmacology , Ciprofloxacin/pharmacology , Escherichia coli/drug effects , Humans , Netilmicin/pharmacology , Ofloxacin/pharmacology , Pseudomonas/growth & development , Pseudomonas/isolation & purification , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/growth & development , Pseudomonas aeruginosa/isolation & purification , Pefloxacin
15.
Chemotherapy ; 46(2): 116-21, 2000.
Article in English | MEDLINE | ID: mdl-10671762

ABSTRACT

The efficacies of amikacin, ofloxacin, pefloxacin, ciprofloxacin, enoxacin and fleroxacin, each as monotherapy, were evaluated in a rabbit model of induced left-sided Pseudomonas aeruginosa endocarditis. Therapy started 48 h after infection and lasted 5 days. All agents were given intramuscularly; amikacin at 7 mg/kg/12 h, and each quinolone at 35 mg/kg/12 h. All animals survived except for 1 of the group that received amikacin, and 2 of the untreated control group. No sterile vegetations were found in the untreated group and the group of fleroxacin, while 3 animals from the amikacin, ofloxacin, and enoxacin groups, and 2 from the ciprofloxacin and pefloxacin groups had sterile vegetations. All agents used significantly reduced the number of CFU per gram of vegetation versus untreated controls. Enoxacin and ciprofloxacin were equipotent and more effective than pefloxacin, ofloxacin and amikacin. Fleroxacin had a weaker activity.


Subject(s)
Amikacin/therapeutic use , Anti-Infective Agents/therapeutic use , Atrial Function, Left/drug effects , Endocarditis, Bacterial/drug therapy , Heart Valve Diseases/drug therapy , Pseudomonas Infections/drug therapy , Ventricular Dysfunction, Left/drug therapy , Animals , Anti-Bacterial Agents/therapeutic use , Ciprofloxacin/therapeutic use , Enoxacin/therapeutic use , Fleroxacin/therapeutic use , Ofloxacin/therapeutic use , Pefloxacin/therapeutic use , Rabbits
16.
Antimicrob Agents Chemother ; 43(12): 2915-21, 1999 Dec.
Article in English | MEDLINE | ID: mdl-10582882

ABSTRACT

Although fluoroquinolone antibacterials have a broad therapeutic use, with a relatively low incidence of severe side effects, they have been reported to induce lesions in the cartilage of growing animals by a mechanism that remains unclear. This study was undertaken to determine the potentially deleterious effect of a high dose of pefloxacin (400 mg/kg of body weight) on two main constituents of cartilage in mice, i.e., proteoglycans and collagen. Variations in levels of proteoglycan anabolism measured by in vivo [(35)S]sulfate incorporation into cartilage and oxidative modifications of collagen assessed by detection of carbonyl derivatives were monitored after administration of pefloxacin. Treatment of mice with 1 day of pefloxacin treatment significantly decreased the rate of biosynthesis of proteoglycan for the first 24 h. However, no difference was observed after 48 h. The decrease in proteoglycan synthesis was accompanied by a marked drop in serum sulfate concentration and a concomitant increase in urinary sulfate excretion. The decrease in proteoglycan synthesis, also observed ex vivo, may suggest a direct effect of pefloxacin on this process, rather than it being a consequence of a low concentration of sulfate. On the other hand, treatment with pefloxacin for 10 days induced oxidative damage to collagen. In conclusion, this study demonstrates, for the first time, that pefloxacin administration to mice leads to modifications in the metabolism and integrity of extracellular proteins, such as collagen and proteoglycans, which may account for the side effects observed. These results offer new insights to explain quinolone-induced disorders in growing articular cartilage.


Subject(s)
Anti-Infective Agents/toxicity , Arthritis/chemically induced , Arthritis/metabolism , Cartilage, Articular/metabolism , Collagen/metabolism , Proteoglycans/metabolism , Animals , Arthritis/pathology , Cartilage, Articular/drug effects , Cartilage, Articular/pathology , Collagen/biosynthesis , Electrophoresis, Polyacrylamide Gel , Male , Mice , Oxidation-Reduction , Pefloxacin/administration & dosage , Pefloxacin/pharmacology , Proteoglycans/biosynthesis , Reactive Oxygen Species/physiology , Sulfates/metabolism , Sulfur Radioisotopes , Time Factors
17.
Antibiot Khimioter ; 44(1): 20-2, 1999.
Article in Russian | MEDLINE | ID: mdl-10095920

ABSTRACT

Pefloxacin was used in the treatment of 25 patients with wound infection in a dose of 400 mg orally twice a day for 10-12 days. As the monotherapy it was applied to 15 patients. 7 patients with clinical signs of non-clostridial anaerobic infection were treated with pefloxacin in combination with intravenous metronidazole. Pefloxacin was highly efficient in 96 per cent of the cases with extensive posttraumatic purulent wounds with and without bone affection, acute purulent wounds of the soft tissue, purulent wounds of the soft tissues in diabetic patients, trophic or decubitus ulcer. 266 clinical isolates of Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Proteus mirabilis, Enterobacter spp. and Acinetobacter spp, were tested and 75 to 100 per cent of them was shown to be susceptible to pefloxacin and ciprofloxacin. At the same time the isolates of Pseudomonas aeruginosa and Klebsiella spp. were more susceptible to ciprofloxacin. The pathogen eradication and eradication with superinfection in the cases treated with pefloxacin amounted to 92 per cent. The drug tolerance was good. No clinically significant adverse events were recorded.


Subject(s)
Anti-Infective Agents/therapeutic use , Pefloxacin/therapeutic use , Soft Tissue Infections/drug therapy , Wound Infection/drug therapy , Adult , Aged , Female , Humans , Male , Microbial Sensitivity Tests , Middle Aged
18.
East Afr Med J ; 76(10): 587-9, 1999 Oct.
Article in English | MEDLINE | ID: mdl-10734512

ABSTRACT

OBJECTIVE: To investigate whether quinolones produce in vivo responses comparable to reported in vitro activity against the spectrum of organisms in uncomplicated urinary tract infection (UTI) in Nigeria. DESIGN: Equal numbers of patients with urine culture positive UTI were randomized to oral quinolone, perfloxacin 400 mg bd twice a day and ofloxacin 200 mg bd twice a day for five days. SETTING: Out-patient clinics and wards at the University College Hospital, Ibadan. SUBJECTS: Sixty patients aged sixteen years and above with uncomplicated UTI. MAIN OUTCOME MEASURES: Number of isolates, number of patients with clinical and bacteriological cure one week after commencing therapy. Relative effectiveness and side effects of the drugs. RESULTS: Sixty- four bacterial isolates were obtained with the enterobacteriaceae comprising 86%. Sixty-two (97%) were sensitive to both drugs in vitro. Clinical cure occurred in 57 patients (95%), being 28 (93%) in those taking perfloxacin and 29 (97%) in those taking ofloxacin. Bacteriological cure occurred in 55 patients (92%), being 27 (90%) in those taking perfloxacin and 28 (93%) in those taking ofloxacin. Fifty-nine of the 64 isolates (92%) were eliminated in one week, 30 of 33 (91%) in those taking perfloxacin, and 29 of 31 (94%) in those taking ofloxacin; the difference was insignificant (p = 1.16). The enterobacteriaceae were generally susceptible to both drugs. Side effects were minor and infrequent. CONCLUSION: Quinolones were highly active against the common urinary pathogens in these Nigerian patients and can be reliably employed in treatment when culture results are unavailable.


Subject(s)
4-Quinolones , Anti-Infective Agents/therapeutic use , Bacterial Infections/drug therapy , Fluoroquinolones , Ofloxacin/therapeutic use , Urinary Tract Infections/drug therapy , Administration, Oral , Adult , Anti-Infective Agents/pharmacology , Bacterial Infections/microbiology , Bacterial Infections/urine , Female , Humans , Male , Microbial Sensitivity Tests , Middle Aged , Nigeria , Ofloxacin/pharmacology , Single-Blind Method , Time Factors , Treatment Outcome , Urinary Tract Infections/microbiology , Urinary Tract Infections/urine , Pefloxacin
19.
Afr J Med Med Sci ; 28(3-4): 151-3, 1999.
Article in English | MEDLINE | ID: mdl-11205820

ABSTRACT

Twenty four women with postoperative sepsis following gynaecological surgery were recruited into a study designed to determine the efficacy of Pefloxacin. With the standard oral dose of Pefloxacin, clinical cure or improvement occurred in 98% of the patients. In-vitro, 90% of bacterial isolates were sensitive to Pefloxacin. No adverse effect was encountered in any of the patients. We concluded that Pefloxacin is effective in the treatment of postoperative bacterial infections following gynaecological surgery.


Subject(s)
Anti-Infective Agents/therapeutic use , Bacterial Infections/drug therapy , Bacterial Infections/etiology , Gynecologic Surgical Procedures/adverse effects , Pefloxacin/therapeutic use , Sepsis/drug therapy , Sepsis/etiology , Administration, Oral , Adolescent , Adult , Aged , Female , Follow-Up Studies , Gynecologic Surgical Procedures/statistics & numerical data , Humans , Microbial Sensitivity Tests , Middle Aged , Treatment Outcome
20.
J Chemother ; 10(3): 248-53, 1998 Jun.
Article in English | MEDLINE | ID: mdl-9669652

ABSTRACT

In the surgical units of our Division, from January 1979 to December 1989, the infection rate in surgical groin hernia repair was much higher than expected, in comparison to other reports in the literature. In order to evaluate if correct preoperative antibiotic prophylaxis could decrease the incidence of postoperative infections (wound, urinary and respiratory tract) after abdominal wall hernia repair surgery, a total of 1,524 consecutive patients undergoing this type of procedure were reviewed between January 1990 and December 1996. The patients were divided in three different groups, according to the antibiotic prophylaxis regimen: i) group A: 606 patients (39.8%) treated with ceftriaxone; ii) group B: 408 patients (26.8%) treated with pefloxacin; and iii) group C: 510 patients (33.4%) treated with different regimens using either cephalosporins or quinolones other than ceftriaxone and pefloxacin. Only 1 surgical wound infection was observed (0.06%). The tolerability was good: no significant side effects related to antibiotic prophylaxis were recorded in our experience. In this study, even though retrospective, single-dose ceftriaxone proved to be a valid and cost-effective choice in antibiotic prophylaxis.


Subject(s)
Anti-Infective Agents/therapeutic use , Antibiotic Prophylaxis , Cefotaxime/therapeutic use , Ceftriaxone/therapeutic use , Cephalosporins/therapeutic use , Ciprofloxacin/therapeutic use , Herniorrhaphy , Pefloxacin/therapeutic use , Surgical Wound Infection/prevention & control , Adolescent , Adult , Aged , Aged, 80 and over , Child , Child, Preschool , Female , Humans , Male , Middle Aged , Retrospective Studies , Treatment Outcome
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