Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new ceclor research articles will be listed here shortly after becoming available to us.
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Plant-derived compounds inactivate antibiotic-resistant Campylobacter jejuni strains.
J Food Prot. 2008 Jun; 71(6): 1145-9
Ravishankar S, Zhu L, Law B, Joens L, Friedman M
Sixty-three Campylobacter jejuni isolates were screened for their resistance to the antibiotics ampicillin, cefaclor, ciprofloxacin, erythromycin, gentamycin, tetracycline, and trimethoprim-sulfamethoxazole. Based on this screen, the resistant strains D28a and H2a and the nonresistant strain A24a were selected for evaluation of their resistance and susceptibility to inactivation by cinnamaldehyde and carvacrol, the main constituents of plant-derived cinnamon and oregano oils, respectively. Different concentrations (0.05, 0.1, and 0.2% [vol/vol] in sterile phosphate-buffered saline) of cinnamaldehyde and carvacrol were added to C. jejuni cultures with initial populations of 10(4) CFU/ml. The samples were then mixed thoroughly and incubated at 37 degrees C. Viable bacterial populations were enumerated at incubation periods of 0, 30, 60, and 120 min. The results indicate that the extent of inhibition of microbial survival was related to both the nature and concentration of antimicrobials and the incubation time. Both cinnamaldehyde and carvacrol exhibited rapid antimicrobial activity against both antibiotic-resistant and non-resistant C. jejuni strains, at concentrations of approximately 0.1% and higher. The antimicrobial efficacy of cinnamaldehyde was greater than that of carvacrol. The possible significance of the results for microbiological food safety is discussed.
[Antibiotic use in the pediatric population: factors to consider]
Rev Esp Quimioter. 2007 Dec; 20(4): 409-20
Quintana VO, Deniz ES, Ortega FD, Ramírez SD, Pita JM, Castro Ade L
The aim of this retrospective study was to analyze the use of antibiotics in pediatrics in the Canary Islands during the period 2001-2005. We used the defined daily dose (DDD) as a technical unit of measurement as well as the DDD/1000 habitants/day (DHD), following the ATC classification system. The demographic data were obtained from individual patient health cards assigned to the primary care pediatricians. During the period 2001-2005, the total number of prescriptions for antibiotics in pediatrics was 1,207,726 at a cost of 6,119,679 Euros to the Canarian Health Service in Tenerife and 4,808,654 Euros in Las Palmas. The annual number of DHD in the Canary Islands decreased from 103,044 in 2001 to 68,168 in 2005. The cost for 1000 inhabitants/day (CHD) was 27,686 Euros and 19,183 Euros in Tenerife and Las Palmas, respectively. In analyzing the therapeutic classes of antibiotics, we found that the consumption of broad-spectrum penicillins (amoxicillin) in Tenerife decreased, while in Las Palmas it remained stable. There was also a significant decrease in the use of tetracyclines in both provinces. The DHD of beta-lactamase inhibitors was more significantly reduced in Tenerife than in LPA. The consumption of cephalosporins, mainly cefixime, was high in Tenerife, while in Las Palmas the second-generation cephalosporins (cefuroxime and cefaclor) were widely consumed. The use of macrolide antibiotics gradually decreased. Interestingly, there were 7,939 prescriptions for fluoroquinolones (mainly ciprofloxacin) in Tenerife and 4,846 in Las Palmas (mainly norfloxacin and ciprofloxacin). There were differences in the prescribing practices between Tenerife and Gran Canaria that don't coincide with changes in the microbiological spectrum. Prescribing practices in Las Palmas are based on scientific data, probably because of the continuing education courses on antibiotherapy that began in 2003.
Tolerability of Aztreonam in patients with IgE-mediated hypersensitivity to beta-lactams.
Int J Immunopathol Pharmacol. 2008 April-June; 21(2): 375-379
Patriarca G, Schiavino D, Lombardo C, Altomonte G, De Cinti M, Buonomo A, Nucera E
Cross-reactivity between aztreonam and penicillins is poor, but clinical tolerance of aztreonam has been assessed, by means of tolerance challenge tests, only in a few groups of penicillin-allergic patients. The aim of this study is to evaluate the tolerability of aztreonam in a large group of betalactam-allergic patients. We studied all patients (greater than 14 years of age), with a clinical history of immediate reactions to any betalactam and with positive immediate-type skin tests and/or positive specific IgE to any of the studied betalactam; they were studied by means of: skin prick and intradermal tests with penicilloyl polylysine, minor determinant mixture, semisynthetic penicillins, cephalosporins, aztreonam and imipenem; detection of specific IgE to penicillin G, penicillin V, ampicillin, amoxicillin, cefaclor and ceftriaxone. Patients with negative immediate-type skin tests with aztreonam then underwent a graded intramuscular challenge. Forty-five patients (mean age 46.1 ± 15.2 years), 27 females and 18 males, had positive skin tests and/or specific IgE to at least one of the studied betalactams. The most involved drugs were amoxicillin (23 cases), ampicillin (9 cases), penicillin G (8 cases) and other betalactams in the remaining cases. The most frequent reactions were anaphylaxis (27 cases) and urticaria (15 cases). All patients had negative intradermal tests with aztreonam and all patients tolerated the intramuscular graded challenge. Our data confirm the lack of cross-reactivity between betalactams and aztreonam. Immediate-type skin tests with aztreonam represent a simple and rapid diagnostic tool to establish tolerability in betalactam-allergic patients who urgently need this drug.
Drug Metab Dispos. 2008 May 27;
Yasuda K, Ranade A, Venkataramanan R, Strom S, Chupka J, Ekins S, Schuetz E, Bachmann K
We have investigated several in silico and in vitro methods in order to improve our ability to predict potential drug interactions of antibiotics. Our focus was to identify those antibiotics that activate PXR and induce CYP3A4 in human hepatocytes and intestinal cells. Human PXR activation was screened using reporter assays in HepG2 cells, kinetic measurements of PXR activation were made in DPX-2 cells, and induction of CYP3A4 expression and activity was verified by quantitative PCR, immunoblotting and testosterone 6â-hydroxylation in primary human hepatocytes and LS180 cells. We found that in HepG2 cells CYP3A4 transcription was activated strongly (>10-fold) by rifampin and troleandomycin; moderately (> 7-fold) by dicloxacillin, tetracycline, clindamycin, griseofulvin and (> 4-fold) by erythromycin; weakly (>2.4-fold) by nafcillin, cefaclor and sulfisoxazole; and (>2-fold) by cefadroxil and penicillin V. Similar though not identical results were obtained in DPX-2 cells. CYP3A4 mRNA and protein expression were induced by these antibiotics to differing extents in both liver and intestinal cells. CYP3A4 activity was significantly increased by rifampin (9.7-fold), nafcillin and dicloxacillin (5.9-fold), and weakly induced (2-fold) by tetracycline, sufisoxazole, troleandomycin and clindamycin. Multiple pharmacophore models and docking indicated a good fit for dicloxacillin and nafcillin in PXR. These results suggest that in vitro and in silico methods can help to prioritize and identify antibiotics that are most likely to reduce exposures of medications (such as oral contraceptive agents) which interact with enzymes and transporters regulated by PXR. In summary, nafcillin, dicloxacillin, cephradine, tetracycline, sulfixoxazole, erythromycin, clindamycin, and griseofulvin exhibit a clear propensity to induce CYP3A4 and warrant further clinical investigation.
Eur J Med Chem. 2008 Apr 4;
Prakash O, Kumar R, Sehrawat R
Seven new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones (5) have been synthesized by the oxidation of 3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromones (4) with iodobenzene diacetate in methanol. The structures of compounds 5 were established by the combined use of (1)H NMR, IR and mass spectra. All the seven compounds (5) were tested in vitro for their antibacterial activity against Gram-positive bacteria namely, Staphylococcus aureus, Staphylococcus epidermidis and Bacillus pumilus and two Gram-negative bacteria namely, Salmonella typhi and Pseudomonas aeruginosa. Three compounds, 5d, 5f and 5g, have displayed antibacterial activity comparable to the commercial antibiotics, Linezolid, Cefaclor and Cefuroxime axetial.
Microb Drug Resist. 2008; 14(2): 155-61
Shen X, Yang H, Yu S, Yao K, Wang Y, Yuan L, Yang Y
This study investigated macrolide-resistant Streptococcus pneumoniae carried by Beijing children presenting with respiratory tract infections. Nasopharyngeal S. pneumoniae strains were tested for sensitivity with 15 antibiotics and further analyzed for phenotypes of macrolide-resistant strains and by PCR for the macrolide-resistant genes ermB, mefA, tetM, and integrase of conjugative transposon (Tn1545) intTn. We found 185 strains of S. pneumoniae relatively highly resistant to erythromycin (78.9%), clindamycin (76.2%), tetracycline (86%), and SMZ-TMP (78.7%) but with relatively low resistance to amoxicillin (2.2%), cefaclor (15.5%), ceftriaxone (2.8%), and cefuroxime (14.1%). The 146 strains of erythromycin-resistant S. pneumoniae showed extensive cross-resistance to other macrolides like azithromycin (100%), clarithromycin (100%), acetylspiramycin (95.2%), and clindamycin (95.9%). Genes ermB and mefA were detected in all erythromycin-resistant strains, with ermB(+) 79.5%, ermB + mefA(+) 17.8%, and mefA(+) 2.7%. About 96.9% of tetracycline-resistant isolates were positive for tetM, compared to 26.9% of sensitive strains. Ninety percent of tetracycline-resistant strains were also erythromycin-resistant versus 11.5% of tetracycline-sensitive strains. The intTn gene was present in 87.6% of S. pneumoniae strains and correlated with erythromycin and tetracycline resistance. The close relationship between the conjugative transposon Tn1545 and the genes ermB and tetM is probably one of the important mechanisms explaining the multiple drug resistance of S. pneumoniae.
J Chemother. 2008 Apr; 20(2): 175-9
Fenoll A, Giménez MJ, Robledo O, Aguilar L, Tarragó D, Granizo JJ, Gimeno M, Coronel P
The aim of this study was to evaluate the effects of penicillin, amoxicillin or erythromycin resistance on the in vitro activity of oral cephalosporins against Streptococcus pneumoniae pediatric isolates. A total of 282 pediatric isolates received during 2005 in the Spanish Reference Pneumococcal Laboratory were tested by agar dilution: 104 strains were penicillin-susceptible, 72 intermediate, and 106 resistant. Serotypes 9 and 14 were the most troublesome with or= 32 microg/ml), with 0% susceptibility to cefaclor, cefuroxime and cefpodoxime. Cefditoren 0.5 microg/ml inhibited 95.3%, 95.5%, and 98.6% of penicillin-, amoxicillin-, and erythromycin-resistant isolates, respectively. Susceptibility to oral cephalosporins shifted from >90% in penicillin-susceptible isolates to approximately 38% for cefuroxime/cefpodoxime and approximately 7% for cefaclor in penicillin-intermediate, and to 0% in resistant isolates. Despite the different in vitro activity of oral cephalosporins, full resistance to penicillin or amoxicillin implied lack of susceptibility to all oral cephalosporins with defined CLSI breakpoints, rendering them inadequate as empirical treatment in countries with a high prevalence of penicillin resistance.
Antimicrob Agents Chemother. 2008 Jul; 52(7): 2407-14
García-Cobos S, Campos J, Román F, Carrera C, Pérez-Vázquez M, Aracil B, Oteo J
Ampicillin resistance in Haemophilus influenzae due to alterations in penicillin-binding proteins (beta-lactamase negative ampicillin resistant [BLNAR]) is acquiring increasing clinical and epidemiological importance. BLNAR strains with low ampicillin MICs (0.5 to 4 microg/ml) represent the majority of this population in Europe and the United States, but separating them from susceptible isolates is challenging. To investigate the best method to identify low-BLNAR strains, we studied the antibiotic susceptibilities of 94 clinical isolates of H. influenzae by microdilution, Etest, and disk diffusion: 25 had no resistance mechanisms (gBLNAS), 34 had mutations in the ftsI gene only (gBLNAR), 20 were beta-lactamase producers only (gBLPAR), and 15 showed beta-lactamase production and mutations in the ftsI gene (gBLPACR). By current CLSI breakpoints, most gBLNAR isolates were ampicillin susceptible by microdilution (76.5%) or by Etest (88.2%). Most gBLNAR strains (79.4%) were nonsusceptible to amoxicillin (the most widely used community antibiotic in the United States and Europe) when tested by microdilution. By Etest, 15% of beta-lactamase-positive isolates were nonresistant to ampicillin or amoxicillin. The poorest agreement between Etest and microdilution results was for the gBLPAR isolates (25% for ampicillin, 15% for amoxicillin, and 10% for cefaclor). Low-strength disks of ampicillin and amoxicillin-clavulanic acid poorly identified low-BLNAR isolates and are not recommended as a screening method. We suggest new amoxicillin breakpoints for BLNAR isolates as follows: susceptible, MIC < or = 0.5 microg/ml (no resistance mechanisms; pharmacokinetic/pharmacodynamic [PK/PD] data favorable); intermediate, MICs = 1 to 2 microg/ml (resistance mechanisms present but PK/PD data favorable), and resistant, MICs > or = 4 microg/ml (resistance mechanisms present and PK/PD data unfavorable).
Pediatr Pulmonol. 2008 May; 43(5): 457-62
Wang A, Yu S, Yao K, Zhang W, Yuan L, Wang Y, Wei J, Shen X, Yang Y
OBJECTIVE: To investigate the nasopharyngeal carriage and antimicrobial susceptibility of H. influenzae among children younger than 5 years old and to assess antibiotics usage patterns in the outpatient department of Beijing Children's Hospital from 2000 to 2004. MATERIALS AND METHODS: From 2000 to 2004, At least 100 strains of H. influenzae were isolated from the pediatric patients who were younger than 5 years and who presented with symptoms of acute upper respiratory tract infections during February to May in each of the study years. Antimicrobial susceptibilities were determined; and antibiotics usage was expressed as defined daily dose (DDD)/100 patient days. RESULTS: The overall nasopharyngeal carriage rate of H. influenzae is 26.3% (562/2,137) in children younger than 5 years old with acute upper respiratory tract infection. The percentage of ampicillin-resistant isolates ranges from 4.0% (4/100) to 14.3% (17/119) from 2000 to 2004. All the ampicillin-resistant isolates are beta-lactamase producers. More than 80% of the isolates are susceptible to amoxicillin, cefaclor, and chloramphenicol; whereas, almost all (99-100%) of the isolates are sensitive to amoxicillin/clavulanic acid, ceftriaxone, and cefuroxime. For antibiotics utilization, macrolides are the predominantly used antibiotics, followed by cephalosporins and penicillins among pediatric patients in the outpatient department during the study period. CONCLUSION: All amoxicillin-resistant isolates of H. influenzae are producing beta-Lactamase; and the rates of amoxicillin-resistant isolates are increasing over time. Amoxicillin/clavulanic acid and cephalosporins are highly sensitive to H. influenzae isolated from Chinese pediatric patients. Macrolides are the most used antibiotics in the outpatient department during the study period.
Eur J Clin Microbiol Infect Dis. 2008 Mar 18;
Yu S, Yao K, Shen X, Zhang W, Liu X, Yang Y
The aims of this study were to estimate pneumococcal carriage rate, antimicrobial resistance and serogroup distribution of nasopharyngeal isolates of Streptococcus pneumoniae among children with acute upper respiratory infections (AURIs) aged 1 month to 5 years attending outpatient department of the Beijing Children's Hospital between 2000 and 2005. Susceptibilities to penicillin, amoxicillin-clavulanic acid, ceftriaxone, cefuroxime, cefaclor, erythromycin, tetracycline, sulfamethoxazole-trimethoprim and chloramphenicol were assessed using the E-test and disc diffusion. We also analyzed the correlation between antibiotic consumption and rates of resistance. The prevalence of penicillin-nonsusceptible pneumococci increased from 26% during 2000-2001 and 21% during 2002-2003 to 31.5% in 2004-2005. The percentage of S. pneumoniae resistant to cefaclor and cefuroxime increased from about 6% during 2000-2001 to about 23% during 2004-2005 (P