A reversed-phase column liquid chromatographic method was developed for the assay of cefadroxil in bulk drugs and pharmaceutical preparations. An equation was derived showing a linear relationship between peak-area ratios of cefadroxil to dimethylphthalate (internal standard) and the cefadroxil concentration over a range of 0.02-0.8 mg/ml (r = 0.9999). Standard addition recoveries were generally greater than 97.7%. The coefficients of variation in the within-day assay were between 0.36 and 0.65, and in the between-day assay was 0.71%. The column liquid chromatographic assay results were compared with those obtained from a microbiological assay, which indicated that the proposed method is a suitable substitute for the microbiological method for potency assays and stability studies of cefadroxil preparations.
Beta-streptococci isolated from patients with acute tonsillitis were tested for penicillin tolerance defined as an MBC/MIC ratio greater than or equal to 16. 11/18 strains recovered from patients with clinical treatment failure were tolerant to penicillin in comparison with 0/15 strains from successfully treated patients. The MBC/MIC ratio was less than 16 for all strains versus cefadroxil but above that ratio for many strains versus clindamycin, doxycycline and erythromycin. We suggest that penicillin tolerance may be one reason to treatment failures in individuals with streptococcal tonsillitis and that other antibiotics could be used to treat these patients since penicillin tolerance is not correlated to a general increase in antibiotic resistance.
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To investigate the distribution and antimicrobial resistance in urinary tract pathogens, primarily Escherichia coli, in two age groups, children < or = 2 y and adults 18-50 y, over a period of 12 y.
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In this study, instrumentation for measuring vapor sorption enthalpies and sorption uptakes simultaneously with an isothermal microcalorimeter is introduced. Various pharmaceutical model substances undergoing phase transitions when exposed to humid conditions (25 degrees C), were employed to evaluate the usefulness and sensitivity of the constructed experimental method.
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Bacteriological, pharmacokinetic and clinical studies on cefpodoxime proxetil (CPDX-PR, CS-807), a new oral cephem antibiotic, were carried out in the field of pediatrics. The results obtained are summarized as follows. 1. Antibacterial activities of R-3746 (Na-salt of cefpodoxime (CPDX] against clinically isolated strains of Streptococcus pneumoniae, Streptococcus pyogenes, Staphylococcus aureus, Enterococcus faecalis, Branhamella catarrhalis, Escherichia coli, Proteus mirabilis and Haemophilus influenzae were compared with those of cefaclor, cephalexin and cefadroxil. R-3746 is superior to other antibiotics against S. pneumoniae, S. pyogenes, B. catarrhalis and Gram-negative rods. 2. Serum concentrations of CPDX after administration of CPDX-PR at doses of 3 mg/kg (fasting), 6 mg/kg (non-fasting) and 6 mg/kg (fasting) were determined. Mean AUC (area under curve)'s of CPDX obtained were 9.60, 31.35 and 17.89 micrograms.hr/ml, respectively for the 3 dosages. The mean half-lives of CPDX were 3.35, 1.88 and 1.76 hours, respectively. The mean urinary recovery rate within 8 hours after administration of CPDX-PR at a dose of 3 mg/kg (fasting) was 39.2%. 3. CPDX-PR was administered to 37 pediatric patients with various bacterial infections (pyelonephritis 9, cystitis 4, pneumonia 7, acute bronchitis 3, otitis media 2, tonsillitis 10, subcutaneous abscess 1 and purulent lymphadenitis 1). The overall clinical efficacy rate was 91.9% and the overall bacteriological eradication rate was also 91.9%. 4. No adverse reactions were observed. Abnormal laboratory findings were moderate, eosinophilia in 2 and slight elevation of GOT and GPT in 1. The taste and the odor of the CPDX-PR preparation was sufficiently tolerable. From the above results we have concluded that CPDX-PR is a useful oral antibiotic in the treatment of bacterial infections in children.
In order to compare the clinical efficacy and safety of cefatrizine (Cefaperos) and cefpodoxime proxetil (Orelox) in the treatment of secondarily infected chronic obstructive pulmonary disease (COPD) in adults, a multicentre, randomized, open study was conducted by 60 general practitioners in two parallel groups of patient suffering from COPD complicated by an acute episode of superinfection (Anthoniesen stages 2 and 3). After verification of the eligibility criteria, written consent and randomization, the patients received, for 10 days, either cefatrizine at the dose of 1 g/day or cefpodoxime proxetil at the dose of 400 mg/day. A self-assessment form was given to the patient. A telephone visit was planned for D3. The final visit on D11 +/- 1 evaluated clinical efficacy (success or failure) and safety. The study population was composed of 250 patients with a mean age of 59.9 +/- 15.9 years (sex ratio M/F = 1.5). The principal etiology of COPD was chronic bronchitis in 67.5% of patients, longstanding asthma in 24.5% and emphysema in 6.8%. The mean history of the disease was 13.0 +/- 10.8 years. The Anthoniesen score was equal to 2 in 73.6% of patients, 3 in 8.8% of patients and 1 in 17.6% of patients. No significant difference concerning these criteria was observed between the two study groups. The clinical success rate was equivalent in the two groups. The time to regression of clinical signs tended to be shorter, up until the sixth day (mainly between D4 and D6) for patients treated with cefatrizine (p = 0.09; NS). The clinical safety was considered to be good and was comparable in the two study groups. This study concluded on the equivalent clinical efficacy of cefatrizine and cefpodoxime proxetil in the treatment of superinfections of COPD in general practice (97.5% and 99%, respectively), with a satisfactory and comparable safety, but with a much lower cost of treatment for cefatrizine. This conclusion is particularly important in the context of opposable medical references, as, although the treatment of superinfections of COPD by second and third generation cephalosporins is frequently proposed, the prescription of a less expensive cephalosporin appears to be more relevant.
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A pathogenetic bacterial strain X-1-06909 was isolated from naturally infected Siberian sturgeon in Beijing. The strain was identified according to its physiological and biochemical properties, and the sequence analysis of 16S rRNA gene. The drugs sensitivity was detected with Kirby-Bauer's agar diffusion method.
A total of 410 strains of viridans group streptococci isolated consecutively from blood were tested by the microdilution method for in vitro susceptibility to 22 beta-lactam antibiotics. One hundred thirty-eight strains (33.6%) were resistant to penicillin with a MIC range of 0.25 to 8 micrograms/ml. MICs of all beta-lactam agents tested were higher for penicillin-resistant strains than for susceptible strains. These antibiotics were classified into three groups according to their in vitro activities (MICs at which 50 and 90% of the isolates are inhibited). Beta-Lactams of the first group (these included imipenem, cefpirome, FK-037, cefditoren, cefotaxime, ceftriaxone, and cefepime) showed activities higher than or similar to that of penicillin against penicillin-resistant viridans group streptococci. However, 80% of highly penicillin-resistant Streptococcus mitis organisms required cefotaxime and ceftriaxone MICs of > or = 2 micrograms/ml (range, 2 to 16 micrograms/ml). Beta-Lactams of the second group (cefpodoxime, ampicillin, amoxicillin-clavulanate, piperacillin, and cefuroxime) showed lower activities than penicillin. Finally, antibiotics of the third group (cephalothin, oxacillin, ceftazidime, cefixime, cefaclor, cefetamet, cefadroxil, cephalexin, and ceftibuten) showed poor in vitro activities. Therefore, some of the beta-lactam agents included in the first group could be an acceptable alternative in the treatment of serious infections due to strains highly resistant to penicillin, although clinical experience is needed.
The susceptibility of 2196 fresh clinical isolates to twelve different oral compounds was assessed in five Swiss microbiology institutions during summer 1992. A standardized microdilution system including all other material necessary was employed to assess the antibacterial activity of penicillin G, ampicillin, ampicillin + sulbactam, amoxycillin + clavulanic acid, cefadroxil, cephalexin, cefaclor, cefuroxime, cefetamet, doxycycline, erythromycin and clindamycin. The aminopenicillins (including the beta-lactamase inhibitor combinations) were highly active against the streptococci, in combination with a beta-lactamase inhibitor they covered the majority of the bla+ E. coli and Proteus mirabilis and between 60 to 80% of the Klebsiella spp. and Proteus vulgaris isolates. All the cephalosporins exhibited good activity against the streptococci, they were active against Gram-negative fermentative rods to a varying degree. Cefetamet was also active against many cefaclor and cefuroxime-resistant isolates. A considerable part of the species studied exhibited resistance to doxycycline; the observed resistance of S. agalactia, P. mirabilis, and Morganella morganii agreed with previous findings. Most of the Streptococcus spp. were inhibited by erythromycin and clindamycin. There were only single penicillin resistant S. pneumoniae isolates in the five Swiss centers. Taking account of the above particulars the epidemiology of antimicrobial resistance in Switzerland can be considered satisfactory.
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A literature search was conducted of the Cochrane Library, EMBASE, and MEDLINE databases, from their inception through July 20, 2009, using the following terms: linezolid, newborn, infant, child, pediatrics, adolescent, human, clinical trial, and case report. Articles were excluded if they were redundant or not pertinent. (Articles that did not focus on the use of linezolid in children were considered not pertinent.) Bibliographies of all relevant articles were also evaluated.
In the 4 studies 958 patients were included in the intent-to-treat analysis. In the linezolid vs. cefadroxil study (Study III), the most common AEs in patients treated with linezolid were diarrhea (7.8%), headache (6.5%) and upper respiratory tract infection (3.7%). In the linezolid vs. vancomycin study (Study IV), the most common AEs in the linezolid group were fever (14.1%), diarrhea (10.8%) and vomiting (9.4%). The most common drug-related AEs for linezolid in all 4 studies were diarrhea, vomiting, loose stools and nausea. None of these common AEs or drug-related AEs occurred more frequently in patients treated with linezolid than in those in the comparator group.