We report an isocratic "high-performance" liquid-chromatographic (HPLC) procedure for measurement of five orally administered cephalosporins (cefixime, cefaclor, cefadroxil, cephalexin, and cephradine) in 0.1 mL of human serum. Serum protein is precipitated with acetonitrile, the sample is centrifuged, and the supernate is evaporated under nitrogen. The residue is reconstituted in 0.1 mL of mobile phase, and 50 to 80 microL of this is injected onto a reversed-phase Altex Ultrasphere Octyl (C8) column. The five cephalosporins are resolved by elution with a pH 2.6 mobile phase of methanol/monobasic phosphate buffer (20/80) by vol), flow rate 2 mL/min. The column effluent is monitored at 240 nm. Cefixime serves as the internal standard for the analysis of the four other compounds, cephalexin as the internal standard for cefixime. We used two standard curves for all compounds: a low-range curve for concentrations commonly observed clinically and a higher-range curve for higher concentrations. The former were linear from 1.0 to 10 mg/L for cefaclor, cefadroxil, cephalexin, and cephradine and from 0.1 to 1 mg/L for cefixime. The high-concentration curves were linear from 1 to 10 mg/L for cefixime and from 10 to 100 mg/L for the other compounds. The detection limits were 0.1 mg/L for cefixime, 1 mg/L for the other cephalosporins. Mean within-run and day-to-day CVs were always less than 15% for all compounds studied.
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Extended-spectrum beta-lactamases which confer resistance to oxymino cephalosporins, are derived from common TEM-1, TEM-2 and SHV-1. beta-lactamases by mutations which alter the configuration of active site and expand their spectrum of activity. The aim of this investigations was to determine the effect of these enzymes on in vitro susceptibility of clinical isolates of Klebsiella pneumoniae to oral cephalosporins. beta-lactamases were characterised by isoelectric focusing and polymerase chain reaction. The susceptibility of K. pneumoniae isolates harboring these enzymes to oral cephalosporins was determined by broth-microdilution method and the stability of these antibiotics to enzyme degradation was tested by macroiodometric method. Based on the isoelectric point beta-lactamases were assigned into three groups: SHV-2 type (pI 7.6), SHV-5 type (pI 8.2) and TEM-1 derivates (pI 5.4). All types of beta-lactamases described in this investigation were associated with high level of resistance to older cephalosporins like cephalexin, cefaclor, cefuroxime, cefotiam, cefprozil and cefadroxil and to amoxycillin too. Third generation oral cephalosporins like ceftibuten and cefetamet were more stable in the presence of beta-lactamases but some of the strains were resistant to these antibiotics too. SHV-5 beta-lactamases producers displayed higher level of resistance to most of oral cephalosporins compared to SHV-2 and TEM producing strains. According to the results of this investigation oral cephalosporins cannot be considered as a therapeutic option for the treatment of infections caused by ESBL producing K. pneumoniae isolates.
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Antigen detection tests (ADTs) were used by 64% of the pediatricians; 85% used throat cultures. Strategies for diagnosing streptococcal pharyngitis were throat culture alone (38%), consider positive ADTs definitive and use throat culture when ADTs are negative (42%), ADT alone (13%), ADT and throat culture for all patients with pharyngitis (5%), and no tests for GABHS performed (2%). Thirty-one percent usually or always treated with antibiotics before test results were available. Only 29% of these "early treaters" always discontinued antibiotics when tests did not confirm the presence of group A streptococci. The drug of choice for treatment was penicillin (73%); another 26% preferred a derivative of penicillin, particularly amoxicillin. Many pediatricians altered their management when a patient had recurrent streptococcal pharyngitis. Nearly half of the respondents would use a different antibiotic than they used for routine acute streptococcal pharyngitis. They most often changed to erythromycin (25%), cefadroxil (23%), or amoxicillin-clavulanate (20%). Follow-up throat culture was obtained by 51% of pediatricians after treatment of recurrent streptococcal pharyngitis. A patient with chronic carriage of GABHS and symptoms of pharyngitis would be treated with an antibiotic by 84%; most (62%) would use a penicillin. Other choices were cephalosporins (19%), erythromycin (12%), clindamycin (3%), or rifampin plus penicillin (3%). Tonsillectomy was recommended for symptomatic carriers by 31% of respondents. Carriers without symptoms were less likely to be treated with antibiotics (23%) or referred for tonsillectomy (21%).
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Linezolid and cefadroxil were consistently effective treatments across all primary and secondary efficacy assessments. At follow-up cure rates were 88.7% (205 of 231) for linezolid-treated and 86.2% (193 of 224) for cefadroxil-treated intent-to-treat patients; cure rates were 91.0% (201 of 221) for linezolid-treated and 90.0% (189 of 210) for cefadroxil-treated clinically evaluable patients. S. aureus was eradicated in 89.6% (120 of 134) linezolid-treated and 88.8% (111 of 125) cefadroxil-treated microbiologically evaluable patients. Gastrointestinal complaints were the most common adverse events reported, without significant differences between treatment groups, and myelosuppression was not observed in this study.
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Cefadroxil was administered at a daily dose of 50 mg/kg in 113 children including acute respiratory tract infections suspected to be a bacterial infection and other febrile diseases. Among 41 cases in which pharyngeal culture was made twice before and after administration or urine and feces cultures were made, 20 cases (48.8%) were good bacteriologically, 5 cases (12.2%) were poor, and 16 cases (39.0%) were unknown. Clinical efficacy was obtained in 105 cases (92.9%) out of 113 cases. Microbial substitution was noticed in 12 cases (29.3%) out of the cases of which pharyngeal culture was made after cefadroxil administration. Haemophilus influenzae was detected newly after the administration in 7 cases (58.3%) out of these 12 cases. Bacteriological efficacy was obtained in 5 cases of acute respiratory tract infection of which pathogen was considered to be Haemophilus influenzae. No microbial substitution was noticed in these 5 cases. As to the side effects of cefadroxil administration, only a slight diarrhea was observed in 2 cases.
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Amorphous lactose and cefadroxil undergo recrystallization when the moisture level in the surroundings exceeds the threshold values specific to each compound. During the sorption phase, heat is evolved fairly linearly as a function of consumed moisture, and also after the recrystallization, the heats indicate linear behavior. The heat values for the desorption phase of amorphous lactose and the adsorption of crystalline lactose coincide. With the different anhydrous forms of theophylline, the hydration takes place more rapidly in the metastable form 1, and generally, the process is more energetic in form 1. In all cases, the gravimetric results agree with the water sorption uptakes calculated from the calorimetric data.
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Dogs with clinical signs of skin infection confirmed via bacteriologic culture were randomly allocated to receive a single SC injection of cefovecin (8 mg/kg [3.6 mg/lb]) followed by placebo administered PO twice daily for 14 days or cefadroxil (22 mg/kg [10 mg/lb]) administered PO twice daily for 14 days following a placebo injection. Two 14-day treatment courses were permitted. Treatment success was defined as reduction of clinical signs to mild or absent at the final assessment.
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In 11 puerperal women, a breast abscess was treated by drainage from the inframammary fold. Eight patients wished to continue breast feeding. During the healing period, the babies were not breast fed on the operated side. In 3 patients, the skin over the abscess necrotised, resulting in a defect of 1 to 2 cm. In 2 patients, a small seroma had to be punctured after removing the drainage tube. Aesthetic results were judged by the patients as good. Resumation of suckling on the operated side revealed only 15 to 20% milk yield compared to that of the other breast. This treatment meets aesthetic and function-preserving criteria.
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In an open study, 30 patients (mean age 43.7 years) with clinical and radiological evidence of sinusitis were studied by transmaxillary sinus aspirations (19 bilateral and 11 unilateral for a total of 49 aspirates). The sinus aspirations were performed with careful sterile intermeatus needle puncture techniques and the material was cultured for aerobic and anaerobic bacteria. The organisms most frequently recovered from the sinus aspirates were Gram-positive (55%), Gram-negative (33%), and anaerobes (6%). Cefadroxil 1g was given every 12 hours (2g daily) for 10 days. Therapeutic efficacy was then evaluated on the basis of changes in clinical status, radiographic findings and, where possible, bacteriological results. Cefadroxil treatment produced a 90% cure rate assessed clinically and by radiological confirmation; moreover, the drug was well tolerated in the majority of patients.
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In this paper, the chiral separation of cefadroxil was studied by capillary electrochromatography. Monolithic capillary column was prepared for the separation of cefadroxil enantiomers. The optimum buffer contained 28.5 mmol/L sodium acetate, 0.95% (v/v) acetic acid, 19 mmol/L beta-cyclodextrin (beta-CD) and 5% (v/v) isopropanol in formamide solution (pH 7.0), with the running voltage of 12 kV, the UV detector wavelength of 254 nm, the sample injected time of 8s and the temperature of 25 degrees C. Under these conditions, the column efficiency of cefadroxil enantiomers were N1=5324 and N2=23,768 with a selectivity factor (alpha) of 1.056 and resolution (Rs) of 0.978. The effect of buffer pH value, beta-CD concentration, organic modifier (isopropanol) concentration and voltage was also investigated for the separation by CEC.