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Oral cephalosporins have not previously been extensively tested against larger numbers of Borrelia burgdorferi isolates derived from different clinical and geographical sources. This study investigated the in vitro activity of eight oral cephalosporins in addition to ceftriaxone and apramycin, against 17 isolates of the B. burgdorferi complex, including one B. valaisiana and one B. bissettii tick isolate. Minimal inhibitory concentrations and minimal borreliacidal concentrations providing 100% killing of the final inoculum were determined by a standardised methodology in Barbour-Stoenner-Kelly-medium after 72 h of incubation. The rank order of potency was ceftriaxone>cefuroxime-axetil>cefixime, cefdinir>cefpodoxime>cefaclor >ceftibuten, loracarbef>cefetamet-pivoxil, apramycin. Our study demonstrates the superior in vitro effectiveness of ceftriaxone with good to excellent activity with the oral agents cefuroxime-axetil, cefixime and cefdinir against B. burgdorferi under strictly standardised test conditions.
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A 5-day regimen of cefdinir was effective in the eradication of the common causative pathogens of nonrefractory AOM, including intermediate penicillin-resistant S. pneumoniae and beta-lactamase-producing organisms. Cefdinir should be considered a suitable second line antibiotic for AOM.
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CS-834 is a prodrug of the carbapenem R-95867, developed by Sankyo Co., Ltd., Tokyo, Japan. To investigate the possibility that CS-834 may be the first carbapenem usable in an oral dosage form, its in vitro antibacterial activity (as R-95867) and in vivo antibacterial activity were compared with those of cefpodoxime proxetil, cefditoren pivoxil, cefdinir, ofloxacin, imipenem, and amoxicillin. R-95867 had high levels of activity against methicillin-susceptible staphylococci and streptococci, including penicillin-resistant Streptococcus pneumoniae, as well as Neisseria gonorrhoeae, Moraxella catarrhalis, the members of the family Enterobacteriaceae (with the exception of Serratia marcescens), Haemophilus influenzae, and Bordetella pertussis; for all these strains, the MICs at which 90% of tested strains are inhibited (MIC90s) were 1.0 microg/ml or less. Against methicillin-resistant staphylococci, enterococci, Serratia marcescens, Burkholderia cepacia, Stenotrophomonas maltophilia, and Acinetobacter calcoaceticus, R-95867 showed activity comparable to or slightly less than that of imipenem, with MIC90s ranging from 2 to >128 microg/ml. The in vivo efficacy of oral CS-834 against experimental mouse septicemia caused by gram-positive and gram-negative bacteria was better than that of comparative drugs. In murine respiratory infection models, the efficacy of CS-834 reflected not only its potent in vitro activity but also the high levels present in the lungs.
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Group A beta-hemolytic streptococcus (GABHS) is the most common bacterial cause of acute pharyngitis. Although children infected with GABHS will recover clinically without antibiotics, treatment is recommended in order to prevent acute rheumatic fever and probably suppurative complications, hasten resolution of clinical signs and symptoms, and prevent transmission to close contacts. Streptococcal pharyngitis usually cannot be reliably distinguished from other etiologies on the basis of epidemiologic or physical findings, and therefore a throat culture or a rapid antigen detection test is generally necessary to confirm the diagnosis. All isolates of GABHS are sensitive to penicillins and cephalosporins, whereas resistance to macrolides has been identified in some geographic regions. The recommended first-line therapy for streptococcal pharyngitis is a 10-day course of penicillin V, usually given 2 or 3 times per day. A number of alternatives to penicillin V are available, including other penicillins, macrolides, and cephalosporins. As a class, the cephalosporins are noteworthy because they may provide somewhat higher bacteriologic eradication rates than penicillin V. Many cephalosporins can be administered twice daily, but they also must be given for 10 days. Two third-generation cephalosporins, cefdinir and cefpodoxime proxetil, are approved for use in a more convenient 5-day dosing schedule, thus possibly increasing the likelihood of adherence to the full course of therapy. Palatability is also an important consideration when prescribing antibiotics to children. In a series of studies, children preferred the pleasant strawberry-cream taste of cefdinir to that of amoxicillin/clavulanate, cefprozil, and azithromycin. Cefdinir may offer an alternative to penicillin V for children with streptococcal pharyngitis, particularly when compliance is a clinical concern.
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Impetigo can result from Staphylococcus aureus (S. aureus). Wolf's isotopic response is the occurrence of a new cutaneous disorder at the site of a previously healed disease. A cutaneous immunocompromised district is an area of skin that is more vulnerable than the rest of the individual's body.
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A multicenter US trial comparing antibiotics-first to appendectomy, including outpatient management, is feasible to evaluate efficacy and safety.
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Cefdinir (CFDN, FK482) was evaluated in children with infections. CFDN was given at a daily dose of 6.4-19.8 mg/kg in 2 or 3 divided portions. CFDN was effective in 94% of 32 cases with respiratory tract, middle ear, urinary tract or skin structure infections. Side effects were loose stool and diarrhea (12.5%). In a pharmacokinetic study, 6.0 mg/kg of CFDN was given to each of the subjects before meal. Cmax was 0.81 +/- 0.38 microgram/ml, T 1/2 was 2.31 +/- 0.77 hours. Antibacterial activity against Staphylococcus aureus was the most excellent of oral cephem antibiotics tested. The data suggest that CFDN 10% granular preparation is safe and effective when used in children with infections caused by susceptible bacteria.
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Etest, a stable-gradient antimicrobial susceptibility test method (AB Biodisk, Solna, Sweden), was compared to the agar dilution method for tests with amikacin, tobramycin, aztreonam, cefdinir, cefprozil, ceftazidime and sparfloxacin. The study design followed recommended guidelines for 510(k) application by the U.S. Food and Drug Administration (FDA). Results demonstrated Etest accuracy (MIC +/- 1.0 log2 dilutions compared to agar dilution MIC) to be 90.4% with only one of 1150 comparisons showing a reproducible variation of 2 log2 dilutions. Categorical equivalency was > or = 92% for all drugs except ceftazidime (82 to 89%), but false-susceptible error was rare (< 0.1%). Etest was very reproducible (100% of results +/- 1.0 log2 dilution) and quality control results conformed to published MIC ranges. The Etest seems to render accurate results for these seven antimicrobial agents evaluated.
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The minimum inhibitory concentrations (MICs) of tosufloxacin (TFLX), levofloxacin (LVFX), ciprofloxacin (CPFX), gatifloxacin (GFLX), sparfloxacin (SPFX), azithromycin (AZM), cefteram (CFTM), cefdinir (CFDN) and cefpodoxime (CPDX) against 337 clinical isolates of Streptococcus pneumoniae isolated from Japanese hospital from 1997 to 2002 were investigated by agar plate method. The incidence of penicillin-susceptible S. pneumoniae (PSSP), penicillin-intermediate resistant S. pneumoniae (PISP), and penicillin-resistant S. pneumoniae (PRSP) in each year was studied, and the MICs of antibacterial agents against these strains were determined. As the results, the total incidence of PSSP, PISP, and PRSP was 51.0%, 40.4% and 8.6%, respectively. The incidences of PSSP from 1997 to 2002 were 46.0-55.9%, and were almost definite in each year. In quinolone antibiotics, the differences of antibacterial activity among TFLX, SPFX, and GFLX against PSSP, PISP, and PRSP, were not observed, and these 3 quinolones had potent antibacterial activity. Although CPFX and LVFX showed antibacterial activity as well as other quinolones by 2001, the CPFX-resistant or LVFX-intermediate resistant strains of PSSP were seen with 56.5% and 91.3% in 2002, respectively. Thirty percents of each PSSP, PISP, and PRSP strains were AZM-resistant strains. Such tendency of increase was recognized in PSSP. Against cephem antibiotics, the incidence of intermediate resistant and resistant strains was higher for PISP and PRSP than for PSSP. No difference in the incidence of resistant strains was noted among CFTM, CFDN, and CPDX.
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The effect of serum on the bactericidal activity of cefdinir, and the ability of the antibiotic to modify the interaction of bacteria with human polymorphonuclear neutrophils were assessed. In the presence of antibiotic, serum-resistant Escherichia coli were sensitised to the bactericidal activity of normal human serum. Cefdinir enhanced opsonophagocytic killing of Escherichia coli and Staphylococcus aureus at suprainhibitory concentrations. Significant potentiation of killing occurred with the combination of inhibitory concentrations of cefdinir, neutrophils and sub-optimal levels of serum opsonins. Pre-exposure of Escherichia coli, but not Staphylococcus aureus, to cefdinir enhanced phagocytic uptake and killing of the antibiotic-damaged bacteria. These results indicate that cefdinir-mediated phenotypic modification of Escherichia coli renders the bacteria susceptible to serum antibacterial activity and phagocytic uptake and intracellular killing.
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Two dosage regimens of cefdinir were compared with amoxicillin/clavulanate for the treatment of suppurative acute otitis media (AOM) in children.
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Presumptive eradication of middle ear pathogens determined by clinical cure of signs and symptoms of AOM at end of therapy (Study Days 7 to 9) and Visit 3 (Study Days 16 to 21).