We collected data from 6,249 ARI emergencies studied on 30 separate days. Antibiotics were prescribed in 58.7% of the ARI (bronchiolitis, 11.5%; bronchitis, 40.2%; pharyngotonsillitis, 80.9%; nonspecified ARI, 34.8%; pneumonia, 92.4%; otitis, 93.4%; sinusitis, 92.6%). The most commonly used antibiotics were amoxicillin/clavulanate (33.2%), amoxicillin (30.2%), cefuroxime axetil (8.5%) and azithromycin (6%). According to the consensus guidelines developed for this study, therapy was considered to be appropriate in 63.1% of the ARI (first choice, 52.1%; alternative choice, 11.0%) and inappropriate in 36.9%. The percentages of inappropriate prescription according to ARI groups were: bronchiolitis, 11.5%; bronchitis, 31.5%; pharyngotonsillitis, 54.8%; nonspecified ARI, 34.7%; pneumonia, 13.9%; otitis, 25.6%; and sinusitis, 22.2%.
The acute otitis media is a frequent infantile disease and, in 80% of cases, a bacterial strain can be isolated from the otorrhoea. Haemophilus influenzae and Streptococcus pneumoniae are the two major species isolated from auricular exudate, and represent two thirds of all isolated strains, with the others comprising Staphylococcus aureus, Branhamella catarrhalis, Pseudomonas aeruginosa, Enterobacteriaceae and corynebacteria. The treatment of this disease is based principally on beta-lactams (aminopenicillins, cephalosporins) administered by the oral route. Cefuroxime is a cephalosporin which is absorbed via the digestive tract in the form of cefuroxim-axetil. The activity of this compound was studied against 210 strains isolated from otorrhoea, collected from children who presented an acute otitis media during the first half of 1989. These strains were: 112 strains of H. influenzae, of which 23 produced a beta-lactamase; 21 strains of Streptococcus pneumoniae; 3 strains of Streptococcus pyogenes; 10 strains of Branhamella catarrhalis of which 9 produced a beta-lactamase; 18 strains of S. aureus; 14 strains of Enterobacteriaceae, and 32 strains of corynebacteria. The minimal inhibitory concentration (MIC) of cefuroxime-axetil was measured by dilution in agar. The MICs of cefuroxime against H. influenzae were low and similar (MIC 50 = 1 mg/l; MIC 90 = 1 mg/l) regardless of whether the strain secreted a beta-lactamase. Overall, 90% and 98% of the 210 strains tested here were inhibited by 1 and 4 mg/l of cefuroxime respectively. These results show that the antibacterial spectrum of cefuroxime-axetil appears to be ideally suited to the bacterial strains isolated from acute otitis media.
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Chemotherapy of community-acquired respiratory tract infections was reviewed from a microbiological perspective. The current worldwide spread of penicillin-resistant Streptococcus pneumoniae and of ampicillin-resistant Haemophilus influenzae has required a reassessment of the antimicrobial agents being used for empiric therapy. In vitro data with different orally administered antibiotics were reviewed in order to identify any deficiencies in their spectra of activity against four common respiratory tract pathogens. Cefixime, cefuroxime axetil, cefprozil, amoxicillin-clavulanic acid and trimethoprim-sulfamethoxazole were active against all four species other than penicillin-resistant pneumococci.
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Acute exacerbations of chronic bronchitis (AECB) are the most common complication of chronic bronchitis. The majority of AECB are caused by infection. The choice of appropriate antibacterial therapy for AECB is becoming more difficult and is usually empirically. Cefaclor and cefuroxime are used for ambulatory treatment of AECB.
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Development of resistance to antibiotics is a major problem worldwide. The normal oropharyngeal flora, the intestinal flora and the skin flora play important roles in this development. Within a few days after the onset of antibiotic therapy, resistant Escherichia coli, Haemophilus influenzae and Staphylococcus epidermidis can be detected in the normal flora of volunteers or patients. Horizontal spread of the resistance genes to other species, e.g. Salmonella spp., Staphylococcus aureus and Streptococcus pneumoniae, occurs by conjugation or transformation. An ecologically sound antibiotic policy favours the use of antibiotics with little or no impact on the normal flora. Prodrug antibiotics which are not active against the bacteria in the mouth and the intestine (before absorption) and which are not excreted to a significant degree via the intestine, saliva or skin are therefore preferred. Prodrugs such as pivampicillin, bacampicillin, pivmecillinam and cefuroxime axetil are favourable from an ecological point of view. Experience from Scandinavia supports this, since resistance to mecillinam after 20 years of use is low (about 5%) and stable.
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This investigation describes the development of an intragastric drug-delivery system for cefuroxime axetil. The 3(2) full factorial design was employed to evaluate contribution of hydroxypropyl methyl cellulose (HPMC) K4M/HPMC K100 LV ratio (polymer blend) and sodium lauryl sulfate (SLS) on drug release from HPMC matrices. Tablets were prepared using direct compression technique. Formulations were evaluated for in vitro buoyancy and drug release study using United States Pharmacopeia (USP) 24 paddle-type dissolution apparatus using 0.1N HCl as a dissolution medium. Multiple regression analysis was performed for factorial design batches to evaluate the response. All formulations had floating lag times below 2 minutes and constantly floated on dissolution medium for more than 8 hours. It was found that polymer blend and SLS significantly affect the time required for 50% of drug release, percentage drug release at 12 hours, release rate constant, and diffusion exponent (P < .05). Also linear relationships were obtained between the amount of HPMC K100 LV and diffusion exponent as well as release rate constant. Kinetic treatment to dissolution profiles revealed drug release ranges from anomalous transport to case 1 transport, which was mainly dependent on both the independent variables.