Additive diuretic effect of S-8666 during furosemide-induced diuresis in rats.
ESBL-producing isolates were rather frequent in urines in French outpatients in 2013. Males and persons residing in nursing homes were at higher risk of ESBL-positive infection. Despite the increase in ESBL-positive isolates, the susceptibility to antibiotics used to treat cystitis remains high.
To determine the benefits and harms of different antibiotic regimens for the treatment of acute pyelonephritis in children.
The activity of BAY v 3522 was tested against over 500 clinical bacterial isolates and compared with the activities of ampicillin, amoxicillin-clavulanate, cefaclor, cefixime, cefuroxime, cephalexin, and/or ciprofloxacin, erythromycin, and metronidazole. BAY v 3522 activity against staphylococci and streptococci equaled or exceeded those of the other agents. BAY v 3522 exhibited no significant advantage over cefaclor, cefuroxime, or cephalexin against gram-negative bacilli.
We undertook to identify the antimicrobial susceptibility of the pathogens isolated from patients with otitis media or maxillary sinusitis who failed to respond to antimicrobial therapy, and correlate it with previous antimicrobial therapy and smoking. We analyzed isolates recovered from 2 consecutive cultures obtained from middle ear aspirate obtained through an open perforation in 22 children with otitis, and maxillary sinus aspirate collected by endoscopy from 20 patients. Forty-seven isolates were repeatedly recovered from 42 culture-positive individuals. The organisms isolated were Streptococcus pneumoniae (15 isolates), Haemophilus influenzae (14), Staphylococcus aureus (7), Moraxella catarrhalis (6), and Streptococcus pyogenes (5). Resistance of at least 2 tube dilutions to the antimicrobial agents used was found in 23 of the 47 (49%) isolates that were found in 20 (48%) of the patients. These included 10 of 15 (67%) isolates of S pneumoniae, 4 of 14 (29%) H influenzae (all were beta-lactamase producers), 4 of 7 (57%) S aureus (all beta-lactamase producers), 5 of 6 (83%) M catarrhalis (all beta-lactamase producers), and none of 5 S pyogenes. In the 21 patients who failed to respond to amoxicillin, H influenzae and S pneumoniae predominated. Streptococcus pneumoniae was recovered from 4 of the 11 (36%) after trimethoprim-sulfamethoxazole, 4 of 21 (19%) after amoxicillin, 2 of 3 (67%) after azithromycin dihydrate, and 1 of 4 (25%) after cefixime. A statistically significant higher recovery of resistant organisms was noted in those treated 2 to 6 months previously, and in those with sinusitis who smoked. The data illustrate the relationship between resistance to antimicrobials and failure of patients with otitis media and sinusitis to improve.
The ecological effects on the normal intestinal microflora after cefixime tablets in doses of 200 mg twice daily for 7 days were studied in 10 healthy volunteers. Stool specimens were collected before and 2, 4, 7, 14 and 21 days after start of treatment. Plasma samples were collected during 12 h after the first dose on day 1 and 1 sample was taken on day 7 for bioassay of cefixime concentration. Peak plasma concentration of cefixime occurred after about 4 h with a mean of 3.0 mg/l. The mean AUC0----oc after a single dose was estimated at 21.9 mg x h/l and the mean elimination half-life was 3.9 h. The mean plasma concentration of cefixime 3 h after the morning dose on day 7 was 2.0 mg/l. The concentrations of cefixime in faeces increased during treatment. One subject had detectable concentrations in faeces on day 2, three subjects on day 4 and 8 subjects on day 7 in the order of 237-912 mg/kg faeces. There was a marked decrease in the numbers of streptococci and Escherichia coli and an increase in the numbers of enterococci during the administration of cefixime. In the anaerobic microflora, the numbers of cocci, clostridia and bacteroides were suppressed while there were minor changes in the numbers of bifidobacteria. Clostridium difficile was isolated in 5 subjects on day 7 but cytotoxin was only detected in one subject. The intestinal microflora was normalized within 2 weeks after treatment had stopped. Slightly soft stools were reported by 7 subjects. One subject had abdominal pain and diarrhoea 1 week after treatment followed by anal irritation and itching.(ABSTRACT TRUNCATED AT 250 WORDS)
The new oral cephalosporins cefpodoxime, cefixime, cefdinir, cefetamet and ceftibuten demonstrate enhanced activity against Enterobacteriaceae susceptible to the established compounds as well (e.g. cefuroxime, cefaclor, cefadroxil). In addition, cefpodoxime, cefixime, cefdinir, cefetamet and ceftibuten include in their spectrum species hitherto resistant to oral cephalosporins (Proteus vulgaris, Providencia spp., Yersinia enterocolitica). Besides, the majority of these compounds demonstrate relevant activity (MIC50 equal to or below 2 mg/l) against Enterobacter spp., Citrobacter freundii, Serratia spp. and Morganella morganii. Ceftibuten is the most potent oral cephalosporin against most of the Enterobacteriaceae. Non-fermentative bacilli (Acinetobacter spp., Pseudomonas spp.) remain completely resistant to oral cephalosporins (except some Acinetobacter species against cefdinir and Pseudomonas cepacia against ceftibuten). Antistaphylococcal activity for oral cephalosporins is highest for cefdinir followed by BAY 3522, cefprozil, cefuroxime and cefpodoxime. Loracarbef, cefaclor and cefadroxil are about equally active, while the other compounds are only weakly active (cefixime) or inactive (cefetamet, ceftibuten). Enterococci are insensitive to new generation oral cephalosporins as they have been to established compounds. The most active oral cephalosporins against hemolytic streptococci are cefdinir and cefprozil. Streptococcus pneumoniae, Streptococcus milleri and Streptococcus mitior are most susceptible to cefpodoxime, cefdinir, cefuroxime and BAY 3522. Penicillin resistant pneumococci have to be regarded as resistant to all oral cephalosporins. Fastidious pathogens like Haemophilus spp., Moraxella catarrhalis and Neisseria gonorrhoeae are more susceptible to cefpodoxime, cefixime, cefdinir, cefetamet and ceftibuten than to the other oral cephalosporins. The activity of oral cephalosporins is only weak against Listeria spp., Helicobacter pylori and anaerobic pathogens (except BAY 3522). Bordetella pertussis remains resistant to all absorbable cephalosporins. Progress in antibacterial activity of oral cephalosporins was mainly achieved by cefpodoxime, cefixime, cefdinir, cefetamet and ceftibuten against Enterobacteriaceae and the fastidious pathogens and against staphylococci and the nonenterococcal streptococci by cefdinir, BAY 3522, cefprozil and cefpodoxime.