The influence of cefpodoxime proxetil (CPDX-PR, CS-807), a new oral cephalosporin, on the intestinal bacterial flora was studied in tetra-contaminated mice and in pediatric patients. CPDX-PR dry syrup was administered at a dose of 10 mg/kg once a day for 5 consecutive days to mice contaminated with 4 different species of bacteria: Escherichia coli, Enterococcus faecalis, Bacteroides fragilis and Bifidobacterium breve. No notable changes were observed in fecal viable cell counts except that slight decreases of E. coli counts were observed on the days 3 to 5 after starting administration. The subjects in the pediatric study were 5 children with infections, 3 boys and 2 girls at ages from 1 year 1 month to 6 years 10 months, with their body weights ranging from 9.3 to 23.8 kg. CPDX-PR dry syrup was administered at a dose between 3.0 to 3.7 mg/kg, 3 times a day for 4 to 7 days. Although some variations of the fecal bacterial flora were noticed between subjects during the administration of CPDX-PR, no notable changes were observed in major aerobic and anaerobic bacteria such as Enterobacteriaceae, Enterococcus, Bacteroides and Bifidobacterium in 4 of the 5 cases. Large decreases in Streptococcus, Enterobacteriaceae, Bifidobacterium, Eubacterium and anaerobic cocci and an increase in Enterococcus were observed in the other case. There was no case in which glucose non-fermenting Gram-negative rods and fungi became predominant. Regarding Enterobacteriaceae, transitory bacterial replacement was observed within the genus. Fecal concentration of CPDX during the administration of CPDX-PR was extremely low or below the detectable limit except one specimen from a case in which intestinal bacterial flora showed remarkable changes. From the above, CPDX-PR appears to be a drug with a relatively small influence on the intestinal bacterial flora.
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The purpose of this research was to assessment of antimicrobial activity and in vitro/in vivo evaluation of cefpodoxime proxetil extended-release (ER) tablet for once daily administration. The tablets were prepared using combination of biodegradable polysaccharides including hydroxypropyl methylcellulose and sodium alginate as matrix material to achieve pH-independent ER release. The tablets were found within the permissible limits for various physicochemical parameters. The in vitro drug release showed that the drug was released over a period of 24h in a sustained release manner. The drug release followed Higuchi kinetics as these plots showed the highest linearity (R(2)=0.9833), but a close relationship was also observed with zero-order kinetics (R(2)=0.9088) and the drug release mechanism was found to be of anomalous or non-Fickian type. Further, in vitro drug release was assessed by antimicrobial assay and it revealed that drug release through 24h periods was above the MIC. In vivo investigation in rabbits showed ER pharmacokinetic profile of cefpodoxime from the matrix tablets. A good correlation of drug absorption in vivo and drug release in vitro (R(2)=0.9785) was observed. These results suggested that the investigated CFP matrix tablets have a potential for extended-release dosage forms.
We studied the efficacy of antimicrobial agents against Staphylococcus aureus (S. aureus) and Streptococcus pyogenes (S. pyogenes) isolated from skin infections in 1992. For S. aureus, we measured the minimum inhibitory concentrations (MICs) of the following 10 drugs: methicillin (DMPPC), cefaclor (CCL), gentamicin (GM), erythromycin (EM), clindamycin (CLDM), minocycline (MINO), vancomycin (VAN), fusidic acid (FA), ofloxacin (OFLX) and nadifloxacin (NDFX); for S. pyogenes, we determined the MICs of the following 9 drugs: ampicillin (ABPC), amoxicillin (AMPC), cefpodoxime proxetil (CPDX-PR), erythromycin (EM), clindamycin (CLDM), minocycline (MINO), norfloxacin (NFLX), of loxacin (OFLX) and nadifloxacin (NDFX). These drugs are frequently used to treat skin infections, either systemically or topically. NDFX is a new synthetic fluoroquinolone, recently developed for use as a topical acne medication in Japan. It is used NDFX for acne, but not for skin infections. There were no strains of S. aureus resistant to NDFX, VAN or FA. The resistance (> or = 12.5 micrograms/ml) of S. aureus was highest to GM and lowest to OFLX. Four strains of methicillin-resistant (> or = 12.5 micrograms/ml) S. aureus (MRSA) were found. In contrast, no resistant strains of S. pyogenes were found except to MINO. Only two strains of S. pyogenes were susceptible to MINO. The sensitivity of S. pyogenes to ABPC, AMPC, CPDX-PR, EM and CLDM was very good. All the strains were susceptible at a MIC below > or = 0.05 microgram/ml. However, the S. pyogenes strains were not very sensitive to the new quinolones, especially NFLX. We concluded that penicillins, cephalosporins and macrolides are still effective against streptococcal infections.(ABSTRACT TRUNCATED AT 250 WORDS)
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In order to evaluate the clinical efficacy and tolerance of cefpodoxime proxetil, compared with that of amoxicillin in the treatment of acute bacterial maxillary sinusitis, a randomized, double-blind, parallel group comparative study was performed. A total of 286 adults patients were included at 12 centres, each treatment group consisting of 143 patients. Each patient was treated for 10 days and observed before and after treatment. The observations included clinical, roentgenological, bacteriological and laboratory examinations. At inclusion, the most common pathogens were Haemophilus influenzae (24%) and Streptococcus pneumoniae (17%). In the per protocol analysis, 117 patients in the cefpodoxime group and 113 in the amoxicillin group were evaluable for clinical efficacy. The clinical response rates were 96% and 91%, respectively. The corresponding figures in the intent-to-treat analysis were 130 and 128 patients, with clinical response rates of 93% and 88%, respectively. Cefpodoxime proxetil proved clinically as effective as amoxicillin in the treatment of acute bacterial maxillary sinusitis. It was more effective in eradicating H. influenzae and was more efficient in improving the radiological score. Adverse events were reported in 20% of cefpodoxime cases and in 16% of amoxicillin cases. There was no statistically significant difference between the groups.
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Data were evaluated with respect to in vitro activity, study design, clinical and microbiologic outcomes, and adverse drug reactions.
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The pharmacokinetics of the broad spectrum cephem RU 29 246 and its prodrug-ester HR 916 B were investigated in mice, rats and dogs and compared to those of cefpodoxime proxetil, cefuroxime axetil and cefixime. HR 916 B is well absorbed following oral administration and efficiently converted to the antibacterially active form. In mice, mean peak blood levels of 31.1 micrograms/ml of the parent compound were recorded within 20 minutes after oral administration of a single dose equivalent to 40 mg/kg RU 29 246. The bioavailability calculated on the basis of the areas under the concentration-time curves (AUC) and the urinary recoveries was about 90%. In rats, peak blood levels of 14.5 micrograms/ml were obtained 1 hour after an oral 20 mg/kg dose. The bioavailability was calculated as 70%. In dogs, 40% of an oral 10 mg/kg dose was recovered in the urine within 24 hours. Cmax was 15.9 micrograms/ml at 4.6 hours. Mean elimination half-lives of RU 29 246 were 0.35, 0.5 and 2.1 hours in mice, rats and dogs, respectively. After an oral HR 916 B dose equivalent to 50 mg/kg of RU 29 246, tissue concentrations at 0.5 hour ranged between 0.8 micrograms/g in brain and 95.7 micrograms/g in murine kidneys. These values of HR 916 B are similar to, or distinctly higher than, those of the reference compounds. Of the oral cephalosporins tested, HR 916 B had the most balanced antibacterial spectrum. With ED50s of between 0.9 and 11.5 mg/kg against staphylococci, its activity was similar to that of the additional reference compound cefaclor and higher than that of cefuroxime. Cefixime and cefpodoxime proxetil displayed low antistaphylococcal activity or were inactive. In septicemias with Enterobacteriaceae, cefixime and cefpodoxime proxetil were more potent than HR 916 B and cefaclor. Cefuroxime axetil was inactive against most of these infections. HR 916 B was also highly effective against murine lung infections caused by Klebsiella pneumoniae DT-S or Streptococcus pneumoniae 1147.
A multicenter study was conducted in which the in vitro activity of cefpodoxime (the active metabolite of the prodrug ester cefpodoxime proxetil) was compared with those of cefixime, cefuroxime, cefaclor, cefadroxil, and clarithromycin against 5556 recent clinical isolates. Cefpodoxime demonstrated potent activity against members of the Enterobacteriaceae, in particular against species generally resistant to the established oral cephalosporins such as Proteus vulgaris [minimum inhibitory concentration (MIC)50, 0.12 microgram/ml], Providencia rettgeri (MIC50, 0.015 microgram/ml), and Serratia marcescens (MIC50, 2 micrograms/ml). Cefpodoxime was very effective against the fastidious organisms most frequently associated with respiratory infections, such as Streptococcus pneumoniae (MIC90, 0.12 microgram/ml), Haemophilus influenzae (MIC90, 0.12 microgram/ml), and Moraxella catarrhalis (MIC90, 1 microgram/ml). In contrast to other orally administrated third-generation cephalosporins (cefixime or ceftibuten), cefpodoxime demonstrated reasonable activity against oxacillin-susceptible staphylococci, with MIC50 ranging from 1 to 2 micrograms/ml. All cephalosporins tested demonstrated poor activity against Pseudomonas spp., Xanthomonas spp., Enterococcus spp., and oxacillin-resistant staphylococci. Cefpodoxime had the widest spectrum of activity of all tested oral cephalosporins.
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From different hydrotropic agents, urea showed best aqueous solubility of cefpodoxime proxetil. The linearity was observed in the concentration range of 10-120 μg/ml. The method was validated and found to be precise. Accuracy (percent recovery) for cefpodoxime proxetil was found to be 99.82 ± 0.106.
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Penicillin (PC) resistance of Streptococcus pneumoniae was tested by oxacillin disk method (Bauer-Kirby method) of the strains collected at the primary pediatric office. The rate of oxacillin resistance of S. pneumoniae was 36.4% in 1990, 41.4% in 1991, and 51.9% in 1992, respectively. The efficacy of oral antibiotics in the treatment of PC-insensitive S. pneumoniae infections was also studied retrospectively in 234 cases. Treatment failure rate was 17.7% in the amoxicillin group, 8.7% in the cefpodoxime proxetil group, while it was 42.9% in the cefixime group. These differences were statistically significant. From these data prevalence of PC-insensitive S. pneumoniae is very high in Japanese children, and amoxicillin and cefpodoxime proxetil can be used for the treatment of outpatients with PC-insensitive S. pneumoniae infections.
Patients received either cefpodoxime proxetil oral suspension (10 mg/kg/day, once daily for 10 days) or cefixime oral suspension (8 mg/kg/day, once daily for 10 days).