Cefcapene

Abstract: Background and objective: Respiratory tract infection is a serious complication associated with bronchoscopic biopsy. This study attempted to examine its incidence and determine an efficacious therapy for preventing such infections. Methods: Nine hundred and thirty patients who underwent bronchoscopic biopsy in Osaka City University Hospital outpatient clinic were enrolled in the study. All patients were randomly assigned to receive a 3-day course of azithromycin (500 mg/day), cefcapene pivoxil hydrochloride (300 mg/day) or no antibiotics. The primary outcome was the incidence of respiratory tract infection after bronchoscopic biopsy among the three groups. Results: In the no-treatment group, nine of the 310 patients (2.9%) had respiratory tract infection after bronchoscopic biopsy. All patients with infection had abnormal bronchoscopic findings. Of the patients with respiratory tract infection, 60% were in the no-treatment group, 26.7% in the cefcapene group and 13.3% in the azithromycin group. Although not statistically significant, the incidence in the azithromycin group (0.7%) was lower than in the no-treatment group (P = 0.06). Among the patients with abnormal bronchoscopic findings, the incidence in the azithromycin group was significantly lower than that in the no-treatment group (3.0% vs. 14.8%; P = 0.02). Moreover, maximum C-reactive protein values also appeared to be lower in the azithromycin group than in the no-treatment group and the cefcapene group. Conclusions: A 3-day course of azithromycin administration is well tolerated and effective in preventing infection post bronchoscopy.

Abstract: Cefcapene pivoxil monohydrochloride monohydrate, a broad spectrum third-generation cephalosporin for oral administration, was prepared by reacting three centers of 7β-amino-3-(hydroxymethyl)cephalosporinic acid (7-HACA), derived from 7β-aminocephalosporanic acid. The coupling of 7-HACA and (Z)-2-[2-(Boc-amino)thiazol-4-yl]pent-2-enoic acid, followed by carbamylation with chlorosulfonyl isocyanate, and precipitation with diisopropylamine gave the key intermediate, in which thiazole side chain and carbamoyl group had been introduced into the 7-amino and 3-hydroxymethyl groups of 7-HACA, respectively, in a continuous procedure. Afterwards, the intermediate was esterified with pivaloyloxymethyl iodide to complete the modification of the C4 carboxy group affording Boc-cefcapene pivoxil, from which the desired product was finally obtained by an economical Boc removal and successive formation of the hydrochloride in 36% overall yield on a decagram scale. This synthesis promises an easy entry to cefcapene pivoxil monohydrochloride monohydrate with convenient manipulation, simple isolation, and good yields; it is of potential value for production on an industrial scale.

Abstract: Periapical periodontitis usually results from microbial infection, with these microorganisms occasionally migrating to the root canal, which can lead to further, potentially life-threatening, complications. Here, the susceptibility of 27 bacterial strains to various antimicrobial agents was evaluated. These strains comprised 13 species; 16 of the strains were clinical isolates from periapical lesions. Each strain was inoculated onto blood agar plates containing one of the antimicrobial agents. The plates were incubated anaerobically at 37°C for 96 hr and the minimal inhibitory concentrations (MICs) determined. Ten strains required an MIC of 32 μg/ml or greater for amoxicillin, 6 for cefmetazole, and 5 for cefcapene among β-lactam antibiotics; 8 strains required an MIC of 32 μg/ml or greater for clindamycin, 4 for azithromycin, and 11 for clarithromycin among macrolide antibiotics; 3 strains required an MIC of 32 μg/ml or greater for ciprofloxacin and 2 for ofloxacin among fluoroquinolones. The effect of cefcapene on 5 strains was evaluated after biofilm formation to investigate the relationship between biofilm formation and susceptibility. All strains showed a decrease in susceptibility after biofilm formation. The results revealed that several antimicrobial agents commonly used in a clinical setting, including amoxicillin, cefmetazole, and clindamycin, are potentially effective in the treatment of orofacial odontogenic infections. The development of resistant strains, however, means that this can no longer be guaranteed. In addition, azithromycin, ciprofloxacin, and ofloxacin were more effective than the 3 β-lactam antibiotics tested. These results suggest that sensitivity testing is needed if odontogenic infections are to be treated safely and effectively.

Abstract: We compared the in vitro antibacterial activity of DU-6681a against Gram-positive and Gram-negative bacteria with that of R-95867, faropenem and oral cephalosporins such as cefcapene, cefotiam and cefpodoxime. DU-6681a is an active form of the new oral carbapenem compound DZ-2640, which is an ester-type prodrug, and R-95867 is an active form of the oral carbapenem CS-834. Against most Gram-positive bacteria, DU-6681a was as active as or two- to 16-fold more potent than R-95867 and faropenem in terms of MIC 90 , and comparable to or two- to 64-fold more effective than the cephalosporins. Against most Gram-negative bacteria, the activity of DU-6681a was the same as or two- to 16-fold more potent than that of R-95867, and comparable to or two- to 2048-fold higher than that of faropenem and the cephalosporins.