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PubMed1988

Cefetamet pivoxil a new oral cephalosporin: clinical evaluation.

Cefetamet pivoxil, an oral cephalosporin, was given to 683 patients; 414 received standard antibiotics. 1.5 and 1.2 g of cefetamet pivoxil were fully effective in gonorrhea. In two trials in uncomplicated urinary tract infections (UTI) 2 g cefetamet as a single dose was significantly superior (93.3% cure) to 2 g cefadroxil (74.4% cure) and 90.8% vs. 74.7% cure. Results in complicated UTI with 2 g cefetamet for 10 days were 87.9% cure and 71.4% cure with cefadroxil. In acute exacerbation of chronic bronchitis 88% were cured with cefetamet (101 patients) and 80% with cefaclor (n = 94). In acute ear-nose-throat infections, the response rate was 89% and 93% with 1 or 2 g cefetamet per day, respectively. Adverse events were noticed in 6% of the 683 cefetamet-treated patients; they were rapidly reversible.

Administration, Oral↗

PubMed1982

Treatment of Group A streptococcal pharyngitis in children. Results of a prospective, randomized study of four antimicrobial agents.

Penicillin V, benzathine/procaine penicillin G, cefadroxil monohydrate, and erythromycin estolate were randomly assigned for therapy of group A streptococcal pharyngitis in 198 children. All patients improved with in 24 hours of initiating therapy. Reinfection with a new group A streptococcal serotype occurred in 13 patients, 12 developing 7 to 12 days after stopping therapy and 11 becoming symptomatic. Relapse with the same organism occurred in 16 patients, only 5 (31%) of whom were symptomatic. Antibody titer rises, antibiotic resistance of group A organisms, presence of penicillinase-producing staphylococci, and lack of compliance were not related to recurrent infections. There were no significant differences between the failure rates of the four test drugs: penicillin V, 12%; benzathine/procaine penicillin G, 12%; cefadroxil monohydrate, 5%; and erythromycin, 2%.

Adolescent↗

PubMed1989

Clinical experience with 1000 patients treated with cefetamet pivoxil.

Clinical studies have been carried out world-wide on cefetamet pivoxil, a new orally active cephalosporin. This paper reports on the first 1000 patients treated with the antibiotic; another 505 patients received standard antibiotics, mainly cefadroxil and cefaclor, for comparison. The results show that single doses of 1500 and 1200 mg cefetamet pivoxil were fully effective in gonorrhoea. Comparative trials in uncomplicated urinary tract infection indicate a significant superiority of a single dose of 2 g cefetamet pivoxil (n = 158; 90.0% cure) versus 2 g cefadrox (n = 162; 77.0% cure). In complicated urinary tract infections, a comparable outcome was achieved with a single daily dose of 2 g cefetamet pivoxil for 10 days (n = 99; 90% cure) and 1 g cefadroxil twice daily for 10 days (n = 98; 76.5% cure). The clinical response rate in acute exacerbation of chronic bronchitis was 89.4% in the group receiving cefetamet pivoxil (136 patients) and 83% in the cefaclor-treated group (n = 122). Treatment with 1000 or 2000 mg cefetamet pivoxil achieved a (bacteriological) success rate of 96% compared to 95% with cefaclor in acute ear, nose and throat-infections (n = 91). Overall, based on 894 isolated pathogens prior to therapy, the bacteriological response rate was 90% and it would appear that in vivo the spectrum of this cephalosporin covers a wide range of Gram-negative and Gram-positive pathogens, including urinary pathogens, but excluding Enterococci and Pseudomonas. Cefetamet pivoxil proved to be well tolerated. Mild to moderate adverse events were reported in 7.1% of patients but only 2 of the 1000 patients treated with cefetamet pivoxil were withdrawn because of diarrhoea, which subsided rapidly. There were no clinically relevant deviations in laboratory parameters.

Adult↗

PubMed1989

Biopharmaceutical evaluation of sustained-release ethylcellulose microcapsules containing amoxicillin using beagle dogs.

A beta-lactam antibiotic, amoxicillin, was microencapsulated with ethylcellulose using a solvent evaporation process in liquid paraffin containing sorbitan tristearate as a dispersing agent, and the microcapsules obtained showed first-order drug release. Usage of the previous log-log relationship of cefadroxil between in vitro dissolution half-lives (T50) and the experimental release rate constants (k'r) of the drug in vivo, and the nomogram for the design of satisfactory sustained-release preparations resulted in the prediction that ethylcellulose microcapsules containing 60% amoxicillin would show the most effective sustained-release pattern. Prepared microcapsules containing various amounts of amoxicillin were administered to beagle dogs and it was found that above prediction was correct. In addition, a more precise log-log correlation concerning amoxicillin was also undertaken, good linearity was observed and the decline was very similar to that of cefadroxil.

Amoxicillin↗

PubMed2003

[Active drug delivery by heterologous expression of membrane transporters].

The oligopeptide transporter PEPT1 is predominantly expressed in the brush-border membranes of small intestinal epithelial cells, where it plays pivotal roles in the efficient absorption of di-/tripeptides. PEPT1 has enormous potential as an oral drug delivery target, because it also mediates the intestinal absorption of peptide-mimetic and nonpeptide substrates. We demonstrated that the peptide derivation of amino acid-related drugs is applicable to improve their intestinal absorption. We have found that oligopeptide transport activity is also expressed in cancer cell lines. The tissue distribution of bestatin was significantly increased in solid tumors that overexpress PEPT1 in nude mice. Orally administered bestatin strongly suppressed tumor growth. These results provided the first demonstration of the tumor-selective delivery of a drug by specific transport activity. The absolute degree of PEPT1 mRNA expression in the small intestine was determined using real-time PCR in rats. Starvation of the animals increased the mRNA expression level profoundly in the upper small intestine. The longitudinal expression pattern was well correlated with the intestinal transport of cefadroxil in rats. We constructed a recombinant adenovirus vector encoding PEPT1 cDNA. Heterologous expression of PEPT1 in the liver was successfully achieved by simple intvavenous. Administration of the vector, resulting in increased liver distribution of [3H] carnosine. In situ perfusion of the brain with the vector doubled the brain distribution of cefadroxil. Heterologous expression of the drug transporter in vivo could be a useful approach for drug delivery.

Adenoviridae↗

PubMed1988

[Comparison of in vitro activity of 4 oral beta-lactams on microorganisms responsible for broncho-pulmonary infections in children].

MIC 90 and MBC 90 of amoxicillin, cefaclor, cefadroxil and cefuroxime axetil have been determined by the microdilution method against 48 organisms responsible of acute respiratory tract infections in children: 17 E. coli, 15 K. pneumoniae, 16 H. influenzae. An inoculum effect and an inhibitory index in blood and bronchial secretions were determined. An inoculum effect was more important for amoxicillin and cefadroxil than for cefuroxime axetil and cefaclor. Against H. influenzae, cefuroxime axetil and cefaclor have a similar activity. Against Enterobacteria, cefuroxime axetil has the lowest MIC 90 and MBC 90 and the highest inhibitory index.

Administration, Oral↗

PubMed1983

Antibacterial activity of nine oral antibiotics against Streptococcus pneumoniae, Haemophilus influenzae and Branhamella catarrhalis.

The efficacy of nine oral antibiotics were analyzed by the agar dilution method against clinical isolates consisting of 87 beta-lactamase positive and negative Haemophilus influenzae and Branhamella catarrhalis strains and 30 Streptococcus pneumoniae strains. The following drugs were tested: cefaclor, cefalexin, cefadroxil, cefradin, phenoxymethylpenicillin, ampicillin, amoxycillin, erythromycin and doxycycline. Inoculations of 10(4) bacteria/plate were made with a Steers inoculator on Mueller-Hinton agar containing 5% blood. Cefaclor was more effective than the other cefalosporins against all H. influenzae and B. catarrhalis strains, regardless of their beta-lactamase production. Cefaclor and cefradin were more effective than cefalexin and cefadroxil against S. pneumoniae strains. Cefaclor was less effective than erythromycin against pneumococci, B. catarrhalis and beta-lactamase positive H. influenzae strains and equally effective against beta-lactamase negative H. influenzae strains. Cefaclor was less active than doxycycline against the B. catarrhalis and H. influenzae strains and showed similar efficacy as doxycycline against pneumococci.

Anti-Bacterial Agents↗

PubMed1994

Noncompetitive inhibition of cephradine uptake by enalapril in rabbit intestinal brush-border membrane vesicles: an enalapril specific inhibitory binding site on the peptide carrier.

ACE inhibitors, as well as aminocephalosporins with peptide-like structures, are transported by the intestinal peptide carrier. We investigated the transport mechanism using intestinal brush-border membrane vesicles from rabbits and observed that enalapril, an angiotensin converting enzyme inhibitor and substrate of the peptide carrier, noncompetitively inhibited the uptake of cephradine, an aminocephalosporin and substrate of the peptide carrier, with an inhibition constant (Ki) of 2.6 mM when it was present on the cis side (outside) of the vesicles. By contrast, enalaprilat, cefadroxil and GlyPro competitively inhibited cephradine transport with Ki values of 5.4, 3.8 and 5.1, respectively. These results suggest the presence of an enalapril-specific inhibitory binding site on the peptide carrier. In addition, enalapril on the trans side (inside) of the vesicles inhibited the uptake of cephradine, suggesting an apparent reduction of carrier availability by a trapping mechanism. On the other hand, cefadroxil stimulated the uptake of cephradine in the trans experiment, consistent with the concept of countertransport. These findings reveal the uniqueness of enalapril regarding its mode of interaction with the peptide carrier(s) which has been of increasing interest regarding its role in the intestinal absorption of peptide-type drugs.

Animals↗

PubMed1996

Influence of cephalosporins on intestinal enzymatic activity.

The effect of the broad spectrum antibiotics cefaclor, cefadroxil, cephradine, cefatrizine, cephaloglycine and cefroxadine was examined on rat intestinal brush border enzymes, aminopeptidase N (E.C. 3.4.11-2), dipeptidyl peptidase IV (E.C. 3.4.14.5) and alkaline phosphatase (E.C. 1.3.1.3.). All the cephalosporins assayed -except cefaclor- inhibit the aminopeptidase N activity, in an uncompetitive manner. Cefatrizine showed the most important inhibitory effect (52.5%; p < 0.001). Cefaclor and cefadroxil have no effect on the activity of the dipeptidyl peptidase IV, while cephaloglycine and cephradine showed a non competitive type inhibition. In contrast, cefatrizine and cefroxadine showed a competitive inhibition for this enzyme. None of the cephalosporins assayed had any effect on alkaline phosphatase activity.

Administration, Oral↗

PubMed1997

Carrier-mediated transport of oligopeptides in the human fibrosarcoma cell line HT1080.

To explore the feasibility of targeting human tumor cells via their transport systems, dipeptide uptake was studied in the human fibrosarcoma cell line HT1080 and the human fibroblast cell line IMR-90 by the use of hydrolysis-resistant glycylsarcosine (Gly-Sar). The uptake of [14C]Gly-Sar into HT1080 was time dependent. Kinetic analysis of the concentration dependence of the initial rate of [14C]Gly-Sar uptake showed that a carrier-mediated transport system with a K(m) of 11.4 +/- 3.3 mM and V(max) of 26.8 +/- 4.0 (nmol/15 min/mg protein) and a nonsaturable component (k(d) of 0.80 microl/15 min/mg protein) were responsible for the dipeptide uptake by HT1080 cells. The optimal pH for the maximal uptake was around 6.0. [14C]Gly-Sar uptake was inhibited by various di- and tripeptides and peptide-mimetic drugs, such as bestatin and cefadroxil. [14C]Gly-Sar uptake was not affected by the presence of amino acids or tetra- or pentapeptides. The uptake of cefadroxil was reduced significantly by unlabeled Gly-Sar. Moreover, Gly-Gly and Gly-Leu produced an increase in the apparent K(m) of the uptake of Gly-Sar without altering V(max). On the other hand, dipeptide uptake by IMR-90, which is a normal diploid cell line (not malignant), showed no saturable transport. These results suggest that HT1080 cells take up dipeptides via a pH-dependent transporter. This is the first report showing that a dipeptide transport system, which is similar but not identical to the well-characterized oligopeptide transporters PepT1 and PepT2, exists in fibroblast-derived tumor cells but not in normal fibroblasts. The present finding could be the basis of a novel strategy for the specific delivery of oligopeptide-mimetic anticancer drugs into tumor cells.

Biological Transport↗

PubMed1989

Comparative antibacterial activity of the new cephalosporin cefcanel against anaerobic bacteria.

The activity of cefcanel against anaerobic cocci, Clostridium perfringens, Bacteroides fragilis, Bacteroides spp. and fusobacteria was determined by the agar dilution method and compared with the activity of cefaclor, cephalexin, cefadroxil, phenoxymethylpenicillin and ampicillin. Cefcanel showed good activity against Clostridium perfringens, Bacteroides spp. and fusobacteria (MIC90 = 1-4 mg/l). Against anaerobic cocci its MIC90 value was 16 mg/l, and against Bacteroides fragilis, 32 mg/l. Cefcanel has an antibacterial activity that warrants investigation in clinical trials.

Ampicillin↗

PubMed1986

Prevention of postoperative infection in cesarean section after rupture of the membranes.

Patients having a cesarean section more than 6 h after rupture of the membranes constitute a high risk group for postoperative infections. Two such groups were studied. Patients were given either cefuroxime 1.5 g every 8th hour for 24 h followed by cefadroxil 0.5 g twice daily for 6 days or received no medication. The infection rate was significantly reduced in the treatment group as compared to the control group (15% vs. 48%). Non-infected patients had a significantly shorter stay in hospital (8 days vs. 12 days). Combined use of these drugs for prevention of post-cesarean infection has not previously been reported. No side effects of the antibiotic prophylaxis were reported.

Cefadroxil↗

PubMed1996

Predictive strategy for the rapid structure elucidation of drug degradants.

Structural information on drug degradants and impurities can serve to accelerate the drug discovery and development cycle. Traditional structure elucidation methodologies for obtaining this information are often slow and resource-consuming; therefore, LC/MS profiling and LC/MS/MS substructural analysis methodologies have been developed to rapidly and accurately elucidate structures of impurities and degradants. This work is a further development of methodologies used for the elucidation of degradation products of paclitaxel [K.J. Volk et al., Proc. 9th AAPS Ann. Meeting, 1994, p.29]. In this study cefadroxil was used as a model compound for the evaluation of a predictive strategy for the production and elucidation of impurities and degradants induced by acid, base, and heat, using LC/MS and LC/MS/MS profiling methodology, resulting in an LC/MS degradant database which includes information on molecular structures, chromatographic behavior, molecular weight, UV data, and MS/MS substructural information. Furthermore, libraries such as this can provide a predictive foundation for pre-clinical development work involving drug stability, synthesis, and monitoring.

Cefadroxil↗

PubMed1988

Antimicrobial activity of MDL 19,592: an oral cephalosporin.

MDL 19,592, a semisynthetic oral cephalosporin, has an antimicrobial spectrum principally directed against Gram-positive cocci (MIC50, 0.25-4 micrograms/ml), Branhamella catarrhalis (MIC50, 1-2 micrograms/ml), and pathogenic Neisseria spp. such as meningococci (MIC50, 4 micrograms/ml). Enterobacteriaceae, enterococci, Pseudomonas spp., Corynebacterium jeikeium, and Acinetobacter calcoaceticus strains had MDL 19,592 MIC50 of greater than or equal to 32 micrograms/ml. Although MDL 19,592 generally had a spectrum most similar to cefadroxil, it could not be represented by the cephalothin susceptibility test because of low predictive values and MIC correlations.

Acinetobacter↗

PubMed1992

Cefdinir (FK482), an orally administered cephalosporin in vitro activity comparison against recent clinical isolates from five medical centers and determination of MIC quality control guidelines.

Cefdinir, a new oral cephalosporin, was compared to cefaclor, cefadroxil, cefixime, and cefuroxime against greater than 5000 recent aerobic clinical isolates. This multicenter study revealed broad-spectrum cefdinir activity against all Enterobacteriaceae (MIC50s, 0.06-2 micrograms/ml) except Enterobacter cloacae, Morganella morganii, Proteus vulgaris, and Serratia marcescens (MIC50s, greater than or equal to 4 micrograms/ml). Oxacillin-susceptible staphylococci (MIC90s, 0.5-2 micrograms/ml), beta-hemolytic Streptococcus group B (MIC90, 0.06 micrograms/ml), and Acinetobacter lwoffii were also susceptible to cefdinir. The activity of cefdinir was similar to that of cefixime and cefuroxime against Gram-negative organisms and superior to all tested oral cephems when tested against Gram-positive cocci. None of the cephalosporins were active against oxacillin-resistant Staphylococcus spp., enterococci, Pseudomonas spp., or Xanthomonas maltophilia. MIC quality control range guidelines were established for the strains recommended by the National Committee for Clinical Laboratory Standards documents.

Anti-Bacterial Agents↗

PubMed2005

A sensitive assay of amoxicillin in mouse serum and broncho-alveolar lavage fluid by liquid-liquid extraction and reversed-phase HPLC.

A sensitive and simple high-performance liquid chromatography (HPLC) method was developed and validated for the analysis of amoxicillin in mouse serum and broncho-alveolar lavage (BAL) fluid. One hundred microlitres of sample were needed for the assay. Sample processing was carried out with liquid-liquid extraction. Cefadroxil was used as an internal standard. The chromatographic separation was achieved on a C18 reversed-phase column with a mobile phase consisting of phosphate buffer, 1-octanesulphonic acid sodium salt and acetonitrile. The detection was conducted at 210 nm. The ranges of the standard curves were 0.2-20 and 0.05-5 microg/ml for serum and BAL samples, respectively. The recoveries of amoxicillin from serum and normal saline were 87 and 88%, respectively. The coefficients of variation were 1.78-6.13% for intra-day and 0.82-6.42% for inter-day analyses. The accuracy was within 100+/-6%. This method was successfully applied to analyze amoxicillin in mouse serum and BAL samples from a pharmacokinetic study.

Amoxicillin↗

PubMed2002

Interaction of human organic anion transporters with various cephalosporin antibiotics.

Cephalosporin antibiotics are thought to be excreted into the urine via organic anion transporters (OATs). The purpose of this study was to elucidate the interaction of human-OATs with various cephalosporin antibiotics, using proximal tubule cells stably expressing human-OAT1, human-OAT3 and human-OAT4. Human-OAT1 and human-OAT3 are localized to the basolateral side of the proximal tubule, whereas human-OAT4 is localized to the apical side. The cephalosporin antibiotics tested were cephalothin, cefoperazone, cefazolin, ceftriaxone, cephaloridine, cefotaxime, cefadroxil and cefamandole. All of these cephalosporin antibiotics significantly inhibited organic anion uptake mediated by human-OAT1, human-OAT3 and human-OAT4. Kinetic analysis revealed that these inhibitions were competitive. The inhibition constant (K(i)) values of cefoperazone, cefazolin, ceftriaxone and cephaloridine for human-OAT1 were much lower than those for human-OAT3 and human-OAT4, whereas the K(i) values of cephalothin and cefotaxime for human-OAT3 were much lower than those for human-OAT1 and human-OAT4. Human-OAT4 mediated the bidirectional transport of estrone sulfate, an optimal substrate for human-OAT4. These results suggest that human-OAT1, human-OAT3 and human-OAT4 interact with various cephalosporin antibiotics, and that human-OAT1 and human-OAT3 play a distinct role in the basolateral uptake of cephalosporin antibiotics. Since the K(i) value of cephaloridine for human-OAT4-mediated organic uptake was much higher than that for human-OAT1, the results indicate the possibility that human-OAT4 limits the efflux of cephaloridine, leading to the accumulation of cephaloridine and the induction of nephrotoxicity.

Animals↗

PubMed2003

Interaction of human and rat organic anion transporter 2 with various cephalosporin antibiotics.

Cephalosporin antibiotics are thought to be excreted into the urine via organic anion transporters (OATs) and OAT can mediate nephrotoxicity by cephalosporins, particularly by cephaloridine. The purpose of this study was to elucidate the interaction of human-OAT2 and rat-OAT2 with cephalosporin antibiotics using proximal tubule cells stably expressing human-OAT2 and rat-OAT2. Human-OAT2 is localized to the basolateral side of the proximal tubule, whereas rat-OAT2 is localized to the apical side of the proximal tubule. Cephalosporins tested were cephalothin, cefoperazone, cefazolin, ceftriaxone, cephaloridine, cefotaxime, cefadroxil and cefamandole. These cephalosporins dose-dependently inhibited organic anion uptake mediated by human-OAT2 and rat-OAT2. There was no species difference observed for the effects of OAT2 with cephalosporins between human and rat transporters. Kinetic analysis revealed that the inhibitory effects for human-OAT2 were competitive. Cephaloridine significantly decreased the viability of cells stably expressing human-OAT2, human-OAT1, human-OAT3 and human-OAT4. The decreased viability of cells stably expressing human-OAT1, human-OAT3 and human-OAT4 but not human-OAT2 was reversed by probenecid. In conclusion, human-OAT2 interacts with cephalosporins, and thus, human-OAT2 may mediate the uptake of cephalosporins on the basolateral side of the proximal tubule. The interaction of human-OAT2 with cephalosporins was the weakest among the basolateral human-OATs tested. In addition, it is suggested that human-OATs mediate cephaloridine-induced nephrotoxicity.

Animals↗