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PubMed2005

Human organic anion transporter hOAT3 is a potent transporter of cephalosporin antibiotics, in comparison with hOAT1.

We examined the substrate specificity of human organic anion transporter (hOAT) 1 and hOAT3 for various cephalosporin antibiotics, cephaloridine, cefdinir, cefotiam, ceftibuten, cefaclor, ceftizoxime, cefoselis and cefazolin by using HEK293 cells stably transfected with hOAT1 or hOAT3 cDNA (HEK-hOAT1, HEK-hOAT3). Additionally, we examined the uptake of various compounds by these transfectants. The mRNA level of hOAT3 in HEK-hOAT3 was about three-fold that of hOAT1 in HEK-hOAT1. Functional expression of hOAT1 and hOAT3 was confirmed by the uptake of p-[14C]aminohippurate and [3H]estrone sulfate, respectively. p-[14C]Aminohippurate, [3H]estrone sulfate, [14C]captopril, [3H]methotrexate, [3H]ochratoxin A, [3H]leucovorin and [3H]cimetidine were shown to be substrates for hOAT1 and hOAT3, and [3H]dehydroepiandrosterone sulfate was shown to be a substrate for hOAT3. All cephalosporin anitibiotics tested were shown to inhibit the uptake of p-[14C]aminohippurate and [3H]estrone sulfate via hOAT1 and hOAT3, respectively, in a dose-dependent manner, and the IC50 values of these antibiotics, except for cefaclor, for the hOAT1-mediated uptake of p-[14C]aminohippurate were within four-fold of those for the hOAT3-mediated uptake of [3H]estrone sulfate. The uptake of cephaloridine, cefdinir and cefotiam by HEK-hOAT3 was 35-50-fold greater than that by control cells. Moreover, the accumulation of the other cephalolsporin antibiotics was significantly greater in HEK-hOAT3 than in control cells. In contrast, the uptake of these antibiotics by HEK-hOAT1 was within two-fold of that by control cells. In conclusion, hOAT3 plays a more important role than hOAT1 in the renal secretion of cephalosporin antibiotics.

Anti-Bacterial Agents↗
PubMed2004

Synthesis and antimicrobial activity of new 7 beta-(benzo[a]dihydrocarbazolyloxyacetyl)-substituted cephalosporins.

Selected 7beta-(benzo[a]dihydrocarbazolyloxyacetyl)-substituted cephalosporins (1a-e) were synthesised and tested for their antimicrobial activity against Gram-positive and Gram-negative clinical pathogens. All compounds synthesised (1a-e) showed an in vitro antimicrobial activity similar to that of ceftriaxone and cefpirome against the Gram-positive bacteria, and superior to that of penicillin and cefaclor against pen-R Staphylococcus aureus species. Like all beta-lactam agents, compounds 1a-e were in an inactive Minimum Inhibitory Concentration (MIC > 32 microg/ml) against methicillin-resistant S. aureus species. Furthermore, as expected, no cross-resistance was observed against the erythromycin-resistant Staphylococcus pyogenes strain. Finally, it is worth underlining that compounds 1a and 1e showed a similar activity to that of ceftriaxone and superior to cefaclor against penicillin-resistant Streptococcus pneumoniae isolates, a key respiratory tract infection (RTI) causing pathogen difficult to treat with currently marketed antibiotics.

Anti-Bacterial Agents↗
PubMed2004

Antimicrobial resistance of Streptococcus pneumoniae and Haemophilus influenzae isolated from children with community-acquired respiratory tract infections in Central Poland.

Resistance to commonly used antimicrobial agents among the key respiratory pathogens is increasing worldwide and therefore a rational choice of an empirical treatment requires knowledge of both global and local resistance patterns. The susceptibility of 185 Streptococcus pneumoniae and 169 Haemophilus influenzae isolates collected from January 1999 to May 2002 at the Children's Memorial Health Institute, Warsaw, Poland, from 351 children with community-acquired respiratory tract infections (RTIs) has been determined. Of S. pneumoniae isolates, 84% were susceptible to penicillin, 91% to cefaclor, 95% to cefuroxime, 98% to cefotaxime, 79% to erythromycin, 46% to co-trimoxazole, 82% to clindamycin and 59% to tetracycline. The majority (83%) of erythromycin-resistant isolates tested carried the erm(B) gene, conferring the MLS(B) phenotype. All tetracycline-resistant S. pneumoniae strains analysed were tet(M) positive and tet(O) negative. A total of 24% of H. influenzae isolates were beta-lactamase-positive. H. influenzae susceptibility to amoxicillin/clavulanate, cefaclor, cefuroxime, azithromycin, tetracycline and co-trimoxazole was 100, 89, 94, 96, 96 and 43%, respectively.

Anti-Bacterial Agents↗
PubMed2000

Optimization of separation and migration behavior of cephalosporins in capillary zone electrophoresis.

The influences of buffer pH, buffer concentration and buffer electrolyte on the migration behavior and separation of 12 cephalosporin antibiotics in capillary zone electrophoresis using three different types of buffer electrolyte, including phosphate, citrate, and 2-(N-morpholino)ethanesulfonate (MES), were investigated. The results indicate that, although buffer pH is a crucial parameter, buffer concentration also plays an important role in the separation of cephalosporins, particularly when cefuroxime and cefazolin, cephalexin and cefaclor, or cefotaxime and cephapirin are present as analytes at the same time. The electrophoretic mobility of cephalosporins and electroosmotic mobility measured in citrate and MES buffers are remarkably different from those measured in phosphate buffer. With citrate buffer, optimum buffer concentration is confined to a small range (35-40 mM), whereas buffer concentrations up to 300 mM can be used with MES buffer. Complete separations of 12 cephalosporins could be satisfactorily achieved with these three buffers under various optimum conditions. However, the separability of 12 cephalosporins with citrate or MES buffer is better than that with phosphate buffer. As a consequence of a greater electrophoretic mobility of cephalosporins than the electroosmotic mobility with citrate buffer at pH below about 5, some cephalosporins are not detectable. The cloudiness of the peak identification and of the magnitudes of the electrophoretic mobility of cefotaxime and cefuroxime reported previously are clarified. In addition, the pKa values of cephradine, cephalexin, cefaclor, and cephapirin attributed to the deprotonation of either an amino group or a pyridinium group are reported, and the migration behavior of these cephalosporins in the pH range studied is quantitatively described.

Alkanesulfonic Acids↗
PubMed1999

Compliance of pediatric patients with treatment involving antibiotic suspensions: a pilot study.

In collaboration with 11 German pediatricians in private practice, this pilot study assessed the treatment compliance of 289 pediatric patients (56.1% male: mean age, 53.9+/-35.6 months) who were given antibiotic suspensions (selection and duration determined by the pediatrician) to treat the following bacterial infections: acute otitis media, 34.6%; group A streptococcal tonsillopharyngitis/scarlet fever, 28.7%; lower respiratory tract infection, 18.3%; sinusitis/sinobronchitis, 9.3%; and other infections, 9.0%. The most frequently used antibiotics were amoxicillin (26.3%), erythromycin estolate (19.0%), penicillin V benzathine (14.2%), and cefaclor (13.5%). Compliance was assessed by means of a standardized telephone interview and a urine test that detects antibacterial activity using a Bacillus subtilis spore suspension. Overall compliance (positive urine test result at the end of the planned treatment period) was 79.6% (230 of 289 patients). Compliance was highest with erythromycin estolate (94.5%), followed by penicillin V benzathine (85.4%), cefaclor (76.9%), and amoxicillin (71.1%). Good compliance was also significantly associated with a patient age of > or =3 years and a treatment duration of > or =7 days. Compliance was not significantly influenced by the underlying bacterial infection. In summary, 20.4% of patients were noncompliant when treated with antibiotic suspensions.

Anti-Bacterial Agents↗
PubMed2003

[Sensitivity of Haemophilus influenzae isolates in Spain to 17 oral antibiotics].

INTRODUCTION: The objective of this study was to assess the sensitivity of 400 strains of Haemophilus influenzae isolated in 21 Spanish laboratories in 1999 to 17 oral antibiotics.Methods. An agar dilution method in HT medium was used for sensitivity testing; interpretation of the results followed NCCLS criteria. RESULTS: Percentages of isolates susceptible to the antibiotics tested were as follows: ampicillin 59.5%, amoxicillin/clavulanate 99.2%, loracarbef 66.2%, cefprozil 70.2%, cefaclor 76.2%, cefuroxime 95%, ceftibuten 100%, cefpodoxime 100%, cefixime 100%, rifampin 99.8%, tetracycline 98.2%, chloramphenicol 99.2%, nalidixic acid 97.5%, ciprofloxacin 100%, trovafloxacin 100%, clarithromycin 74%, and azithromycin 100%. CONCLUSIONS: Geographic distribution of sensitivity rates was not homogeneous for some antibiotics. Around 24% of strains were betalactamase producers, requiring higher MICs of antibiotics such as loracarbef, cefprozil and cefaclor than non betalactamase producers. Nevertheless MICs of ceftibuten, cefpodoxime and cefixime were similar in both betalactamase producers and non-producers. Five strains (1.25%) were beta -lactamase (2), but resistant to ampicillin (MIC > or = 8 mg/L) and to amoxicillin/clavulanic acid (MIC > or = 4/2 mg/L). Only three strains showed intermediate sensitivity to chloramphenicol. These strains and four others were inhibited with > or = 4 mg/L of tetracycline. Only one strain was resistant to tetracycline (MIC: 64 mg/L) and to rifampin (MIC: 256 mg/L). All strains were sensitive to azithromycin (MICs < or = 4 mg/L) and all were sensitive to ciprofloxacin and trovafloxacin (MICs < or = 0.5 mg/L). However, ten strains (2.5%) were resistant to nalidixic acid (MIC > or = 4 mg/L).

Administration, Oral↗
PubMed1997

A 1994-95 survey of Haemophilus influenzae susceptibility to ten orally administered agents. A 187 clinical laboratory center sample in the United States.

During August, 1994 to April, 1995, a total of 2278 clinical isolates of Haemophilus influenzae were obtained from 187 clinical laboratories in the United States (U.S.). The vast majority of these isolates (75%) were from respiratory sites, and the remaining organisms were from blood, ear, eye, and spinal fluid sources. The overall rate of beta-lactamase production and ampicillin resistance was 36%. The antimicrobial susceptibility of isolates was determined by reference broth microdilution testing against ten orally administered agents. MIC values were compared according to 12 geographical regions, inpatient or outpatient status, gender, and eight age groupings. Modest and occasionally significant differences were observed: 1) greater numbers of beta-lactamase-producing strains among outpatients, in males, in the mid-Atlantic region, and in children < or = 12 years of age; 2) lower prevalence of beta-lactamase-producing isolates in the Southeast and Pacific regions; 3) cefaclor, cefprozil, and loracarbef activity was lowest among the younger children (< or = six years); and 4) macrolide in vitro efficacy was lowest in patients > 50 years of age and in three eastern regions. Overall, more than 99% of the strains were susceptible to amoxicillin/clavulanic acid, cefixime, and cefpodoxime (e.g., widest potential clinical use). Susceptibilities using National Committee for Clinical Laboratory Standards (NCCLS) breakpoint criteria for the other agents were: 96.6% to cefuroxime, 86.5% to loracarbef, 84.0% to clarithromycin, 81.8% to cefaclor, and 80.7% to cefprozil. Non-beta-lactamase mechanisms of resistance to ampicillin were rare (0.2%) or episodic and were attributed to altered penicillin-binding proteins. Although there is an increased prevalence of beta-lactamase production among H. influenzae isolates compared to prior years, four beta-lactams remain highly active (> 95% susceptibility) against contemporary strains of H. influenzae. Other monitored compounds seem to have declined in spectrum and surveillance trials for resistance among H. influenzae isolates should continue in an effort to identify trends in the U.S.

Adult↗
PubMed2001

Antimicrobial susceptibility of nasopharyngeal isolates of Haemophilus influenzae from healthy children in day-care centres: results of multicentre study in Russia.

Resistance of Haemophilus influenzae from clinical isolates can be predicted on the basis of results of antimicrobial susceptibility of nasopharyngeal isolates. The carriage rate and the antimicrobial susceptibility of H. influenzae isolated in healthy children attending day-care centres in Moscow, Smolensk and Yartsevo was studied. The susceptibility of ampicillin, amoxycillin/clavulanate, cefaclor, erythromycin, roxithromycin, clarithromycin and trimethoprim-sulphamethoxazole were determined by the E-test. The mean carriage rate of H. influenzae was 44%. Resistance of H. influenzae to ampicillin was 2.3%, to amoxycillin/clavulanate 0.7%, to cefaclor 0.7%, to clarithromycin 18.7% and to trimethoprim-sulphamethoxazole 21%. These included strains that showed intermediate-resistance. The antimicrobial resistance profiles varied in different centres. The clinical use of trimethoprim-sulphamethoxazole should be restricted because of the high resistance of H. influenzae to antifolate compounds.

Anti-Bacterial Agents↗
PubMed2003

Antimicrobial resistance in Gram-negative bacteria from Intensive Care Units and Urology Services. A nationwide study in The Netherlands 1995-2000.

A nationwide 6-year surveillance of resistance in Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and Pseudomonas aeruginosa from clinical specimens of patients from ten Intensive Care Units and ten Urology Services was started in 1995. MICs of amoxycillin, amoxycillin/clavulanate, trimethoprim, cotrimoxazole, norfloxacin, ciprofloxacin, cefaclor, ceftazidime, imipenem and gentamicin were determined by broth microdilution. Intensive Care Units had higher resistance levels of amoxycillin/clavulanate, cefaclor and ceftazidime (P<0.005) and lower resistance levels of nitrofurantoin, trimethoprim, cotrimoxazole and quinolones (P<0.01) than Urology Services. Changes in MIC distributions in time and development of resistant clusters were observed for nitrofurantoin (E. coli), amoxycillin (E. coli, P. mirabilis), amoxycillin/clavulanate (E. coli) and for quinolones (E. coli). The overall resistance level of ceftazidime and gentamicin was <5%, but this fluctuated with the appearance and disappearance of resistant clones in some Intensive Care Units. Quinolone resistance among P. aeruginosa from Intensive Care Units fluctuated between 7 and 14%.

Anti-Bacterial Agents↗
PubMed1999

A 1997-1998 national surveillance study: Moraxella catarrhalis and Haemophilus influenzae antimicrobial resistance in 34 US institutions.

From November 1, 1997 to April 30, 1998, 726 Moraxella catarrhalis isolates and 1529 Haemophilus influenzae isolates were obtained from 34 medical centres throughout the United States. Rates of beta-lactamase production were 94.6% among M. catarrhalis and 31.1% among H. influenzae strains. Susceptibility rates of M. catarrhalis isolates to selected antimicrobial agents were greater than 99% for amoxycillin-clavulanate, cefixime, cefpodoxime, cefuroxime, cefaclor, loracarbef, clarithromycin, azithromycin, chloramphenicol and tetracycline, 97.8% for cefprozil, 50.4% for trimethoprim-sulphamethoxazole and 28.1% for ampicillin. Of the antimicrobials tested against H. influenzae, the only agents with susceptibility rates below 96% were loracarbef (87.6%), cefprozil (83.4%), cefaclor (82.7%), trimethoprim-sulphamethoxazole (67.3%) and ampicillin (64.7%). The clarithromycin susceptibility rate was 67.4% but this agent was not tested in the presence of its 14-OH metabolite.

Adolescent↗
PubMed2000

Susceptibility of Polish clinical strains of Yersinia enterocolitica serotype O3 to antibiotics.

A total of 199 clinical strains of Yersinia enterocolitica serotype O3, biotype 4 were tested for their susceptibility to antibiotics (158 strains carried the virulence plasmid pYV and 41 strains did not). A total of 114 isolates were tested by a standard disk diffusion method for 21 antibiotics. Almost all strains tested were resistant to ampicillin and cefazolin and susceptible to amoxycillin/clavulanate, cefaclor, cefamandole, cefuroxime, cefotaxime, ceftriaxone, aztreonam, imipenem, gentamicin, amikacin, netilmicin, tetracycline, doxycycline, chloramphenicol, ciprofloxacin, sulphamethoxazole, trimethoprim, co-trimoxazole and furazolidone. In addition, minimal inhibitory concentrations of 15 antibiotics were determined by the agar dilution method for all 199 strains (158 carrying plasmid pYV and 41 strains that did not). Third-generation cephalosporins such as cefotaxime and ceftriaxone and a fluoroquinolone (ciprofloxacin) were the most active antimicrobial agents tested followed by aztreonam, imipenem, trimethoprim, tetracycline, gentamicin, chloramphenicol, amoxycillin/clavulanate, cefaclor, cefuroxime, amikacin, furazolidone and sulphamethoxazole. The present study demonstrated a high susceptibility of clinical strains of Y. enterocolitica to most of the tested antibiotics. In general there was no significant difference between susceptibility to antibacterial agents of strains with or without plasmid pYV.

Drug Resistance, Microbial↗
PubMed1989

Transport characteristics of ceftibuten, a new oral cephem, in rat intestinal brush-border membrane vesicles: relationship to oligopeptide and amino beta-lactam transport.

Ceftibuten undergoes H+-coupled uphill transport across rat small intestinal brush-border membrane vesicles. The effects of amino acids, peptides, folate, and beta-lactams on the uptake of ceftibuten were examined. Uptake of ceftibuten was competitively inhibited by dipeptides or tripeptides. A counter-transport effect on ceftibuten uptake was observed in the vesicle preloaded with these peptides, and the transport was temporarily against a concentration gradient (overshooting). On the other hand, ceftibuten uptake was not changed by amino acids and a tetrapeptide. Therefore, ceftibuten is predominantly transported via the oligopeptide transport system in the brush-border membranes. The relationship of ceftibuten transport to folate and other oral antibiotics was also investigated. Cyclacillin, cephradine, and cefadroxil exhibited both inhibitory and countertransport effects, but folate, cefaclor, and cephalexin showed only a slight inhibitory effect. As the transport of cefaclor showed no uphill uptake in the presence of a H+ gradient and its H+ stimulated uptake was small, a H+ gradient-independent carrier-mediated system seems to participate in its transport. These findings suggest that two different carrier-mediated transport systems, H+ gradient dependent and independent, may exist for oral cephems.

Amino Acids↗
PubMed1989

Transport characteristics of ceftibuten (7432-S), a new oral cephem, in rat intestinal brush-border membrane vesicles: proton-coupled and stereoselective transport of ceftibuten.

The transport characteristics of ceftibuten in rat intestinal brush-border membrane vesicles were investigated by a rapid filtration technique. Ceftibuten uptake was markedly stimulated by an inwardly directed H+ gradient (pH 7.5 inside, pH 5.5 outside) in comparison with that in the absence of a H+ gradient. The uptake at 30 sec was four times greater than that observed at equilibrium (overshoot phenomenon), while the H+ gradient-stimulated uptake of ceftibuten was markedly reduced in the presence of FCCP, a protonophore. These results suggested H+-coupled uphill transport of ceftibuten. In contrast, an inwardly directed Na+ gradient had no effect on ceftibuten uptake. The valinomycin-induced K+ diffusion potential (inside positive) significantly stimulated the ceftibuten uptake, suggesting net transfer of the negative charge. In contrast to the cis-isomer ceftibuten, the trans isomer of ceftibuten is not readily absorbed from the intestine, and its uptake was found not to be affected by a H+ gradient. Since the lipophilicity of the trans isomer is similar to that of ceftibuten, the uptake process appears to be stereoselective. The initial uptake of ceftibuten and its analogue cefaclor was concentration dependent under a H+ gradient. The apparent Km value was 0.2 mM for ceftibuten and 3.0 mM for cefaclor.

4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid↗
PubMed2003

Thrombotic thrombocytopenic purpura after cephalosporin administration: a possible relationship.

BACKGROUND: Acquired thrombotic thrombocytopenic purpura (TTP) is an autoimmune disorder. The pathogenesis is believed to be mediated by an autoantibody directed against the metalloproteinase responsible for the degradation of the very-high-molecular-weight multimers of the vWF. The syndrome can be precipitated by a variety of conditions, and certain medications also have been implicated. CASE REPORTS: The cases of two patients who took a cephalosporin antibiotic, cephalexin (Keflex, Eli Lilly), and then developed TTP are reported. One patient subsequently received a third-generation cephalosporin, ceftriaxone (Rocephin, Roche), without adverse reaction. Of interest, one patient had taken cefaclor (Ceclor, Eli Lilly) 8 years before and had also developed TTP at that time. The other patient also took cefaclor for approximately 3 weeks before taking cephalexin. In addition, she had had a dose of clarithromycin (Biaxin, Abbott Laboratories) the day before the onset of the TTP symptoms. CONCLUSIONS: To our knowledge, TTP has not been reported previously after administration of cephalosporin antibiotics. Attention is called to the possibility that this syndrome may occur after exposure to some of these drugs, although the incidence is very rare or, alternatively, underdiagnosed.

Adult↗
PubMed2001

Competition of IL-1 and IL-1ra determines lymphocyte response to delayed stimulation with PHA.

BACKGROUND: Human peripheral blood mononuclear cells (PBMC) left in microcultures for 24h without mitogen do not respond to subsequent stimulation with PHA. They regain reactivity if the native culture medium is absorbed with other party lymphocytes or partially replaced with the medium from a PHA-stimulated culture. The observations suggest that, during the incubation, some inhibitory agent had accumulated in the culture medium. AIM: The study was performed to determine the nature of the observed phenomenon in respect of the possible role of monocytes and their products IL-1 and IL-1 receptor antagonist (IL-1ra), and to test for immunodiagnostic purposes the significance of quantifying the lymphocyte response to delayed stimulation with PHA in patients suffering from inflammatory prosesses. METHODS: Lymphocyte response to delayed stimulation with PHA, calculated as the lymphocyte-monokine interaction (LM) index, was determined in the microcultures of PBMC isolated from the blood of healthy donors or of patients with acute tonsilitis. The values of LM indices were compared with the ratios of IL-1ra/IL-1beta concentration estimated by enzyme-linked immunosorbent assay method in the culture supernatants. The influences of exogenous IL-1beta, IL-1ra, anti-IL1ra antibodies and antibiotic cefaclor on the monokine concentrations and on the values of LM index were tested. RESULTS AND CONCLUSIONS: The results show that the level of lymphocyte response to delayed stimulation with PHA (LM index) is inversely proportional to the ratio of IL-1ra/IL-1beta concentration in the culture. The low LM values at high IL-1ra/IL-1beta ratios in PBMC cultures from healthy donors, reversed proportions found in patients' PBMC (acute tonsilitis), and the cefaclor-induced reduction of LM value with correlated increase of the IL-1ra/IL-1beta ratio suggest that the LM assay may prove to be useful for immunodiagnostic purposes.

Adult↗
PubMed1994

Susceptibility of respiratory and urinary pathogens to ceftibuten and other comparative drugs: results of an Italian multicenter survey. The Italian Ceftibuten Study Group.

A survey aimed at assessing the ability of ceftibuten, a new oral third-generation cephalosporin, to eradicate in vitro selected bacterial pathogens was conducted in 1991 in 17 microbiology laboratories evenly distributed in Italy. Over 8700 organisms collected from in- and outpatients affected mainly by respiratory and urinary tract infections were analyzed. This collection of bacteria did not include staphylococci, enterococci, Pseudomonas and other oxidative species naturally refractory to the action of most antibiotics employed. Susceptibility to ceftibuten, cefaclor, cefuroxime, amoxicillin, amoxicillin-clavulanate, cotrimoxazole and erythromycin was assessed using a standardized agar-diffusion method. Production of beta-lactamases was confirmed by the nitrocefin test. Among the microorganisms studied E. coli (32.1%) prevailed, followed by P. mirabilis (17.1%), K. pneumoniae (10.9%), S. pyogenes (6.6%), E. cloacae (5.1%), Serratia spp. (4.5%), Enterobacter spp. (4.2%), H. influenzae (3.6%), S. pneumoniae (2.2%) and M. catarrhalis (2%). Within this group of pathogens amoxicillin resistance, often mediated by synthesis of beta-lactamases, was widely diffused (46.2%). The overall inhibitory activity of the drugs tested decreased as follows: ceftibuten (90.4%), cefuroxime (80.4%), amoxicillin-clavulanate (77.4%), cotrimoxazole (75.3%), cefaclor (72.6%), amoxicillin (53.8%) and erythromycin (32.8%). When the efficacy of the antibiotics was assessed against the collection of respiratory isolates producing beta-lactamases only ceftibuten maintained the same overall potency manifested against the general population while the comparative agents were far less effective. The results of this national survey indicate that, given the low incidence of resistance among the most prevalent causative agents of respiratory and urinary tract infections, ceftibuten can be safely used at present in the empiric therapy of these conditions especially when they occur in community settings.

Ceftibuten↗
PubMed1992

Review of the in vitro antibacterial activity of cefprozil, a new oral cephalosporin.

Cefprozil is a newer oral cephalosporin with a spectrum of activity against organisms that include gram-positive and gram-negative pathogens. A review of published data shows that cefprozil is active (susceptibility, less than or equal to 8 micrograms/mL; moderate susceptibility, 16 micrograms/mL; resistance, greater than or equal to 32 micrograms/mL) against gram-positive species such as streptococci, methicillin-susceptible staphylococci, and Listeria monocytogenes; it may have marginal activity against some enterococci. Among the gram-negative species, cefprozil has activity against Escherichia coli, Proteus mirabilis, Citrobacter diversus, Klebsiella pneumoniae, Klebsiella oxytoca, Haemophilus influenzae, and Moraxella catarrhalis. For anaerobic species, cefprozil has activity against clostridial species, including Clostridium difficile, peptostreptococci, and possibly Bacteroides melaninogenicus and Eubacterium. The activity of cefprozil is generally greater than that of cephalexin and generally similar to that of cefaclor. In these reports, cefprozil showed more in vitro activity than cephalexin and cefaclor against penicillin-resistant pneumococci, penicillin-resistant viridans streptococci, beta-lactamase-positive methicillin-susceptible Staphylococcus aureus, and C. difficile, although the clinical significance of some of these differences has yet to be studied.

Cephalosporins↗
PubMed1977

Standardization of a preparative ultracentrifuge method for quantitative determination or protein binding of seven antibiotics.

A preparative ultracentrifuge method was standardized for determination of quantitative binding of cephalothin, cefamandole, cefazolin, cefaclor, erythromycin, gentamicin, and chloramphenicol to human serum proteins. At achievable in vivo concentrations, serum binding was 78.5% for cephalothin, 79.9% for cefamandole, 88.5% for cefazolin, 23.5% for cefaclor, 41.9% for erythromycin, 22.7% for gentamicin, and 59.5% for chloramphenicol. Techniques that use semipermeable cellophane or diaflow membranes, cross-linked dextran, inhibition of bacterial growth, protein precipitation, or liquid partitioning all have inherent problems with either the ligand or the antibiotic adversely interacting with the experimental apparatus. Ultracentrifugation provides a rapid, reproducible technique for protein-binding determinations of the classes of antibiotics described.

Anti-Bacterial Agents↗