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PubMed1998

Comparison of E test and agar dilution methods for determining antibiotic susceptibilities of anaerobic bacteria and viridans streptococci isolated from blood.

The antimicrobial susceptibilities of 311 strains of anaerobic bacteria and 140 strains of aerobic bacteria, isolated from blood after dental extraction, were determined by the E test and compared with the results obtained by the agar dilution method on PDM-ASM 2 agar. E test MICs agreed within +/-1 dilution step to the agar dilution MICs in 93%, 52%, 90%, 94% of the tested anaerobes for penicillin V, cefaclor, clindamycin and erythromycin, respectively. For aerobic bacteria the agreement was > or = 90% for the antibiotics tested. The in vitro activities of penicillin V, clindamycin and erythromycin were higher than the activity of cefaclor against the majority of bacteria tested.

Journal Article↗
PubMed1993

Antimicrobial resistance among clinical isolates of Haemophilus influenzae in northern Italy. Collaborative Study on Pediatric Infectious Diseases.

Only scanty data are available on the susceptibility of Haemophilus influenzae in Italy. The in vitro activity of ampicillin, ampicillin-sulbactam, cefaclor, cefuroxime, cefotaxime, chloramphenicol, erythromycin and trimethoprim-sulfamethoxazole against 327 strains of Haemophilus influenzae (55 encapsulated, 272 non-typeable) isolated from adults and children in northern Italy, between January 1984 and December 1989, was compared. Patients were affected by meningitis or other invasive infections, conjunctivitis, otitis, sinusitis, pneumonia or bronchitis. Minimal inhibiting concentrations were determined by a microdilution technique in Mueller Hinton broth supplemented with 10 microliters/ml NAD and 2-5% lysed horse blood. A concentration of 1 x 10(5) to 5 x 10(5) CFU/ml was used as the inoculum. The antibiotics were tested at concentrations ranging from 0.03 to 64 microliters/ml with the exception of trimethoprim-sulfamethoxazole, for which the range of concentrations examined were 0.01/0.25 to 32/512 microliters/ml. All the strains tested were susceptible to ampicillin-sulbactam, cefuroxime and cefotaxime, and more than 95% were susceptible to ampicillin, cefaclor and chloramphenicol. Only 4% were susceptible to erythromycin but most minimal inhibiting concentrations fell into the intermediate category. Strains isolated from adults were more susceptible to trimethoprim-sulfamethoxazole than strains isolated from children (85% vs 66%; p = 0.011).

Adult↗
PubMedDate not supplied

In vitro activity of cefpodoxime and ten other cephalosporins against gram-positive cocci, Enterobacteriaceae and Pseudomonas aeruginosa, including beta-lactamase producers.

Cefpodoxime, the deesterified part of the orally available cefpodoxime proxetil, is active against most Enterobacteriaceae with MIC50 of 0.06 to 2 mg/l. Only Enterobacter cloacae and Citrobacter freundii strains show MIC50 of 4 mg/l. Coagulase negative staphylococci have a MIC50 of 2, while Staphylococcus aureus strains have a MIC of 4 mg/l. In comparison to other orally available cephalosporins cefpodoxime is slightly less active than cefixime and cefotiam against gram-negative bacteria but more active than cefuroxime, cefaclor, and cephalexin. Against staphylococci the activity of cefpodoxime is comparable to that of cefotiam and cefuroxime and superior to cefaclor and cephalexin, while cefixime does not have sufficient activity against these species. Like all cephalosporins cefpodoxime has no activity against enterococci.

Bacteria↗
PubMed1987

[Infections of the lower respiratory tract in general practice].

Haemophilus influenzae and Streptococcus pneumoniae are found in 87% of all cases of exacerbated chronic obstructive bronchopulmonary disease. Complications of viral respiratory tract disease are most frequently caused by H. influenzae. Not only encapsulated forms of H. influenzae, but also non-encapsulated strains may be responsible for the onset of pneumonia and acute exacerbations of chronic bronchitis in adults. The most common symptoms of infections with H. influenzae are cough, dyspnoea, increase in purulent sputum and wheezing. A quantitative sputum culture is recommended for diagnosing chronic obstructive bronchopulmonary disease. Acute exacerbations of chronic bronchitis are always treated with antibiotics effective against H. influenzae and pneumococci. As a rule, empirical treatment should suffice in general practice. In the comparison between ampicillin, co-trimoxazole and cefaclor included in the study protocol appended to this report, the latter produced the most favourable results both in the empirical and specific forms of treatment. We would recommend cefaclor as the antibiotic of choice for this disease.

Anti-Bacterial Agents↗
PubMed1989

In vitro antibacterial properties of cefetamet and in vivo activity of its orally absorbable ester derivative, cefetamet pivoxil.

The in vitro activity of cefetamet, the microbiologically active metabolite of the orally administered prodrug cefetamet pivoxil, was compared with that of cephalexin, cefaclor, cefuroxime and amoxicillin. Cefetamet was highly active against Enterobacteriaceae, Neisseria spp., Vibrio spp., Haemophilus influenzae and streptococci other than enterococci. Cefetamet inhibited cefaclor-resistant species such as Proteus vulgaris, Providencia stuartii, Providencia rettgeri and Serratia marcescens. Staphylococci, Pseudomonas aeruginosa and cephalosporinase-overproducing strains of Enterobacter cloacae were resistant to cefetamet. The superior activity of cefetamet compared with older oral beta-lactam antibiotics against a large number of gram-negative pathogens correlated with enhanced stability towards beta-lactamases. In accordance with the in vitro findings, cefetamet pivoxil showed good activity in experimental infections in the mouse and rat, suggesting satisfactory bioavailability in these animals after oral administration.

Animals↗
PubMed1993

Comparative activity of the new fluoroquinolone Bay y3118 against 177 penicillin susceptible and resistant pneumococci.

The activity of a new fluoroquinolone, Bay y3118, was evaluated in comparison to three quinolones (ciprofloxacin, ofloxacin, lomefloxacin) and four broad-spectrum oral cephalosporins (cefpodoxime, cefuroxime, cefaclor, cefixime) against 49 penicillin-susceptible pneumococci, 77 pneumococci with intermediate resistance and 51 penicillin-resistant pneumococci. Quinolone activity was not affected by the penicillin susceptibility status of the organisms. Bay y3118 was very active against all strains, with an MIC90 of 0.015 microgram/ml. Other quinolones were less active, with MIC90s of 4 micrograms/ml (ciprofloxacin and ofloxacin) and 8 micrograms/ml (lomefloxacin). Cephalosporin MICs rose parallel to those of penicillin. Cefuroxime and cefpodoxime were the most active cephalosporins, with MIC90s for strains showing susceptibility, intermediate resistance and resistance of 0.125-0.25, 2-4 and 4 micrograms/ml, respectively. Cefaclor and cefixime were less active, with corresponding MIC90s of 1-2, 8-16 and > 16 micrograms/ml, respectively.

Anti-Infective Agents↗
PubMed2001

Upper respiratory tract infections.

Acute respiratory infections accounts for 20-40% of outpatient and 12-35% of inpatient attendance in a general hospital. Upper respiratory tract infections including nasopharyngitis, pharyngitis, tonsillitis and otitis media constitute 87.5% of the total episodes of respiratory infections. The vast majority of acute upper respiratory tract infections are caused by viruses. Common cold is caused by viruses in most circumstances and does not require antimicrobial agent unless it is complicated by acute otitis media with effusion, tonsillitis, sinusitis, and lower respiratory tract infection. Sinusitis is commonly associated with common cold. Most instances of rhinosinusitis are viral and therefore, resolve spontaneously without antimicrobial therapy. The most common bacterial agents causing sinusitis are S. pneumoniae, H. influenzae, M. catarrhalis, S. aureus and S. pyogenes. Amoxycillin is antibacterial of choice. The alternative drugs are cefaclor or cephalexin. The latter becomes first line if sinusitis is recurrent or chronic. Acute pharyngitis is commonly caused by viruses and does not need antibiotics. About 15% of the episodes may be due to Group A beta hemolytic streptococcus (GABS). Early initiation of antibiotics in pharyngitis due to GABS can prevent complications such as acute rheumatic fever. The drug of choice is penicillin for 10-14 days. The alternative medications include oral cephalosporins (cefaclor, cephalexin), amoxicillin or macrolides.

Anti-Bacterial Agents↗
PubMed1998

[Antibiotic sensitivity of important pathogens of bacterial respiratory tract infections in Northeast Germany].

BACKGROUND: There is still a lack of comprehensive study results about resistance of bacterial respiratory pathogens from the east of the Federal Republic of Germany. METHODS: In Greifswald we isolated in 1995 and 1996 320 strains of typical pathogens and tested their susceptibility to 14 antibiotics, using the microbouillon dilution method. RESULTS: Pneumococci and beta-haemolytic streptococci were completely susceptible to penicillin and all other beta-lactam-antibiotics, clindamycin and vancomycin. 4.8% of pneumococci and 10.0% of Streptococcus pyogenes isolates were resistant to erythromycin. This should lead to a more differentiated use of macrolides as concerns these pathogens, especially as penicillin still has high efficacy in these cases. Pneumococci had resistance rates of 4.8%, 9.5% and 6.7% to cotrimoxazole, tetracycline and ofloxacin, respectively. No strain of Haemophilus influenzae produced a beta-lactamase, 2.6% of strains were relatively resistant to ampicillin, even in combination with sulbactam. Cefaclor, erythromycin and tetracycline had restricted efficacy of 16.7%, 14.1% and 53.8%, respectively. Cefuroxime, cefixime, cefepime, imipenem and ofloxacin all had complete efficacy. 77.8% of Moraxella catarrhalis isolates were beta-lactamase positive. Strains were susceptible to erythromycin, ofloxacin and all tested beta-lactam-antibiotics except ampicillin and cefaclor. There was a relative resistance to clindamycin and tetracyclin of 22.2% and 2.2%, respectively. DISCUSSION: We present our results in national and international comparison, describe tendencies of resistance, give reasons for the low incidence of penicillin resistance in pneumococci in Germany and draw conclusions for empirical chemotherapy.

Anti-Bacterial Agents↗
PubMed2005

Antibiotic resistance patterns among respiratory pathogens at a German university children's hospital over a period of 10 years.

UNLABELLED: Growing antimicrobial resistance among Streptococcus pneumoniae, Haemophilus influenzae and Moraxella catarrhalis is raising major concern worldwide. Strains of S. pneumoniae, H. influenzae and M. catarrhalis isolated from children with respiratory tract as well as invasive infection in a South-Western region of Germany between 1993 and 2002 were tested for susceptibility to common antibiotics including penicillins, cephalosporins and macrolides. A total of 2,362 S. pneumoniae, 2,501 H. influenzae, and 1,982 M. catarrhalis isolates were tested. Only two S. pneumoniae strains were found to be highly resistant to penicillin. The overall rate of intermediate resistance to penicillin was 3.5%. There was a significant increase in erythromycin resistance from 5% in 1993 to 12.2% in 2002 (P=0.001). No increase in ampicillin resistance was observed for H. influenzae over time. The rate of cefaclor resistance, however, increased from 4.5% to 11.8% (P<0.0001). Furthermore, a massive increase in erythromycin resistance from 26% to 40% was observed (P<0.0001). The vast majority of M. catarrhalis isolates were beta-lactamase positive, the minimal inhibitory concentration to ampicillin, however, exceeded only in 3% of all strains the cut-off of 1.5 mg/l. The erythromycin resistance rate of M. catarrhalis was 0.3%. CONCLUSION: There is still a low rate of penicillin/ampicillin resistance in S. pneumoniae, and H. influenzae, but an alarming increase in resistance to erythromycin, and in H. influenzae a significant increase in cefaclor resistance was observed over the 10-year period in South-Western Germany.

Child↗
PubMed1999

Antimicrobial activities of cefditoren against respiratory pathogens isolated from children in Japan.

There is an increasing spread and incidence of penicillin-resistant bacteria that are becoming less susceptible to commonly prescribed oral antimicrobials, including extended-spectrum cephalosporins. Against this background, we undertook this study to determine the prevalence of penicillin resistance in Streptococcus pneumoniae and the in-vitro activity of oral antimitrobials. Between April 1996 and December 1997, in 245 children with respiratory tract infections (bronchitis in 61, pharyngitis in 115, and tonsillitis in 69), 119 strains of Haemophilus influenzae, 89 strains of Streptococcus pyogenes, 61 strains of Streptococcus pneumoniae, 36 strains of Staphylococcus aureus, and 34 strains of Moraxella catarrhalis were isolated from the pharynx. The antimicrobial susceptibility of these isolates was assessed by a broth microdilution method. The isolation incidence of penicillin-intermediately resistant S. pneumoniae (PISP) and penicillin-highly resistant S. pneumoniae (PRSP) was 59.0% and 13.1%, respectively. Most strains of PISP and PRSP were highly resistant to cefaclor, cefpodoxime, cefteram, cefdinir, clarithromycin, ampicillin, and minocycline, but susceptibile to ofloxacin and cefditoren (CDTR). The in-vitro activity of CDTR was superior to that of other cephalosporins, such as cefaclor, cefdinir, and cefpodoxime, when tested against both the beta-lactamase-positive and -negative H. influenzae isolated. CDTR was also active against all the other strains, including methicillin-sensitive S. aureus, S. pyogenes, and M. catarrhalis. This study suggested that CDTR was a useful oral antibiotic for pediatric respiratory tract infections.

Journal Article↗
PubMed2002

Differentiation of beta-lactamase-negative ampicillin-resistant Haemophilus influenzae from other H. influenzae strains by a disc method.

We established breakpoints for differentiating ampicillin (ABPC)-susceptible strains from resistant strains among Haemophilus influenzae isolates according to susceptibility to various beta-lactam antibiotics, using a disc method. Susceptibility testing of isolates for 13 beta-lactam agents was followed by analysis of the resistance genes, using a polymerase chain reaction (PCR) to identify the TEM-1 beta-lactamase gene ( bla) and the ftsI gene encoding penicillin-binding protein (PBP) 3, which affects beta-lactam minimum inhibitory concentrations (MICs). A total of 228 H. influenzae isolates were classified into 114 beta-lactamase-negative, ABPC-susceptible (BLNAS) strains; 29 beta-lactamase-negative, ABPC-resistant (BLNAR) strains; 53 low-BLNAR strains with a low degree of ABPC resistance; 27 TEM-1-producing strains (BLPAR); and 5 strains with ftsI gene mutations in addition to TEM-1 production (BLPACR) according to the PCR results. To identify resistant strains by disc-method susceptibility testing, the zone of inhibition was measured for ABPC (10 microg/disc), cefaclor (30 microg/disc), cefpodoxime (10 microg/disc), and cefdinir (5 microg/disc) discs. Strains were identified as BLNAS without resistant genes when the diameter was > or =27 mm for the ABPC disc and > or =21 mm for the cefaclor disc. Other strains were identified as BLNAR when the diameter was < or =22 mm for the cefpodoxime disc and < or =17 mm for the cefdinir disc. Remaining strains were identified as low-BLNAR. These criteria differentiated resistance types with high accuracy. A discrepancy was noted between genetic results and disc-testing breakpoints for differentiating resistant from susceptible H. influenzae. A disc-testing breakpoint for cefditoren (5 microg/disc) was proposed, with the susceptibility statistically defined as a diameter of > or =24 mm, which corresponds to the breakpoint (1 microg/ml) of the microdilution method recommended by the Japanese Society of Chemotherapy.

Ampicillin Resistance↗
PubMed1992

Acute bronchitis: results of U.S. and European trials of antibiotic therapy.

Acute bronchitis, an illness frequently encountered by primary-care physicians, is an inflammation of the tracheobronchial tree that results from a respiratory tract infection. It is characterized by persistent cough and sputum production and is occasionally accompanied by fever and/or chest pain. Acute bronchitis may have a viral or bacterial origin and is often treated with antibiotics. Four clinical trials were conducted to compare high and low doses of loracarbef, a new oral beta-lactam antibiotic, with three agents commonly used to treat acute bronchitis: amoxicillin/clavulanate, cefaclor, and amoxicillin. Results of these studies indicated that loracarbef, 400 and 200 mg twice daily, had clinical and bacteriologic efficacy against the common respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella (Branhamella) catarrhalis that was comparable with that of the comparative agents. Loracarbef was as well tolerated as cefaclor and amoxicillin; moreover, it produced a significantly lower incidence of diarrhea than did amoxicillin/clavulanate. Loracarbef may be considered a safe and effective alternative agent for the treatment of patients with acute bronchitis.

Acute Disease↗
PubMed1994

Transport mechanisms responsible for the absorption of loracarbef, cefixime, and cefuroxime axetil into human intestinal Caco-2 cells.

Loracarbef, cefixime and cefuroxime axetil are beta-lactam antibiotics that are administered orally. Oral absorption of loracarbef is nearly complete, while that of cefixime and cefuroxime axetil is 30-50%. To investigate this we used the human intestinal cell line Caco-2 that possesses the proton-dependent peptide transporter that takes up cephalexin and cefaclor. Drug uptake was measured at pH 6 by high performance liquid chromatography or with radioactively labelled drug. The initial uptake rate of 1 mM cefixime was lower than that of 1 mM loracarbef. By 2 h both drugs were concentrated intracellularly against a gradient; however, the accumulation of cefixime was only 40% of that of loracarbef. The uptake rate of both drugs was sodium-independent, temperature- and energy-dependent, and was inhibited by dipeptides, cephalexin, cefaclor, but not by amino acids. Kinetic analysis of the concentration-dependence of the uptake rates for loracarbef and cefixime indicated that diffusion and a single transport system were responsible for uptake. The kinetic parameters for loracarbef and cefixime, respectively, were: Km values of 8 and 17 mM and Vmax values of 6.5 and 2 nmol/min per mg protein. Loracarbef and cefixime were competitive inhibitors of each other's uptake. By contrast, cefuroxime axetil was taken up and rapidly hydrolyzed to cefuroxime by Caco-2 cells. Cefuroxime axetil uptake was not dependent on energy and was not affected by dipeptides. Thus, cefuroxime axetil apparently enters Caco-2 cells by simple diffusion. By contrast, loracarbef and cefixime share a common transport mechanism, the proton-dependent dipeptide transporter. Cefixime was taken up less well than loracarbef due to a substantial reduction in the turnover rate and decreased affinity of the transporter for cefixime.

Adenocarcinoma↗
PubMed1987

In vitro evaluations of U-76,252 (CS-807): antimicrobial spectrum, beta-lactamase stability, and enzyme inhibition.

Compound U-76,252 (Upjohn) is a cephalosporin ester that enhances oral absorption of the active free acid cephem, U-76,253. The active form structurally resembles parenteral aminothiazolyl-methoxyimino cephalosporins such as cefotaxime and its desacetyl metabolite. The g-negative antimicrobial activity of U-76,253 A (sodium salt of U-76,253) was most similar to that of cefixime and more potent than that of cefaclor or cefuroxime among the orally administered cephalosporins. Against g-positive bacteria, U-76,253 A was more active than cefixime. U-76,253 A was relatively stable to hydrolysis by five beta-lactamases (Type Ia, TEM-1, K1, CARB-2, and OXA-1), a stability most similar to cefotaxime and superior to that of cefaclor. Only the Type Ia (P99) enzyme was significantly inhibited by U-76,253 (IC 50 = 2.0 microM).

Anti-Bacterial Agents↗
PubMed1987

Susceptibility of relatively penicillin-resistant Streptococcus pneumoniae to newer cephalosporin antibiotics.

Antimicrobial susceptibilities were performed at the Centers for Disease Control on 3400 Streptococcus pneumoniae isolates that were collected during a national survey of serotype-distribution of pneumococci found in normally sterile body fluids. The results showed 126 isolates (3.7%) to be relatively resistant to penicillin (RPR). The RPR strains were tested for susceptibility to cefuroxime, ceftriaxone, cefotaxime, cefamandole, cefaclor, ceftazidime, and moxalactam. These newer generation cephalosporin drugs were tested either because of their ability to penetrate into the cerebrospinal fluid (CSF) or for their activity against pneumococci. Three hundred ninety-one pneumococci were tested with 179 resistant to at least one antimicrobial. The RPR strains were not categorically resistant to the cephalosporins but were fourfold more resistant to them than were the penicillin-susceptible strains. The three most effective antimicrobials in the study for RPR were cefuroxime, cefotaxime, and ceftriaxone [corrected]. Each gave MICs that were attainable in CSF for RPR. Fifty percent of the RPR were inhibited by 0.06 mg/ml and 90% by 0.25 micrograms/ml of these antimicrobials. The least effective were cefaclor, moxalactam, and ceftazidime.

Cephalosporins↗
PubMedDate not supplied

Antibacterial activity and beta-lactamase stability of MDL 19,592, an oral cephalosporin.

We compared the in vitro activity and beta-lactamase stability of MDL 19,592, an orally absorbed cephalosporin, with that of cephalexin and cefaclor. It inhabited Staphylococcus aureus at less than or equal to 4 micrograms/ml, Streptococcus pyogenes at 0.25 microgram/ml, sero groups B, C and G streptococci at 1 microgram/ml, and Streptococcus pneumoniae at 2 micrograms/ml. It was slightly more active than cefaclor and cephalexin. MDL 19,592 did not significantly inhibit Enterobacteriaceae, enterococci, Listeria monocytogenes, Pseudomonas aeruginosa, and Acinetobacter spp. strains (MIC greater than or equal to 32 micrograms/ml). MDL 19,592 was not hydrolyzed by the plasmid beta-lactamases TEM-1 and SHV-1 of Klebsiella but was hydrolyzed by the TEM-3, Staphylococcus aureus beta-lactamase, and the chromosomal-mediated Enterobacter cloacae P99 enzymes.

Bacteria↗
PubMedDate not supplied

In vitro activity of BAY v 3522, a new oral cephalosporin tested against Haemophilus influenzae and Branhamella catarrhalis.

The in vitro activity of BAY v 3522, a new orally absorbed cephalosporin, was assessed against 150 clinical isolates each of Haemophilus influenzae and Branhamella catarrhalis. The MIC90S for beta-lactamase-positive and -negative strains of H. influenzae were 8 and 2 micrograms/ml, respectively. For beta-lactamase-positive and -negative strains of B. catarrhalis, the BAY v 3522 MIC90S were 4 and 0.25 micrograms/ml, respectively. In general, BAY v 3522 was less active against H. influenzae than amoxicillin/clavulanic acid and cefixime, equivalent in activity to cefuroxime, and more active than cefaclor. BAY v 3522 had activity most similar to cefuroxime and cefaclor for B. catarrhalis but was less active than amoxicillin/clavulanic acid and cefixime.

Administration, Oral↗
PubMed1992

Ofloxacin, a new broad-spectrum fluoroquinolone. Results from a Multicenter, National Comparative Activity Surveillance Study. The Ofloxacin Surveillance Group.

Ofloxacin, a newer broad-spectrum fluoroquinolone, was evaluated against 6967 clinical isolates in a multicenter surveillance trial using a standardized disk diffusion method. Thirty-five geographically diverse laboratories contributed zone diameter results for two (ofloxacin and ciprofloxacin) to five (ofloxacin, ciprofloxacin, ampicillin, cefaclor, and cefixime) antimicrobial agents, depending on the site of infection. Ofloxacin was determined to have the widest spectrum of activity and potential empiric use (90.6%, range 87.1%-92.2%) for respiratory tract, urinary tract, and cutaneous infections. The spectrum was superior to ciprofloxacin (average 85.3% versus three sites), ampicillin (35.5%, respiratory tract), cefaclor (60.5%, respiratory tract), cefixime (60.9%, respiratory tract), and norfloxacin (87.3%, urinary tract). Strains resistant to ofloxacin (35 isolates, 0.5%) were confirmed by reference laboratory tests and cross resistance was observed among several current and investigational fluoroquinolone agents. The species most often found to be fluoroquinolone resistant among the Enterobacteriaceae were Klebsiella pneumoniae, Serratia marcescens, and Providencia spp. Monitoring for increasing fluoroquinolone resistance should be considered as greater use of drugs in this class develops. By these cited statistics, ofloxacin appears to have a broad and balanced spectrum of potential use, particularly against Gram-positive pathogens.

Anti-Infective Agents↗