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PubMed1975

[Total count and bacterial flora of minced meat with special reference to enterobacteria and pseudomonads (author's transl)].

The bacterial flora of minced meat is dominated by Micrococcaceae. In addition lactobacilli, pseudomonads, and enterobacteria are present in high numbers. The most important groups of spoiled meat are lactobacilli and pseudomonads. Enterobacteria develop predominantly at higher spoilage temperatures (15 degrees C). A more detailed study was conducted on 1076 cultures of enterobacteria and 915 cultures of pseudomonads. The main groups of enterobacteria found on minced meat are Enterobacter liquefacines, Erwinia, Citrobacter and Klebsiella. In spoiled meat E. liquefaciens and Erwinia predominate. Basicly, however, the enterobacteria flora of fresh and spoiled meat is rather similar. The same applies to the pseudomonads flora which at a rate of 60-70% consists of Pseudomonads fragi. The total count of minced meat is subject to large variations.

Bacteria↗
PubMed1992

Comparative in vitro activity and beta-lactamase stability of RU29246, the active metabolite of HR916B.

HR 916B is a new orally absorbed cephalosporin. In tests its active metabolite, RU29246, inhibited Streptococcus pyogenes, Streptococcus agalactiae and Streptococcus pneumoniae at less than or equal to 0.12 micrograms/ml, which is similar to the antibacterial activity of cefuroxime, and was more active than cefaclor. It was also more active (MIC 2 micrograms/ml) than cefixime, cefuroxime, cefaclor and cefotaxime against staphylococci. RU29246 inhibited Escherichia coli, Klebsiella pneumoniae, Citrobacter diversus, Klebsiella oxytoca, Proteus mirabilis, Providencia stuartii and Salmonella spp. at less than or equal to 1 microgram/ml, thus being more active than cefuroxime and cefaclor, but was less active than cefixime and cefotaxime. It did not inhibit Pseudomonas aeruginosa and other Pseudomonas spp., Enterobacter spp., Serratia marcescens or Bacteroides fragilis. RU29246 was not hydrolyzed by TEM-1, Staphylococcus aureus TEM-2 or Moraxella catarrhalis beta-lactamases, but was hydrolyzed by TEM-3 and the chromosomal beta-lactamases of Proteus vulgaris and Morganella morganii. Plasmid and chromosomal beta-lactamases were inhibited by RU29246.

Cephalosporins↗
PubMed1992

In vitro activity of OPC-17116 compared to other broad-spectrum fluoroquinolones.

The in vitro activity of OPC-17116 was compared to that of five similar fluoroquinolones (ciprofloxacin, enoxacin, norfloxacin, ofloxacin and temafloxacin). A total of 700 isolates from recent cases of clinical bacteremia were tested. Fifty additional stock strains with well-characterized resistance mechanisms were also processed. The minimal concentrations inhibiting 90% of strains (MIC90) of Enterobacteriaceae species were for OPC-17116 0.015-0.5 micrograms/ml and for ciprofloxacin 0.015-0.25 micrograms/ml. Moraxella catarrhalis, Haemophilus influenzae and Neisseria gonorrhoeae were very susceptible to OPC-17116 (MIC90 0.015 micrograms/ml) thus being fourfold more active than ciprofloxacin. For all beta-hemolytic streptococci and pneumococci OPC-17116 MICs were less than or equal to 0.5 micrograms/ml. The most resistant enteric bacilli were among the Citrobacter freundii and Providencia rettgeri strains (MIC90 0.5 micrograms/ml). Pseudomonas aeruginosa strains were comparably susceptible to OPC-17116 (MIC90 0.5 micrograms/ml). Low pH and CO2 incubation had an adverse effect on OPC-17116 MICs, and resistance development was documented among current clinical isolates of staphylococci, pseudomonas and some Enterobacteriaceae.

Anti-Infective Agents↗
PubMed1988

In vitro activity of temafloxacin, a new difluoro quinolone antimicrobial agent.

Temafloxacin, a new difluoro quinolone, inhibited the majority of Enterobacteriaceae at less than or equal to 1 microgram/ml. It was 4-8-fold less active than ciprofloxacin and 2-fold less active than ofloxacin. Cefotaxime and imipenem-resistant isolates such as Enterobacter cloacae, Citrobacter freundii, Pseudomonas aeruginosa, and Acinetobacter spp. were inhibited. Temafloxacin inhibited Neisseria, Branhamella, and Haemophilus species at less than 0.25 microgram/ml. Methicillin-susceptible and methicillin-resistant Staphylococcus aureus, Staphylococcus epidermidis and Clostridium spp. were inhibited at concentrations less or equal to that of ciprofloxacin and ofloxacin.

Anti-Bacterial Agents↗
PubMed1988

Comparative in vitro activity of the new oral cephalosporin cefixime.

Cefixime was 8 to 10 times more active than cefaclor and augmentin against isolates of Escherichia coli, Klebsiella pneumoniae and Salmonella typhi, MIC90 values ranging from 0.06 to 0.25 micrograms/ml. However, none of these three drugs was particularly active against isolates of more resistant gram-negative bacilli such as Enterobacter, Serratia, Citrobacter, Acinetobacter, Providencia and Achromobacter spp. The lowest MIC values for gram-negative bacilli were seen with ciprofloxacin, except for isolates of Acinetobacter, where cotrimoxazole was the most active of the five drugs studied. Augmentin and ciprofloxacin exhibited the lowest MICs for isolates of streptococci and corynebacteria. Although cefixime may be among the most active oral beta-lactam drugs, it does not appear to be useful for treatment of infections caused by more resistant gram-negative bacilli.

Amoxicillin↗
PubMed1989

In vitro antibacterial activity and beta-lactamase stability of the new carbapenem SM-7338.

The in vitro activity of the new carbapenem SM-7338 was tested in comparison with imipenem, ceftazidime, cefotaxime, flomoxef, cefuzonam and cefmetazole against 2850 clinical bacterial isolates. SM-7338 showed good activity against a broad spectrum of gram-positive and gram-negative bacteria. SM-7338 was very active against gram-negative bacteria, inhibiting all Enterobacteriaceae, except 25% of Serratia marcescens isolates, at a concentration of 0.78 mg/l. SM-7338 inhibited the majority of Pseudomonas spp. at concentrations of less than or equal to 3.13 mg/l, its activity being twofold higher than that of imipenem. However, the activity of SM-7338 against gram-positive cocci was about one-fourth that of imipenem. Against anaerobes, SM-7338 also had the best activity of the beta-lactams tested. The compound was inactive against methicillin-resistant staphylococci, Enterococcus faecium, Xanthomonas maltophilia and Flavobacterium spp., as were the other beta-lactams. SM-7338 was quite stable in the presence of various types of beta-lactamase, but was hydrolyzed by Xanthomonas maltophilia beta-lactamase, as was imipenem. This high degree of stability was responsible for the potent activity of SM-7388 against beta-lactamase-producing species such as Enterobacter cloacae, Citrobacter freundii and Proteus vulgaris. SM-7338 also showed bactericidal activity against clinical isolates at the MIC or at concentrations slightly above the MIC.

Anti-Bacterial Agents↗
PubMed1990

In vitro activity and beta-lactamase stability of the new oral cephalosporin Bay v 3522.

The activity of the new oral cephalosporin Bay v 3522 was compared to that of six other beta-lactam agents. Bay v 3522 inhibited methicillin-susceptible Staphylococcus aureus and Staphylococcus epidermidis at less than or equal to 2 micrograms/ml, compared to MICs of greater than or equal to 8 micrograms/ml for the other cephalosporins tested. It was more active against Streptococcus pyogenes (MIC less than or equal to 0.06 microgram/ml) than cefuroxime, cefixime, cephalexin and cefaclor. Groups B, C and G streptococci were inhibited at less than or equal to 0.12 microgram/ml, while the MI"90 for Streptococcus bovis and viridans streptococci was 0.5 and 2 micrograms/ml, respectively. The MIC90 for enterococci and Listeria monocytogenes was 8 micrograms/ml. Clostridium perfringens was inhibited by 0.12 microgram/ml, but most Bacteroides spp. were resistant. The MIC90 for beta-lactamase positive Escherichia coli (producing primarily TEM-1) was greater than 64 micrograms/ml and for beta-lactamase negative strains 16 micrograms/ml. The MIC90 for high-level beta-lactamase producing Klebsiella pneumoniae was greater than 64 micrograms/ml versus 4 micrograms/ml for other isolates. The MIC90 for Moraxella catarrhalis was 2 micrograms/ml, for Haemophilus influenzae 1 micrograms/ml, and for Neisseria gonorrhoeae 4 micrograms/ml. Enterobacter cloacae, Citrobacter freundii, Proteus mirabilis, Providencia spp. and Pseudomonas aeruginosa were resistant. Bay v 3522 was destroyed by TEM-1, SHV-1, TEM-3 and P99 beta-lactamases.

Administration, Oral↗
PubMed1993

Comparative in vitro activity of biapenem, a new carbapenem antibiotic.

Biapenem is a new carbapenem antibiotic with high stability to human renal dehydropeptidase I. Its in vitro activity was compared with that of imipenem, meropenem, ceftazidime, ceftriaxone, piperacillin and gentamicin against a total of 650 recent clinical isolates. MICs were determined by a standard agar dilution procedure and all isolates were tested at two inocula (10(4) and 10(6) cfu). Biapenem inhibited 90% of isolates of Escherichia coli, Klebsiella spp., Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia stuartii, Enterobacter spp., Citrobacter freundii, Serratia marcescens, Salmonella typhi, Shigella sonnei and Yersinia enterocolitica at < or = 2 mg/l and was as active as or two- to four-fold more active than imipenem against all these species, with the exception of Serratia marcescens, against which imipenem was two-fold more active. Biapenem was two-fold more active than imipenem against Pseudomonas aeruginosa (MIC90 4 mg/l) and had activity similar to that of imipenem against the Bacteroides fragilis group (MIC90 0.5 mg/l) but was two-fold less active than imipenem against methicillin-susceptible Staphylococcus aureus (MIC90 0.06 mg/l) and was, like imipenem, inactive against methicillin-resistant Staphylococcus aureus.

Anti-Bacterial Agents↗
PubMed1992

Antibacterial activity of the investigational oral and parenteral cephalosporin BK-218.

BK-218 is a novel cephalosporin with a dual route of administration and spectrum of activity most similar to that of second-generation cephalosporins. BK-218 was active against Streptococcus pneumoniae, Haemophilus influenzae and Moraxella catarrhalis but strains resistant to penicillins had higher MICs. BK-218 had greater activity (8-fold) than cefuroxime or cefaclor against oxacillin-susceptible Staphylococcus spp. Moderate BK-218 activity was observed against Neisseria gonorrhoeae and commonly isolated Enterobacteriaceae such as Escherichia coli (MIC90, 1 mg/l), Klebsiella spp. (MIC90, 2 mg/l), and Proteus mirabilis (MIC90, 2 mg/l). The following organisms were generally BK-218-resistant (MIC90, greater than 16 mg/l): Bacteroides fragilis, Pseudomonas spp., Acinetobacter spp., Xanthomonas maltophilia, Citrobacter spp., Enterobacter spp., indole-positive Proteus, Serratia spp., enterococci and oxacillin-resistant staphylococci.

Cefaclor↗
PubMed1990

In vitro antibacterial activity and beta-lactamase stability of the new carbapenem LJC10,627.

In in vitro susceptibility tests the new carbapenem LJC10,627 showed potent antibacterial activity against gram-positive and gram-negative bacteria, except that most methicillin-resistant Staphylococcus aureus strains tested were found to be resistant to LJC10,627. LJC10,627 showed high activity against Pseudomonas aeruginosa and was active against Enterobacter cloacae and Citrobacter freundii strains which were resistant to ceftazidime and cefpirome. The Ki values of LJC10,627 for penicillinase Type I, cephalosporinase and oxyiminocephalosporinase were low, whereas the Ki value for L-1 enzyme from Xanthomonas maltophilia was high.

Bacteria↗
PubMed1991

In vitro activity of cefpodoxime against bacterial isolates obtained from patients with cancer.

The in vitro activity of cefpodoxime, an oral cephalosporin ester, against 792 bacterial isolates representing 36 species was evaluated in comparison to that of ciprofloxacin and trimethoprim/sulfamethoxazole (TMP/SMX). Cefpodoxime inhibited the majority of Streptococcus spp., Haemophilus influenzae and Proteus mirabilis at a concentration of less than or equal to 0.12 microgram/ml. It was also active against Citrobacter diversus, Escherichia coli, Klebsiella spp., Proteus vulgaris, Serratia marcescens and methicillin-susceptible Staphylococcus aureus isolates. Overall, cefpodoxime appeared to be less active than ciprofloxacin and TMP/SMX against many pathogens common in cancer patients.

Bacteria↗
PubMed1990

Antimicrobial activity and beta-lactamase stability of BMY-28232, parent compound of an oral cephalosporin.

BMY-28232, an aminothiazolyl imino methoxy cephalosporin which is available as an orally absorbed acetoxyethyl ester, inhibited strains of methicillin-susceptible Staphylococcus aureus, hemolytic streptococci, Streptococcus pneumoniae, Escherichia coli, Klebsiella species, and many strains of Proteus and Providencia stuartii at concentrations less than 1 microgram/ml, including isolates resistant to cephalexin and cefaclor. It had activity similar to that of cefixime, but was more active against methicillin-susceptible staphylococci. BMY-28232 was a poor substrate for beta-lactamases but was destroyed by the new TEM-3 enzyme, and had less activity against Enterobacter species, Citrobacter freundii, and Proteus vulgaris isolates. Methicillin-resistant staphylococci, Pseudomonas species, enterococci, Listeria monocytogenes, Corynebacterium jeikeium, Bacteroides fragilus and some strains of Clostridium species were resistant to BMY-28232.

Bacteria↗
PubMed1989

In vitro activity of PD 117596-2, a broad-spectrum difluoroquinolone.

The activity of PD 117596-2, a novel quinolone, was compared to that of other quinolones, ceftazidime, imipenem and gentamicin. PD 117596-2 inhibited most Enterobacteriaceae at concentrations less than 0.25 micrograms/ml, being equal or superior in activity to ciprofloxacin and 2- to 4-fold more active than ofloxacin. It inhibited ceftazidime-resistant Enterobacter spp., Citrobacter spp. and Serratia marcescens. The MIC90 for Pseudomonas aeruginosa, including strains with imipenem MICs of 8 micrograms/ml and gentamicin MICs greater than 16 micrograms/ml, was 0.25 micrograms/ml. PD 117596-2 was more active than ciprofloxacin against Pseudomonas cepacia and Pseudomonas maltophilia, and it inhibited Neisseria gonorrhoeae and Haemophilus influenzae at less than 0.03 micrograms/ml. PD 117596-2 inhibited staphylococci at 0.5 micrograms/ml, being 2-fold superior to other quinolones, and with an MIC of 0.25 micrograms/ml was more active against group A, B, C and G streptococci and Streptococcus pneumoniae. MICs for Bacteroides spp. were 2 micrograms/ml compared to 8-32 micrograms/ml for other agents. The frequency of spontaneous resistance was low (less than 10(-10]. Differences in MICs and MBCs were within one dilution, and there was a minimal effect of inoculum size. Although PD 117596-2 was less active at pH 5.5, MICs were less than 0.5 micrograms/ml.

Anti-Infective Agents↗
PubMed1994

In vitro antimicrobial activity of cefpirome against ceftazidime-resistant isolates from two multicenter studies.

The in vitro activity of cefpirome against ceftazidime-resistant (MIC > 16 mg/l) isolates from two multicenter studies was analyzed. The first investigation carried out in the USA, was an in vitro comparison of cefpirome and five third-generation cephalosporins in which more than 6,000 isolates were evaluated, including 97 Enterobacteriaceae and 1,509 staphylococci resistant to ceftazidime. The second study was a multicenter international study (> 5,000 strains total) in which 160 ceftazidime-resistant gram-negative bacilli and 509 staphylococci from five countries (Australia, France, Germany, Italy and UK) were tested against cefpirome. The results from the US trial indicated that only 0.8% of enteric bacilli were resistant to cefpirome compared to 4.9% and 4.7% resistant to ceftazidime and cefoperazone, respectively. In the international trial, cefpirome was also active against ceftazidime-resistant, class I beta-lactamase producing enteric bacilli (75% susceptibility, MIC50 of 4 mg/l) especially against Citrobacter spp., Enterobacter spp. and Morganella morganii. Cefpirome was 8- to 64-fold more active than ceftazidime against seven different staphylococcal species. The antimicrobial activity of cefpirome against routine clinical isolates and those organisms resistant to third-generation cephalosporins was highly consistent within a nation (USA) and among various developed countries.

Bacterial Infections↗
PubMed1991

In vitro activity of cefcanel versus other oral cephalosporins.

Cefcanel is a new orally absorbed cephalosporin. Its activity was compared with that of cefuroxime, cefaclor, cephalexin, and cefixime against gram-positive and negative aerobic and anaerobic bacteria. Cefcanel had excellent activity against methicillin-susceptible Staphylococcus aureus and Staphylococcus epidermidis, MIC90 1 micrograms/ml, superior to the other oral cephalosporins. However, methicillin-resistant staphylococci were resistant, MIC greater than or equal to 16 micrograms/ml. Streptococcus pyogenes and Streptococcus pneumoniae were inhibited by 0.015-1 micrograms/ml, concentrations comparable to other cephalosporins. Clostridium spp. were inhibited by 0.25 micrograms/ml, 8- to 128-fold lower concentrations than were found for other agents, but the MICs were greater than 64 micrograms/ml for Bacteroides spp. The MIC90 for Moraxella catarrhalis was 1 micrograms/ml, similar to cefuroxime but 16-fold greater than the MICs of cefixime. Escherichia coli and Klebsiella pneumonia which were high beta-lactamase producers were resistant, MICs greater than 64 micrograms/ml, and 50% of Enterobacter cloacae and Citrobacter freundii were resistant. Cefcanel was hydrolyzed by TEM-1, TEM-3 and Moraxella Bro-1 beta-lactamases. Escherichia coli containing TEM-1, 2, 3, 5, 7, and 9 had cefcanel MICs of greater than or equal to 16 micrograms/ml. Although cefcanel inhibited gram-positive species as well as or at lower concentrations than other cephalosporins, it lacked activity against gram-negative species that produced common plasmid beta-lactamase although it inhibited Haemophilus influenzae carrying TEM-1.

Administration, Oral↗
PubMed1991

In vitro activity of the novel cephalosporin GR69153.

The in vitro activity of GR69153 was compared to that of ceftazidime, ceftriaxone, imipenem and gentamicin against a total of 702 recent clinical isolates. MICs were determined by a standard agar dilution procedure and two inocula (10(4) and 10(8) cfu) were used throughout. GR69153 inhibited 90% of isolates of Escherichia coli, Klebsiella pneumonia and Proteus mirabilis at less than or equal to 0.25 mg/l and 90% of isolates of Pseudomonas aeruginosa at less than or equal to 1 mg/l. Citrobacter freundii (MIC90 16 mg/l), Morganella morganii (MIC90 128 mg/l) and Enterobacter spp. (MIC90 greater than 128 mg/l) were considerably more resistant to GR69153. GR69153 was four-fold more active than ceftazidime against methicillin-sensitive Staphylococcus aureus but was inactive against methicillin-resistant Staphylococcus aureus, Enterococcus faecalis and Bacteroides fragilis group.

Bacteria↗
PubMed1987

Clinical significance of beta-lactamase induction and stable derepression in gram-negative rods.

Most strains of enterobacteria and Pseudomonas aeruginosa produce chromosomally-determined Class I beta-lactamases. When synthesized copiously these enzymes cause resistance to almost all beta-lactams, except imipenem and, sometimes, carbenicillin and tenocillin. Elevated beta-lactamase production arises transiently, via induction, in Pseudomonas aeruginosa and Enterobacter, Citrobacter, Morganella, indole-positive Proteus and Serratia spp. when these organisms are exposed to beta-lactams. Permanent high-level enzyme production arises via mutation, in the stably-derepressed mutants of these species. These mutants arise spontaneously at high frequency (10(-5) -10(-8). Most early penicillins and first-generation cephalosporins are strong inducers of Class I enzymes at sub-inhibitory concentrations, as are cefoxitin and imipenem. Consequently their MICs reflect what lability these antibiotics have to inducibly-expressed beta-lactamase. Except with imipenem this lability usually is so great that the inducible enzyme causes clinical resistance. Although most other newer cephalosporins and ureidopenicillins are labile to the Class I enzymes they induce poorly below the MIC, and their lability is not reflected in resistance unless secondary inducers (e.g. cefoxitin or imipenem) are present. Although the weak inducer activity of these agents helps to maintain their activity against the inducible cells it renders the drugs highly selective for the pre-existing stably-derepressed mutants. Many cases have been reported where stably-derepressed mutants have overrun inducible populations of bacteria in patients undergoing therapy with beta-lactamase-labile weak inducers such as ureidopenicillin and third-generation cephalosporins.

Anti-Bacterial Agents↗
PubMed1986

Clinical experience with ciprofloxacin in the USA.

This interim analysis of the efficacy and safety of ciprofloxacin is based on case reports of 1241 adult patients treated primarily in the USA; 1026 were suitable for analysis of drug efficacy. The daily dose ranged from 500 to 1500 mg, the unit dose being given every 12 h. Duration of treatment ranged from 5 to 211 days (mean 12.6 days). In 1046 cases of infection the site was the urinary tract (514), skin structures (218), respiratory tract (215), blood (43), bone (27), abdomen (13), gastrointestinal tract (13) and pelvis (3). Organisms responsible for infection were Escherichia coli (282), Pseudomonas aeruginosa (238), Staphylococcus spp. (149), Streptococcus spp. (107), Klebsiella spp. (105), Proteus spp. (97), Haemophilus spp. (71), Enterobacter spp. (58), Salmonella spp. (44), Citrobacter spp. (27), and Serratia spp. (22). Signs and symptoms of infection resolved in 84% of all cases; 12.6% improved and 3.4% failed to improve. Pathogens were eradicated in 91% of urinary tract infections and in 87% of all other cases of infection combined; superinfections occurred in 5.3% of all patients. At the four-week follow-up 83% of patients with urinary tract infection still had sterile urine. Adverse reactions during therapy were considered probably or possibly drug-related in 166 patients. Nausea (37), diarrhea (25), vomiting (15), nervousness (28), and rash (9) were the most frequent; in only 2% of cases was it necessary to discontinue the drug. Results of ophthalmologic studies were generally unremarkable. Occasional elevations of SGOT and SGPT, and rare elevations of NPN related to ciprofloxacin therapy were seen.

Administration, Oral↗