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The wide and potent in vitro activity of cefixime, a new oral broad spectrum cephalosporin, has been confirmed on a collection of respiratory and urinary pathogens recently isolated in Italy. The new cephem emerged as the most bactericidal of all the comparators tested against several fast as well as slowly-growing gram-negative species including Enterobacteria, Haemophilus and Moraxella, irrespective of their ability to synthetize beta-lactamases. Among the gram-positive species Streptococcus pyogenes and S. pneumoniae were effectively covered. Cefixime activity was not adversely influenced by several important variables such as pH (over the range from 5 to 8), inoculum size (from 10(5) to 10(8) CFU per ml) and the presence of 50% human serum or urine. Time-kill tests confirmed a pronounced bactericidal potency of the drug especially towards common respiratory pathogens (H. influenzae, M. catarrhalis, S. pneumoniae and S. pyogenes). Killing of urinary strains was optimal at cefixime concentrations reached in urine since eradication, except for Proteus mirabilis, was enhanced with increasing levels of the drug. The absence of an untoward paradoxic effect on the rate of cefixime bactericidal action was confirmed by employing a dynamic bladder model simulating the pharmacokinetic parameters of the drug after a single 200 mg daily dosage. Interactions of cefixime with several other drugs that may be employed in combination therapy were generally prone to provide indifference and synergism while antagonism was never observed. Favorable interactions were also registered when cefixime acted with other antibiotics on partially resistant species such as Staphylococci and Pseudomonas. The new cephem seems to provide excellent opportunities for expanding oral cephalosporin therapy to a wide range of infections produced by susceptible pathogens in the adult and pediatric populations.
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PMID:Parameters characterizing the in vitro activity of cefixime, a new oral broad spectrum cephalosporin, against respiratory and urinary pathogens. 151 6

Antibiotic activities (MICs) of ceftriaxone (CTRX) against 1,210 strains of bacteria including 28 spp. isolated in 1987 and 1990 were compared with those of other cephems. 1. When compared to data on clinically isolated strains reported in the early 1980s, strains of the following species isolated in 1990 showed extremely elevated MIC90s of CTRX: Staphylococcus spp., Streptococcus pneumoniae, Escherichia coli, Citrobacter spp., Enterobacter spp., Serratia spp., Proteus vulgaris, Morganella morganii and Providencia spp. No changes were observed in MIC90s between the 2 periods for microorganisms such as Streptococcus pyogenes, Haemophilus influenzae, Klebsiella pneumoniae, Proteus mirabilis and Peptostreptococcus spp. 2. The MIC90 of CTRX to S. pneumoniae was high because a large number of benzylpenicillin (PCG)-insensitive S. pneumoniae (PISP) was present among this species. The MIC80 to Bacteroides fragilis group was also high because highly resistant B. fragilis and B. thetaiotaomicron were isolated in large proportions among the bacteria of this group. Other oxime-type cephems also had high MICs against the above mentioned bacteria. Therefore, a further evaluation has to be made with regard to activities of oxime-type cephems such as CTRX against PISP and B. fragilis group. 3. Sample strains included, in high ratios, methicillin-resistant Staphylococcus aureus (MRSA), cephamycin-resistant as well as oxime-type cephem-resistant intestinal bacteria, Gram-negative bacteria, and new-quinolone-resistant bacteria. Some of there resistant bacteria are also CTRX-resistant, and CTRX had insufficient activities against them. 4. With regard to the assessment of changes of frequencies of specific drug-resistant bacteria, including those with CTRX-resistance from year to year, the authors would like to point out the following comment of theirs made in 1989 and 1991, which appears to be increasing its significance, "Subjects of future studies should include dose on the mechanisms for the acquisition of bacterial resistance to entire beta-lactam antibiotics and the social circumstances in which resistant bacteria appear". 5. It appears that those strains resistant to cephems including CTRX are increasingly found among clinically isolated strains in recent years. CTRX, however, was found still effective against most clinical pathogens. Furthermore, considering that CTRX is one of the few drugs which sustain high blood concentrations of active forms we concluded that CTRX is a useful cephem-group antibiotic.
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PMID:[Antimicrobial activities of ceftriaxone against clinically isolated strains]. 152 69

Cefodizime is a bactericidal cephem with the typical broad spectrum activity of an aminothiazolyl cephalosporin, including both gram-positive and gram-negative bacteria: its MIC90 is 0.125 mg/l for Streptococcus pneumoniae, Streptococcus pyogenes and other streptococci; and 0.05 mg/l for Haemophilus spp., Neisseria meningitidis, Neisseria gonorrhoeae and Moraxella catarrhalis; while beta-lactamase positive strains of M. catarrhalis require 1 mg/l. Less than 1 mg/l is needed for Escherichia coli, Klebsiella spp., Proteus spp. and Shigella spp. The MIC90 is 4 mg/l for methicillin-sensitive Staphylococcus aureus, Morganella morganii, Providencia spp. and most strains of Serratia marcescens, Citrobacter spp. and Enterobacter spp. Staphylococcus epidermidis, Enterococcus faecalis and most strains of Pseudomonas spp. and Acinetobacter spp. are considered cefodizime-resistant. Cefodizime is unaffected by plasmid-mediated beta-lactamases, but it is hydrolyzed by some chromosomally mediated enzymes, thus resembling other third-generation cephalosporins. Cefodizime has high affinity for PBP 3 and PBP IA and IB (Escherichia coli); in S. aureus it shows the highest affinity for PBP 1.
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PMID:In vitro activity of cefodizime. 152 73

The serum bactericidal activity (SBA) was studied one hour and four hours after intravenous administration of 1 g and 2 g cefotiam, 1.5 g cefuroxime and 2 g cefazolin to six volunteers. The 136 clinical isolates tested included Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and Haemophilus influenzae. One hour after administration no significant differences in the activity against staphylococci were noted in the antibiotics tested. Four hours after administration of cefazolin 96% of the Staphylococcus aureus strains were killed at a serum dilution of 1:8, whereas only one strain was killed by cefuroxime and none by cefotiam under the same conditions. The highest SBA-titers against Haemophilus influenzae were achieved with cefotiam at a dosage of 2 g. SBA-titers against Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis were higher after administration of 1 g cefotiam than after administration of 1.5 g cefuroxime and 2 g cefazolin, respectively.
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PMID:[Evaluation of the so-called basic cephalosporins using the serum bactericidal test]. 154 83

Meropenem, a new broad-spectrum carbapenem antibiotic, demonstrated excellent in vitro activity against major respiratory pathogens including Moraxella catarrhalis, Haemophilus influenzae and Streptococcus pneumoniae. Minimal inhibitory concentrations of meropenem for Moraxella catarrhalis and Haemophilus influenzae isolates were frequently less than those of imipenem. For nosocomial amikacin-resistant gram-negative bacilli, meropenem had eightfold lower MIC90 values compared to imipenem against strains of Serratia marcescens, Enterobacter cloacae and Escherichia coli; it was 32-fold more active than imipenem against Proteus mirabilis isolates. Activity was similar to that of imipenem against Pseudomonas aeruginosa isolates. Overall, meropenem showed excellent activity against common community-acquired pathogens as well as amikacin-resistant nosocomial pathogens.
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PMID:Comparative activity of meropenem (SM-7338) against major respiratory pathogens and amikacin-resistant nosocomial isolates. 156 88

The aminothiazolyl-cephalosporin RU 29 246 is the active metabolite of the prodrug-pivaloyl-oxyethyl-ester HR 916. RU 29 246 in vitro activity includes a wide range of clinically relevant bacterial pathogens. Against methicillin-sensitive Staphylococci RU 29 246 (MIC90 of 0.25 approximately 2 micrograms/ml) was clearly more active than cefaclor, cefuroxime, cefpodoxime, cefixime and ceftibuten, but slightly less active than cefdinir. RU 29 246 inhibited hemolytic Streptococci of the serogroups A, B, C and G as well as penicillin-sensitive Streptococcus pneumoniae at concentrations similar to cefdinir, cefpodoxime and cefuroxime (MIC90 less than or equal to 0.13 micrograms/ml), but less than the other oral cephalosporins investigated (cefixime, cefaclor and ceftibuten). MIC90s of RU 29 246 against Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Salmonella spp., Shigella spp., Proteus mirabilis and Haemophilus influenzae were less than or equal to 0.5 micrograms/ml. Only RU 29 246 and cefdinir demonstrated moderate activity against Acinetobacter baumannii (MIC90 greater than or equal to 4 micrograms/ml). Most strains of Pseudomonas spp., Serratia marcescens, Enterobacter spp., Hafnia alvei and Bacteroides spp. were resistant to RU 29 246. RU 29 246 killed Escherichia coli and Staphylococcus aureus at a rate of 99% to 99.9% at concentrations of two times MIC. The pH value of the medium (range 5.5 to 8.5) and the inoculum size (range 10(5) to 10(7) cfu/ml) had no or only low influence on the antibacterial activity of RU 29 246. RU 29 246 is a broad spectrum cephalosporin including in its activity both Gram-positive and Gram-negative pathogens and therefore--depending on the bioavailability of its prodrug--looks promising as to its therapeutic perspective.
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PMID:RU 29 246, the active compound of the cephalosporin-prodrug-ester HR 916. I. Antibacterial activity in vitro. 159 83

The in vitro activity of cefquinome, a new aminothiazolyl cephalosporin with a C-3 bicyclic pyridinium group, was compared with ceftazidime, cefpirome, and cefepime. Cefquinome inhibited members of the Enterobacteriaceae at less than or equal to 0.5 microgram/ml for Escherichia coli, Klebsiella pneumoniae, K. oxytoca, Citrobacter diversus, Salmonella Shigella, Proteus mirabilis, Morganella, and Providencia. Although most Citrobacter freundii and Enterobacter cloacae were inhibited by less than 2 micrograms/ml, some strains resistant to ceftazidime were resistant, [minimum inhibitory concentration (MIC) greater than 16 micrograms/ml]. Serratia marcescens were inhibited by less than 1 microgram/ml and Pseudomonas aeruginosa by 8 micrograms/ml similar to the activity of cefepime. The majority of Haemophilus influenzae and Neisseria gonorrhoeae were inhibited by less than 0.25 microgram/ml. Most enterococci had cefquinome MICs of 4-8 micrograms/ml. Cefquinome was extremely active against group-A streptococci and Streptococcus pneumoniae with MICs less than 0.12 microgram/ml. 90% of methicillin-susceptible Staphylococcus aureus 90% were inhibited by 2 micrograms/ml. Overall, the in vitro activity of cefquinome was comparable with aminothiazolyl cephalosporins. It inhibited some Enterobacter and Citrobacter freundii resistant to ceftazidime as did cefpirome and cefepime. Cefquinome was not destroyed by the common plasmid beta-lactamases TEM-1, TEM-2, SHV-1, or by the chromosomal beta-lactamases of Klebsiella, Branhamella, and Pseudomonas, but it was hydrolyzed by TEM-3, TEM-5, and TEM-9. Its activity was not adversely decreased in different medium or protein, and minimum bactericidal concentrations (MBCs) for most species except for Enterobacter were within a dilution of MICs.
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PMID:In vitro activity of cefquinome, a new cephalosporin, compared with other cephalosporin antibiotics. 161 48

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.
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PMID:Review of the in vitro antibacterial activity of cefprozil, a new oral cephalosporin. 161 37

Loracarbef is a new oral antimicrobial of the carbacephem class with in vitro activity against the common pathogens associated with skin infections, otitis media, sinusitis, bronchopulmonary infections, and urinary tract infections. A review of the literature shows the following ranges for 90% minimum inhibitory concentration (MIC90) values (microgram/mL) against the organisms that commonly cause these illnesses: Streptococcus pneumoniae, 0.25-2.0; Moraxella (Branhamella) catarrhalis (beta-lactamase positive), 0.5-8.0; M. catarrhalis (beta-lactamase negative), 0.12-0.25; Haemophilus influenzae (beta-lactamase positive), 0.5-16.0; H. influenzae (beta-lactamase negative), 0.25-8.0; Escherichia coli, 2.0-25; Klebsiella pneumoniae, 0.25-8.0; Proteus mirabilis, 1.0-8.0; Streptococcus pyogenes, less than or equal to 0.06-1.0; Staphylococcus aureus (beta-lactamase positive), 8.0; S. aureus (beta-lactamase negative), 1.0-2.0. The in vitro activity of loracarbef against these common outpatient pathogens is similar to that of other oral antimicrobials such as cefaclor, cefuroxime axetil, cefixime, amoxicillin/clavulanate, and trimethoprim/sulfamethoxazole. The results of in vitro susceptibility tests with any antimicrobial, including loracarbef, are somewhat dependent on the specific test method that is employed in the laboratory. This is particularly true with H. influenzae. Furthermore, the results of loracarbef susceptibility tests are of uncertain value in predicting therapeutic outcome.
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PMID:In vitro activity of loracarbef and effects of susceptibility test methods. 162 48

The therapeutic perspectives of flomoxef, SCE 2787, cefpirome, cefepime, latamoxef, cefotaxime and of piperacillin plus tazobactam were comparatively evaluated by their in vitro activity against 1119 clinical isolates of 83 bacterial species. Escherichia coli, Klebsiella spp. Enterobacter sakazakii, Proteus spp. and Shigella spp. were about equally susceptible to the cephalosporins (MIC90: 0.06 to 0.5 mg/l), while the MIC90 for piperacillin plus tazobactam was between 2 and 16 mg/l. Enterobacter cloacae, Enterobacter aerogenes and Serratia spp. were most susceptible to SCE 2787, cefpirome and cefepime (MIC90: 0.06 to 2 mg/l) followed by latamoxef, cefotaxime, flomoxef and piperacillin plus tazobactam. For Citrobacter spp., Providencia spp. and Yersinia enterocolitica MIC90 were between 0.06 and 0.5 mg/l. Flomoxef was between 2 to 4 log2 less active against these species but more active than piperacillin plus tazobactam (MIC90: 2 and 8 mg/l). Morganella morganii and Hafnia alvei were most susceptible to cefepime, cefpirome and latamoxef (MIC90: 0.13 to 0.5 mg/l) while cefotaxime (MIC90: 8 mg/l) and piperacillin plus tazobactam (MIC90: 8 and greater than 64 mg/l) were the least active compounds. SCE 2787, cefepime and cefpirome were the most potent beta-lactams against the majority of the 13 species of non-fermentative bacilli (NFB) investigated (MIC90: 0.5 to 16 mg/l). The oxacephems were the least active compounds against NFB. Cefepime was the most active of the compounds included against Pseudomonas aeruginosa (MIC90: 16 mg/l). Haemophilus spp., Neisseria gonorrhoeae and Bordetella pertussis were most susceptible to cefotaxime (MIC90: 0.03 to 0.06 mg/l). Latamoxef had the lowest activity of all compounds against gram-positive cocci. Flomoxef was the most active compound against penicillinase producing Staphylococcus aureus and about equally active as the other betalactams against methicillin susceptible staphylococci of other staphylococcal species.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:In vitro activity and stability against novel beta-lactamases of investigational beta-lactams (cefepime, cefpirome, flomoxef, SCE2787 and piperacillin plus tazobactam) in comparison with established compounds (cefotaxime, latamoxef and piperacillin). 166 18


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