cefoselis has been researched along with Staphylococcal-Infections* in 2 studies
2 other study(ies) available for cefoselis and Staphylococcal-Infections
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Comparison of the in-vitro and in-vivo efficacy of FK037, vancomycin, imipenem and nafcillin against staphylococcal species.
The activity of methicillin, oxacillin, vancomycin, imipenem and FK037 against 106 isolates of staphylococci was assessed using a microbroth dilution method with low (10(5) cfu/mL) and high (10(7) cfu/mL) inoculum sizes. Overall, FK037, an oxime-type cephem antibiotic, was as active as imipenem, but less active than vancomycin (MIC90s 25, 25 and 6.25 mg/L, respectively) at the lower inoculum. Efficiency of plating experiments were also performed to characterize phenotypic expression of resistance to FK037, imipenem and methicillin. Five of 24 isolates and 18 of 24 isolates contained subpopulations resistant to FK037 and imipenem, respectively. In a rabbit model of endocarditis, FK037 was equally effective as other antibiotics tested in the treatment of methicillin-sensitive Staphylococcus aureus infection. In the treatment of endocarditis due to a homotypic methicillin-resistant S. aureus, FK037 and vancomycin were the most active antibiotics. The presence of subpopulations resistant to imipenem and FK037, as demonstrated by efficiency of plating and high inoculum MIC testing, did not correlate with antibiotic effectiveness in the rabbit model of endocarditis. Cultures of vegetation material following treatment with imipenem and FK037 demonstrated a lower frequency of organisms resistant to FK037 when compared with imipenem. Thus FK037 shows in-vitro and in-vivo activity against some methicillin-resistant staphylococcal species. Topics: Animals; Bacteriological Techniques; beta-Lactam Resistance; Ceftizoxime; Drug Resistance, Microbial; Endocarditis; Imipenem; Methicillin Resistance; Microbial Sensitivity Tests; Nafcillin; Rabbits; Staphylococcal Infections; Staphylococcus; Staphylococcus aureus; Vancomycin | 1997 |
Excellent activity of FK037, a novel parenteral broad-spectrum cephalosporin, against methicillin-resistant staphylococci.
FK037 exhibits potent in vitro and in vivo antibacterial activity against methicillin-resistant staphylococci. In in vitro studies, FK037 was the most active of the cephalosporins and imipenem tested against the highly methicillin-resistant staphylococci (MIC > 100 micrograms/ml). Only 2 of 57 strains of highly methicillin-resistant Staphylococcus aureus (H-MRSA) had a FK037 MIC value of 50 micrograms/ml. On the other hand, 55, 40 and 19 strains had MICs of 50 or > or = 100 micrograms/ml to cefpirome, flomoxef and imipenem, respectively. Against 13 strains of highly methicillin-resistant coagulase-negative staphylococci (H-MRCNS), FK037 inhibited all the strains at < or = 50 micrograms/ml, but there were many strains highly resistant to the reference drugs with MICs of > or = 100 micrograms/ml. The influence of culture conditions such as low temperature, high inoculum and supplementation with 4% NaCl on the anti-MRSA activity of FK037 was less than those with cefpirome, flomoxef and imipenem. The in vitro frequency of spontaneous mutant cells highly resistant to FK037 in MRSA was lower than that to cefpirome and flomoxef. These findings were supported by lack of colonies inside the inhibition zone demarcated by FK037 in a disk sensitivity test, although many colonies proliferated inside the inhibition zone demarcated by flomoxef and imipenem. The increase in MIC of FK037 against a MRSA strain during subculture in the presence of the drug was smaller than that noted with the reference drugs. FK037 had higher affinity and faster binding for the PBP 2a of MRSA than that of the reference drugs. Moreover, the capacity to induce PBP 2a was lower for FK037 than that of cefpirome but higher than that of flomoxef. In an in vitro pharmacokinetic model simulating human plasma concentrations, FK037 showed potent bactericidal activity against H-MRSA in the plasma concentrations after intravenous infusion dosing with 1.0 g. FK037 was synergistically active against H-MRSA in combination with either imipenem of fosfomycin. The in vitro post-antibiotic effect (PAE) of FK037 against H-MRSA ranged from 1.2 to 1.7 hours at one to four times the MIC. FK037 had potent therapeutic effects against lethal systemic infections and experimental local infections in mice such as pneumonia, endocarditis, subcutaneous abscess, intrauterine infection and granuloma pouch infection due to MRSA or methicillin-resistant Staphylococcus epidermidis (MRSE). FK037 was about 4, 8 and 1.5 times mo Topics: Abscess; Animals; Anti-Bacterial Agents; Bacterial Proteins; Carrier Proteins; Ceftizoxime; Cell Membrane Permeability; Drug Synergism; Endocarditis, Bacterial; Female; Granuloma; Hexosyltransferases; Male; Methicillin Resistance; Mice; Mice, Inbred ICR; Microbial Sensitivity Tests; Muramoylpentapeptide Carboxypeptidase; Penicillin-Binding Proteins; Peptidyl Transferases; Pneumonia; Staphylococcal Infections; Staphylococcus aureus; Uterine Diseases | 1993 |