Optimization of dose and dose regimen of biapenem based on pharmacokinetic and pharmacodynamic analysis.

Pharmacokinetic and pharmacodynamic (PK/PD) parameters, which are important indices of the therapeutic efficacy of antimicrobials, and the minimum inhibitory concentration (MIC) predictive of clinical efficacy at common clinical doses, were examined for biapenem (BIPM; 300 mg b.i.d.

[Activity of fosfomycin against Escherichia coli O157:H7--morphological changes and production of Shiga toxins].

We examined the effects of fosfomycin (FOM), norfloxacin (NFLX), kanamycin (KM), chloramphenicol (CP), and ampicillin (ABPC) on the morphology of E. coli O157:H7, and the accumulation (cell fraction) and release (medium fraction) of Shiga toxins (Stxs: Stx1 and Stx2) in E. coli O157:H7 three hours after treatment with the antibiotics.

[Antimicrobial activity of fosfomycin against beta-lactamase-producing methicillin-sensitive Staphylococcus aureus and methicillin-sensitive coagulase-negative staphylococci].

Antimicrobial activity of fosfomycin (FOM), cefazolin (CEZ), cefmetazole (CMZ), cefotiam (CTM) and piperacillin (PIPC) against clinical isolates of methicillin-sensitive Staphylococcus aureus (MSSA) (beta-lactamase-producing or non-producing) and methicillin-sensitive coagulase-negative Staphylococci (MSCNS) (beta-lactamase-producing or non-producing) were determined to make clear the differences in antimicrobial activity of FOM and beta-lactam antibiotics. The antimicrobial activity of PIPC against beta-lactamase-producing strains of MSSA was lower than that against non-producing ones, judging from the distribution patterns of susceptibility of the strains to PIPC. There were no differences in the antimicrobial activity of FOM, CEZ and CMZ for the producing and non-producing strains.

[Antibacterial activity of biapenem against recent clinical isolates].

Antibacterial activity of biapenem (BIPM) against clinical isolates of 8 species between 2000 and 2002 was compared with those of imipenem/cilastatin (IPM/CS), meropenem (MEPM), panipenem/betamipron (PAPM/BP) and ceftazidime (CAZ). The MICs of biapenem for Gram-positive bacteria were higher than those of IPM/CS and PAPM/BP, equal to those of MEPM and lower than those of CAZ. The MICs of BIPM for Gram-negative bacteria were higher than those of MEPM, equal to those of IPM/CS and PAPM/BP, and lower than those of CAZ.

[Inhibitory activity of NM394, the active form of prodrug prulifloxacin against type II topoisomerase from Pseudomonas aeruginosa].

The inhibitory activity of NM394, the active form of the prodrug prulifloxacin, against type II topoisomerase from Pseudomonas aeruginosa was compared with those of ciprofloxacin (CPFX), levofloxacin (LVFX) and gatifloxacin (GFLX). The 50% inhibitory concentrations (IC50S) of NM394 for supercoiling activity of DNA gyrase and the decatenation activity of topoisomerase IV were 1.21 and 21.

[Antibacterial activities of fosfomycin against several fresh clinical isolates--comparison of the test methods for antibacterial activity].

In vitro antibacterial activity of fosfomycin was evaluated by various methods. Strains of methicillin-sensitive Staphylococcus aureus, methicillin-sensitive coagulase-negative Staphylococci and Escherichia coli were much more susceptible when glucose-6-phosphate was added to the test medium, but strains of Serratia marcescens and Pseudomonas aeruginosa were not affected. Nutrient agar instead of Mueller-Hinton agar allowed to exhibiting the higher activity of fosfomycin against all the species tested.

[In vitro short-term bactericidal activity and accumulation of NM394, the active metabolite of prulifloxacin, for Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa: comparison with ciprofloxacin, levofloxacin, and gatifloxacin].

The in vitro short-term bactericidal activity and accumulation of NM394, the active metabolite of prulifloxacin, was compared with those of ciprofloxacin (CPFX), levofloxacin (LVFX) and gatifloxacin (GFLX), using Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Of the 4 fluoroquinolones examined, NM394 accumulated to the highest concentration in all three strains. The order of concentration of the fluoroquinolones accumurated in S.

[In vitro antibacterial activity of prulifloxacin, a new oral fluoroquinolone].

We compared antibacterial activity of NM394, which is the active metabolite of a prodrug of new fluoroquinolone prulifloxacin (PUFX), against clinical isolates of bacteria with those of ciprofloxacin (CPFX), levofloxacin (LVFX), gatifloxacin (GFLX), tosufloxacin (TFLX) and fleroxacin (FLRX). 1. NM394 showed a broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria.

PF1163A, a novel antifungal agent, inhibit ergosterol biosynthesis at C-4 sterol methyl oxidase.

PF1163A and B are a pair of antifungal agents isolated from a fermentation broth of Penicillium sp. PF1163A inhibited ergosterol synthesis in Saccharomyces cerevisiae, resulting in an accumulation of 4,4-dimethylzymosterol and a decrease of ergosterol. The ERG25 strain overexpressing the ERG25 gene was resistant to PF1163A.