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Biomedical subjects

R Wise

Publications and source records attributed to R Wise.

At least 235 records · Page 13Linked to original sources
PubMed1991

In-vitro activity and beta-lactamase stability of SR 44337, a new long acting cephalosporin.

The in-vitro activity of SR 44337 was compared with that of other broad-spectrum parenteral cephalosporins, plus imipenem and co-amoxiclav. SR 44337 showed good activity against the Enterobacteriaceae, with MIC90s of less than 0.5 mg/L against all species tested, with the exception of Citrobacter spp. (MIC90 2 mg/L) and Serratia spp. (MIC90 4 mg/L). Of the agents tested, only ceftriaxone showed consistently greater activity against this family of organisms. SR 44337 had higher activity than ceftriaxone against Acinetobacter spp. and Pseudomonas aeruginosa, and was the most active agent tested against Neisseria meningitidis (MIC90 0.004 mg/L). All strains of N. gonorrhoeae, Haemophilus influenzae and the streptococci (excluding the enterococci) were susceptible to less than or equal to 0.25 mg/L of SR 44337, which was also the most active cephalosporin tested against Staphylococcus aureus. SR 44337 was stable to hydrolysis by the TEM-1, SHV-1 and P99 beta-lactamases, and was more stable than ceftriaxone to the K-1 beta-lactamase.

Amoxicillin↗
PubMed1991

The in-vitro activity of cefdinir (FK482), a new oral cephalosporin.

The in-vitro activity of cefdinir (FK482), an orally absorbed aminothiazolyl cephalosporin, was compared with that of cefuroxime, cefixime, cephalexin, cefaclor and co-amoxiclav. Cefdinir was highly active against Staphylococcus aureus, inhibiting 90% of strains at 0.03 mg/L. The respiratory pathogens Haemophilus influenzae, Streptococcus pneumoniae, and Moraxella catarrhalis were also susceptible (MIC90 less than or equal to 1 mg/L). The common members of the Enterobacteriaceae were susceptible (MIC90 less than or equal to 1 mg/L), but those possessing chromosomal beta-lactamases were more resistant. Cefdinir appeared highly stable to the TEM-1 and SHV-1 beta-lactamases with only relatively minor degrees of hydrolysis being seen with TEM-3, -5 and -9.

Bacteria↗
PubMed1991

Bactericidal activity of sparfloxacin and ciprofloxacin under anaerobic conditions.

The kill kinetics of sparfloxacin and ciprofloxacin have been investigated under anaerobic conditions against Bacteroides fragilis and Escherichia coli. The results for E. coli were compared with those obtained under aerobic conditions. It was found that the quinolones were bactericidal under anaerobic conditions. This bactericidal activity is inhibited by the presence of chloramphenicol, a known protein synthesis inhibitor. Filamentation was seen with B. fragilis after 2 h exposure to either agent.

Anaerobiosis↗
PubMed1991

In-vitro susceptibility of Chlamydia pneumoniae (TWAR) to seven antibiotics.

A modification of an immunofluorescence method previously used to study the in-vitro antimicrobial susceptibilities of Chlamydia trachomatis was used to investigate the activity of seven antimicrobials against a strain of C. pneumoniae. Our results differed from those obtained by other workers, so we modified our original method and repeated the study. Adding antimicrobial to pre-infected cells gave higher MICs and MLCs than when cells were infected in the presence of the antimicrobials, and this difference in methodology could account for the discrepancy between our results and those of others. Of the antimicrobials studied, clarithromycin and its 14-hydroxy metabolite were the most active agents; sparfloxacin was more active than ciprofloxacin, but no more active than more conventional antichlamydial agents.

Anti-Bacterial Agents↗
PubMed1991

Pharmacokinetics and tissue penetration of rufloxacin, a long acting quinolone antimicrobial agent.

The pharmacokinetics of rufloxacin after a single 400 mg oral dose were studied in eight volunteers, measuring plasma, inflammatory fluid and urine concentrations. Mean peak plasma concentrations of 4.4 mg/L were achieved at a mean time of 1.9 h after administration. The mean plasma elimination half-life was 28.2 h. Mean peak levels in inflammatory fluid reached 3.2 mg/L after 3.5 h, and 30.7% of the dose was eliminated in urine by 96 h. The apparent mean volume of distribution of rufloxacin, at steady state, was 109.5 L. The mean percentage penetration of rufloxacin into the inflammatory exudate, as measured by ratios of AUC0-50 h was 90%.

Administration, Oral↗
PubMed1991

Comparative pharmacokinetic disposition of fluoroquinolones in the lung.

The problems associated with the study of the penetration of quinolones into the respiratory tract are discussed. New techniques allow the study of the penetration of these agents into bronchial mucosa, alveolar macrophages and epithelial lining fluid. In general quinolones are concentrated in bronchial mucosa approximately 1.5 times compared with serum. In alveolar macrophages, the agents are concentrated 14- to 18-fold compared with serum and the ratio of alveolar macrophage levels to those in epithelial lining fluid are 7.7 to 5.7:1. The concentrations of temafloxacin and ciprofloxacin in these sites suggests that these agents will be efficacious in the therapy of respiratory infections caused by Streptococcus pneumoniae.

Administration, Oral↗
PubMed1991

In vitro activity of a catechol-substituted cephalosporin, GR69153.

The in vitro activity of GR69153, a new catechol-substituted cephalosporin, was compared with those of ceftazidime, imipenem, meropenem, and ceftriaxone against 604 recent clinical isolates and other strains with known mechanisms of resistance. The MICs of GR69153 for 90% of the members of the family Enterobacteriaceae tested were less than 0.5 micrograms/ml, with the exceptions of those for Serratia spp. (4 micrograms/ml), Citrobacter spp. (2 micrograms/ml), and Enterobacter spp. (8 micrograms/ml). Ninety percent of Pseudomonas aeruginosa isolates were susceptible to less than or equal to 1 microgram of GR69153 per ml. With the exception of methicillin-resistant strains, 90% of Staphylococcus aureus isolates were susceptible to less than or equal to 2 micrograms/ml, and GR69153 was four- to eightfold more active than ceftazidime and ceftriaxone against these strains. Isolates of Haemophilus influenzae, Branhamella catarrhalis, Neisseria spp., and Streptococcus pneumoniae (penicillin susceptible) were highly susceptible (MIC for 90% of the strains, less than or equal to 0.12 micrograms/ml). GR69153 was stable to hydrolysis by the TEM-1 and TEM-5, SHV-1 and SHV-2, and K1 beta-lactamases, but some susceptibility to hydrolysis by the TEM-3, TEM-9, and P99 enzymes was observed. The protein-binding activity of GR69153 was 74.5 to 66.8%, depending on the concentration, and serum had little effect upon activity.

Bacteria↗
PubMed1991

Pharmacokinetics and tissue penetration of tazobactam administered alone and with piperacillin.

The pharmacokinetics of tazobactam (500 mg) administered intravenously alone were compared with the pharmacokinetics of tazobactam coadministered with piperacillin (4 g), and the penetration into an inflammatory exudate in six healthy males was studied. Piperacillin influenced the pharmacokinetics of tazobactam. The mean levels of tazobactam in plasma at 4 h were 0.6 microgram/ml when it was given alone and 1.2 micrograms/ml when it was given with piperacillin (P = 0.0003). The mean total clearances of tazobactam were 203.5 and 134.2 ml/min (P = 0.035) when it was given alone and with piperacillin, respectively There were no significant differences in the elimination half lives, areas under the concentration-time curve from 0 h to infinity, or volumes of distribution. Inflammatory exudate penetration was rapid, and the mean maximum levels of tazobactam attained were 6.4 and 11.3 micrograms/ml when it was given alone or with piperacillin, respectively (P less than 0.06). The mean percent penetration of tazobactam and the area under the concentration-time curve from 0 h to infinity in inflammatory exudate were greater when tazobactam was given with piperacillin. The mean 24-h urinary recoveries of tazobactam were 63.7% +/- 7.9% when it was given alone and 56.8% +/- 2.7% when it was given with piperacillin. The explanation for the differences in the pharmacokinetics of tazobactam when it was administered alone compared with those when it was given with piperacillin was unclear.

Adult↗
PubMed1991

Microlavage: a technique for determining the volume of epithelial lining fluid.

A new technique ("microlavage") was used to determine the volume of epithelial lining fluid recovered by bronchoalveolar lavage. A standard bronchial brush tube is used to lavage a peripheral lung subsegment rapidly with 20 ml of normal saline and the concentrations of urea and total protein are measured in the aspirated fluid. Using a very short dwell time for fluid (less than 20 seconds), this technique allows the urea dilution method to be used to quantify the epithelial lining fluid protein concentration, which is then used as an endogenous marker of the epithelial lining fluid in conventional bronchoalveolar lavage fluid. The reproducibility of the calculation of the concentration of the lining fluid protein was assessed in 10 patients by performing the method in three separate lung subsegments. The mean coefficient of variation of the urea to protein ratio was 9.0%. A comparison of microlavage and conventional lavage was made in a further 28 patients. The differential cell counts were similar by the two methods, suggesting that similar epithelial lining fluid was sampled. The application of the microlavage technique to the calculation of epithelial lining fluid volume gave a lower value than the urea dilution method in association with conventional lavage. Microlavage should provide more accurate quantification of epithelial lining fluid volume and could be used in conjunction with conventional lavage, which is still required for an adequate harvest of alveolar cells.

Aged↗