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Biomedical subjects

R Wise

Publications and source records attributed to R Wise.

At least 451 records · Page 25Linked to original sources

The influence of protein binding upon tissue fluid levels of six beta-lactam antibiotics.

The effect of protein binding upon the penetration of six-beta-lactam (three penicillins and three cephalosporins) antibiotics into tissue fluid was studied in humans. A cantharides blister technique was used. It was found that there was a linear relationship between the percentage of protein binding and the penetration into the blister fluid of the antibiotic as measured by the area under the curve of the protein-free fraction. This finding is further evidence that protein binding may have important influence upon the likely efficacy of an antimicrobial agent.

Adult↗

Activity of the cefotaxime (HR756) desacetyl metabolite compared with those of cefotaxime and other cephalosporins.

The desacetyl metabolite (DES) of cefotaxime (HR756) is formed in vivo to a significant extent. The in vitro activities of DES, the parent compound, and cefazolin, cefoxitin, and cefuroxime were compared against 70 bacterial isolates. DES was found to possess approximately 1/10th the activity of the parent compound against the common Enterobacteriaceae, but was somewhat more active than the other three compounds tested. DES had no useful activity against Pseudomonas aeruginosa and was less active than cefotaxime or cefoxitin against Staphylococcus aureus or Bacteroides fragilis. Because DES may accumulate in renal failure or be concentrated in the biliary tract, its antimicrobial activity may have considerable clinical significance.

Bacteria↗

UK31214, a new aminoglycoside and derivative of kanamycin B.

The in vitro activity of UK31214, a kanamycin B derivative, was studied against 250 recent isolates and compared with other aminoglycosides. Against the Enterobacteriaceae (with the exception of Proteus mirabilis and Providencia stuartii) UK31214 and amikacin had similar degrees of activity (mode minimum inhibitory concentration [MIC], 1 microgram/ml). Proteus mirabilis and P. stuartii strains were four- to eight-fold more susceptible to amikacin than to UK31214. Pseudomonas aeruginosa strains were equally susceptible to both amikacin and UK31214 (mode MIC, 4 microgram/ml), but tobramycin was the most active antimicrobial agent tested (mode MIC, 0.25 microgram/ml). The gentamicin-resistant strains of P. aeruginosa were equally susceptible to UK31214 and amikacin. Strains of Staphylococcus aureus were more susceptible to gentamicin or tobramycin than to UK31214 or amikacin (mode MIC, 0.5 microgram/ml). A synergistic interaction between UK31214 and carbenicillin was demonstrated.

Drug Resistance, Microbial↗

Comparison of in vitro activity of GR 20263, a novel cephalosporin derivative, with activities of other beta-lactam compounds.

The in vitro activity of GR 20263, a new cephalosporin, was compared primarily with the activities of moxalactam (LY 127935), cefotaxime, cefoxitin, cefuroxime, and cefazolin against 293 clinical isolates of a variety of gram-positive and -negative bacteria. The minimal inhibitory concentrations of GR 20263 for 90% of group isolates were between 0.06 and 0.5 microgram/ml for the Enterobacteriaceae, Haemophilus influenzae, Neisseria gonorrhoeae, and Lancefield group A beta-hemolytic streptococci; 2 micrograms/ml for Pseudomonas aeruginosa; 16 micrograms/ml for Staphylococcus aureus; and in excess of 128 micrograms/ml for Bacteroides fragilis and Lancefield group D streptococci. In comparison with the other agents, GR 20263 was markedly more active against the Enterobacteriaceae than cefuroxime, cefoxitin, and cefazolin, but marginally less active than moxalactam or cofotaxime. Aganist S. aureus, cefazolin was 16-fold and cefotaxime was 4-fold more active than GR 20263 and moxalactam. GR 20263 was eight-fold more active than cefotaxime and moxalactam against P. aeruginosa.

Anti-Bacterial Agents↗

Pharmacokinetics of Ro 13-9904, a broad-spectrum cephalosporin.

The pharmacokinetics of the new cephalosporin Ro-13-9904 were studied in six healthy male volunteers receiving a 500-mg dose as a bolus intravenously. Tissue penetration of the antibiotic was estimated by using a cantharides blister method. The data obtained fitted a two-compartment open model. The mean elimination half-life was about 8 h, which is considerably longer than that of other beta-lactam compounds. The distribution volume was 4.3 liters in the central compartment. Levels of Ro 13-9904 in blister fluid exceeded those in serum after 6.5 h. Approximately 60% of the antibiotic was excreted in the urine.

Adult↗

Comparison of cefotaxime and moxalactam pharmacokinetics and tissue levels.

The pharmacokinetics of cefotaxime and moxalactam were compared in six healthy male volunteers aftr the administration of 1-g doses intravenously. Penetration of the compounds into tissue fluid was studied in cantharides-induced blisters. Both serum and tissue fluid levels of moxalactam were higher than those of cefotaxime. The elimination half-life of cefotaxime was 1.2 h, and that of moxalactam was 2.85 h. On the average, 50.5% of cefotaxime and 87.5% of moxalactam were recovered in the urine in 24 h.

Adult↗

Comparison of sensititre dried microtitration trays with a standard agar method for determination of minimum inhibitory concentrations of antimicrobial agents.

A total of 222 clinical isolates were used to test the accuracy of Sensititre dried microtitration trays for determining minimum inhibitory concentrations (MICs) of antimicrobial agents. In comparison with an agar dilution technique, 89.5% of all the pairs of results were within one doubling dilution. The 2,420 pairs of MIC results with finite values gave a corresponding figure of 86.8%. Exclusion of sulfisoxazole results, which demonstrated a significant interlaboratory variation in accuracy, raised this value to 89.1%. Very good differentiation of beta-lactamase-producing strains of Staphylococcus aureus (24 of 24 giving an MIC greater than or equal to 0.25 micrograms/ml) and Haemophilus influenzae (3 of 3 giving an MIC greater than or equal to 32 micrograms/ml) was obtained with the Sensititre system. This method also clearly distinguished erythromycin-resistant S. aureus strains (7 of 7 giving an MIC greater than 32 micrograms/ml) from the susceptible strains (26 of 28 giving an MIC less than or equal to 0.5 microgram/ml plus 1 strain at 1.0 microgram/ml and 1 at 2.0 micrograms/ml). Sensititre offers an accurate and convenient method of determining MICs comparable to those obtained with the agar dilution procedure, with the advantage of an extended shelf life when stored at room temperature.

Aminoglycosides↗

A unit for source and protective isolation in a general hospital.

An isolation unit consisting of 12 ventilated cubicles was investigated over 18 months. Out of 462 patients admitted, 262 (57%) required source and 200 (43%) protective isolation. Admissions of patients with staphylococcal sepsis fell from 16 in the first three months to six in the last three months. Staphylococcus aureus was recovered from 12% of nurses' fingers and often in small numbers from protective clothing and uniforms, but only two patients acquired a strain from a nurse or another patient. Gram-negative bacilli were rarely recovered from hands or protective clothing of nurses, and there was no evidence of spread of infectious diseases. This inexpensive unit, with simple but efficient isolation-nursing techniques, successfully prevented the spread of infection.

Air Microbiology↗