GR 20263, a new broad-spectrum cephalosporin with anti-pseudomonal activity.
GR 20263 is a new broad-spectrum injectable cephalosporin which is stable to most beta-lactamases. Its in vitro activities were of the same order as those of cefotaxime against most gram-negative bacteria, were clearly inferior to cefotaxime against Staphylococcus aureus, but were significantly more active against Pseudomonas aeruginosa. Against the 25 strains used, GR 20263 was significantly more active than any of the other agents tested: piperacillin, azlocillin, gentamicin, amikacin, and carbenicillin. GR 20263 protected mice against experimental infections with P. aeruginosa more effectively than other beta-lactam antibiotics; its general effectiveness in this test was comparable with gentamicin. Studies on human volunteers showed that it produces high, long-lasting blood levels, with much of the antibiotic being recovered in the urine. Intramuscular and intravenous injections were well tolerated by the volunteers, and there were no untoward side effects.
D000328:Adult; D000818:Animals; D001419:Bacteria / Q000187:drug effects; D001424:Bacterial Infections / Q000188:drug therapy; D001798:Blood Proteins / Q000378:metabolism; D002442:Ceftazidime; D002511:Cephalosporins / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D006801:Humans; D006868:Hydrolysis; D007273:Injections, Intramuscular; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D008875:Middle Aged; D011339:Probenecid / Q000494:pharmacology; D011485:Protein Binding; D011549:Pseudomonas / Q000187:drug effects*; D001618:beta-Lactamases / Q000378:metabolism
D001798:Blood Proteins; D002511:Cephalosporins; D002442:Ceftazidime; D001618:beta-Lactamases; D011339:Probenecid