[In vitro activities of sulopenem, a new parenteral penem, against anaerobes].
In vitro activities of sulopenem, a novel parenteral penem, was compared with those of imipenem, flomoxef, cefuzonam, cefoperazone and sulbactam/ampicillin against 66 reference strains (19 genera, 61 species) and 392 recent clinical isolates of anaerobic bacteria and fastidious aerobic bacteria. Sulopenem had a very broad spectrum against anaerobic bacteria. In general, this compound was active against anaerobic reference strains with MICs of < or = 0.78 micrograms/ml, while being the least active against Bifidobacterium spp. and less active than imipenem against Lactobacillus spp. Sulopenem was more active against Bacteroides fragilis isolates than imipenem and had the highest activities against Bacteroides thetaiotaomicron, Prevotella intermedia, Porphyromonas gingivalis, Fusobacterium spp. and Peptostreptococcus spp. among the antibiotics tested. Sulopenem was not hydrolyzed by oxyiminocephalosporinase type 1 produced by B. fragilis GAI-0558, GAI-7955 and GAI-10150 and its stability was comparable to imipenem. Its susceptibilities to hydrolysis by a metallo-beta-lactamase from B. fragilis GAI-30144 was less than imipenem. Sulopenem (120 mg/kg, 3 times a day for 4 days) was as effective as imipenem/cilastatin against a mixed intraabdominal mice infection due to E. coli and B. fragilis. Sulopenem (20 mg/kg twice a day for 5 days) did not induce an overgrowth of Clostridium difficile in the caecum of mice.
Watanabe
K
K
Institute of Anaerobic Bacteriology, Gifu University School of Medicine.
Kato
N
N
Tanaka-Bandoh
K
K
Tanaka
Y
Y
Kato
H
H
Ueno
K
K
D000667:Ampicillin / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001421:Bacteria, Anaerobic / Q000187:drug effects*; D002432:Cecum / Q000382:microbiology; D002438:Cefoperazone / Q000494:pharmacology; D015296:Ceftizoxime / Q000031:analogs & derivatives / Q000494:pharmacology; D002511:Cephalosporins / Q000494:pharmacology; D016360:Clostridioides difficile / Q000187:drug effects; D004355:Drug Stability; D004359:Drug Therapy, Combination / Q000494:pharmacology; D015378:Imipenem / Q000494:pharmacology; D007769:Lactams; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D013407:Sulbactam / Q000494:pharmacology; D013845:Thienamycins / Q000494:pharmacology; D001618:beta-Lactamases / Q000494:pharmacology; D047090:beta-Lactams
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D007769:Lactams; D013845:Thienamycins; D047090:beta-Lactams; C082897:sulopenem; C035444:sultamicillin; D015378:Imipenem; D000667:Ampicillin; D002438:Cefoperazone; C049934:cefuzonam; D015296:Ceftizoxime; D001618:beta-Lactamases; D013407:Sulbactam