In-vitro and in-vivo antibacterial activity of imipenem against clinical isolates of bacteria.
Imipenem, a derivative of thienamycin, a carbapenem antibiotic, has a broad spectrum of activity against aerobic (Gram-positive and Gram-negative) and anaerobic bacteria. It is quite stable to all tested beta-lactamases produced by various species of bacteria isolated from clinical specimens, whether plasmid or chromosomally mediated. One exception is its hydrolysis by the beta-lactamase produced by Pseudomonas maltophilia which is thus usually resistant to imipenem. Imipenem was found to be hydrolysed by renal dehydropeptidase-I residing on the luminal surface of the renal tubular epithelium. A dehydropeptidase-I inhibitor, cilastatin (MK-0791) was developed with specific inhibitory activity toward the renal dehydropeptidase-I and showed detectable effects in humans.
D000818:Animals; D001419:Bacteria / Q000187:drug effects*; D001426:Bacterial Proteins; D002352:Carrier Proteins / Q000378:metabolism; D004150:Dipeptidases / Q000037:antagonists & inhibitors / Q000378:metabolism; D004352:Drug Resistance, Microbial; D004355:Drug Stability; D006602:Hexosyltransferases; D006801:Humans; D015378:Imipenem; D007668:Kidney / Q000201:enzymology; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008826:Microbial Sensitivity Tests; D002267:Muramoylpentapeptide Carboxypeptidase / Q000378:metabolism; D046915:Penicillin-Binding Proteins; D010458:Peptidyl Transferases; D013552:Swine; D013845:Thienamycins / Q000378:metabolism / Q000494:pharmacology*; D001618:beta-Lactamases / Q000378:metabolism
D001426:Bacterial Proteins; D002352:Carrier Proteins; D046915:Penicillin-Binding Proteins; D013845:Thienamycins; D015378:Imipenem; D010458:Peptidyl Transferases; D006602:Hexosyltransferases; D004150:Dipeptidases; C038937:dipeptidase; D002267:Muramoylpentapeptide Carboxypeptidase; D001618:beta-Lactamases