[Fundamental and clinical studies on imipenem/cilastatin sodium in pediatrics].
Fundamental and clinical studies were carried out on imipenem/cilastatin sodium (MK-0787/MK-0791) in pediatric patients. The following results were obtained. A total of 238 clinical isolates stocked by our department was employed to determine the minimum inhibitory concentrations (MICs) of MK-0787 against various species of bacteria. The MK-0787 showed strong antibacterial activities against E. coli, Salmonella, Klebsiella, Proteus, Serratia, E. faecalis and S. epidermidis. Somewhat weaker activities were observed against P. aeruginosa and S. aureus. The MK-0787/MK-0791 was drip-infused intravenously into patients over a period of 1 hour, and serum levels of MK-0787 and MK-0791 were determined. At the dose level of 10 mg/10 mg/kg, the mean serum levels of MK-0787 and MK-0791 were 29.9 micrograms/ml and 18.1 micrograms/ml at 1 hour and 3.4 micrograms/ml and 1.3 micrograms/ml at 3 hours, respectively. The half-lives were 0.89 hour for MK-0787 and 0.99 hour for MK-0791. At the dose level of 20 mg/20 mg/kg, the mean serum levels of MK-0787 and MK-0791 were 46.3 micrograms/ml and 45.2 micrograms/ml at 1 hour and 5.5 micrograms/ml and 3.1 micrograms/ml at 3 hours, respectively. The half-lives were 0.97 hour for MK-0787 and 0.83 hour for MK-0791. At the dose level of 40 mg/40 mg/kg, the mean serum levels of MK-0787 and MK-0791 were 104.0 micrograms/ml and 80.9 micrograms/ml at 1 hour and 7.8 micrograms/ml and 5.9 micrograms/ml at 3 hours, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
Shiro
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Kusumoto
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Oikawa
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Osano
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D000293:Adolescent; D001419:Bacteria / Q000187:drug effects; D001424:Bacterial Infections / Q000188:drug therapy*; D002648:Child; D002675:Child, Preschool; D015377:Cilastatin; D003521:Cyclopropanes / Q000008:administration & dosage* / Q000378:metabolism / Q000494:pharmacology; D004338:Drug Combinations; D005260:Female; D006801:Humans; D015378:Imipenem; D007223:Infant; D007262:Infusions, Intravenous; D007700:Kinetics; D008297:Male; D013845:Thienamycins / Q000008:administration & dosage* / Q000378:metabolism / Q000494:pharmacology
D003521:Cyclopropanes; D004338:Drug Combinations; D013845:Thienamycins; D015377:Cilastatin; D015378:Imipenem