Basic and clinical studies have been performed on
imipenem/cilastatin sodium (
MK-0787/
MK-0791) in the pediatric field. Antibacterial activities of
MK-0787 against 14 clinical isolates of S. aureus and 67 isolates of E. coli were determined. The MIC of
MK-0787 was 0.10 microgram/ml or less against all 14 strains of S. aureus. The MIC of
MK-0787 was 0.39 microgram/ml or less against all 67 strains of E. coli. The pharmacokinetics of
MK-0787/
MK-0791 was studied at dose levels of 10 mg/10 mg/kg and 20 mg/20 mg/kg. The peak serum levels of
MK-0787 achieved approximately 1 hour after the administration of 10 mg/10 mg/kg and 20 mg/20 mg/kg doses were 38.6 micrograms/ml and 36.2 micrograms/ml, respectively. The serum half-lives were 0.8 hour and 0.9 hour, respectively. The total 6-hour urinary excretions were 82.1% and 66.7%, respectively. The
MK-0787/
MK-0791 was administered to 13 children with
bacterial infections. The clinical results were excellent or good in all cases. The overall efficacy rate was 100%. As a side effect,
diarrhea was observed in 1 patient. Abnormalities in laboratory findings observed were elevation of direct
bilirubin in 1 patient,
thrombocytosis in 2, and a prolonged prothrombin time in 1 patient. Based on the above results, it can be concluded that
MK-0787/
MK-0791 is a safe and effective
drug to use for the treatment of pediatric
infections.