FUNDAMENTAL AND CLINICAL STUDIES WITH IMIPENEM/CILASTATIN SODIUM, A NEW CARBAPENEM ANTIBIOTIC, IN THE FIELD OF PEDIATRICS

Fundamental and clinical evaluations of imipenem/cilastatin sodium (MK-0787/MK-0791) were carried out in pediatric patients. The following results were obtained: 1. After intravenous drip infusion of single doses of 10mg/10mg/kg to 20mg/20mg/kg of MK-0787/MK-0791 in children, peak plasma levels of MK-0787 ranged from 32.0 to 82.0μg/ml at the end of the infusion. The half-life was 49.9 to 64.0 minutes. 2. The cumulative urinary recovery at 6 to 7 hours after the 1 hour drip infusion ranged from 65.5 to 88.9%. 3. Fecal levels of MK-0787 were 4.2 and 23.1μg/g at 6 hours after a 30-minute intravenous drip infusion of 200mg/200mg of MK-0787/MK-0791. 4. MK-0787/MK-0791 was administered by intravenous drip infusion to patients with purulent meningitis. Penetration into the cerebrospinal fluid was satisfactory, as were the clinical responses. 5. MK-0787/MK-0791 was administered clinically in doses of 30mg/30mg/kg/day to 200mg/200mg/kg/day by intravenous drip infusion 3 or 4 times a day for 3 to 22 days to 26 patients with acute pediatric infections. The clinical response was excellent in 18 patients and good in 8 patients. 6. Eradication occurred with 16 isolates; only two strains of Salmonella-B were not eradicated. 7. Anorexia in 1 patient was the only clinical adverse effect reported, and the only adverse effects found in laboratory tests were eosinophilia and thrombocytosis in 1 patient, respectively, and elevation of the S-GOT and S-GPT in 1 patient.