CLINICAL STUDY ON IMIPENEM/CILASTATIN SODIUM IN THE FIELD OF PEDIATRICS
1986 Volume 39 Issue 7 Pages 1817-1827
Details
1986 Volume 39 Issue 7 Pages 1817-1827
Imipenem/cilastatin sodium (MK-0787/MK-0791) was administered to pediatric patients with infections, and the following results were obtained.
1. Pharmacokinetic study
Two children, 11 years of age (38kg body weight) and 3 years of age (15.5kg body weight), were administered by 30 minutes intravenous drip infusion a single dose of 500mg/500mg (13.2mg/13.2mg per kg) and 250mg/250mg (16.1mg/16.1mg per kg) of MK-0787/MK-0791, respectively. Serum concentrations of MK-0787 reached their peaks at the end of drip infusion at a value of 56.33μg/ml and 55.98μg/ml, respectively. Concentrations of the drug decreased as the time after the administration increased, and they reached 0.14μg/ml and 0.12μg/ml, respectively in the older and the younger children at 6 hours after the administration.
Half-lives (T 1/2) of the drug in serum were calculated to be 1.21 hours and 1.04 hours, respectively. The concentration of the drug in cerebrospinal fluid for the 11 years old was 0.52μg/ml 2 hours after the drip infusion and the serum concentration at the time was 4.02μg/ml. Peak serum concentrations of MK-0791 in the 2 children were 53.73μg/ml and 22.99μg/ml, respectively, at the end of drip infusion. After 1 hour, the serum concentration of the drug decreased to 10.54μg/ml in 1 case and not detectable in the other case.
Urinary recovery rates of MK-0787 in 6 hours after the drip infusion was 82.9% and 63.6% in the 2 children and those of MK-0791 were 57.9% and 74.6%.
2. Clinical study
Clinical studies on MK-0787/MK-0791 were carried out in 6 pediatric patients; 1 each with femoral cellulitis, sepsis suspected, salmonellosis, acute tonsillitis, bronchopneumonia and streptococcosis.
Lengths of treatment were 22/3-4 days for 5 cases and 6 days for 1 case. The patients were treated by 30-60 minutes intravenous drip infusions twice a day for 1 case, and 3 times a day for 5 cases at daily doses of 54.5-66.7mg/kg. The treatment was effective in all cases, with 3 cases judged excellent and 3 cases good.
The safety of the drug was studied in 7 patients. No side effects nor clinically abnormal values were observed in any cases.
