[Fundamental and clinical evaluation of ceftriaxone in the pediatric field].

Fundamental and clinical evaluation on ceftriaxone (Ro 13-9904, CTRX), a newly-developed injectable cephem antibiotic was performed as follows. The serum and urine concentrations of CTRX as well as the urinary recovery rate were determined in 7 children at 3 different dose levels; 3 cases administered with 10 mg/kg, 3 with 20 mg/kg and 1 with 48 mg/kg by one shot intravenous injection. The concentration in the cerebrospinal fluid was determined in 1 case of purulent meningitis associated with bacteremia, administered by one shot intravenous injection with 47.6 mg/kg. CTRX was also examined in its clinical and bacteriological efficacies by one shot intravenous injection for 8 days on average in a mean daily dose of 46.5 mg/kg, divided into twice a day in 31 cases, 3 times in 1 case, and 4 times changed from twice in 1 case; in a total of 33 children consisting of 3 with tonsillitis, 1 with chronic bronchitis, 20 with pneumonia, 2 with purulent meningitis associated with bacteremia, 3 with urinary tract infections, 1 with osteomyelitis associated with phlegmon, 3 with purulent lymphadenitis. The adverse reactions and laboratory test values were examined in a total of 40 cases, i.e., the above-mentioned 33 cases plus the 7 drop-out cases in which the clinical efficacy could not be evaluated. The results were as follows. The serum levels of CTRX in 7 cases consisting of 3 administered with 10 mg/kg, 3 with 20 mg/kg and 1 with 48 mg/kg reached their peaks 5 minutes after one shot intravenous injection and the mean values of them were 93.6 mcg/ml, 143.0 mcg/ml and 558.0 mcg/ml, respectively, indicating the existence of a dose-response among these groups, while the half-life times were 4.41, 5.86 and 4.09 hours. Among the 7 cases examined in the urinary levels as well as the serum levels, the 3 cases administered with 10 mg/kg reached the mean peak of 334.0 mcg/ml 2 to 4 hours after administration, while another 3 cases administered with 20 mg/kg showed peaks of 793.0, 522.0 and 536.0 mcg/ml, respectively, 2 to 4 hours, 4 to 6 hours and 6 to 12 hours after injection; this dispersion being partly because of that the urine specimen was unable to be collected regularly every hour in this dose group. In the case administered with 48 mg/kg, urinary level reached the highest value of 6,100.0 mcg/ml from 0 to 2 hours.(ABSTRACT TRUNCATED AT 400 WORDS)