[Fundamental and clinical studies of aspoxicillin in the pediatric field].
Aspoxicillin (ASPC), a new semisynthesized penicillin, was administered to 20 children; by one shot intravenous injection in the doses of 10, 20 and 40 mg/kg to each of 3 children, and by intravenous drip infusion in the doses of 20 and 40 mg/kg over a period of 1 hour to 8 and 3 children, respectively, and the serum levels, urinary levels and recovery rates were determined. ASPC was administered to 1 patient with tuberculous pleurisy in the dose of 20 mg/kg by one shot intravenous injection, then the thoracic fluid level and serum level were determined. In addition, ASPC was administered to 3 children with tonsillitis, 3 with bronchitis, 40 with pneumonia, one each for pleuropneumonia, pleurisy, lung abscess, scarlet fever, staphylococcal scalded skin syndrome and purulent lymphadenitis and 2 with UTI (total 54 children), in the mean dose of 81.4 mg/kg/day t.i.d. (12 children) or q.i.d. (42 children) by one shot intravenous injection for 6 days on the average, and clinical effectiveness and bacteriological response were evaluated in these cases, and adverse reactions and abnormal laboratory findings were examined in the 60 cases which included 6 drop-out cases. After the administration of ASPC to 9 children; 10, 20 and 40 mg/kg to each of 3 children, by one shot intravenous injection, the mean serum levels reached to the peak of 58.4, 147.0 and 221.0 mcg/ml, respectively, in 5 minutes. The mean half-lives were 1.03, 1.01 and 1.23 hours, and the mean areas under the curve (AUCs) were 44.9, 94.1 and 192.9 mcg X hr/ml, respectively. A dose response was seen among the 3 dosage levels. After the administration of ASPC to 11 children; 20 and 40 mg/kg to 8 and 3 children, respectively, by intravenous drip infusion over a period of 1 hour, the mean serum levels reached to the peak of 58.2 and 114.0 mcg/ml, respectively, on completion of the administration. The mean half-lives were 1.22 and 1.09 hours, and the mean AUCs were 109.4 and 181.7 mcg X hr/ml, respectively. A dose response was observed between the 2 dosage levels. In the above mentioned each 3 cases receiving one shot intravenous injection in the dose of 10, 20 and 40 mg/kg, the mean urinary levels of ASPC reached to the peak of 1,000.0, 2,300.0 and 4,350.0 mcg/ml, respectively, at 0 approximately 2 hours after the administration, and the urinary recovery rates during the first 6 hours were 66.1, 66.5 and 56.9%, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)
D000658:Amoxicillin / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000378:metabolism / Q000627:therapeutic use; D001424:Bacterial Infections / Q000188:drug therapy* / Q000382:microbiology; D002648:Child; D002675:Child, Preschool; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D007223:Infant; D007263:Infusions, Parenteral; D007275:Injections, Intravenous; D008297:Male
C037485:aspoxicillin; D000658:Amoxicillin