[Laboratory and clinical studies on aspoxicillin in the field of pediatrics].
Laboratory and clinical studies were carried out with aspoxicillin (TA-058, ASPC), a new semisynthetic penicillin, in pediatric infectious disease, and following results were obtained. The average serum concentrations of ASPC after intravenous injection were 53.6, 151.2 micrograms/ml at 15 minutes, 28.0, 72.8 micrograms/ml at 30 minutes, 17.6, 43.3 micrograms/ml at 1 hour, 7.0, 19.9 micrograms/ml at 2 hours, 0.3, 1.8 micrograms/ml at 6 hours, when the doses were 20 mg/kg and 40 mg/kg, respectively. The mean half-lives of ASPC in blood after injection were 0.87 hour and 1.1 hours when the doses were 20 mg/kg and 40 mg/kg, respectively. The mean recovery rates in the urine during 6 hours after intravenous injection of 20 mg/kg and 40 mg/kg were 62.0 and 62.8%, respectively. The antibacterial activity of ASPC against clinically isolated organisms was determined. ASPC had good activity against H. influenzae, H. parainfluenzae, S. pneumoniae and S. pyogenes. Thirty-four patients; 26 cases of respiratory tract infections, 6 cases of urinary tract infections, 1 case of bacterial meningitis and 1 case of bacterial lymphadenitis, were treated with 57.0-159 mg/kg daily dose of ASPC for 4-19 days. The rate of satisfactory clinical response was 85.3%. As to side effects, loose stool was observed in 3 cases, slight elevation of GOT & GPT and elevation of platelet were noted, in 2 cases, respectively. All were transient and considered to be minor.
D000658:Amoxicillin / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects; D001424:Bacterial Infections / Q000188:drug therapy* / Q000382:microbiology; D002648:Child; D002675:Child, Preschool; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D008297:Male; D010403:Penicillin Resistance
C037485:aspoxicillin; D000658:Amoxicillin