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Laboratory and clinical studies on aspoxicillin in the field of pediatrics



Laboratory and clinical studies on aspoxicillin in the field of pediatrics



Japanese Journal of Antibiotics 38(7): 1853-1867



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. 1. The average serum concentrations of ASPC after intraveous injection were 53.6, 151.2 .mu.g/ml at 15 minutes, 28.0, 72.8 .mu.g/ml at 30 minutes, 17.6, 43.3 .mu.g/ml at 1 hour, 7.0, 19.9 .mu.g/ml at 2 hours, 0.3, 1.8 .mu.g/ml at 6 hours, when the doses were 20 mg/kg and 40 mg/kg, respectively. 2. The mean half-lives of ASPC in blood after injection of 0.87 hour and 1.1 hours when the doses were 20 mg/kg and 40 mg/kg, respectively. 3. The mean recovery rates in urine during 6 hours after intravenous injection of 20 mg/kg and 40 mg/kg were 62.0 and 62.8%, respectively. 4. The antibacterial activity of ASPC against clinically isolated organisms was determined. ASPC had good activity against Haemophilus influenzae, H. parainfluenzae, Streptococcus pneumoniae, and S. pyrogenes. 5. 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 .apprx. 159 mg/kg daily dose of ASPC for 4 .apprx. 19 days. The rate of satisfactory clinical response was 85.3%. 6. As to side effects, loose stool was observed in 3 cases, slight elevation of GOT and GT and elevation of platelet were noted, in 2 cases, respectively. All were transient and considered to be minor.

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Accession: 005787336

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PMID: 3851859


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