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[Fundamental and clinical studies on aspoxicillin in the pediatric field]
Insights
Aspoxicillin (ASPC) shows potent activity against S. pyogenes and moderate activity against S. aureus, H. influenzae, and E. coli, but is ineffective against K. pneumoniae. Pharmacokinetic studies in pediatric patients reveal favorable absorption and excretion profiles for ASPC.
Area of Science:
- Pharmacology and Microbiology
- Pediatric Infectious Diseases
Background:
- Evaluation of a novel penicillin antibiotic, aspoxicillin (ASPC, TA-058), in pediatric patients.
- Comparative analysis of ASPC's antimicrobial activity against key clinical isolates, including S. aureus, S. pyogenes, H. influenzae, E. coli, and K. pneumoniae.
Observation:
- ASPC demonstrated superior Minimum Inhibitory Concentration (MIC) values against S. pyogenes (<0.39 µg/ml).
- Dual-peak MIC distributions were observed for S. aureus, H. influenzae, and E. coli, suggesting beta-lactamase producing strains.
- ASPC exhibited significantly inferior antimicrobial activity against K. pneumoniae (MIC >12.5 µg/ml).
Findings:
- ASPC showed comparable activity to piperacillin (PIPC) and ampicillin (ABPC) against S. pyogenes, and superior activity to carbenicillin (CBPC).
- Against S. aureus, H. influenzae, and E. coli, ASPC's activity was generally less potent than PIPC but superior to CBPC, with varying degrees of activity compared to ABPC.
- Pharmacokinetic assessment in pediatric patients indicated a mean serum half-life of 1.03 hours and a 6-hour urinary recovery rate of 64.7% following intravenous administration.
Implications:
- Aspoxicillin presents a promising therapeutic option for infections caused by susceptible Gram-positive and Gram-negative bacteria in pediatric populations.
- The drug's pharmacokinetic profile supports its potential for effective clinical use in children.
- Further investigation into beta-lactamase producing strains and resistance mechanisms is warranted for optimizing ASPC's application.
Abstract:
Fundamental and clinical studies of aspoxicillin (ASPC, TA-058), a new penicillin antibiotic, were performed in pediatric field. Antimicrobial activity MIC of ASPC was compared with that of piperacillin (PIPC), ampicillin (ABPC) and carbenicillin (CBPC) for clinical isolates of S. aureus (24 strains), S. pyogenes (22 strains), H. influenzae (18 strains), E. coli (21 strains) and K. pneumoniae (23 strains). MIC of ASPC against S. pyogenes was distributed in less than 0.39 microgram/ml and this numerical value of MIC was very superior. MIC distributions of ASPC against S. aureus, H. influenzae and E. coli had 2 peaks respectively. It was presumed that the results are due to an existence of beta-lactamase producing strains. The sensitive strains in those were distributed in less than 1.56-12.5, less than or equal to 0.10 and 0.78-3.13 micrograms/ml, respectively, and those numerical value of MIC was superior. While against K. pneumoniae, all strains were distributed in more than 12.5 micrograms/ml and the antimicrobial activity of ASPC was very inferior. ASPC was as active as PIPC and ABPC against S. pyogenes, but more active then CBPC, ASPC was less active against S. aureus than PIPC and ABPC, but more active than CBPC. And ASPC was less active against H. influenzae and E. coli than PIPC, but more active than ABPC and CBPC. Against K. pneumoniae, strains that showed somewhat low numerical value of MIC at only PIPC were observed, but antimicrobial activities of ABPC and CBPC, as well as ASPC were very inferior. Absorption and excretion Serum level and urinary excretion of ASPC in 6 pediatric patients of 4 months to 12 years of age after one shot intravenous injection of 20 mg/kg were examined. The serum mean levels were 51.7 micrograms/ml at 1/4 hour, 38.2 micrograms/ml at 1/2 hour, 22.9 micrograms/ml at 1 hour, 3.0 micrograms/ml at 4 hours and 1.0 microgram/ml at 6 hours after injection, respectively. The mean half-life of serum level was 1.03 hours. The mean urinary levels were 4,646 micrograms/ml for 0-2 hours, 1,773 micrograms/ml for 2-4 hours and 299 micrograms/ml for 4-6 hours. The mean urinary recovery rate within 6 hours after injection was 64.7%. Clinical studies In order to evaluate clinical response, bacteriological response and side effects, ASPC was applied to 28 cases, i.e., 5 cases of acute purulent tonsillitis, 2 cases of acute purulent otitis media, 2 cases of acute bronchitis and 19 cases of acute pneumonia.(ABSTRACT TRUNCATED AT 400 WORDS)