Related Experiment Videos
[Clinical and laboratory evaluation of aspoxicillin in the pediatric field]
Abstract:
The authors have carried out the clinical and laboratory evaluation of aspoxicillin (ASPC, TA-058). The results were as follows: Antibacterial activities The susceptibility to ASPC was estimated by plate dilution method on 26 strains each of S. aureus, E. coli, Salmonella and P. aeruginosa and 19 strains of S. marcescens isolated from clinical specimens. Minimum inhibitory concentration (MIC) of ASPC against E. coli and Salmonella was about twice active to compare with ampicillin (ABPC), but MIC of ASPC against S. aureus was two-fold less active than that of ABPC. Antimicrobial activities of ASPC against S. marcescens were similar to that of ABPC, while against P. aeruginosa its activities were two-fold higher than that of carbenicillin. Serum levels and urinary excretions When ASPC was administered at 20 mg/kg by one shot intravenous injection, serum concentration was 75 micrograms/ml after 15 minutes and half-life (T 1/2 beta) was 1.65 hours. Urinary excretion within 6 hours after ASPC injection reached to 245.6 mg (26.1%). The reason of this law urinary excretion rate was due to the underlying disease (hydronephrosis). In case of 20 mg/kg administration of ASPC by intravenous drip infusion, peak serum level reached to 88 micrograms/ml at the end of injection, and half-life (T 1/2 beta) was 0.77 hour. Since ASPC degradation by beta-lactamase was proceeded, urinary excretion of this case was not measured by microbiological method. Penicillonic acid and its epimer were detected by HPLC method. It was found that beta-lactamase producing strain was S. marcescens which was isolated by urine culture.(ABSTRACT TRUNCATED AT 250 WORDS)
Insights
Aspoxicillin (ASPC) shows varied antibacterial activity, with higher efficacy against E. coli and Salmonella compared to ampicillin. ASPC demonstrates potential in clinical settings, though its excretion is affected by conditions like hydronephrosis.
Area of Science:
- Pharmacology
- Microbiology
- Clinical Medicine
Context:
- The study evaluates aspoxicillin (ASPC), a novel antibiotic, for its clinical and laboratory efficacy.
- ASPC's antibacterial spectrum and pharmacokinetic properties were assessed against common clinical isolates.
Purpose:
- To determine the antibacterial activity of ASPC against various bacterial strains, including S. aureus, E. coli, Salmonella, P. aeruginosa, and S. marcescens.
- To investigate the serum levels, urinary excretion, and metabolic profile of ASPC following intravenous administration.
- To assess the impact of beta-lactamase activity on ASPC's pharmacokinetics.
Summary:
- ASPC demonstrated potent activity against E. coli and Salmonella, with minimum inhibitory concentrations (MICs) twice as effective as ampicillin (ABPC).
- Against S. aureus, ASPC was less active than ABPC, while its activity against S. marcescens was comparable.
- ASPC showed enhanced activity against P. aeruginosa compared to carbenicillin.
- Intravenous administration resulted in a serum half-life of 1.65 hours, with 26.1% urinary excretion within 6 hours, influenced by hydronephrosis.
- Degradation by beta-lactamase was observed, with S. marcescens identified as a beta-lactamase-producing strain.
Impact:
- This research provides crucial data on ASPC's antimicrobial potential and pharmacokinetic behavior, informing its potential therapeutic applications.
- Understanding ASPC's activity against specific pathogens and its metabolic fate is vital for optimizing antibiotic therapy.
- The findings highlight the need to consider patient-specific factors, such as renal function and bacterial resistance mechanisms, when using ASPC.