[Clinical and laboratory evaluation of aspoxicillin in the pediatric field].
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)
D000658:Amoxicillin / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects; D001424:Bacterial Infections / Q000188:drug therapy*; D001991:Bronchitis / Q000188:drug therapy; D002648:Child; D002675:Child, Preschool; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D007223:Infant; D007275:Injections, Intravenous; D008297:Male; D010403:Penicillin Resistance; D011014:Pneumonia / Q000188:drug therapy; D011704:Pyelonephritis / Q000188:drug therapy / Q000378:metabolism
C037485:aspoxicillin; D000658:Amoxicillin