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[Laboratory and clinical studies on aspoxicillin in the field of pediatrics]
Insights
New penicillin aspoxicillin (ASPC) shows promising results in pediatric infections. It demonstrates good antibacterial activity and an 85.3% clinical response rate with minor side effects.
Area of Science:
- Pharmacology
- Microbiology
- Pediatrics
Context:
- Pediatric infectious diseases pose significant health challenges.
- Novel antimicrobial agents are crucial for combating resistant pathogens.
- Aspoxicillin (ASPC) is a new semisynthetic penicillin derivative.
Purpose:
- To evaluate the pharmacokinetic properties of aspoxicillin (ASPC) in pediatric patients.
- To assess the in vitro antibacterial activity of ASPC against clinically relevant microorganisms.
- To determine the clinical efficacy and safety of ASPC in treating pediatric infections.
Summary:
- Laboratory and clinical studies investigated aspoxicillin (TA-058, ASPC) in pediatric infectious diseases.
- Pharmacokinetic data showed dose-dependent serum concentrations and mean half-lives of 0.87-1.1 hours.
- ASPC exhibited good activity against H. influenzae, S. pneumoniae, and S. pyogenes, with an 85.3% satisfactory clinical response rate in 34 patients.
Impact:
- Aspoxicillin (ASPC) demonstrates favorable pharmacokinetic and pharmacodynamic profiles for pediatric use.
- The study supports ASPC as a potentially effective treatment option for various pediatric bacterial infections.
- Observed side effects were transient and minor, suggesting a good safety profile for aspoxicillin.
Abstract:
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.