[Pharmacokinetic, bacteriological and clinical evaluation of cefditoren pivoxil in pediatrics].

Pharmacokinetic, bacteriological, and clinical studies were performed in pediatrics on cefditoren pivoxil (CDTR-PI, ME1207) in granules. 1. Serum concentrations and urinary excretions of CDTR after administration of CDTR-PI to children (ages between 1 and 10) were investigated. Five cases were administrated with CDTR-PI at a dose level of 3 mg/kg 30 minutes after meal. Serum concentrations in these cases reached their peaks at 2 hours after administration with an average level of 1.23 +/- 0.34 micrograms/ml and diminished to 0.04 +/- 0.04 micrograms/ml at 8 hours after administration with a half-life of 1.60 +/- 0.38 hours. Urinary recovery rates of CDTR in the first 8 hours after administration of CDTR-PI averaged 14.9 +/- 0.9%. Five cases were administered with CDTR-PI at a dose level of 6 mg/kg 30 minutes after meal. Serum concentrations with the drug after meal reached their peaks at 1 hour after administration with an average level of 2.62 +/- 0.42 micrograms/ml and diminished to 0.21 +/- 0.11 micrograms/ml at 8 hours after administration with a half-life of 1.58 +/- 0.31 hours. Urinary recovery rates of CDTR in the first 8 hours after administration of CDTR-PI averaged 17.0 +/- 0.7%. These data also showed that serum and urinary concentrations of the drug depended on dose levels. 2. CDTR-PI was administered to 31 pediatric patients (their ages ranged between 1 year and 10 years) with various infections, and clinical and bacteriological effects and adverse reactions were investigated. Clinical effects were evaluable in 24 cases including 2 cases of scarlet fever, 1 case of acute pharyngitis, 12 cases of acute purulent tonsillitis, 4 cases of acute bronchitis, 5 cases of acute pneumonia. Clinical responses were excellent in 16 cases, effective in 8 cases, with an efficacy rate of 100%. Antimicrobial effects against a total of 16 strains identified or assumed to be pathogenic bacteria were evaluated. The 16 strains of bacteria included 4 strains of Staphylococcus aureus, 6 strains of Streptococcus pyogenes, 2 strains of beta-Streptococcus, 4 strains of Haemophilus influenzae. All the bacteria listed here were judged to have been eradicated except 2 strains of H. influenzae (1 was decreased and 1 was unchanged) thus, the eradication rate was 87.5%. Two strains of bacteria replaced infection causing bacteria. Streptococcus pneumoniae replaced S. pyogenes and S. aureus replaced H. influenzae. No adverse side reactions were observed.(ABSTRACT TRUNCATED AT 400 WORDS)