[Pharmacokinetic, bacteriological and clinical evaluations of cefdinir 10% fine granules in pediatrics]

Pharmacokinetic, bacteriological, and clinical studies on cefdinir (CFDN, FK482) (10% fine granules), a new oral cephem, were performed in pediatrics. 1. Bioequivalencies of plasma concentrations and urinary excretions of CFDN 5% and 10% fine granules were investigated on 3 pediatric patients with ages between 5 to 13 years administered with a drug in fasting state at a dose level of 3 mg/kg using a cross over method. Average plasma concentrations in a group of patients administered with 5% fine granules peaked at 3 hours after administration with a level of 1.05 +/- 0.29 micrograms/ml (mean +/- S.E.) and decreased to 0.12 +/- 0.05 micrograms/ml at 8 hours with a half-life of 1.48 +/- 0.09 hours. In the group administered with 10% fine granules, average plasma concentrations peaked at 2 hours after administration with a level of 1.32 +/- 0.12 micrograms/ml, and decreased to 0.20 +/- 0.11 microgram/ml at 8 hours with a half-life of 1.68 +/- 0.28 hours. The first 8-hour urinary recovery rates of CFDN in the 5% and 10% fine granules groups averaged 19.64 +/- 5.69% and 23.37 +/- 2.36%, respectively. Both average and individual plasma concentrations and urinary recovery rates in the patients of the 10% fine granules group were somewhat higher than those of the 5% fine granules group, but no significant differences were observed between the 2 groups including areas under concentrations. 2. CFDN 10% fine granule preparation was administered to 33 pediatric patients with ages between 1 to 13 years with various infections, and its clinical effects, bacteriological effects and safety were assessed. In 31 of the 33 patients (2 patients were excluded since they were with non-bacterial infections) clinical effects were excellent in all of 9 patients with scarlet fever (3), acute pharyngitis (3) or impetigo (3), excellent in 12 and good in 3 of 15 patients with acute purulent tonsillitis, and excellent in 4 and good in 3 of 7 patients with acute pneumonia. The overall efficacy rate was 100%. Bacteriological effects against causative organisms were evaluated. All the identified Staphylococcus aureus (4 strains) and Streptococcus agalactiae (1) were eradicated. Of 10 strains of Streptococcus pyogenes, 9 strains were eradicated and the other one was reduced. Of 7 strains of Haemophilus influenzae 4 were eradicated, 1 persisted and the fate of the remaining 2 were unknown. The overall eradication rate was 90.0%. Microbial substitutions were observed in 5 patients. The new, replacing bacteria were all Haemophilus spp.(ABSTRACT TRUNCATED AT 400 WORDS)