cefdinir and Pneumonia

Cefdinir (CFDN), a newly developed oral cephalosporin in 5% fine granular form, was administered to 10 boys at 1 hour before meal (in the fasting state) and concentrations of the drug in plasma and urine and its urinary recovery rates were determined. The subjects were divided into 2 groups of 5 boys each; one group received 3 mg/kg of CFDN, and the other, 6 mg/kg. To 6 of the 10 children the drug was administered in the two different dose levels using the cross-over method. To study clinical and bacteriological effects of this drug, a mean dose of 4.6 mg/kg t.i.d. was administered for 8 days on the average to 40 children with various infections; pharyngitis (4 cases), tonsillitis (2), acute bronchitis (2), pneumonia (8), scarlet fever (6), acute purulent otitis media (1), urinary tract infection (12), impetigo (2), phlegmon (1), lymphadenitis (1) and subcutaneous abscess (1). MICs were determined for 6 drugs including CFDN, cefaclor, cefixime (CFIX), methicillin, cloxacillin (MCIPC), amoxicillin (AMPC) against 13 strains of 6 species freshly isolated from children receiving CFDN. An inoculum size of 10(6) cfu/ml was used in the MIC-determinations. Adverse reactions and abnormal laboratory findings attributable to this drug were also examined in these patients. The results obtained are summarized as follows. 1. Mean plasma peak levels of CFDN were observed at 3 hours after administration in both the 3 mg/kg and 6 mg/kg groups with mean peak values of 0.68 and 1.35 micrograms/ml, respectively. Mean half-lives were 2.06 hours in the 3 mg/kg group and 1.61 hours in the 6 mg/kg group, and mean AUCs were 3.5 in the former and 6.5 micrograms.hr/ml in the latter. Thus, dose-response between the 2 doses was observed in plasma levels and AUCs. 2. To 3 patients, CFDN was given in the two different doses using the cross-over method. Mean plasma peak levels of CFDN were 0.71 and 1.31 micrograms/ml in the doses of 3 mg/kg and 6 mg/kg, respectively. Half-lives were 1.39-2.90 hours in the 3 mg/kg group and 1.21-1.48 hours in the 6 mg/kg group, with AUCs of 3.4-3.7 and 4.1-7.5 micrograms.hr/ml, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)

Topics: Administration, Oral; Age Factors; Bacteria; Bacterial Infections; Cefdinir; Cephalosporins; Child; Child, Preschool; Dosage Forms; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Male; Pharyngitis; Pneumonia; Urinary Tract Infections

The therapeutic activities of orally administered FK482 were compared with those of reference antibiotics against systemic and local infections with a variety of bacteria in mice and rabbits. In systemic infections in mice, oral FK482 was almost as effective as oral cefaclor (CCL) and more effective than oral cephalexin (CEX) against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis infections. However, FK482 afforded superior protective activity when given subcutaneously against E. coli infection in mice, and this activity was more potent than that of subcutaneously given CCL. In comparison with CCL, the reason that the in vivo activity of orally given FK482 against mouse systemic infections was weaker than had been anticipated from its potent in vitro activity was due to its poor oral absorption in mice. In local infections in rabbits, a species in which FK482 was better absorbed than in mice, FK482 was more effective than CCL, CEX or amoxicillin (AMPC). Against pneumonia induced by S. aureus or Streptococcus pyogenes, FK482 was as effective as AMPC and more effective than CCL in reducing the number of viable bacteria in the lungs of infected rabbits. In the oral treatment of experimental ascending pyelonephritis in rabbits, FK482 was superior to CCL and AMPC against methicillin-resistant S. aureus infection, as effective as AMPC and more effective than CCL against Enterococcus faecalis infection, and as effective as cefixime (CFIX) and more effective than CCL and AMPC against E. coli infection in reducing the number of viable bacteria in the kidneys and urine.

Topics: Administration, Oral; Animals; Bacterial Infections; Cefaclor; Cefdinir; Cephalosporins; Male; Mice; Mice, Inbred ICR; Pneumonia; Pyelonephritis; Rabbits