title: [Pharmacokinetic and clinical studies of S-1108 in the pediatric field].
abstract: Pharmacokinetic and clinical studies on S-1108, a new oral cephem antibiotic, were performed in the field pediatrics. The following results were obtained. 1) Antibacterial activities Antibacterial activities of S-1006, the active form of S-1108, were studied against clinically isolated strains of (Staphylococcus aureus (n = 5), Streptococcus pneumoniae (n = 6), Streptococcus pyogenes (n = 3), Haemophilus influenzae (n = 8), Branhamella catarrhalis (n = 5) and Haemophilus parainfluenzae (n = 2). MIC values ranged < or = 0.025-1.56 for GPC and < or = 0.025-0.78 microgram/ml for GNR. 2) Absorption and excretion Blood concentrations and urinary excretion rates of S-1108 were measured upon administration of S-1108 after meal at dose of 3 mg/kg (n = 4), 4 mg/kg (n = 1) and 6 mg/kg (n = 1). The peak blood concentrations of S-1006 at a dose of 3 mg/kg (n = 4), ranged from 0.57 to 1.82 micrograms/ml at 1, 2 and 4 hours after dosing. Mean pharmacokinetic parameters T1/2 and AUC were 1.29 +/- 0.69 hours and 4.47 +/- 2.25 micrograms.hr/ml, respectively. At a dose of 4 mg/kg and 6 mg/kg, peak concentrations were 1.79 and 1.27 micrograms/ml at 2 and 3 hours after treatment. T1/2 and AUC were 1.34 and 1.11 hours, and 8.19 and 5.65 micrograms.hr/ml, respectively. Urinary recovery rates ranged from 13.0 to 37.2% for the first 8 hours after administration. 3) Clinical studies Clinical efficacies were examined in 32 cases of various pediatric infections including 5 cases of acute pneumonia, 11 cases of bronchitis, 2 cases of scarlet fever, 8 cases of tonsillitis, 1 case of pharyngitis, 2 cases of otitis media and 3 cases of UTI. Clinical efficacy rate was 96.9% (31/32) and bacteriological eradication rate was 87.1% (27/31). There were no side effects and abnormal laboratory test values except 1 case (Eosino. 2-->10%) in the 32 cases.
authors.affiliation: Department of Pediatrics, Yamanashi Red Cross Hospital.
authors.forename: Y
authors.initials: Y
authors.lastname: Toyonaga
authors.forename: T
authors.initials: T
authors.lastname: Ishihara
authors.forename: T
authors.initials: T
authors.lastname: Tezuka
authors.forename: T
authors.initials: T
authors.lastname: Sano
authors.forename: H
authors.initials: H
authors.lastname: Nakamura
mesh_terms: D000042:Absorption; D001419:Bacteria / Q000187:drug effects / Q000302:isolation & purification; D001424:Bacterial Infections / Q000188:drug therapy* / Q000378:metabolism / Q000382:microbiology; D002511:Cephalosporins / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use* / Q000652:urine; D002648:Child; D002675:Child, Preschool; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D007223:Infant; D008297:Male; D008826:Microbial Sensitivity Tests
chemical_list: D002511:Cephalosporins; C076133:S 1108; C076134:S 1006