[A study on pharmacokinetics, antimicrobial activity and clinical efficacy of sultamicillin in children].
Sultamicillin (SBTPC), a mutual prodrug for ampicillin (ABPC) and beta-lactamase inhibitor sulbactam (SBT), was evaluated for its antibacterial activity, pharmacokinetics and clinical efficacy. Pharmacokinetic studies were done in 2 subjects (a male and a female) following single oral administrations of 5 mg/kg and 10 mg/kg SBTPC fine granules after meal. Peak serum concentrations of ABPC and SBT in the 2 cases were 0.85 and 0.38 micrograms/ml and 3.74 and 3.79 micrograms/ml, respectively. Urinary excretion rates in 6 hours were 43.5-58.1% for ABPC and 33.6-53.6% for SBT. A total of 20 patients including 14 with respiratory infections, 1 with urinary tract infection and 5 with skin and soft tissue infections were treated with daily oral dose of 15.4-39.3 mg/kg SBTPC fine granules t.i.d. for 4 to 13 days. Responses were excellent in 5, good in 13 and fair in 2, hence the overall efficacy rate was 90.0%. Bacteriological responses were confirmed on 5 (62.5%) out of 8 strains which were eradicated by the treatment. SBTPC showed strong antibacterial activities against an ABPC-resistant strain of Escherichia coli. Side effects of the drug were observed in 3 patients: diarrhea in 2 and loose stool in 1. An abnormal laboratory test value, eosinophilia, was observed in only one patient.
Okazaki
H
H
Department of Pediatrics, Kansai Medical University.
Kitamura
N
N
Hirabayashi
Y
Y
Higashino
H
H
Kobayashi
Y
Y
D000293:Adolescent; D000367:Age Factors; D000667:Ampicillin / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000627:therapeutic use; D000668:Ampicillin Resistance; D001419:Bacteria / Q000187:drug effects* / Q000302:isolation & purification; D001424:Bacterial Infections / Q000188:drug therapy* / Q000382:microbiology; D002648:Child; D002675:Child, Preschool; D004304:Dosage Forms; D004341:Drug Evaluation; D004359:Drug Therapy, Combination / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D005260:Female; D006801:Humans; D007223:Infant; D008297:Male; D013407:Sulbactam / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000627:therapeutic use
D004304:Dosage Forms; C035444:sultamicillin; D000667:Ampicillin; D013407:Sulbactam