title: [Antimicrobial activities of sultamicillin against clinical isolates from upper respiratory tract infections].
abstract: Sultamicillin (SBTPC) is a mutual prodrug in which ampicillin (ABPC) and a potent beta-lactamase inhibitor sulbactam (SBT) are ester-bound in an equimolar ratio. SBTPC is hydrolyzed during absorption after oral administration to provide ABPC and SBT for systemic circulation. In the present study, the antimicrobial activities of SBTPC against 50 isolates each of 6 species (Staphylococcus aureus, Klebsiella pneumoniae subsp. pneumoniae, Branhamella catarrhalis, Haemophilus influenzae, Streptococcus pneumoniae and Streptococcus pyogenes) of bacteria freshly obtained from upper respiratory tract infections were examined in relation to their bacterial beta-lactamase producing abilities. beta-Lactamase producing strains were identified using the acidometry disc method with benzylpenicillin (PCG) of cefazolin (CEZ) as a substrate, and their frequencies of appearance were calculated as follows: S. aureus 86%; K. pneumoniae subsp. pneumoniae 100%; B. catarrhalis 68%; H. influenzae 24%. Fourteen per cent of S. aureus strains examined were beta-lactamase positive using both PCG and CEZ acidometry discs. SBTPC, however, demonstrated excellent antimicrobial activities even against these beta-lactamase producing strains. Good activities were observed especially against those bacterial strains producing penicillinase (PCase). Average MIC80 values of SBTPC were 3.13 micrograms/ml for S. aureus and K. pneumoniae subsp. pneumoniae, 0.39 micrograms/ml for B. catarrhalis and H. influenzae, 0.05 micrograms/ml for S. pneumoniae and 0.025 micrograms/ml for S. pyogenes. As SBTPC was shown to possess excellent antimicrobial activities against PCase producing strains, the enhancement in activities of SBTPC compared to ABPC alone can be attributed to the inhibition of beta-lactamase by SBT which, as noted above, is a component of SBTPC in an equimolar ratio to ABPC.
authors.affiliation: Section of Studies, Tokyo Clinical Research Center.
authors.forename: K
authors.initials: K
authors.lastname: Deguchi
authors.forename: N
authors.initials: N
authors.lastname: Yokota
authors.forename: M
authors.initials: M
authors.lastname: Koguchi
authors.forename: Y
authors.initials: Y
authors.lastname: Nakane
authors.forename: S
authors.initials: S
authors.lastname: Fukayama
authors.forename: Y
authors.initials: Y
authors.lastname: Nishimura
authors.forename: S
authors.initials: S
authors.lastname: Oda
authors.forename: S
authors.initials: S
authors.lastname: Tanaka
authors.forename: M
authors.initials: M
authors.lastname: Kato
authors.forename: K
authors.initials: K
authors.lastname: Sato
mesh_terms: D000208:Acute Disease; D000667:Ampicillin / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects* / Q000302:isolation & purification / Q000378:metabolism; D004359:Drug Therapy, Combination / Q000494:pharmacology; D006801:Humans; D010403:Penicillin Resistance; D012141:Respiratory Tract Infections / Q000382:microbiology*; D013407:Sulbactam / Q000494:pharmacology*; D001618:beta-Lactamases / Q000096:biosynthesis
chemical_list: C035444:sultamicillin; D000667:Ampicillin; D001618:beta-Lactamases; D013407:Sulbactam