Revision Year: 2018
Ampicillin is an aminopenicillin which exerts its bactericidal activity by interfering with the synthesis of the bacterial cell wall. It inhibits transpeptidase, an enzyme responsible for the synthesis of the peptidoglycan layer of the bacterial cell wall. This results in the interruption of peptidoglycan synthesis causing spheroplast formation and bacterial lysis.
Sulbactam is a penicillanic acid sulfone with beta-lactamase inhibitory properties. It is an irreversible inhibitor of many plasmid-mediated and some chromosomal beta- lactamases and has a similar spectrum of beta-lactamase inhibition as clavulanic acid. Sulbactam can therefore enhance the activity of penicillins and cephalosporins against many strains of bacteria.
Sultamicillin has demonstrated bactericidal activity against the following microorganisms:
Aerobic Gram-positive:
Staphylococcus aureus penicillin-resistant and some methicillin-resistant Haemophilus parainfluenzae (both beta-strains)
Staphylococcus epidermidis (including penicillin-resistant and some methicillin-resistant strains)
Streptococcus pneumoniae
Streptococcus faecalis
Other Streptococcus spp.
Aerobic Gram-negative:
Haemophilus influenzae (both beta-lactamase positive and negative strains)
Haemophilus parainfluenzae (both beta-lactamase positive and negative strains)
Moraxella catarrhalis
Escherichia coli
Klebsiella spp.
Proteus spp. (both indole-positive and indole-negative)
Enterobacter spp.
Morganella morganii
Citrobacter spp.
Neisseria meningitidis
Neisseria gonorrhoeae
Anaerobes:
Bacteroides fragilis and related species
After oral administration, sultamicillin is hydrolyzed during absorption to equivalent molar quantities (1:1) of ampicillin and sulbactam. The bioavailability of an oral dose of sultamicillin is 80% of an equal intravenous (IV) dose of ampicillin and sulbactam.
Food does not affect the systemic bioavailability of sultamicillin. After sultamicillin administration, peak serum levels of ampicillin are approximately twice those of an equal dose of oral ampicillin. Elimination half-lives are about 1 hour and 0.75 hour for ampicillin and sulbactam, respectively, in healthy volunteers, with 50-75% of each drug being excreted unchanged in the urine. The elimination half-lives are increased in the elderly and in patients with renal impairment. Probenecid decreases the renal tubular secretion of both ampicillin and sulbactam.
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