Sulbactam Sodium is an irreversible inhibitor of several bacterial penicillinases and cephalosporinases. In the presence of low concentrations of sulbactam, ampicillin and other β-lactams readily inhibit the growth of a variety of resistant bacteria that contain β-lactamases. Sulbactam was developed by Pfizer, Inc. and was first described in 1978.
Sulbactam Sodium used alone has weak antibacterial activity, with the notable exception of its potent effects on susceptible and resistant strains of Neisseria gonorrhoeae. Sulbactam Sodium appears to be somewhat less potent but markedly more stable (in aqueous solution) than the β-lactamase inhibitor clavulanic acid.
Sulbactam Sodium inhibits common β-lactamases but cannot interact with the AmpC cephalosporinase. It confers little protection against Pseudomonas, Citrobacter, Enterobacter, and Serratia, which often express this gene.
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|Mechanism of Action
|Sulbactam Sodium contains a β-lactam ring that binds strongly to β-lactamase at or near its activation site, thereby permanently inhibiting enzymatic activity. This action protects other β-lactam antibiotics (penicillins, cephalosporins, etc.) from β-lactamase catalysis, thereby enhancing their antibacterial activity.
Sulbactam also shows antibacterial activity against various strains, sulbactam able to bind to and inhibit penicillin binding proteins PBP1 and PBP3. This antibacterial activity varies depending on species.
Sulbactam Sodium inhibits a wide range of group 2 β-lactamases, including those from Staphyloccus aureus, K. pneumoniae and B. fragilis. It is a good-to-moderate inhibitor of the TEM enzymes of groups 2b and 2be but has little effect on Group 1, Group 2br or Group 3 β-lactamases. It does not induce the activity of cephalosporinases from Gram-negative bacteria but is a weak inducer of penicillinases from S. aureus.
A concentration of 4–8 mg/L restores the activity of ampicillin for many β-lactamase-producing strains of S. aureus, H. influenzae, M. catarrhalis, enterobacteria and B. fragilis, but there is a large inoculum effect.
|Sulbactam is commonly used in combination with β-lactam antibiotics to prevent degredation by β-lactamase enzymes.
Sulbactam has recently been used against Acinetobacter septicemia.
|Plant Biology Applications
|Sulbactam can be used in combination with ampicillin and cefoperazone to suppress β-lactamase activity when used in Agrobacterium-mediated plant genetic modifications (Ogawa and Mii, 2004).
|Eukaryotic Cell Culture Applications
|Studies have shown that Sulbactam may protect cerebral neurons against oxygen-glucose deprivation (OGD) by up-regulating astrocytic GLT-1 expression via p38 MAPK signal pathway.
English AR et al (1978) CP-45,899, a beta-lactamase inhibitor that extends the antibacterial spectrum of beta-lactams: initial bacteriological characterization. Antimicrob. Agents Chemother. 14(3):414-419
Jie Q et al (2018) Sulbactam protects hippocampal neurons against oxygen-glucose deprivation by up-regulating astrocytic GLT-1 via p38 MAPK signal pathway. Front. Molec. Neurosci. 11:281
Noguchi JA, Gill MA (1988) Sulbactam: A beta-lactamase inhibitor. Clin. Pharm. 7:37–51
Ogawa Y et al (2004) Screening for highly active beta-lactam antibiotics against Agrobacterium tumefaciens. Arch Microbiol, 181: 331-336
Penwell WF (2015) Molecular mechanisms of sulbactam antibacterial activity and resistance determinants in Acinetobacter baumanni. Antimicrob. Agents Chemother. 59(3):1680-1689