Sulbactam

Sulbactam 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 first developed by the central research division of Pfizer, Inc. and was first described in 1978.

Sulbactam used alone displays only 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 is able to inhibit the most common forms of β-lactamase but is not able to interact with the AmpC cephalosporinase. Thus, it confers little protection against bacteria such as Pseudomonas aeruginosa, Citrobacter, Enterobacter, and Serratia, which often express this gene.

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Background

Sulbactam 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 can also bind to and inhibit penicillin binding proteins PBP1 and PBP3. This antibacterial activity varies depending on the species.