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Cefoperazone/sulbactam is a combination drug used as an antibiotic. It is effective for the treatment of urinary tract infections . [ 2 ] It contains cefoperazone , a β-lactam antibiotic , and sulbactam , a β-lactamase inhibitor , which helps prevent bacteria from breaking down cefoperazone.
Cefoperazone [Unlike most third-generation agents, cefoperazone is active against Pseudomonas aeruginosa], combination Cefoperazone with Sulbactam makes more effective antibiotic, because Sulbactam avoid degeneration of Cefoperazone: Cefobid (discontinued) Cefotaxime: Claforan: Cefpodoxime: Vantin, Banadoz
Cefoperazone contains an N-methylthiotetrazole (NMTT or 1-MTT) side chain.As the antibiotic is broken down in the body, it releases free NMTT, which can cause hypoprothrombinemia (likely due to inhibition of the enzyme vitamin K epoxide reductase) and a reaction with ethanol similar to that produced by disulfiram (Antabuse effect), due to inhibition of aldehyde dehydrogenase.
Sulbactam is a β-lactamase inhibitor. This drug is given in combination with β-lactam antibiotics to inhibit β-lactamase , an enzyme produced by bacteria that destroys the antibiotics . [ 1 ]
Vaborbactam is a boronic acid β-lactamase inhibitor with a high affinity for serine β-lactamases, including Klebsiella pneumoniae carbapenemase (KPC). [5] Vaborbactam inhibits a variety of β-lactamases, exhibiting a 69 nM K i against the KPC-2 carbapenemase and even lower inhibition constants against CTX-M-15 and SHV-12.
[12] [13] [14] While β-lactam ring in meropenem is more accessible to water molecules than in the other β-lactam antibiotics, that facilitates the hydrolysis process and faster degradation of meropenem's antibacterial properties in aqueous solutions, it is more resistant to degradation by β-lactamase enzymes produced by bacteria than the ...
The β-lactam core structures. (A) A penam.(B) A carbapenam.(C) An oxapenam.(D) A penem.(E) A carbapenem.(F) A monobactam.(G) A cephem.(H) A carbacephem.(I) An oxacephem. This is a list of common β-lactam antibiotics—both administered drugs and those not in clinical use—organized by structural class.
Meropenem works by blocking the construction of the bacterial cell wall while vaborbactam blocks the breakdown of meropenem by some beta-lactamases. [ 4 ] The combination was approved for medical use in the United States in 2017, [ 6 ] in the European Union in 2018, [ 4 ] [ 3 ] and in Canada in December 2024. [ 1 ]