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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 ...
Overall, 2.3% of Acinetobacter baumannii strains are resistant to sulbactam/durlobactam. This percentage increases to 3.4% and 3.7% in the subgroups of carbapenem-resistant and colistin-resistant Acinetobacter, respectively. In Acinetobacter strains producing metallo-beta-lactamases, sulbactam/durlobactam resistance is 100%. [3]
[15] [16] These include latamoxef , cefmenoxime, cefoperazone, cefamandole, cefmetazole, and cefotetan. This is thought to be due to the methylthiotetrazole side-chain of these cephalosporins, which blocks the enzyme vitamin K epoxide reductase (likely causing hypothrombinemia) and aldehyde dehydrogenase (causing alcohol intolerance). [ 17 ]