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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 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.
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
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 ...
Sulbactam is primarily used as a suicide inhibitor of β-lactamase, shielding more potent beta-lactams such as ampicillin. [6] Sulbactam itself contains a beta-lactam ring, and has weak antibacterial activity by inhibiting penicillin binding proteins (PBP) 1 and 3, but not 2.
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 ]
β-Lactam antibiotics are indicated for the prevention and treatment of bacterial infections caused by susceptible organisms. At first, β-lactam antibiotics were mainly active only against gram-positive bacteria, yet the recent development of broad-spectrum β-lactam antibiotics active against various gram-negative organisms has increased their usefulness.