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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.
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.
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.
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.
Meropenem, sold under the brand name Merrem among others, is an intravenous carbapenem antibiotic used to treat a variety of bacterial infections. [3] Some of these include meningitis, intra-abdominal infection, pneumonia, sepsis, and anthrax.
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]
ATC code J01 Antibacterials for systemic use is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products.
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]