Indications
Relebactam, when used in conjunction with imipenem and cilastatin, is approved for the treatment of complex urinary tract infections, including pyelonephritis, and complicated intra-abdominal infections in adults. It is specifically indicated for infections caused by susceptible organisms.
Pharmacodynamics
Relebactam functions by inhibiting the hydrolysis of imipenem. This action allows imipenem to retain its bactericidal properties, effectively combating bacterial infections.
Absorption
Currently, relebactam is available exclusively as an intravenous formulation. As a result, there is no available absorption data from oral administration in the medical literature.
Metabolism
Relebactam is not significantly metabolized in the body. It remains largely unchanged in human plasma, indicating minimal metabolic processing.
Mechanism of Action
Relebactam functions as a beta-lactamase inhibitor, effectively targeting and inhibiting various beta-lactamase enzymes, including those classified under Ambler class A and class C. This mechanism supports imipenem's stability and prevents its degradation within the body. Initially, relebactam attaches non-covalently to a specific beta-lactamase binding site. Subsequently, it covalently acylates the serine residue at the enzyme's active site, resembling the action of the structurally similar avibactam. Notably, unlike some other beta-lactamase inhibitors, relebactam, upon de-acylation, has the unique ability to reform its five-membered ring and rebind to target enzymes, enhancing its inhibitory effectiveness.
