Imipenem/cilastatin/relebactam

Imipenem/cilastatin/relebactam is a combination drug used for the treatment of bacterial infections. It is a combination of three active ingredients: imipenem, a carbapenem antibiotic; cilastatin, a renal dehydropeptidase inhibitor; and relebactam, a beta-lactamase inhibitor. This combination is used to treat complicated urinary tract infections, including pyelonephritis, and complicated intra-abdominal infections.

Etymology

The name "imipenem" is derived from the compound's chemical structure, which includes an imino group and a penem group. The "cilastatin" part of the name comes from the compound's ability to inhibit the enzyme dehydropeptidase in the kidneys, which would otherwise degrade imipenem. The name "relebactam" is derived from the compound's ability to inhibit beta-lactamase enzymes, which are produced by some bacteria to resist beta-lactam antibiotics.

Mechanism of action

Imipenem works by inhibiting the synthesis of bacterial cell walls, leading to cell death. Cilastatin prevents the degradation of imipenem in the kidneys, thereby increasing its concentration in the urine and its antibacterial activity. Relebactam inhibits beta-lactamase enzymes, which are produced by some bacteria to resist beta-lactam antibiotics. By inhibiting these enzymes, relebactam allows imipenem to remain effective against beta-lactamase-producing bacteria.

Side effects

Common side effects of imipenem/cilastatin/relebactam include diarrhea, nausea, headache, fever, and rash. Serious side effects may include allergic reactions, seizures, and Clostridium difficile-associated diarrhea.

Related terms

• Antibiotic
• Beta-lactam antibiotic
• Carbapenem
• Dehydropeptidase
• Beta-lactamase