Products
Imipenem is commercially available as an infusion preparation and fixed combination with cilastatin (Tienam, generics). Imipenem was approved in many countries in 1985 as the first member of the carbapenems.
Structure and properties
Imipenem (C12H17N3O4S, Mr = 299.3 g/mol) is present in drugs as imipenem monohydrate, a white or pale yellow powder that is sparingly soluble in water.
Effects
Imipenem (ATC J01DH51) is bactericidal against aerobic and anaerobic Gram-positive and Gram-negative pathogens. It inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins and has a half-life of approximately one hour. Imipenem is degraded to a relevant extent in the kidney by the enzyme dehydropeptidase-I. Therefore, it is combined with the enzyme inhibitor cilastatin, which inhibits the renal enzyme and thus increases imipenem concentrations in the urinary tract. Cilastatin does not itself have antibacterial activity.
Indications
For treatment of bacterial infectious diseases with susceptible pathogens.
Dosage
According to the SmPC. The drug is administered as an intravenous infusion.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Imipenem is secreted on the kidney, so drug interactions with probenecid are possible. Other interactions have been described with ganciclovir and valproic acid.
Adverse effects
The most common possible adverse effects include a rash, nausea, vomiting, diarrhea, and phlebitis.