Imipenem + cilastatin + relebactam
Carbapenems
Carbapenems
A carbapenem with a beta-lactamase inhibitor that restores activity against many carbapenemase-producing (KPC) Enterobacterales, not metallo-beta-lactamases.
Also called: imipenem/cilastatin/relebactam
Quick facts
- Group
- Carbapenems
- Target
- Bacterial PBPs (imipenem) and class A and C beta-lactamases, including KPC (relebactam)
- Used for
- Complicated urinary tract infections
- Key effects
- Nausea · Headache · Pain
- Monitor
- Kidney function to adjust the dose
- ATC
- J01DH56
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows relebactam bound to KPC-2, the Klebsiella pneumoniae carbapenemase it blocks; imipenem's target, PBP3, is shown on the imipenem with cilastatin page.
Imipenem acylates the PBPs and halts wall synthesis. Cilastatin inhibits the renal tubular dehydropeptidase that would destroy it. Relebactam, a non-beta-lactam inhibitor similar to avibactam, blocks class A beta-lactamases (including the KPC carbapenemase) and class C enzymes, restoring imipenem's activity against most carbapenemase-producing Enterobacterales; it does not inhibit metallo-beta-lactamases.
- Relebactam inactivates KPC and other A and C beta-lactamases
- Cilastatin protects imipenem in the kidney
- Intact imipenem acylates the PBPs
- Wall synthesis halts and the bacterium lyses
Indications
- Complicated urinary tract infections, including pyelonephritis, by resistant gram-negatives Acute pyelonephritis →
- Complicated intra-abdominal infections Intra-abdominal abscess →
- Hospital-acquired and ventilator-associated pneumonia Hospital-acquired and ventilator-associated pneumonia →
Adverse effects
Common
- Nausea, vomiting and diarrhoea
- Headache
- Pain, swelling or redness at the infusion site
Contraindications
- Severe allergy to any component
Key interactions
- Valproic acid
- Carbapenems sharply lower the levels of this antiepileptic; they are not given together.
What is monitored
- Kidney function to adjust the dose
- Neurological status (seizures, tremor, confusion)
- Culture and susceptibility: kept for multidrug-resistant gram-negatives
Administration and safety
- IV infusion over about 30 minutes
- Kept for multidrug-resistant gram-negatives according to susceptibility testing
- Name looks like imipenem with cilastatin (without relebactam): the product is checked
Nursing care
- Ask about epilepsy and valproic acid
- Ask about severe beta-lactam allergy
- Watch for seizures, tremor or confusion, above all in kidney failure
- Watch for watery or bloody diarrhoea
Pharmacokinetics
- Absorption
- Not absorbed by mouth; IV only.
- Elimination
- Renal; needs adjustment in kidney failure.
- Half-life
- Short, around one hour for each component.
Test yourself
Think of the answer, then tap the question to see it.
What does each component of imipenem-cilastatin-relebactam do?
Imipenem kills the bacterium; cilastatin stops its renal breakdown; relebactam blocks beta-lactamases such as KPC.
Which carbapenemases does relebactam not protect against?
Metallo-beta-lactamases.
Why is a carbapenem not combined with valproic acid?
Carbapenems sharply lower valproate levels, which can leave the person unprotected against seizures.
Connections
← Back to the class: Carbapenems
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Imipenem, Cilastatin, and Relebactam Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Crystal structure of KPC-2 complexed with relebactam (16 hour soak) (RCSB Protein Data Bank, 2026).
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Representative model, for educational purposes only.