[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Carbapenems](https://durgical.com/en/pharmacology/classes/carbapenems/) › Imipenem + cilastatin + relebactam

# 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.

Updated Nov 1, 2026

Also called: imipenem/cilastatin/relebactam

## Quick facts

**Group**
[Carbapenems](https://durgical.com/en/pharmacology/classes/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.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

✂**Bacterial PBPs (imipenem) and class A and C beta-lactamases, including KPC (relebactam)**Imipenem + cilastatin + relebactam

ⓘ 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.

**Target in 3D:** Bacterial PBPs (imipenem) and class A and C beta-lactamases, including KPC (relebactam). PDB structure 6QW9 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/6QW9) · Drag to rotate · pinch to zoom

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 →](https://durgical.com/en/conditions/acute-pyelonephritis/)
- Complicated intra-abdominal infections [Intra-abdominal abscess →](https://durgical.com/en/conditions/intra-abdominal-abscess/)
- Hospital-acquired and ventilator-associated pneumonia [Hospital-acquired and ventilator-associated pneumonia →](https://durgical.com/en/conditions/hospital-acquired-and-ventilator-associated-pneumonia/)

## Adverse effects

### Common

- Nausea, vomiting and diarrhoea
- Headache
- Pain, swelling or redness at the infusion site

### Serious (rare, important)

- Seizures, confusion and myoclonus, above all with central nervous system lesions or kidney failure
- Severe allergic reactions
- Clostridioides difficile diarrhoea

## 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.

## Memory aid

«ReLEBactam, the KEY for KPC»: imipenem walks through the door KPC had shut, but the metal lock (metallo-beta-lactamase) stays jammed.

## 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.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/imipenem-cilastatin-relebactam/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## Connections

## Related drugs 3

- [Imipenem–cilastatin](https://durgical.com/en/pharmacology/imipenem-cilastatin/)
- [Meropenem–vaborbactam](https://durgical.com/en/pharmacology/meropenem-vaborbactam/)
- [Ceftazidime + avibactam](https://durgical.com/en/pharmacology/ceftazidime-avibactam/)

## Related conditions 3

- [Acute pyelonephritis](https://durgical.com/en/conditions/acute-pyelonephritis/)
- [Intra-abdominal abscess](https://durgical.com/en/conditions/intra-abdominal-abscess/)
- [Hospital-acquired and ventilator-associated pneumonia](https://durgical.com/en/conditions/hospital-acquired-and-ventilator-associated-pneumonia/)

[← Back to the class: Carbapenems](https://durgical.com/en/pharmacology/classes/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](https://medlineplus.gov/druginfo/meds/a619046.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [Crystal structure of KPC-2 complexed with relebactam (16 hour soak)](https://www.rcsb.org/structure/6QW9) (RCSB Protein Data Bank, 2026).

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Representative model, for educational purposes only.

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License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/imipenem-cilastatin-relebactam/