Drug reference

relebactam

Beta-lactamase inhibitor (diazabicyclooctane) · β-Lactamase Inhibitor (Co-formulated with β-lactam antibiotics)

START

Imipenem 500 mg / cilastatin 500 mg / relebactam 250 mg IV q6h

TYPICAL MAX

Relebactam 250 mg per dose every 6 h (1 g/day)

STOP IF

Severe hypersensitivity, seizures, or C. difficile colitis

WATCH

Renal function (dose-banding), seizures, hypersensitivity

CDSCO approvedATC J01CR05

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 6min · infusion start
PEAK: 30min · end infusion
t½: 1.2h · t½
DURATION: 6h · q6h

EXCRETION

Renal — >90% unchanged

route + CYP

INTERACTIONS

2 major

SEVERE in our sources

PREGNANCY

Use only if benefit outweighs risk; limited data.

FDA category + note

Top interactionssee all 5 →

GanciclovirSevereDatabaseKimi deep-research + Cla
Valproic AcidSevereDatabaseKimi deep-research + Cla

Mechanism

Non-beta-lactam, diazabicyclooctane beta-lactamase inhibitor that inhibits class A and class C (including KPC) beta-lactamases, restoring imipenem activity against many resistant Gram-negatives; itself lacks meaningful antibacterial activity.

Indications

Complicated urinary tract infections / pyelonephritis (with imipenem/cilastatin)Complicated intra-abdominal infections (with imipenem/cilastatin)Hospital-acquired/ventilator-associated bacterial pneumonia (with imipenem/cilastatin)

Dosing

Adult: Imipenem 500 mg/cilastatin 500 mg/relebactam 250 mg IV every 6 h over 30 min (i.e., relebactam 250 mg/dose).
Pediatric: Not established.
Renal adjustment: Reduce dose per CrCl band (e.g., CrCl 60–89: 1.0 g/250 mg q6h; <60: stepwise reductions per label).
Hepatic adjustment: No specific adjustment.
Geriatric: Adjust for renal function.
Max dose: Relebactam 250 mg per dose every 6 h (1 g/day)

Pharmacokinetics

Onset

Bactericidal levels from infusion

Peak effect

End of infusion

Duration

Dose every 6 h

Half-life

~1.2 h

Bioavailability

IV 100%

Protein binding

~22%

Metabolism

Not metabolised significantly

Excretion

Renal (>90% unchanged)

Contraindications

Hypersensitivity to relebactam, imipenem/cilastatin or beta-lactams (cross)

Side effects

Common

DiarrhoeaNausea/vomitingPhlebitis at infusion siteHeadacheRash

Serious

Severe hypersensitivity / anaphylaxis
Seizures (imipenem component — high doses / renal failure)
Clostridioides difficile colitis
Hepatotoxicity

Pregnancy & lactation

Pregnancy

Use only if benefit outweighs risk; limited data.

Lactation

Limited data; caution.

Drug interactions

Ganciclovir

Severe

Database

Additive seizure risk

Avoid combination