Relebactam

Relebactam Uses, Dosage, Side Effects, Food Interaction and all others data.

Relebactam is a diazabicyclooctane beta-lactamase inhibitor, similar in structure to avibactam. It includes a piperidine ring which reduces export from bacterial cells by producing a positive charge. It is currently available in a combination product which includes imipenem and cilastatin to treat complicated urinary tract infections (UTIs), pyelonephritis, and complicated intra-abdominal infections in adults. It is considered to be a last-line treatment option and gained FDA approval as part of the combination product RecarbrioⓇ in July 2019.

Relebactam prevents the hydrolysis of imipenem, allowing it to exert its bactericidal effect.

Relebactam
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Relebactam
Generic	Relebactam
Relebactam Other Names	Relebactam
Type
Formula	C₁₂H₂₀N₄O₆S
Weight	Average: 348.37 Monoisotopic: 348.110355554
Protein binding	Relebactam is approximately 22% plasma protein bound.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Relebactam is a beta-lactamase inhibitor used to prevent hydrolysis of beta-lactam antibiotics, leading to increased effectiveness.

Relebactam is indicated in combination with imipenem and cilastatin for the treatment of complicated urinary tract infections (including pyelonephritis), and complicated intra-abdominal infections caused by susceptible organisms in adults.

Relebactam is also used to associated treatment for these conditions: Complicated Intra-Abdominal Infections, Complicated Urinary Tract Infection, Pyelonephritis

How Relebactam works

Relebactam is a beta-lactamase inhibitor known to inhibit many types of beta-lactamases including Ambler class A and Ambler class C enzymes, helping to prevent imipenem from degrading in the body. Similar to the structurally-related avibactam, first, relebactam binds non-covalently to a beta-lactamase binding site, then, it covalently acylates the serine residue in the active site of the enzyme. In contrast to some other beta-lactamase inhibitors, once relebactam de-acylates from the active site, it can reform it's 5 membered ring and is capable of rebinding to target enzymes.

Toxicity

If overdose with the combination product which includes relebactam, imipenem and cilastatin occurs, the drug should be stopped immediately and the patient should be provided with supportive care. Relebactam, imipenem, and cilastatin may be removed via hemodialysis; however, the use of hemodialysis to manage cases of overdose has not been studied.

Food Interaction

No interactions found.

Volume of Distribution

Relebactam has a volume of distribution of approximately 19 L with both single and steady state dosing.

Elimination Route

Currently, relebactam is only available as an intravenous product; therefore, there is no relevant absorption data in the literature.

Half Life

Relebactam has a half-life of 1.2 hours as per official FDA labeling. Values reported in pharmacokinetic studies vary from 1.35-1.8 hours.

Clearance

Relebactam has a reported total clearance of approximately 130-150 mL/min (8 L/h). About 30% of the total drug clearance can be attributed to active tubular secretion.