Difelikefalin (Topical)

Class: Skin and Mucous Membrane Agents, Miscellaneous
Chemical Name: 4-amino-1-[(2R)-6-amino-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid
Molecular Formula: C₃₆H₅₃N₇O₆
CAS Number: 1024828-77-0
Brands: Korsuva

Medically reviewed by Drugs.com on Sep 13, 2021. Written by ASHP.

Introduction

Difelikefalin acetate is a kappa opiate receptor agonist that is used for its antipruritic effects.

Uses for Difelikefalin (Topical)

Difelikefalin acetate has the following uses:

Difelikefalin acetate is a kappa opiate receptor agonist indicated for the treatment of moderate-to-severe pruritus associated with chronic kidney disease (CKD-aP) in adults undergoing hemodialysis (HD).

Difelikefalin acetate has the following limitations of use:

Difelikefalin acetate has not been studied in patients on peritoneal dialysis and is not recommended for use in this population.

Difelikefalin (Topical) Dosage and Administration

General

Difelikefalin acetate is available in the following dosage form(s) and strength(s):

Injection: 65 mcg /1.3 mL (50 mcg/mL) of difelikefalin

Dosage

It isessentialthat the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

Adults

Dosage and Administration

• Recommended dosage is 0.5 mcg/kg.

• Administer by intravenous bolus injection into the venous line of the dialysis circuit at the end of each HD treatment.

• Do not mix or dilute difelikefalin acetate prior to administration.

• Administer within 60 minutes of syringe preparation.

Cautions for Difelikefalin (Topical)

Contraindications

• None.

Warnings/Precautions

Dizziness, Somnolence, Mental Status Changes, and Gait Disturbances

Dizziness, somnolence, mental status changes, and gait disturbances (including falls) have occurred in patients taking difelikefalin acetate and may subside over time with continued treatment. In 2 clinical trials, 17.0% of patients randomized to receive difelikefalin acetate reported at least one of these adverse reactions, compared to 12.0% of patients who received placebo. The incidence of somnolence was higher in difelikefalin acetate-treated subjects 65 years of age and older (7.0%) than in difelikefalin acetate-treated subjects less than 65 years of age (2.8%). Concomitant use of cent...