Parenteral Moderate to severe pruritus associated with chronic kidney disease
Adult: In patients undergoing haemodialysis: 0.5 mcg/kg dry body weight (target postdialysis weight) 3-4 times/week, given via IV bolus inj into the venous line of the dialysis circuit at the end of the haemodialysis treatment during or after rinse-back. No more than 4 doses/week should be given even if the number of haemodialysis treatments in a week exceeds 4. For haemodialysis treatments less than 1 hour, administration should be withheld until the next haemodialysis session. Dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).
Hepatic Impairment
Severe: Not recommended.
Special Precautions
Patient with NYHA class IV heart failure, history of atrial fibrillation; impaired blood-brain barrier (e.g. primary brain malignancies, CNS metastases or other inflammatory conditions, active multiple sclerosis, advanced Alzheimer's disease). Severe hepatic impairment. Pregnancy and lactation.
This drug may cause somnolence, dizziness or mental status changes, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor serum K frequently. Assess mental status and relief of itching.
Overdosage
Symptoms: Dizziness, somnolence, mental status changes, paraesthesia, fatigue, hypertension and vomiting. Management: Provide appropriate medical treatment according to the patient's clinical status. Perform haemodialysis for 4 hours using a high-flux dialyser to effectively clear difelikefalin from plasma.
Drug Interactions
Increased risk of dizziness and somnolence with sedating antihistamines, opioid analgesics and other CNS depressants (e.g. ondansetron, clonidine, gabapentin, pregabalin, zolpidem, alprazolam, trazodone, sertraline).
Action
Description: Mechanism of Action: Difelikefalin is a selective kappa opioid receptor agonist. It is believed to alleviate itchiness and exert anti-inflammatory effects through the activation of kappa opioid receptors on peripheral sensory neurons and immune cells. Pharmacokinetics: Distribution: Volume of distribution: Approx 238 mL/kg. Plasma protein binding: 23-28%. Excretion: Via urine (11%); faeces (59%); dialysate fluid (20%). Elimination half-life: 23-31 hours.
Chemical Structure
Difelikefalin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 24794466, Difelikefalin. https://pubchem.ncbi.nlm.nih.gov/compound/Difelikefalin. Accessed May 28, 2024.
V03AX04 - difelikefalin ; Belongs to the class of other therapeutic products. Used in the management of pruritus in haemodialysis patients.
References
Anon. Difelikefalin Acetate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 11/04/2024.Buckingham R (ed). Difelikefalin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2024.Difelikefalin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 04/04/2024.Joint Formulary Committee. Difelikefalin. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2024.Kapruvia 50 micrograms/mL Solution for Injection (Vifor Fresenius Medical Care Renal Pharma France). MHRA. https://products.mhra.gov.uk. Accessed 04/04/2024.Korsuva 50 micrograms/mL Solution for Injection (Vifor Fresenius Medical Care Renal Pharma Ltd.). MIMS Singapore. http://www.mims.com/singapore. Accessed 21/05/2024.Korsuva Injection, Solution (Vifor [International] Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/04/2024.
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