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difelikefalin

V03AX04

Forms & Strengths

Sterile lyophilized powder for injection
Reconstituted with sterile water to 0.5 µg/mL solution
Supplied as 1 mg vial (≈2000 µg)
Prefilled syringes for IV administration after hemodialysis

Adult Dosing

0.5 µg/kg intravenous bolus administered at the end of each hemodialysis session (3×/week)
Maximum single dose ≈70 µg (based on 140 kg patient)
Can be increased to 1 µg/kg if itch persists after ≥4 weeks under physician supervision
No dose adjustment needed for hepatic impairment; use with caution in severe hepatic dysfunction
Treatment duration studied up to 12 weeks; continue as long as benefit outweighs risk

Pediatric Dosing

Not approved for patients <18 years; safety and efficacy not established
Use not recommended in pediatric dialysis population

Indications

Moderate‑to‑severe pruritus associated with chronic kidney disease in patients receiving maintenance hemodialysis

Mechanism of Action

Highly selective peripherally acting κ‑opioid receptor agonist
Activates κ‑OR on peripheral sensory neurons, reducing release of pruritogenic mediators
Limited central nervous system penetration minimizes classic opioid side‑effects

Contraindications

Known hypersensitivity to difelikefalin or any excipients
Not indicated for use in patients not receiving hemodialysis

Adverse Reactions

Nausea (≈13 %)
Diarrhea (≈12 %)
Headache (≈9 %)
Somnolence (≈8 %)
Dizziness
Hypotension or transient blood pressure drop
Infusion‑site pain or erythema
Potential worsening of pruritus in rare cases

Drug Interactions

Minimal CYP450 metabolism; low potential for pharmacokinetic interactions
Caution when co‑administered with other κ‑opioid agonists (additive effect)
Additive CNS depression possible with other opioids or sedatives, though central penetration is low
No dose adjustment required when given with dialysis‑compatible medications

Curated Content: Needs Vetting Before Put to Clinical Use