Difelikefalin Trade name Korsuva.
Pregnancy category AU: B1
Routes of administration Intravenous.
Drug class Kappa opioid receptor agonist.
Bioavailability 100% (IV)
Metabolism Not metabolized
Elimination half-life 2 hours
Excretion Excreted as unchanged
drug via bile and urine
It is an analgesic opioid peptide used for the treatment of moderate to severe itching.
It acts as a peripherally specific, highly selective agonist of the κ-opioid receptor (KOR).
Difelikefalin acts as an analgesic by activating KORs on peripheral nerve terminals and KORs expressed by certain immune system cells.
Activation of KORs on peripheral nerve terminals results in the inhibition of ion channels responsible for afferent nerve activity.
Activation of KORs on peripheral nerve terminals reduces transmission of pain signals, while activation of KORs expressed by immune system cells results in reduced release of proinflammatory, nerve-sensitizing mediators, such as prostaglandins.
It is intended for treatment of moderate-to-severe pruritus associated with chronic kidney disease.
It is affective for Notalgia Paresthetica.
Due to its peripheral selectivity, difelikefalin lacks the central side effects like sedation, dysphoria, and hallucinations of previous KOR-acting analgesics such as pentazocine and phenazocine.
A peripherally restricted, selective kappa opioid receptor agonist that exerts anti-pruritic effect by means of activation of kappa opioid receptors on peripheral neurons and immune cells.
It restricts passive diffusion across membranes, thereby limiting access to kappa opioid receptors in the CNS.
In patients undergoing hemodialysis with moderate to severe pruritus there is significant reductions in itch intensity and significant improvement in it h related quality-of-life and sleep.