2012
DOI: 10.2340/00015555-1353
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Systemic Kappa Opioid Receptor Agonists in the Treatment of Chronic Pruritus: A Literature Review

Abstract: Chronic pruritus is frequently refractory to currently available treatments. Studies suggest that pruritus may arise from an imbalance of the mu- and kappa-opioid receptor system activity in either the skin or the central nervous system. Stimulation of kappa-opioid receptors by their agonists inhibits pruritus in both animals and humans. The antipruritic effect of kappa-opioid receptors agonists can currently be assumed to be related to their binding to kappa-opioid receptors on keratinocytes and cutaneous and… Show more

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Cited by 126 publications
(87 citation statements)
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“…101) Thus, opioid μ-and κ-receptors are potential therapeutic targets for pruritus. In the spinal cord, the opioid μ-receptor isoform MoR1d heterodimerizes with the bombesin BB 2 receptor, and the stimulation of MoR1d by morphine produces an effect similar to the stimulation of the BB 2 receptor.…”
Section: Itch-inhibitory Systemmentioning
confidence: 99%
“…101) Thus, opioid μ-and κ-receptors are potential therapeutic targets for pruritus. In the spinal cord, the opioid μ-receptor isoform MoR1d heterodimerizes with the bombesin BB 2 receptor, and the stimulation of MoR1d by morphine produces an effect similar to the stimulation of the BB 2 receptor.…”
Section: Itch-inhibitory Systemmentioning
confidence: 99%
“…It is generally thought that the mu-opioid system induces itch, whereas the kappaopioid system suppresses itch at the central level. 7,67) Recently, the effectiveness of nalfurafine hydrochloride (reMItcH ® ), a selective kappa-opioid receptor agonist, on hemodialysis-related uremic pruritus was validated in a Phase III, randomized double-blind placebo-controlled trial. 68) This drug is also expected to make further contributions to the treatment of patients with intractable itch, such as those with cholestasis and atopic dermatitis.…”
Section: New Anti-pruritic Drugsmentioning
confidence: 99%
“…for 24 h), naltrexone (50-100 mg/day orally) or nalmefene (20-120 mg/day orally) may show considerable relief of itch (48). Butorphanol is a κ-opioid agonist and a μ-antagonist and possess (weak) analgesic and antipruritic effects in non-Hodgkin lymphoma when given at a dose of intranasally 1 mg/day (49,50).…”
Section: Diagnostics and Treatmentmentioning
confidence: 98%