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. 2023 Jan 13;24(2):1559. doi: 10.3390/ijms24021559

Table 2.

Effectiveness of opioid agonists and antagonists.

Drug Class Effectiveness
Difelikefalin KOR agonist
  • Worst Itching Intensity Numerical Rating Scale (WI-NRS) improved by 3 points or more in 51.9% of the patients in a double-blinded, randomized, controlled phase 3 clinical trial

  • Itch-related quality of life in the 5-D itch scale and the skindex-10 significantly improved in the trial

Nalbuphine KOR agonist
MOR antagonist
  • Mean visual analog scale for pruritus significantly improved in an open-label trial (4.0 to 1.2 at 180 mg/day and 0.4 at 240 mg/day)

  • Numerical rating scale for pruritus improved with nalbuphine 120mg, but not nalbuphine 60mg in a randomized, double-blind, placebo-controlled multi-center trial

Naltrexone Nonselective opioid antagonist
  • Beneficial effect not demonstrated in a randomized, double-blind, placebo-controlled crossover study

Nalfurafine hydrochloride KOR agonist
  • Significant reduction of pruritus shown in phase 3 clinical trial and open-label long-term study