Kappa-opioid agonist
Kappa-opioid receptor agonist
- Analgesia without mu-type reward
- Moderate analgesia
- Peripherally restricted agonism → ↓ pruritus
- Central activation brings dysphoria and dissociation — the “anti-reward”
- Anxiety, dysphoria, “anti-reward”
- Sedation
- Hallucinogenic at high dose
- ↓ post-anesthesia shivering
- Inhibition of orexin neurons
Drugs with this mechanism (9)
- Butorphanol — Mixed opioid agonist-antagonist; intranasal analgesia can precipitate opioid withdrawal.
- Difelikefalin — Peripheral kappa-opioid agonist for uremic itch; minimal CNS effects.
- Dynorphin — Endogenous kappa-opioid peptide linked to dysphoria.
- Eluxadoline — Gut-focused mixed opioid for IBS-D; contraindicated without a gallbladder.
- Ibogaine — Psychoactive alkaloid studied for addiction; cardiac (QT) risk.
- Nalbuphine — Mixed opioid agonist-antagonist analgesic with a ceiling on respiratory depression.
- Noribogaine — Long-acting active metabolite of ibogaine.
- Pentazocine — Mixed opioid agonist-antagonist; can precipitate withdrawal.
- Salvinorin A — Potent kappa-opioid psychedelic of Salvia divinorum; non-nitrogenous.
Self-check
- What symptom can peripherally restricted kappa agonism reduce?
Pruritus. - What central effects give kappa activation its anti-reward character?
Dysphoria and dissociation.
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