Kappa-opioid partial agonist
Kappa-opioid receptor partial agonist
- Mixed effects with a ceiling
- Direction depends on endogenous opioid tone
- Kappa activation → analgesia, dysphoria, sedation, diuresis
Drugs with this mechanism (2)
- Nalmefene nasal — Long-acting opioid antagonist nasal spray for opioid overdose; outlasts naloxone, prolonging precipitated withdrawal.
- Nalmefene auto-injector — Long-acting opioid antagonist auto-injector for intramuscular or subcutaneous use in opioid overdose.
Self-check
- What determines the direction of kappa partial-agonist effects?
Endogenous opioid tone. - Do kappa partial-agonist effects have a ceiling?
Yes.
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