Opioid Agonists and Antagonists (M3) Flashcards
What are all compounds that work at opiod receptors (agonists, partial agonists, and antagonists) called?
opioid
What are naturally occurring alkaloids (morphine, codeine, thebaine, papaverine) called?
opiates
What are sleep-inducing medications called?
narcotics
What are the three opioid receptor types?
- mu
- delta
- kappa
What are the three families of endogenous opioid peptides?
- endorphins
- enkephalins
- dynorphins
Where can opioids accumulate?
muscle and fat
Where is heroin metabolized?
plasma
What is the mechanism of opioids?
bind G-protein-coupled receptors in brain and spinal cord involved in transmission and modulation of pain
What is the cellular mechanism of opioids?
- close voltage gated Ca2+ channels on presynaptic nerve terminal, reducing NT release
- open K+ channels and hyperpolarize, inhibiting postynaptically
What are the unique functions of mu receptors? 1. What is the relative affinity for the peptides? 2
- sedation, inhibition of resp, slow GI transit, modulate hormone and NT release
- endorphins > enkephalins > dynorphins
What are the unique functions of delta receptors? 1. What is the relative affinity for the peptides? 2
- modulation of hormone ant NT release
2. enkephalins > endorphins > dynorphins
What are the unique functions of kappa receptors? 1. What is the relative affinity for the peptides? 2
- psychotomimetic effects, slowed GI transit
2. dynorphins»_space; endorphins and enkephalins
What peptide do most opioid analgesics act on?
mu receptor
What peptide do most endogenous opioids act on?
delta and kappa
What pathways do opioids act on?
- ascending pain pathways
2. descending (modulatory) pathways