Opoids Flashcards
1. List the three opioid receptor subtypes, the endogenous ligands for each receptor subtype, and the prototype exogenous opioid agonists that bind to each receptor subtype 2. List at least 8 important pharmacological effects produced by opioid agonists and name the receptor subtype that mediates each effect 3. Describe the differences in the pharmacology between full and partial opioid agonists 4. List the prototype opioid receptor antagonists, list which receptor subtype they bind to,
three opioid receptor subtypes
Mu, Delta, Kappa
role of Mu receptor
supraspinal analgesia, miosis, respiratory depression, euphoria, dependance
role of kappa receptor
spinal analgesia, sedation
opioid receptor type
G protein
endogenous opioid that has affinity to mu
Beta
endogenous opioid that has affinity to delta
enkephalin
endogenous opioid that has affinity to kappa
dynorphins
path of pain sensation
peripheral stimulation creates APs –> APs travel up nerve to dorsal horn of SC –> up 2nd nerve to thalmus/brainstem –> 3rd nerve to cortex for pereption
where opiods work
spinal and supraspinal levels
opioid MOA in presynaptic terminal
decreases Ca++ influx in response to incoming APs - keeps neuron bouton from releasing NT
NT in pain circiut
substance P
opioid MOA in postsynaptic terminal
increases K+ conductance and thereby decreases the postsynaptic response to exitatory neurotransmission
analgesic effects of opioids
effective against dull pain
decreases response to pain
increases pain threshold
GI theraputic effects of opioids
increased tone and decreased motility
antitusive MOA of opioids
suppression of cough reflex in medullary center
adverse effects of opioids
respiratory depression, miosis, sedation, euphoria, emesis, urinary retention, bilary spasm, chest wall rigidity