opioids Flashcards
what is opium
dries latex obtained from poppy
what are opiates
any drug derived from opium
what is an opioid
any drug that binds to an opioid receptor
what is a narcotic
illegal use of opioids for non-medical purposes
what kind of receptors are opioid receptors
Gi
what are the downstream effects of opioid receptors
inhibit calcium channels, activate K channel, inhibit adenylyl cyclase
what are the 4 types of opioid receptors
mu kappa delta ORL1
What affects does a mu opioid receptor agonist have
analgesia, reward, antitussive, respiratory depression, constipation
what affects does a mu opioid antagonist have
aversive, prevent reward, block overdose
what does a delta opioid agonist do
not rewarding, no analgesia, seizure inducing
what does a delta agonist do?
no obvious affects
what effects does a kappa agonist have
aversive, hallucinogenic, anxiogenic
what effects does a kappa antaonist have
antidepressent, anxiolytic
What kind of action does morphine have
full mu opioid receptor agonist
what kind of action does buprenorphine have
partial mu opioid agonist
antagonist at delta and kappa
what kind of action does methadone have
full mu opioid receptor agonist
what kind of action does fentanyl have
full mu opioid receptor agonist
what kind of action does heroin have
full mu opioid receptor agonist
how do biased agonists work
arrests G protein signalling and activates its own
what are beta-arrestins
blocks further G protein signalling
what is UGT2B7
most important glucoronidation enzyme of morphine
what metabolizes codeine into morphine
CYP2D6
what are the 3 endogenenous opioid peptides
beta endorphins, enkephalins, dynorphins
describe the affinity of pro-enkephalin
delta»mu»kappa
what is the affinity of pro-opiomelanocortin
mu=delta»kappa
what is the affinity of pro-dynorphin
kappa»mu=delta
how do opioid receptors affect noxious inhibitory control
increase
how does opioid receptors affect the net nociceptive signals reaching the brain
reduction
how do opioids effect dopamine
increase (they inhibit the inhibitory GABAergic interneurons)
which agonists are being developved for migraines
delta opioid
what drug is being developed for migraine
TRV250 delta opioid biased agonist
what is CR845
analgesic, anit-inflammatory, anti itch
what is naloxone
non-selective competitive opioid receptor antagonist
