Opioids Flashcards
Opioids MOA
Opioid receptor agonists, blocks release of pain neurotransmitters from nociceptors and inhibits GABA release
Opioid receptors
Mu receptors, kappa receptors, delta,
Mu receptor location
found in the brainstem and medial thalamus
Mu receptor actions
analgesia, respiratory depression, euphoria, sedation, decreased GI motility, physical dependence
Kappa receptor location
limbic and other diencephalic areas, brainstem, spinal cord
Kappa receptor actions
analgesia, sedation, dyspnea, dysphoria, respiratory depression
Delta receptor location
brain
Opioid agonists
morphine, fentanyl, hydromorphone, codeine, oxycodone, methadone, heroin
Partial agonists
buprenorphine, butorphanol
anatagonists
Naloxone, naltrexone
Suboxone
buprenorphine + naloxone
Short acting
codeine, hydrocodone, hydromorphone, morphine, oxycodone, oxymorphone, fentanyl
Long acting
fentanyl, levorphanol, methadone, morphine, oxycodone, oxymorphone
ADR
sedation, lethargy, constipation, respiratory depression, NV, pruritis/urticaria
Over dose triad
miosis, loss of consciousness, respiratory depression
Over dose antidote
naloxone
Morphine ADR
direct histamine release, respiratory depression, orthostasis, constipation, NV
Codeine MOA
weak mu agonist, metabolized to morphine
Codeine drug interactions
inhibited by bupropion, cimetidine, celecoxib, cocaine
Oxycodone MOA
activity at mu and kappa receptors, high potency analgesic
Hyrocodone MOA
weak activity at mu receptor
Hydromorphine MOA
activity at mu and delta receptors
Fentanyl MOA
strong mu agonist
Meperidine (demerol) MOA
weak mu agonist