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
Meperidine interactions
MAOI- respiratory depression
Propoxyphene MOA
weak mu agonist, NMDA antagonist
porpoxyphene ADR
dizziness, sedation, weakness, falls, agitation, insomnia, neurotoxic, cardiotoxic
Methadone MOA
mu agonist serotonin-norepinephrine reuptake inhibitor, analgesic effect
Methadone ADR
cardiotoxicity- torsades
Buprenorphine MOA
mu receptor partial agonist, kappa receptor antagonist
Buprenorphine ADR
sedation, NV, dizziness, HA, respiratory depression
Naloxone (Narcane) MOA
mu receptor antagonist. reversal agent for opioid OD, reverses respiratory depression, sedation, hypotension
Naltrexone (vivitrol)
opioid receptor antagonist
Tramadol
synthetic codeine analog
tramadol ADR
seizure risk, suicide risk, serotonin syndrome risk, dizziness, vertigo, nausea, constipation, HA, somnolence, vomiting, pruritis
Tramadol interactions
CYP2D6, CYP3A4 inhibitor, serotinonergic drugs, Carbamazepine
Tapentadol MOA
mu opioid agonist, NE reuptake inhibitor
Tapentadole indication
specifically approved for diabetic neuropathy
Tapentadole ADR
fatal if taken with EtOH, drowsiness/dizziness
Opioid withdrawal symptoms
irratbility, anxiety, restlessness, chills, sweating, abd pain, ND, sneezing, rinorrhea, dilated pupils, muscle weakness, pain, insomnia