Opioids Flashcards
Opioid MOA, class
- Opioid receptor agonist
- Blocks release of pain neurotransmitters from nociceptive fibers
- Inhibits GABA release so that dopamine fire more vigorously and can accumulate in the gap ( = pleasure)
Pain neurotransmitters
Substance P
Glutamate
Calcitonin gene peptide
Opioid receptors
Mu - brainstem and medial thalamus
Kappa - limbic, spinal cord
Delta - brain, not well studied
Opioid receptor responsible for analgesia, respiratory depression, euphoria, sedation, decreased GI motility, addiction
Mu
Mu = Morphine Agonist
Opioid receptor responsible for dyspnea, dependence, dysphoria
Kappa
Full Opioid Agonists
Morphine
Fentanyl
Hydromorphone
Codeine
Oxycodone
Methadone
Heroin
Partial Opioid Agonists
Buprenorphine
Butorphenal
Suboxone (buprenorphine + Naloxone)
Opioid antagonists
Naloxone (Narcan)
Naltrexone
Morphine, oxycodone, methadone, fentanyl, amphetamine - what schedule?
Schedule II
Schedule III drugs
Moderate addiction potential
Hydrocodone, codeine, anaboilc steroids
Schedule IV drugs
Low addiction potential
Benzodiazepine, Meprobamate Butorphenol Pentazocine Propoxyphene
Why opioids can cause pruritus / uriticaria
Direct histamine response
Can also cause bronchospasm
Opioid overdose triad
Miosis
Loss of consciousness
Respiratory depression
much worse w alcohol or other CNS depressants
Antidote to opioid overdose
Naloxone
Half life of morphine
2 hours
Morphine drug interactions
RARE
Which opioid crosses the BBB
Morphine
Codeine is metabolized to
Morphine
Potency of Codeine vs Morphine
Codeine has 50% potency of morphine
What drugs inhibit effect of codeine and why?
2D6!
Buproprion
Cimetidine
Cocaine
Celecoxib
Codeine warning
ULTRA METABOLIZERS
esp infants nursing from mothers who take it
3 Kinds of oxycodone
Roxicodone
Percocet
Oxycontin
Why is oxycodone such a high potency analgesic?
Mu AND Kappa activity