Opiod Drug I Flashcards
Morphine works on what receptor
Mu agonist
4-5 hrs analgesia for mod to severe pain
morphine
Side effects of all Mu agonists
Constipation, euphoria, sedation, resp. depression, nausea, decreased LH release, increased ADH secretion (mu) or decreased (kappa), pupillary constriction
Has a large 1st pass in oral dose
morphine
Constipation, euphoria, sedation, resp. depression, nausea, decreased LH release, increased ADH secretion (mu) or decreased (kappa), pupillary constriction
side effects of all mu agonists
Can cause gall stones!
Fentanyl
i would faint if i had gall stones!
100x as potent as Morphine, short duration (1-1.5 hrs)
Fentanyl
Fentanyl uses:
100x potent as morphine and short duration
given as patch or IM
Used for moderate to severe pain. Conscious sedation (short-duration) as a patch or IM
Fentanyl
“its Fen-tastic!!! its 100x more potent AND i’m conscious”
Fentanyl works on which R
mu agonist
MOderate to severe pain but longer acting then morphine
methedone
because of it’s longer duration… some concern with OD fatality and abuse
Methadone
methadone… you could be DONE :(
Forms toxic metabolite normeperidine
Meperidine
…NO..meperidine~ normeperidine = toxic
Moderate to severe pain.
Conscious sedation
(short-duration)
Meperidine (opioid)
Meperidine:
pain
type of sedation
duration
moderate to sevre
short duration
consious sedation
Contraindicated if you use Meperidine (opioid)
MAOIs
Prodrug, highly lipophilic and gets to brain quickly
Heroin (opioid)
weak mu agonist
Codeine
used for mild pain and is antitussive
codeine
—codeine for cough but a bitchy pain helper
uses of codeine
mostly antitussive, some pain relief and given in mixutre with acetominophen or aspirin
Pro-drug - some is metabolized to morphine. Antitussive.
Codeine
more efficacious then codeine and for moderate to severe pain
oxycodone
Oxycodone is a
mu agonist opioid
Sustained release oral (major abuse)
oxycodone
Codeine like efficacy for mild to moderate pain
Hydrocodone `aka Vicodin
opiod that is 2-3x as potent as Morphine
hydromorphone~~~ Mu agonist
Nalbuphine receptor actitivity:
mu antagonist,
kappa agonist
Mu antagonist, kappa agonist
Nalbuphine
Nalbuphine’s efficacy profile
Similar to Morphine, but little euphoria and low abuse
Who would get nalbuphine?
used to precipitate opioid withdrawl
used to precipitate opioid withdrawl
nalbuphine or Buprenorphine
Delivery of Nalbuphine
IM only
Buprenorphine receptor activity
partial mu agonist
Given oral or as a patch to opioid dependents along with naloxone for opioid dependence
Buprenorphine
Naloxone (opioid antagonist) on what receptors
Mu antagonist, less so for kappa and delta
Only works when injected/crushed; not orally.
Thus, prevents abuse when given with opioid (buprenorphine). 1-2 hr duration.
Naloxone
How do we deliver naloxone
crushed/injected with opiod (buprenorphine)
Naloxone is most active:
given parenterally then orally
you mix this with buprenorphine to help with opiod withdrawl
Naloxone
Inhibits reward of opiates and alcohol. 24+ hr duration
Naltrexone
Naltrexone is a (receptro)
Mu antagonist
na—-TREX–one) trex aren’t something we want… antagonist (vs naloxone are agonist
What does Naltrexone do
inhibits the reward system of opioites
What drug tx alcohol and opioate abuse
naltrexone
Dextramethorphan works on what R
NMDA antagonist… antitussive
-dextramethorphaNNNNN…..NMDA
NMDA antagonist that is antitussive
Dextramethorphan (opioid related)
Weak Mu agonist, blocks NET and SERT
Tramadol (opioid related)
Tramadol R activity
weak Mu agonist and blocks NET and SERT
transvestite because does both Mu agonist then NET and SERT
Tramadol is used for
mild to moderate pain (oral and sustained release)
Combination of Buprenorphine and Naloxone to tx opioid dependence
Suboxone
Cough suppresants
Codeine, hydrocodone and dextromethorphan
Codeine and heroin are activated by
metabolism
