Flashcards in Opioids Deck (25)
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1
neurotransmitters in ascending pain pathways
glutamate and substance P
2
neurotransmitters in descending pathways
norepinephrine, serotonin, and enkephalin
3
endogenous ligands of mu receptors
enkephalins, beta-endorphin
4
drugs that are mu receptor agonists
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morphine, codeine, methadone, meperidine, fentanyl, buprenorphine (partial)
5
drugs that are mu receptor antagonists
naloxone, naltrexone
6
kappa receptor endogenous ligand
dynorphins
7
kappa receptor drug ligand
nalbuphine
8
morphine: what it is, administration, bioavialability
-mu agonist
-injectable or oral
-extensive first pass effect when taken orally
9
codeine: what it is, comparison with morphine
-mu agonist
-not as efficacious as morphine
10
methadone: what it is, comparison with morphine, uses
-mu agonist
-longer duration of action than morphine and has better oral bioavailability
-used in treatment of opioid addiction and chronic pain
11
mepiridine: what it is, comparison with morphine, side effect
-mu agonist
-shorter duration of analgesia than morphine
-side effect: forms toxic metabolite that can accumulate
12
fentanyl: what it is, comparison with morphine, administration
-mu agonist
-100X as potent as morphine
-injectable, transdermal patches
13
mixed-action agonist/antagonists (2)
nalpbuphine, buprenorphine
14
nalbuphine: what it is, comparison with morphine
-mu antagonist and kappa agonist
-much lower abuse potential
15
buprenorphine: what it is, use
-partial mu agonist
-oral buprenorphine combined with naloxone is used to treat opioid addiction
16
mu antagonists (2)
naloxone, naltrexone
17
naloxone: what it is, uses
-mu antagonist
-opioid overdoses
-combined with buprenorphine to treat opioid addiction
18
naltrexone: what it is, uses
-mu antagonist
-used to treat alcoholism, opiate addiction
19
dextromethorphan: use
antitussive
20
significant tolerance develops to what effects of opioids?
emetic action, analgesic, respiratory, euphoria and endocrine effects
21
no tolerance develops to what effects of opioids?
constipation and miosis
22
drugs given to treat opioid addiction (3)
methadone, buprenorphine+naloxone, naltrexone
23
why is naloxone added to buprenorphine to treat opioid addiction?
this preparation is given orally because if given parenterally, naloxone would block the effect of buprenorphine due to its much higher bioavailability
24
treats opioid overdoses
naloxone
25
