Opoids Flashcards

1. List the three opioid receptor subtypes, the endogenous ligands for each receptor subtype, and the prototype exogenous opioid agonists that bind to each receptor subtype 2. List at least 8 important pharmacological effects produced by opioid agonists and name the receptor subtype that mediates each effect 3. Describe the differences in the pharmacology between full and partial opioid agonists 4. List the prototype opioid receptor antagonists, list which receptor subtype they bind to,

1
Q

three opioid receptor subtypes

A

Mu, Delta, Kappa

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2
Q

role of Mu receptor

A

supraspinal analgesia, miosis, respiratory depression, euphoria, dependance

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3
Q

role of kappa receptor

A

spinal analgesia, sedation

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4
Q

opioid receptor type

A

G protein

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5
Q

endogenous opioid that has affinity to mu

A

Beta

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6
Q

endogenous opioid that has affinity to delta

A

enkephalin

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7
Q

endogenous opioid that has affinity to kappa

A

dynorphins

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8
Q

path of pain sensation

A

peripheral stimulation creates APs –> APs travel up nerve to dorsal horn of SC –> up 2nd nerve to thalmus/brainstem –> 3rd nerve to cortex for pereption

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9
Q

where opiods work

A

spinal and supraspinal levels

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10
Q

opioid MOA in presynaptic terminal

A

decreases Ca++ influx in response to incoming APs - keeps neuron bouton from releasing NT

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11
Q

NT in pain circiut

A

substance P

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12
Q

opioid MOA in postsynaptic terminal

A

increases K+ conductance and thereby decreases the postsynaptic response to exitatory neurotransmission

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13
Q

analgesic effects of opioids

A

effective against dull pain
decreases response to pain
increases pain threshold

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14
Q

GI theraputic effects of opioids

A

increased tone and decreased motility

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15
Q

antitusive MOA of opioids

A

suppression of cough reflex in medullary center

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16
Q

adverse effects of opioids

A

respiratory depression, miosis, sedation, euphoria, emesis, urinary retention, bilary spasm, chest wall rigidity

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17
Q

effects of opioids that tolerance occurs to

A

deppressent effects

18
Q

timimg of opioid withdrawal

A

begins 6 hrs after last dose, peaks at 48 hours, declines for 10 days

19
Q

sx of opioid withdrawal

A

sweating, nausea, vomiting, cramps, shivering, shakes, restlessness,

20
Q

most active forms of opioids

A

levo forms

21
Q

example mu-agonists (9)

A

morphine, heroin, codine, meperidine, fentanyl, congeners, methadone, propoxyphene, pentazocine, buprenorphine, tramadol

22
Q

reason heroin is more abused

A

higher potency, higher lipid soluability

23
Q

protoype mu agonist

24
Q

used as antitussive

25
mu agonist with anticholenergic effects
meperidine
26
OD of this can lead to convulsions
meperidine
27
opioids used as anesthetic adjuvants
fentanyl/ xxxx-entanil
28
opioid that uses the dextro form
propoxyphene (darvocet)
29
popular opioid for mild to moderate pain
propoxyphene
30
partial mu agonist
pentazocine/buprenorphine
31
alternative to methadone
buprenorphine
32
use of tramadol
restless leg, fibromyalgia, acid reflux, premature ejacualtion
33
MOA of tramadol
weak partial mu agonist, blocks NE reuptake, releases serotonin
34
opioids that are metabolized to active compounds
morphine, meperidine, heroin, hydrocodone, oxycodone
35
opioid antagonists
naloxone, naltrexone,
36
short acting opioid antagonist
naloxone
37
long acting opioid antagonist
naltrexone
38
opioid antagonist used in maintaince therapy
naltrexone
39
opioid antagonist used in emergency
naloxone
40
anti-tussive that does NOT work on opiod receptors
dextromethorphan
41
opioids used at anti-diarreha
loperamide and diphenoxylate
42
widely abused prescription opioid
oxycodone