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

A

morphine

24
Q

used as antitussive

A

codine

25
Q

mu agonist with anticholenergic effects

A

meperidine

26
Q

OD of this can lead to convulsions

A

meperidine

27
Q

opioids used as anesthetic adjuvants

A

fentanyl/ xxxx-entanil

28
Q

opioid that uses the dextro form

A

propoxyphene (darvocet)

29
Q

popular opioid for mild to moderate pain

A

propoxyphene

30
Q

partial mu agonist

A

pentazocine/buprenorphine

31
Q

alternative to methadone

A

buprenorphine

32
Q

use of tramadol

A

restless leg, fibromyalgia, acid reflux, premature ejacualtion

33
Q

MOA of tramadol

A

weak partial mu agonist, blocks NE reuptake, releases serotonin

34
Q

opioids that are metabolized to active compounds

A

morphine, meperidine, heroin, hydrocodone, oxycodone

35
Q

opioid antagonists

A

naloxone, naltrexone,

36
Q

short acting opioid antagonist

A

naloxone

37
Q

long acting opioid antagonist

A

naltrexone

38
Q

opioid antagonist used in maintaince therapy

A

naltrexone

39
Q

opioid antagonist used in emergency

A

naloxone

40
Q

anti-tussive that does NOT work on opiod receptors

A

dextromethorphan

41
Q

opioids used at anti-diarreha

A

loperamide and diphenoxylate

42
Q

widely abused prescription opioid

A

oxycodone