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Dental Pharmacology > Opioid Analgesics and Antagonists > Flashcards

Opioid Analgesics and Antagonists Flashcards

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1
Q

Strong agonists?

A

fentanyl, sufentanil, hydromorphone, meperidine, morphine, methadone, buprenorphrine, oxymorphone

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2
Q

Moderate agonists?

A

codeine, oxycodone

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3
Q

Weak agonists?

A

propoxyphene, tramadol

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4
Q

Mixed agonists/antagonists?

A

pentazocine, nalbuphine, butorphanol

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5
Q

Antagonists?

A

naloxone, naltrexone, nalmefene

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6
Q

Antitussives?

A

codeine, dextromethorphan, levopropoxyphene

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7
Q

opium resin contains 3 major alkaloids?

A

morphine, codeine, thebaine

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8
Q

a 30 amino acid long peptide released from a precursor called POMC protein?

A

B-endorphin

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9
Q

2 pentapeptides (enkephalins)?

A

Met-enkephalin and Leu-enkephalin

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10
Q

dynorphin A and dynorhpin B are produced from pro-dynorphin in ….?

A

the pituitary, hypothalamus, midbrain and striatum

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11
Q

opioid bind to ….?

A

mu, delta and kappa receptors

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12
Q

morphine and other pure agonists have greater affinity for … and lower affinity for …?

A

mu

kappa and delta

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13
Q

neospinothalamic?

A

fast Adelta fibers

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14
Q

paleospinothalamic?

A

slow C fibers

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15
Q

CNS distribution of mu and kappa receptors?

A

cerebral cortex, striatum, hippocampus, dorsal horn, midbrain

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16
Q

How is CNS distribution of delta receptor different?

A

amygdala instead of midbrain

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17
Q

pharmacologic functions of mu receptors?

A

analgesia, sedation, miosis, euphoria, constipation, respiratory depression, pruritus

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18
Q

pharmacologic functions of kappa receptors?

A

analgesia, sedation, miosis, dysphoria, micturition, diuresis, hallucinations

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19
Q

pharmacologic functions of delta receptors?

A

analgesia, emotion/reward, seizures (?)

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20
Q

prototypic ligands of mu receptors?

A

morphine, methadone, endorphin

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21
Q

prototypic ligands of kappa receptors?

A

dynorphin A and ethylketocyclazocine

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22
Q

prototypic ligands of delta receptors?

A

enkephalins and deltorphin II

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23
Q

effects of morphine binding at mu?

A

agonist

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24
Q

effects of morphine binding at kappa?

A

agonist (weak)

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25
effects of buprenorphine binding at mu?
mixed agonist/antagonist
26
effects of buprenorphine binding at kappa?
antagonist
27
effects of buprenorphine binding at delta?
antagonist
28
effects of pentazocine binding at mu?
antagonist (weak)
29
effects of pentazocine binding at kappa?
agonist
30
effects of nalbuphine binding at mu?
antagonist
31
effects of nalbuphine binding at kappa?
agonist
32
effects of nalaxone binding at mu?
antagonist
33
effects of nalaxone binding at kappa?
antagonist
34
effects of nalaxone binding at delta?
antagonist (weak)
35
which semi synthetic opioid drug is 40x more potent than morphine?
buprenorphine
36
which synthetic opioid drug can be given to those who need pain managed for awhile?
fentanyl
37
codeine is only ... as potent as morphine?
half
38
CNS depression of Morphine is enhanced by ...
sedative-hypnotics, antipsychotic drugs, antidepressants
39
... may interfere with opioid induced analgesia?
sedative-hypnotics
40
opioids (esp. meperidine) are contraindicated with ...
MAOI antidepressants
41
CNS effect of morphine?
analgesia, euphoria, stupor or tupor
42
morphine: respiratory center depression or excitation?
depression
43
True or False: cough reflex center is depressed by morphine
true
44
True or false: miosis by morphine
true
45
1/10 potency of morphine; cough suppression; mild to moderate pain?
codeine
46
1/2 the potency of morphine; mild to moderate pain and antitussive?
hydorcodone/dihydrocodone
47
moderate to severe pain; 2x potency of morphine; high abuse potential; bioavailability 80%?
oxycodone
48
combo of oxycodone w/ acetaminophen?
percoset
49
severe pain relief (acute pain); high potency (7-10x ) at Mu receptor sites?
hydromorphone
50
severe pain relief; 7x more potent than morphine?
oxymorphone
51
first fully synthetic; 1/10 potency of morphine; respiratory depression in neonates?
meperidine
52
nor-meperidine is ...?
neurotoxic
53
moderate to severe pain relief (traditional use); opiate dependence treatment?
buprenorphine
54
buprenorphine and naloxone?
suboxone
55
severe pain relief; fully synthetic; most potent opioid?
fentanyl
56
moderate to severe pain; mainstay of opiate dependence treatment; fully synthetic?
methadone
57
moderate to severe pain; fully synthetic; atypical opioid; partially blocked by naloxone; inhibits reuptake of NE and 5-HT?
tramadol
58
opioid receptor antagonist; short duration of action; only injectable?
naloxone
59
opioid receptor antagonist; long duration of action?
nalmefene
60
opioid receptor antagonist; long duration of action; long duration of action; reduces craving?
naltrexone
61
routes of admin of fentanyl?
IM, IV, transdermal
62
duration of action of fentanyl?
1 hr
63
elimination half life of fentanyl?
4 hrs
64
does fentanyl have active metabolite?
No
65
routes of admin of methadone?
oral and parenteral
66
duration of action of methadone?
8 hrs
67
elimination half life of methadone?
24 hrs
68
does methadone have active metabolite?
No
69
route of admin of propoxyphene?
oral
70
duration of action of propoxyphene?
4 hrs
71
elimination half life of propoxyphene?
9 hrs
72
does propoxyphene have active metabolite?
Yes
73
route of admin of naloxone?
parenteral
74
duration of action of naloxone?
2 hrs
75
elimination half life of naloxone?
4 hrs
76
does naloxone have active metabolite?
No
77
route of admins of naltrexone?
oral
78
duration of action of naltrexone?
24 hrs
79
elimination half life of naltrexone?
12 hrs
80
does naltrexone have active metabolite?
Yes
81
two opioid receptor agonists with no analgesic effects and used mainly as antidiarrheal?
diphenoxylate and loperamide

Dental Pharmacology (30 decks)

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