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dental pharmacology > Opioid Analgesics and Antagonists > Flashcards

Opioid Analgesics and Antagonists Flashcards

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
Q

effects of buprenorphine binding at mu?

A

mixed agonist/antagonist

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26
Q

effects of buprenorphine binding at kappa?

A

antagonist

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27
Q

effects of buprenorphine binding at delta?

A

antagonist

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28
Q

effects of pentazocine binding at mu?

A

antagonist (weak)

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29
Q

effects of pentazocine binding at kappa?

A

agonist

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30
Q

effects of nalbuphine binding at mu?

A

antagonist

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31
Q

effects of nalbuphine binding at kappa?

A

agonist

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32
Q

effects of nalaxone binding at mu?

A

antagonist

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33
Q

effects of nalaxone binding at kappa?

A

antagonist

34
Q

effects of nalaxone binding at delta?

A

antagonist (weak)

35
Q

which semi synthetic opioid drug is 40x more potent than morphine?

A

buprenorphine

36
Q

which synthetic opioid drug can be given to those who need pain managed for awhile?

A

fentanyl

37
Q

codeine is only … as potent as morphine?

A

half

38
Q

CNS depression of Morphine is enhanced by …

A

sedative-hypnotics, antipsychotic drugs, antidepressants

39
Q

… may interfere with opioid induced analgesia?

A

sedative-hypnotics

40
Q

opioids (esp. meperidine) are contraindicated with …

A

MAOI antidepressants

41
Q

CNS effect of morphine?

A

analgesia, euphoria, stupor or tupor

42
Q

morphine: respiratory center depression or excitation?

A

depression

43
Q

True or False: cough reflex center is depressed by morphine

A

true

44
Q

True or false: miosis by morphine

A

true

45
Q

1/10 potency of morphine; cough suppression; mild to moderate pain?

A

codeine

46
Q

1/2 the potency of morphine; mild to moderate pain and antitussive?

A

hydorcodone/dihydrocodone

47
Q

moderate to severe pain; 2x potency of morphine; high abuse potential; bioavailability 80%?

A

oxycodone

48
Q

combo of oxycodone w/ acetaminophen?

A

percoset

49
Q

severe pain relief (acute pain); high potency (7-10x ) at Mu receptor sites?

A

hydromorphone

50
Q

severe pain relief; 7x more potent than morphine?

A

oxymorphone

51
Q

first fully synthetic; 1/10 potency of morphine; respiratory depression in neonates?

A

meperidine

52
Q

nor-meperidine is …?

A

neurotoxic

53
Q

moderate to severe pain relief (traditional use); opiate dependence treatment?

A

buprenorphine

54
Q

buprenorphine and naloxone?

A

suboxone

55
Q

severe pain relief; fully synthetic; most potent opioid?

A

fentanyl

56
Q

moderate to severe pain; mainstay of opiate dependence treatment; fully synthetic?

A

methadone

57
Q

moderate to severe pain; fully synthetic; atypical opioid; partially blocked by naloxone; inhibits reuptake of NE and 5-HT?

A

tramadol

58
Q

opioid receptor antagonist; short duration of action; only injectable?

A

naloxone

59
Q

opioid receptor antagonist; long duration of action?

A

nalmefene

60
Q

opioid receptor antagonist; long duration of action; long duration of action; reduces craving?

A

naltrexone

61
Q

routes of admin of fentanyl?

A

IM, IV, transdermal

62
Q

duration of action of fentanyl?

A

1 hr

63
Q

elimination half life of fentanyl?

A

4 hrs

64
Q

does fentanyl have active metabolite?

A

No

65
Q

routes of admin of methadone?

A

oral and parenteral

66
Q

duration of action of methadone?

A

8 hrs

67
Q

elimination half life of methadone?

A

24 hrs

68
Q

does methadone have active metabolite?

A

No

69
Q

route of admin of propoxyphene?

A

oral

70
Q

duration of action of propoxyphene?

A

4 hrs

71
Q

elimination half life of propoxyphene?

A

9 hrs

72
Q

does propoxyphene have active metabolite?

A

Yes

73
Q

route of admin of naloxone?

A

parenteral

74
Q

duration of action of naloxone?

A

2 hrs

75
Q

elimination half life of naloxone?

A

4 hrs

76
Q

does naloxone have active metabolite?

A

No

77
Q

route of admins of naltrexone?

A

oral

78
Q

duration of action of naltrexone?

A

24 hrs

79
Q

elimination half life of naltrexone?

A

12 hrs

80
Q

does naltrexone have active metabolite?

A

Yes

81
Q

two opioid receptor agonists with no analgesic effects and used mainly as antidiarrheal?

A

diphenoxylate and loperamide

dental pharmacology (30 decks)

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