Opioid Analgesics and Antagonists Flashcards Preview

Dental Pharmacology > Opioid Analgesics and Antagonists > Flashcards

Flashcards in Opioid Analgesics and Antagonists Deck (81):
1

Strong agonists?

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

2

Moderate agonists?

codeine, oxycodone

3

Weak agonists?

propoxyphene, tramadol

4

Mixed agonists/antagonists?

pentazocine, nalbuphine, butorphanol

5

Antagonists?

naloxone, naltrexone, nalmefene

6

Antitussives?

codeine, dextromethorphan, levopropoxyphene

7

opium resin contains 3 major alkaloids?

morphine, codeine, thebaine

8

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

B-endorphin

9

2 pentapeptides (enkephalins)?

Met-enkephalin and Leu-enkephalin

10

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

the pituitary, hypothalamus, midbrain and striatum

11

opioid bind to ....?

mu, delta and kappa receptors

12

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

mu
kappa and delta

13

neospinothalamic?

fast Adelta fibers

14

paleospinothalamic?

slow C fibers

15

CNS distribution of mu and kappa receptors?

cerebral cortex, striatum, hippocampus, dorsal horn, midbrain

16

How is CNS distribution of delta receptor different?

amygdala instead of midbrain

17

pharmacologic functions of mu receptors?

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

18

pharmacologic functions of kappa receptors?

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

19

pharmacologic functions of delta receptors?

analgesia, emotion/reward, seizures (?)

20

prototypic ligands of mu receptors?

morphine, methadone, endorphin

21

prototypic ligands of kappa receptors?

dynorphin A and ethylketocyclazocine

22

prototypic ligands of delta receptors?

enkephalins and deltorphin II

23

effects of morphine binding at mu?

agonist

24

effects of morphine binding at kappa?

agonist (weak)

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