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Flashcards in Opioids Module Deck (48)
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1

MOA of Codeine

potency

- full MOR agonist

0.01

2

MOA of Morphine

potency

- full MOR agonist

1

3

MOA of Hydrocodone

potency

- full MOR agonist

1

4

MOA of Oxycodone

potency

- full MOR agonist

1.5

5

MOA of heroin

potency

- full MOR agonist

2

6

MOA of Buprenorphine


used for


negative effects


when do we give it

- partial MOR agonist (more potent)
- full kappa and delta antagonist

- reduces withdrawal symptoms without producing same level of addictive effects

- more potent and will displace opioids from receptor if taken at the same time precipitating withdrawal symptoms

- after withdrawal symptoms begin

7

MOA of Nalbuphine

- partial MOR agonist
- full kappa agonist

8

MOA of Methadone

potency

used for/benefits

negative effects

- full MOR agonist

1

- reduce withdrawal symptoms and ease detox
- long biological half life (24 hours)

- can be addictive

9

MOA of Meperidine

potency

- full MOR agonist

0.1

10

MOA of fentanyl

potency

- full MOR agonist

100

11

MOA of Remifentanil

potency

- full MOR agonist

200

12

MOA of carfentanil

potency

- full MOR agonist

10000

13

MOA of Butorphanol

- partial MOR agonist
- full kappa agonist

14

MOA of methylnaltrexone




what does it treat

- neutral MOR antagonist

- inhibit effects of other opioids through competition for receptor binding

- opioid induced constipation

15

MOA of pentazocine

- neutral MOR antagonist
- full kappa agonist

16

MOA of Naltrexone


used for

- inverse MOR agonist
- inhibit basal, opioid-independent activity of the receptor

- treat acute opioid overdoses

17

MOA of Naloxone


used for

- inverse MOR agonist
- inhibit basal, opioid-independent activity of the receptor

- treat acute opioid overdoses

18

what happens in transduction step of pain

- nociceptors increase rate of depolarization in response to noxious stimulus

19

what happens in the modulatory step of pain

- descending pathway of nerve impulse modules pain perception

20

both the ascending and descending pathway intersect where

what is this the site of

- in the dorsal horn of the spinal cord


- summation of intensity of pain
- site of opioid action

21

endorphins act on which opioid receptor

- mu

22

enkephalins act on which opioid receptor

- delta

23

dynorphins act on which opioid receptor

- kappa

24

opioids produce analgesia by agonizing receptors in the

- brain and spinal cord
- peripheral nociceptor neurons

25

opioids produce sedation and respiratory depression by acting on receptors in the

- brain

26

opioids produce constipation by acting on receptors in the

- myenteric/submucosal plexus of the enteric nervous system in the GI tract

27

can partial agonists produce full analgesia

- no, but still clinically useful

28

oral administration of opioids subjects them to the ____-

- first pass effect

29

opioids are metabolized by what reactions

what is the product

eliminated by

significance of the product

- phase I/phase II

- highly polar glucuronidated metabolites

- eliminated by kidneys

- can have more potent analgesic effects or more toxicity

30

some opioids can be metabolized into ______ drugs through ______ mediated reactions

which ones

- more potent
- CYP2D6

- codeine, hydrocodone, and oxycodone