Specific opioid agents Flashcards Preview

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Flashcards in Specific opioid agents Deck (34):
1

Agonists with high oral bioavailability

Levorphanol
Codeine
Methadone

2

Agonists with low/no oral bioavailability

Fentanyl
Morphine

3

Morphine

Mu agonist (kappa and delta at higher)

4

Hydromorphone

Mu agonist (kappa and delta at higher)

5

Oxymorphone

Mu agonist (kappa and delta at higher)

6

Heroin

Full mu agonist

7

Codeine

Mu agonist

8

Oxycodone

Mu agonist

9

Hydrocodone

Mu agonist

10

Meperdine

Mu agonist
DOESNT CROSS PLACENTA!

11

Fentanyl

Mu agonist
VERY POTENT
Fast onset, SHORT duration

12

Sufentanil

Mu agonist
VERY potent
FAST onset, SHORT duration

13

Remifentanyl

Mu agonist
VERY potent
FAST onset, SHORT duration

14

Levorphanol

Mu agonist (synthetic)
Also antagonizes NMDA receptors

15

Methadone

WEAK mu agonist (used for addiction to reduce cravings and withdrawal symptoms)

16

Naloxone

Mu, Kappa, and Delta ANTAGONIST

SHORT acting

17

Naltrexone

Mu, Kappa, and Delta ANTAGONIST

LONG acting

18

Nalmefene

SELECTIVE mu antagonist

19

Pentazocine

Partial mu agonist, K agonist

Low doses good
High doses bad, start getting dysphoria/psychomimetic activity from k agonism

20

Which antagonists are injectable only?

All of them!

21

Which antagonists are available orally?

None of them!

22

Nalbuphine

Full K agonist, mu antagonist

More effective in women

23

Butorphanol

Partial mu agonist, full K agonist

24

Buprenorphine

Partial mu agonist, full K antagonist

In suboxone!

25

Tramadol

Weak mu agonist + SERT/NET inhibition

26

Tapentadol

Weak mu agonist + NET inhibition

27

Spiradoline

Full K antagonist

BAD

28

CR845

Didn't say what it does?
Doesn't cross BBB!
Outstanding analgesia!

29

Dextramorphan

D-isomer of codeine
No analgesia; does not bind opioid receptor
Used for cough

30

Diphenoxylate

Weak mu agonist
Used as antidiarrheal
Schedule V - high doses can cause CNS effects (euphoria, abuse liability)

31

Loperamide

Weak mu agonist, crosses BBB but is pumped out by P-GP transporter

32

Which mixed action drugs are available orally?

Pentazokine
CR845
Buprenorphine

33

Which mixed action drugs are not available orally?

Nalbuphine
Spiradoline

34

Which mixed action drug is a nasal spray?

Butorphanol