Specific opioid agents

Question 1

Agonists with high oral bioavailability

Answer 1

Levorphanol
Codeine
Methadone

Question 2

Agonists with low/no oral bioavailability

Answer 2

Fentanyl

Morphine

Question 3

Morphine

Answer 3

Mu agonist (kappa and delta at higher)

Question 4

Hydromorphone

Answer 4

Mu agonist (kappa and delta at higher)

Question 5

Oxymorphone

Answer 5

Mu agonist (kappa and delta at higher)

Question 6

Heroin

Answer 6

Full mu agonist

Question 7

Codeine

Answer 7

Mu agonist

Question 8

Oxycodone

Answer 8

Mu agonist

Question 9

Hydrocodone

Answer 9

Mu agonist

Question 10

Meperdine

Answer 10

Mu agonist

DOESNT CROSS PLACENTA!

Question 11

Fentanyl

Answer 11

Mu agonist
VERY POTENT
Fast onset, SHORT duration

Question 12

Sufentanil

Answer 12

Mu agonist
VERY potent
FAST onset, SHORT duration

Question 13

Remifentanyl

Answer 13

Mu agonist
VERY potent
FAST onset, SHORT duration

Question 14

Levorphanol

Answer 14

Mu agonist (synthetic)
Also antagonizes NMDA receptors

Question 15

Methadone

Answer 15

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

Question 16

Naloxone

Answer 16

Mu, Kappa, and Delta ANTAGONIST

SHORT acting

Question 17

Naltrexone

Answer 17

Mu, Kappa, and Delta ANTAGONIST

LONG acting

Question 18

Nalmefene

Answer 18

SELECTIVE mu antagonist

Question 19

Pentazocine

Answer 19

Partial mu agonist, K agonist

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

Question 20

Which antagonists are injectable only?

Answer 20

All of them!

Question 21

Which antagonists are available orally?

Answer 21

None of them!

Question 22

Nalbuphine

Answer 22

Full K agonist, mu antagonist

More effective in women

Question 23

Butorphanol

Answer 23

Partial mu agonist, full K agonist

Question 24

Buprenorphine

Answer 24

Partial mu agonist, full K antagonist

In suboxone!

Question 25

Tramadol

Answer 25

Weak mu agonist + SERT/NET inhibition

Question 26

Tapentadol

Answer 26

Weak mu agonist + NET inhibition

Question 27

Spiradoline

Answer 27

Full K antagonist BAD

Question 28

CR845

Answer 28

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

Question 29

Dextramorphan

Answer 29

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

Question 30

Diphenoxylate

Answer 30

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

Question 31

Loperamide

Answer 31

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

Question 32

Which mixed action drugs are available orally?

Answer 32

Pentazokine CR845 Buprenorphine

Question 33

Which mixed action drugs are not available orally?

Answer 33

Nalbuphine | Spiradoline

Question 34

Which mixed action drug is a nasal spray?

Answer 34

Butorphanol