Opioids

Question 1

neurotransmitters in ascending pain pathways

Answer 1

glutamate and substance P

Question 2

neurotransmitters in descending pathways

Answer 2

norepinephrine, serotonin, and enkephalin

Question 3

endogenous ligands of mu receptors

Answer 3

enkephalins, beta-endorphin

Question 4

drugs that are mu receptor agonists

Answer 4

Must Catch Mike McMahon Fall

morphine, codeine, methadone, meperidine, fentanyl, buprenorphine (partial)

Question 5

drugs that are mu receptor antagonists

Answer 5

naloxone, naltrexone

Question 6

kappa receptor endogenous ligand

Answer 6

dynorphins

Question 7

kappa receptor drug ligand

Answer 7

nalbuphine

Question 8

morphine: what it is, administration, bioavialability

Answer 8

• mu agonist
• injectable or oral
• extensive first pass effect when taken orally

Question 9

codeine: what it is, comparison with morphine

Answer 9

• mu agonist

- not as efficacious as morphine

Question 10

methadone: what it is, comparison with morphine, uses

Answer 10

• mu agonist
• longer duration of action than morphine and has better oral bioavailability
• used in treatment of opioid addiction and chronic pain

Question 11

mepiridine: what it is, comparison with morphine, side effect

Answer 11

• mu agonist
• shorter duration of analgesia than morphine
• side effect: forms toxic metabolite that can accumulate

Question 12

fentanyl: what it is, comparison with morphine, administration

Answer 12

• mu agonist
• 100X as potent as morphine
• injectable, transdermal patches

Question 13

mixed-action agonist/antagonists (2)

Answer 13

nalpbuphine, buprenorphine

Question 14

nalbuphine: what it is, comparison with morphine

Answer 14

• mu antagonist and kappa agonist

- much lower abuse potential

Question 15

buprenorphine: what it is, use

Answer 15

• partial mu agonist

- oral buprenorphine combined with naloxone is used to treat opioid addiction

Question 16

mu antagonists (2)

Answer 16

naloxone, naltrexone

Question 17

naloxone: what it is, uses

Answer 17

• mu antagonist
• opioid overdoses
• combined with buprenorphine to treat opioid addiction

Question 18

naltrexone: what it is, uses

Answer 18

• mu antagonist

- used to treat alcoholism, opiate addiction

Question 19

dextromethorphan: use

Answer 19

antitussive

Question 20

significant tolerance develops to what effects of opioids?

Answer 20

emetic action, analgesic, respiratory, euphoria and endocrine effects

Question 21

no tolerance develops to what effects of opioids?

Answer 21

constipation and miosis

Question 22

drugs given to treat opioid addiction (3)

Answer 22

methadone, buprenorphine+naloxone, naltrexone

Question 23

why is naloxone added to buprenorphine to treat opioid addiction?

Answer 23

this preparation is given orally because if given parenterally, naloxone would block the effect of buprenorphine due to its much higher bioavailability

Question 24

treats opioid overdoses

Answer 24

naloxone

Question 25

treats alcoholism

Answer 25

naltrexone