Opioid Analgesics

Question 1

How is morphine metabolized?

Answer 1

By conjugation with glucuronic acid in the liver

*slowed metabolism in impaired renal and liver patients

Question 2

Morphine therapeutic effects

Answer 2

Analgesia
Dull pain > sharp pain 
Act at peripheral, spinal, and brain level 
Sedation
Euphoria

Question 3

Major side effect of morphine

Answer 3

Respiratory depressoin

Question 4

Mechanism of respiratory depression

Answer 4

decreased sensitivity of the chemoreceptors to CO2

Question 5

What is the first dose effect?

Answer 5

Nausea and vomiting after the first time you take opioid (due to trigger of the CTZ) - develop tolerance

Question 6

Which effects do not develop tolerance to morphine?

Answer 6

Constipation

Miosis

Question 7

Which opioid is associated with biliary pain?

Answer 7

Morphine

Question 8

Which opioid can cause pruritus and itching due to histamine release?

Answer 8

Morphine

Question 9

Which opioid prolongs labor and is consequently contraindicated in pregnancy?

Answer 9

Morphine

Question 10

What are the contraindications of morphine

Answer 10

Decreased respiratory reserve
Head injuries (obscure signs/increase pressure)
CNS tumors
Pregnancy

Question 11

What happens when morphine is combined with ETOH?

Answer 11

dissolves the coating of morphine of sustained release causing sudden dangerous release

Question 12

What is the difference between codeine and morphine potency

Answer 12

Codeine 10x LESS potent

Question 13

Codeine MOA

Answer 13

Prodrug converted to morphine by CYP2D6

Question 14

What is a concern with codeine metabolism with some patients?

Answer 14

Ultra fast metabolizers will get morphine effects

worry about with children

Question 15

Which analgesic is used for cough suppression?

Answer 15

Codeine

Question 16

What are some key differences between codeine and morphine?

Answer 16

Less likely to cause addiction

More likely to cause constipation

Question 17

Which analgesic has been combined with soda “sizzurp”

Answer 17

Codeine

Question 18

Which is the most commonly prescribed analgesic that it has now become a schedule three drug?

Answer 18

Hydrocodone

Question 19

True or false oxycodone is more potent than codeine

Answer 19

True

Question 20

Which analgesic is 100x more potent than Morphine?

Answer 20

Fentanyl

Question 21

Which drug is used for neuroleptanalgesia for cardiac patients?

Answer 21

Fentanyl

Question 22

Compared to morphine what are some key effects that only fentanyl has?

Answer 22

Does not induce histamine release
Cardiovascular system is less affected (cardiac stability during surgery)
High addiction potential

Question 23

Which opioid is metabolized very slowly?

Answer 23

Methadone

Question 24

Duration of action of methadone

Answer 24

1/2 life: 15 hr acute, 22 hr chronically

Question 25

What are some serious side effects of methadone?

Answer 25

Cardiovascular effects QT prolongation Torsades de pointes

Question 26

Which opioid is used to maintain addicts but not cure them?

Answer 26

Methadone

Question 27

How does maintenance therapy work?

Answer 27

Addict is given low dose methadone for slow onset and prevent immediate rush, long duration last throughout day, prevents withdrawal symptoms satisfies dependence must go to methadone clinic

Question 28

Which drug is a rapid acting, more lipid soluble agent that has a high abuse potential and schedule 1 drug?

Answer 28

Heroin

Question 29

Buprenorphine MOA

Answer 29

Partial agonist at Mu | Antagonist at Kappa (prevent dysphoria)

Question 30

Which paritial agonist analagesic has a cieling effect for analgesia and respiratory depression?

Answer 30

Buprenorphine

Question 31

Which analgesic lacks dysphoric effects?

Answer 31

Buprenorphine

Question 32

Which analgesic can also treat opioid dependence outside of a maintenance clinic but will also precipitate withdrawal?

Answer 32

Buprenorphine

Question 33

Which drug was designed to be a Kappa agonist and minimal mu agonist but failed

Answer 33

Pentazocine

Question 34

Pentazocine MOA

Answer 34

Partial agonist mu and kappa | Kappa >>> Mu

Question 35

Difference between Pentazocine and Buprenorphine?

Answer 35

Pentazocine produces dysphoria at high doses, Buprenorphine does not

Question 36

which analgesic is used safely as an anti-diarrheal OTC?

Answer 36

Loperamide

Question 37

Which drug is an anti-diarrheal agent but it still requires an Rx?

Answer 37

Diphenoxylate

Question 38

Which drug prefers the D-isomer and thus is used to treat cough and not pain?

Answer 38

Dextromethorphan

Question 39

Which drug is used to antagonize opioid effects in overdose?

Answer 39

Naloxone (Narcan)

Question 40

Naloxone MOA

Answer 40

Competitive antagonist of opioid receptors | Full agonist >> partial agonist

Question 41

Which antagonist has been approved for nasal spray use?

Answer 41

Naloxone (good for patients because they are unconscious and cannot swallow)

Question 42

Which antagonist is used to treat opioid dependence by preventing the effects of opioids?

Answer 42

Naltrexone

Question 43

Which drug is now being added to opioids to prevent abuse if crushed and injected?

Answer 43

Naloxone (Narcan)

Question 44

Which opioid antagonist is used to treat opioid induced constipation?

Answer 44

Methylnaltrexone

Question 45

Methylnaltrexone MOA

Answer 45

Does not cross BBB (cannot prevent opioid analgesia) limited to the gut and prevent constipation