Opioid analgesics

Question 1

Which two drugs are classified as strong opioid agonists?

Answer 1

Morphine and Methadone

Question 2

Class of morphine

Answer 2

Strong opioid agonist

Question 3

For which receptors does morphine have an affinity. Describe the affinity.

Answer 3

High affinity for mu receptors

Question 4

What is the active metabolite of morphine?

Answer 4

morphine-6-glucuronide

Question 5

Which drug is 10% opium?

Answer 5

Morphine

Question 6

Morphine is what % opium?

Answer 6

10%

Question 7

Morphine-6-glucuronide

Answer 7

Active metabolite of morphine

Question 8

Morphine treats severe pain, commonly in cases of:

Answer 8

Trauma, cancer, MI

Question 9

Which drug is considered the prototypical opioid?

Answer 9

Morphine

Question 10

Duration of action of morphine?

Answer 10

4-6 hours

Question 11

Which drug can be turned into heroin via acetylation?

Answer 11

Morphine

Question 12

When you acetylate morphine, you make:

Answer 12

heroin

Question 13

Why is heroin a much more powerful drug than morphine?

Answer 13

Acetylation makes it much more fast-acting and lipid-soluble.

Question 14

Which strong opioid agonist is orally affective?

Answer 14

Methadone

Question 15

Use of methadone?

Answer 15

Used for detox/controlled withdrawal from heroin and morphine

Question 16

Duration of action of methadone?

Answer 16

15-20 hours

Question 17

Which strong opioid agonist is mainly used for detox?

Answer 17

Methadone

Question 18

Which drug is considered a moderate opioid agonist?

Answer 18

Codeine

Question 19

Class of codeine?

Answer 19

Moderate opioid agonist

Question 20

Which drug is 0.5% opium?

Answer 20

Codeine

Question 21

Codeine is what % opium?

Answer 21

0.5%

Question 22

How is codeine used for analgesia?

Answer 22

It is metabolized into morphine.

Question 23

Codeine is less abused than morphine because it is:

Answer 23

less potent.

Question 24

How do we supplement the lower potency of codeine in providing analgesia to patients?

Answer 24

Combine it with non-opioids–multi-modal pain relief

Question 25

Which two drugs are mixed opioid agonist-antagonists?

Answer 25

Pentazocine and Buprenorphine

Question 26

Class of pentazocine?

Answer 26

Mixed opioid agonist-antagonist

Question 27

Mechanism of action of pentazocine?

Answer 27

K-receptor agonist with weak mu receptor antagonist

Question 28

Pentazocine is a K-receptor _____________ and a weak mu receptor ____________

Answer 28

agonist; antagonist

Question 29

Which mixed opioid agonist-antagonist is a K-receptor agonist?

Answer 29

Pentazocine

Question 30

Which mixed opioid agonist-antagonist is a weak mu-receptor antagonist?

Answer 30

Pentazocine

Question 31

Method of administration of Pentazocine?

Answer 31

Orally

Question 32

What level of pain does Pentazocine treat?

Answer 32

Moderate to severe pain

Question 33

Which mixed opioid agonist-antagonist precipitates withdrawal in morphine users?

Answer 33

Pentazocine

Question 34

Class of Buprenorphine?

Answer 34

Mixed opioid agonist-antagonist

Question 35

Mechanism of action of Buprenorphine?

Answer 35

Partial agonist at mu receptors and antagonist at K-receptors

Question 36

Buprenorphine is a partial ___________ at mu receptors and ___________ at K-receptors

Answer 36

Agonist; antagonist

Question 37

Which mixed opioid agonist-antagonist is a partial agonist at mu receptors?

Answer 37

Buprenorphine

Question 38

Which mixed opioid agonist-antagonist is an antagonist at K receptors?

Answer 38

Buprenorphine

Question 39

Which mixed opioid agonist-antagonist is used to manage cocaine addiction and heroin abuse?

Answer 39

Buprenorphine

Question 40

Use of buprenorphine?

Answer 40

Used to manage cocaine addiction and heroin abuse

Question 41

Which two drugs are opioid antagonists?

Answer 41

Naloxone and naltrexone

Question 42

Class of naloxone?

Answer 42

Opioid antagonist

Question 43

What type of antagonist is naloxone?

Answer 43

Competitive antagonist at opioid receptors

Question 44

Half life of naloxone?

Answer 44

1-2 hours

Question 45

Which opioid antagonist is used as an IV injection to treat opioid overdose?

Answer 45

Naloxone

Question 46

Class of naltrexone?

Answer 46

Opioid antagonist

Question 47

What type of antagonist is naltrexone?

Answer 47

Competitive antagonist at opioid receptors

Question 48

Half-life of naltrexone?

Answer 48

10 hours

Question 49

Which opioid antagonist is considered a maintenance drug for addicts and alcoholics?

Answer 49

Naltrexone

Question 50

How does naltrexone maintain abstinence for recovering alcoholics?

Answer 50

Decreases rewarding effects of alcohol