Opioids (Wolff)

Question 1

What are the three major classes of opioid receptors?

Answer 1

mu, kappa and delta

Question 2

Morphine and other pure opioid agonists relieve pain by mimicking the action of?

Primarily at what receptors?

Answer 2

1) Endogenous opioid peptides (endorphins, enkephalins, etc.)
2) Mu receptors but partly at kappa receptors

Question 3

What is the most serious adverse effect of opioids?

Answer 3

Respiratory depression

Question 4

What precautions are there for opioid use?

Answer 4

1) Pregnancy

2) Head injury

Question 5

Opioid overdose produces what classic triad of signs?

Answer 5

1) Coma
2) Respiratory depression
3) Pinpoint pupils

Question 6

Which pure opioid is 100X more potent than morphine, has the same adverse effects, and is notable for having multiple formulations?

Answer 6

fentanyl

Question 7

alfentanil, remifentanil, and sufentanil are pure opioids used for?

Which is an IV opioid with rapid onset and brief duration due to rapid metabolism by blood esterase?

Answer 7

1) Induction and maintenance of anesthesia

2) remifentanil

Question 8

Meperidine (Demerol) which is often abused by healthcare workers because of its anticholinergic effects lacks what classic sign of other opioids?

Answer 8

Lacks pinpoint pupils

Question 9

Methadone which shares major properties of morphine, is also an antagonist of what other receptor?

Answer 9

NMDA receptor

Question 10

Which pure opioid is indicated for moderate to severe pain, adverse effects are similar to morphine and reversed by naloxone, and is more water soluble so can be diluted in a smaller volume for injection?

Answer 10

hydromorphone (Dilaudid)

Question 11

What is the prototype for moderate to strong opioid agonists?

Answer 11

Codeine

Question 12

~10% of each dose of codeine is metabolized to morphine by what CYP?

Answer 12

CYP2D6

Question 13

Oxycodone which is a moderate to strong opioid agonist similar to codeine, is metabolized by which CYP?

Answer 13

CYP3A4

Question 14

What type of opioid is pentazocine and butorphanol?

Answer 14

Mu antagonist and Kappa agonist

Question 15

What type of opioid is buprenorphine?

Answer 15

Mu partial agonist and Kappa antagonist

Question 16

Naloxone and naltrexone are what type of drugs?

Answer 16

Pure Opioid Antagonists

Question 17

What effect does Naloxone have?

Answer 17

Reverses most effects of opioid agonists including respiratory depression

Question 18

What does naloxone precipitate in people who are psychically dependent on opioids?

Answer 18

Immediate withdrawal reaction

Question 19

What effects do naltrexone have?

Answer 19

1) Prevents euphoria from opioids but does not prevent craving
2) Reduces craving and heavy drinking associated with alcoholics

Question 20

What is methylnaltrexone?

What is it indicated for?

Answer 20

1) μ-opioid antagonist that cannot readily cross BBB

2) Opioid-induced constipation

Question 21

What is loperamide?

What is it indicated for?

Answer 21

1) μ-opioid agonist that cannot readily cross BBB

2) Acute and chronic diarrhea

Question 22

Patients that ingest loperamide in large quantities to get high or alleviate withdrawal symptoms have a great risk of?

Answer 22

Torsade’s de pointes due to QT prolongation

Question 23

How is it best to administer opioids?

Answer 23

On a fixed schedule

Question 24

In the setting of renal insufficiency which opioid is safe for use?

Which are not recommended because of toxicity of their metabolites?

Answer 24

1) Fentanyl

2) Meperidine and codeine

Question 25

In the setting of hepatic insufficiency which opioid is safe for use?

Which are not recommended because of toxicity of their metabolites?

Answer 25

1 Fentanyl

2) Meperidine, codeine, and methadone

Question 26

What is the outcome of adverse interactions between opioids and CNS depressants such as:

Barbiturates
Benzodiazepines
Alcohol
General anesthetics
Antihistamines
Phenothiazines

Answer 26

Increased respiratory depression and sedation

Question 27

What is the outcome of adverse interactions between opioids and Agonist-antagonist opioids?

Answer 27

Precipitation of withdrawal reaction

Question 28

What is the outcome of adverse interactions between opioids and Anticholinergic Drugs such as:

Atropine-like drugs
Antihistamines
Phenothiazines
Tricyclic antidepressants

Answer 28

Increased constipation and urinary retention

Question 29

What is the outcome of adverse interactions between opioids and hypotensive agents?

Answer 29

Increased hypotension

Question 30

What is the outcome of adverse interactions between opioids and Monoamine oxidase inhibitors?

Answer 30

Hyperpyrexic coma