Narcotics

Question 1

What type of receptor is the opioid receptors?

Answer 1

GPCR

Question 2

Effect of opioid receptor

Answer 2

decreased adenyl cyclase, Ca2+ channel activity
increase K+ channel activity
(hyperpolarizes)

Question 3

What is the main opioid receptor targeted by analgesics?

Answer 3

u (Mu)

Question 4

Describe morphine’s structure and sites that account for variation

Answer 4

5 ring structure

modifications at positions 3,6, and 17

Question 5

What do opioid receptor agonists do?

Answer 5

Inhibit the release of substance P and ascending transmission of pain from dorsal horn neurons.

Question 6

Possible mechanism of tolerance?

Answer 6

internalization/ phosphorylation of receptors

Question 7

What two side effects do patient’s on opioids exhibit little tolerance to?

Answer 7

Miosis and constipation

Question 8

What are the SE of opioids?

Answer 8

Miosis, constipation, respiratory depression

N/V, uticaria, bad dreams, sedation, delirium, Seizures, urinary retention

Question 9

Where and how are opioids metaboilized?

Answer 9

Liver, conjugation w/ glucoronic acid

Question 10

Why is the Cmax for oral opioids lower than IV?

Answer 10

first pass metabolism

Question 11

How do you address the bolus effect of IV/IM dosing?

Answer 11

Consider CI or extended release oral formulations

Question 12

Why are opioids often used in with adjuvants?

Answer 12

To reduce the necessary dose, decreasing unwanted SE.

Question 13

When are opioids used?

Answer 13

To treat moderate or severe pain.

Question 14

What metabolite of morphine is the most active/ highest potency?

Answer 14

M-6- glucuronide

Question 15

What is morphine’s MOA?

Answer 15

Mu- opioid receptor agonist

Question 16

What are the effects of morphine?

Answer 16

severe analgesia, mood alteration, antitussive, sedation

Question 17

What pathway is responsible for conversion of 10% of codeine into morphine?

Answer 17

CYP2D6

Question 18

What are the effects of codeine?

Answer 18

moderate analgesia, antitussive

Question 19

What is codeine’s MOA?

Answer 19

Mu- opioid receptor agonist

Question 20

What concern is there for codeine use in Caucasians?

Answer 20

10% can’t convert to morphine, but still experience SE

Question 21

How does tramadol work?

Answer 21

weak Mu receptor agonist, inhibition of NE/5HT uptake

Question 22

What are the effects of tramadol?

Answer 22

moderate analgesia

Question 23

What are the effects of fentanyl?

Answer 23

severe analgesia

Question 24

How is fentanyl delivered?

Answer 24

IV or transdermal

Question 25

How long should you wait before increasing the does of fentanyl?

Answer 25

1 week

Question 26

What is MOA of fentanyl?

Answer 26

Mu-opioid receptor agonist, highly lipid soluble

Question 27

What is the MOA of methadone, oxycodone, and meperidine?

Answer 27

Mu-opioid receptor agonist

Question 28

What is methadone used to treat?

Answer 28

chronic severe pain | treatment of heroine and opioid addicts

Question 29

When initially treating with methadone, what precautions should be taken?

Answer 29

Do not raise dose more than 1/ wk | Overdose common in initial treatment

Question 30

What is oxycodone used to treat?

Answer 30

moderate to severe analgesia

Question 31

What two opioids are no longer used?

Answer 31

Meperidine and Propoxyphene

Question 32

What are Loperamide (Imodium) and Diphenoxylate (Lomotil) used to treat?

Answer 32

DIarrhea

Question 33

Loperamide (Imodium) and Diphenoxylate (Lomotil) MOA?

Answer 33

slows peristalsis by binding opioid receptors in intestine, possibly decreases GI secretions

Question 34

What is Naloxone (Narcan) used to treat?

Answer 34

opioid toxicity

Question 35

Naloxone (Narcan) MOA?

Answer 35

competitive mu, delta, and kappa opioid receptor antagonist

Question 36

SE of Naloxone?

Answer 36

can precipitate withdrawal | N/V/D, piloerection, yawning, irritabilty

Question 37

What is Naltrexone (Revia) used to treat?

Answer 37

Alcoholism

Question 38

SE of Naltrexone?

Answer 38

prolonged withdrawal- N/V, piloerection, yawning

Question 39

MOA of Naltrexone (Revia)?

Answer 39

Mu-opioid receptor antagonist

Question 40

What must you be cautious of when prescribing a opioid in combination with acetaminophen?

Answer 40

At home, OTC use. Risk of overdose

Question 41

How long between doses for oral immediate release preparations vs extended release preparations?

Answer 41

immediate- every 4 hours | extended- 8-24 hrs

Question 42

What should you not use to treat breakthrough dosing?

Answer 42

extended release opioids

Question 43

What should you do if pain is poorly responsive to opioids?

Answer 43

Try alternative route or rotate opioid | Try coanalgesic

Question 44

What must be kept in mind when changing drugs or route?

Answer 44

Equianalgesic dosing | When changing drug or route, decrease equianalgesic dose by 25-50% at first to avoid bad SE

Question 45

What should be done to avoid constipation w/ opioid use?

Answer 45

Prescribe stool softener w/ stimulant laxative at the same time you start opioid.

Question 46

If respiratory depression begins in a patient taking opioids, what should you do?

Answer 46

Give IV Naloxone (Narcan)

Question 47

How do you decrease risk of delirium in patient being treated with opioids?

Answer 47

Confirm normal liver (metabolism) / kidney (excretion) function