Pharm: Opioids

Question 1

Which opioids are U+K agonists?

(hint: it’s most of them)

Answer 1

morphine

fentanyl

alfentanil/sufentanil

remifentanil

meperidine

codeine

hydrocodone

oxycodone

methadone

hydromorphine

Question 2

Which opioids are U antagonists and K agonists?

Answer 2

pentazocine

butorphanol

Question 3

Which opioids are U ptAg and K antagonists?

Answer 3

buprenorphine

Question 4

Which drugs are opioid antagonists?

Answer 4

Naloxone

Naltrexone

Question 5

Which opioids are “non-absorbed”?

Answer 5

Loperamine

Methylnaltrexone

Question 6

What is the most serious adverse effect of opioids?

Answer 6

respiratory depression

Question 7

Why are oral doses of morphine higher than parental doses?

Answer 7

due to significant first-pass metabolism

Question 8

Why are smaller doses of opioids necessary in infants?

Answer 8

due to poorly developed BBB

Question 9

With prolonged use, tolerance develops to which effects of opioids?

Tolerance does not develop to which symptoms?

Answer 9

tolerance develops to analgesia, euphoria, sedation and respiratory depression

Tolerance does not develop to constipation and miosis

Question 10

Is opioid withdrawal deadly?

Answer 10

No, but abstinence syndrome is unpleasant and can be avoiding by gradually withdrawing the medication

Question 11

Opioids should be used with caution or avoided in whom?

Answer 11

pregnant patients

avoided with alcohol

avoided with anticholinergics

Question 12

What is the classic triad of opioid overdose?

Answer 12

coma

respiratory depression

pinpoint pupils

Question 13

Which drug is 100x more potent with the same adverse effect profile as morphine?

Answer 13

Fentanyl

*has multiple formulations-IM, IV, patch, spray, lozenge, etc.

Question 14

Which drugs can be used as induction of anesthesia, maintenance of or sole agents for anesthesia?

Of these, which is the IV opioid with the most rapid onset and briefest duration?

Answer 14

Alfentanil, Remifentanil, Sufentanil

Remifentanil

Question 15

What drug was considered first line therapy for migraines and other pain conditions but is now in decline?

Answer 15

Meperidine (Demerol)

Question 16

Why is Demerol use (Meperidine) in decline?

Answer 16

it has a short half life and needs frequent dosing

has several adverse interactions with other drugs

often abused by healthcare professionals due to anticholinergic effects (no pinpoint pupils, etc)

Question 17

Which opioid also acts as an NMDA receptor antagonist?

What are some reasons that this drug causes disproportionate numbers of deaths?

Answer 17

Methadone

can cause QT prolongation and Torsades especially when combined with other drugs that prolong QTI

Question 18

Why does heroin give a better “high” than morphine?

Answer 18

due to it’s higher lipid solubility

schedule I substance in US, but available therapeutically elsewhere

Question 19

What is the indication for hydromorphone (Dilauded)?

How can it be reversed?

Is it more lipid or water soluble?

Answer 19

indicated for moderate to severe pain with similar adverse effects to morphine

Reverse with naloxone

More water soluble, so can be diluted in smaller volume for injection

Question 20

What drug is the prototype for moderate to strong opioid agonists?

How is it metabolized?

Answer 20

Codeine

10% of each dose is metabolized to morphine by

CYP2D6–>required for analgesia

Question 21

What are two special features of Codeine?

Answer 21

It can be formulated with nonopioid analgesics or used alone

It is an effective cough suppressant

Question 22

What is special about oxycodone’s metabolism?

Answer 22

It is metabolized by CYP3A4 so inducers like carbamazepine or phenytoin can lower levels, and inhibitors like “azoles” can raise levels

Question 23

What is Naloxone (Narcan) and what is it used for?

Answer 23

pure opioid antagonist

can reverse most effects of opioid agonists

*if given in the absence of opioids, it has no significant effect

Question 24

What happens if Naloxone is given to a patient with a physical dependence on opioids?

Answer 24

It will precipitate immediate withdrawal reactions

Question 25

What is Naltrexone and what is it used for?

Answer 25

pure opioid antagonist

prevents euphoria, not cravings

can be used in alcoholics (can reduce craving and drinking in this case) while Acamprosate can decrease ETOH consumption to a greater degree with lesser effect on cravings

Question 26

What is methylnaltrexone?

Answer 26

u-opioid antagonist that cannot readily cross the BBB

indicated for opioid-induced constipation in patients with end-stage disease

Question 27

What is loperamide?

Answer 27

u-opioid agonist that cannot readily cross the BBB

indicated for acute and chronic diarrhea

in large doses, can cause Torsades (QT prolongation)

Question 28

What are three keys to remember about the clinical use of opioids?

Answer 28

Pain is subjective and cannot be measured

No such thing as a “Standard Dose” of opioids

Best to administer with a fixed schedule and tx breakthrough pain as necessary

Question 29

For mild-severe pain, after topical agents, and OTC analgesics have proved ineffective and TCAs are not alleviating the pain, what is the next best option?

Answer 29

Opioids +/- Baclofen if spasmodic component

Question 30

What is the safest option for patients with renal and hepatic insufficiency?

Answer 30

Fentanyl

(methadone is safe in renal insuf., but can only be used by docs with prior experience)

Question 31

Why is fentanyl safe for patients with hepatic insuffiecient?

Answer 31

metabolized by CYP3A4 but pharmokinecally has no significant effect from cirrhosis due to normally high rate of elimination in a single pass through the liver

Question 32

What technique can be employed to have a favorable balance between pain relief and adverse effects when treating with opioids?

Answer 32

Can place pt on opioid rotation