21 Opioids III

Question 1

What are the routes of administration available for hydromorphone?

Answer 1

IV, PO

Question 2

Why does hydromorphone have a faster onset than morphine?

Answer 2

it is more lipid soluble

Question 3

Is hydromorphone or morphine more potent?

Answer 3

hydromorphone is 5x more potent

Question 4

what is vicodin?

Answer 4

hydrocodone + acetaminophen

Question 5

what is hydrocodone metabolized to? What enzyme catalyzes this conversion?

Answer 5

hydromorphone, CYP2D6

Question 6

what is percocet?

Answer 6

oxycodone + acetaminophen

Question 7

what is oxycodone metabolized to? What enzyme catalyzes this conversion?

Answer 7

oxymorphone, CYP2D6

Question 8

Why are opioids sometimes administered in combination with acetaminophen (eg vicodin, percocet)

Answer 8

Formulations of opioids with acetaminophen provide
additional pain relief while avoiding severe opioid side
effects.

Question 9

What is the name of the prodrug that is converted to morphine by CYP2D6?

Answer 9

codeine

Question 10

What prodrug is converted to monoacetyl morphine and morphine in the brain?

Answer 10

heroin

Question 11

what opioid is used for maintenance of opioid drug addiction?

Answer 11

methadone

Question 12

what is the half life of methadone?

Answer 12

Very long; 15 - 60 hours

Question 13

is meperidine slower or faster onset than morphine?

Answer 13

faster, because it is more lipid soluble

Question 14

is meperidine more or less potent than morphine?

Answer 14

1/10 as potent

Question 15

in what type of patient does nor-meperidine have a prolonged half life?

Answer 15

patients with renal failure, due to decreased elimination

Question 16

What are the signs and symptoms of serotonin syndrome?

Answer 16

1. Neuromuscular hyperactivity; tremor, clonus, myoclonus,
   hyper-reflexia and (in the advanced stage) pyramidal
   rigidity.
2. Autonomic hyperactivity; diaphoresis, fever, tachycardia
   and tachypnea.
3. Altered mental status; agitation, excitement and (in the
   advanced stage) confusion.

Question 17

which opioid can cause serotonin sydrome, particularly when combined with SSRIs and MAOIs?

Answer 17

meperidine

Question 18

Which two drugs are partial mu agonists?

Answer 18

tramadol and tapentadol

Question 19

what metabolizes tramadol?

Answer 19

CYP2D6 (produces active metabolite) and CYP3A4

Question 20

what metabolizes tapentadol?

Answer 20

CYP2C9, CYP2C19, and a little by CYP2D6

Question 21

what do pentazocrine, butorphanol, and nalbuphine have in common?

Answer 21

they all act at opioid k receptors but also mu partial agonist/antagonist

Question 22

what receptors does buprenorphine act on?

Answer 22

partial mu receptor agonist and kappa agonist

Question 23

What is buprenorphine used for?

Answer 23

treating drug abuse and addiction

Question 24

What percentage of the us population are rapid metabolizers of CYP2D6?

Answer 24

4-5%

Question 25

which opioid agonists are used as antidiarrheals?

Answer 25

diphenoxylate and loperamide

Question 26

which opioid antagonists are used to antagonize the GI side effects of opiates?

Answer 26

alvimopan and methylnaltrexone

Question 27

What is a REMS?

Answer 27

Risk Evaluation and Mitigation strategy, strategy used to manage known or potential serious risks associated with a drug product; required by the RDA to ensure that the benefits of a drug outweigh the risks