Opioids (Iszard)

Question 1

What are the opioid agonists (9)?

Answer 1

Morphine
Hydromorphine
Methadone
Meperidine
Fentanyl
Codeine
Oxydocone
Hydrocodone
Propoxyphene

Question 2

What are the mixed agonist/antagonists (partial opioid agonists) (4)?

Answer 2

Pentazocine
Nalbuphine
Buprenorphine
Butorphanol

Question 3

What are the opioid antagonists (2)?

Answer 3

Naloxone

Naltrexone

Question 4

What is the MOA/onset of action of opioid drugs?

Answer 4

binds to opioid receptors in CNS, causing inhibition of ascending pain pathways, altering perception of and response to pain; produces generalized CNS depression

onset of action:
oral- 30 mins
IV - 5-10 mins

Question 5

What are some warnings/precautions you might want to tell your patients about the use of opioid drugs?

Answer 5

CNS depression
Constipation (espec if have unstable angina and post-MI)
Hypotension (espec in pts w/ hypovolemia, CV dz, etc bc can exaggerate hypotension)

Black Box warning: serious, life-threatening or fatal respiratory depression may occur; monitor closely especially during initiation + dose escalation

Question 6

Which opioid drug is the most potent? least potent?

Answer 6

most: fentanyl
least: hydrocodone

Question 7

What are the indications for opioid therapy?

Answer 7

pain management, acute and chronic pain

use in relieving pain in: MI, sickle cell crisis, post op procedures, trauma, cancer, kidney stones, back pain

other indications: adjunct to general anesthesia, epidural anesthesia, palliative care, antitussive, antidiarrheal (loperamide)

Question 8

What receptors to opioids act at?

Answer 8

mu, delta, kappa

Question 9

What is the endogenous opioid peptide affinity of mu receptors?

Answer 9

endorphins>enkephalins>dynorphins

Question 10

What is the endogenous opioid peptide affinity of delta receptors?

Answer 10

enkephalins>endorphins + dynorphins

Question 11

What is the endogenous opioid peptide affinity of kappa receptors?

Answer 11

dynorphins»endorphins + enkephalins

Question 12

Which opioid is a full agonist at Mu receptors?

Answer 12

methadone

Question 13

Which opioid is a partial agonist at mu, kappa, and delta receptors?

Answer 13

buprenorphine

Question 14

What opioid is an antagonist at mu receptors and partial @kappa?

Answer 14

naltrexone

Question 15

What can morphine overdose lead to?

Answer 15

respiratory depression

Question 16

What effects would develop from high tolerance of opioids?

Answer 16

analgesia, euphoria/dysphoria, mental clouding, sedation, respiratory depression, antidiuresis, N/V, cough suppression

Question 17

What effects would develop from moderate tolerance of opioids?

Answer 17

bradycardia

Question 18

What effects would develop from low tolerance of opioids?

Answer 18

miosis, constipation, convulsions

Question 19

What are some adverse effects of chronic use of opioids?

Answer 19

hypogonadism, immunosuppression, increased feeding, increased GH secretion, withdrawal effects, tolerance/dependence, abuse/addiction, hyperalgesia, impairment while driving

Question 20

What is the drug- drug intx bw opioids and sedative-hypnotics?

Answer 20

increased CNS depression, particularly resp depression

Question 21

What is the drug- drug intx bw opioids and antipsychotic agents?

Answer 21

increased sedation; variable effects on resp depression; accentuation of CV effects

Question 22

What is the drug- drug intx bw opioids and MAOis?

Answer 22

relative CI to all opioid analgesics bc of high incidence of HYPERPYREXIC coma; HTN also reported

Question 23

What is the indication for Morphine sulfate?

Answer 23

management of pain not responsive to non-narcotic analgesics

Question 24

What are the CIs to Morphine sulfate?

Answer 24

hypersensitivity or allergy to morphine

bronchial asthma or upper airway obstrxn

resp depression in absence of resuscitative equipment

Question 25

What are some warnings and precautions in morphine sulfate usage?

Answer 25

dosing errors, respiratory depression, CNX toxicity and CNS depressants

Question 26

What are some adverse rxns to morphine sulfate?

Answer 26

sedation, lightheadedness, dizziness, n/v, constipation

Question 27

What is the indication for buprenorphine?

Answer 27

treatment of opioid dependence and preferred for induction

Question 28

What are some adverse effects of buprenorphine?

Answer 28

HA, N/V, hyperhidrosis, constipation, signs and syxs of withdrawal, insomnia, and pain

Question 29

What drug interactions should you be aware of when prescribing buprenorphine?

Answer 29

CYP3A4 inhibitors or inducers (potential over or under dosing)

Question 30

What is the MOA of naloxone?

Answer 30

pure opioid antagonist that competes and displaces opioids at receptor sites

Question 31

What is a labeled indication of naloxone?

Answer 31

complete or partial reversal of opioid depression induced by natural and synthetic opioids

also indicated for diagnosis of suspected or known acute opioid OD

Question 32

What is precaution to have with naloxone?

Answer 32

acute opioid withdrawal (release of catecholamines, may precipitate withdrawal symptoms in those that take opioid regularly)

Question 33

What is the MOA of naltrexone?

Answer 33

pure opioid antagonist; competetive antag; showing highest affinity for mu receptors

Question 34

What are indications of naltrexone?

Answer 34

alcohol use disorder treatment

blockade of effects of exogenously adminsitered opioids

Question 35

What are some warnings regarding naltrexone usage?

Answer 35

Accidental opioid overdose - ppl using this drug may respond to lower opioid doses than previously used; can result in life-threatening opioid intoxication

acute opioid withdrawal- symptoms of acute withdrawal in opioid-depdt patients (neonates - shrill cry, failure to feed; adults- pain, HTN, sweating, agitation/irritable)

Question 36

What is the importance of loperamide?

Answer 36

it is a diarrhea drug that can also be used in overdose (but extremely safe at recommended doses; can also decrease amt of drainage in pts with ostomies)

in OD give naloxone