Opioid Agonists and Antagonists

Question 1

Prototype

Answer 1

Morphone

Question 2

morphine indications

Answer 2

… Clinical indication: moderate to severe pain

Question 3

morphine pharmacokinetics and dynamics

Answer 3

† ½ life 2-4 h
† Oral doses 50% as effective as parenteral
† Least lipophilic
† Active mebolite M6G
† Causes histamine release

Question 4

Morphine is the lest

Answer 4

liphophilic

Question 5

morphine has low penetration of

Answer 5

BBB

Question 6

Hydromorphine (Dilaudid) is a

Answer 6

Semisynthetic, derived from morphine

Question 7

Hydromorphine (Dilaudid) indications

Answer 7

moderate to severe pain

† Good choice for patient with renal disease

Question 8

Hydromorphine (Dilaudid) pharmacokinetics

Answer 8

† ½ life 1-3 hours
† Oral doses <50% as effective as IV
† No active metabolites
… Similar analgesic and SE profile to morphine

Question 9

dilaudided is usefull to prevent

Answer 9

shivering

Question 10

Meperidine (Demerol) - Indications

Answer 10

† Moderate to severe pain, anesthesia adjunct, OB
analgesia, pre-op sedation
† Avoid in renal failure, seizure history, elderly
† Not appropriate for chronic pain management

Question 11

Meperidine (Demerol) pharmacokinetics

Answer 11

† ½ life 2.5-4h

† Active metabolite (1/2 life 15-30h)

Question 12

Meperidine (Demerol) SE

Answer 12

… S.E.: may precipitate tremors, myoclonus, seizures

Question 13

Fentanyl - Indications

Answer 13

† Moderate to severe chronic or break through pain
† 80x more potent than morphine
† The fentanyl patch should only be used by patients who
are opioid-tolerant and have chronic pain that is not well
controlled with other pain medicines.

Question 14

Fentanyl administration

Answer 14

Administration: oral, IV, neuraxial, lozenge, patch

Question 15

Fentanyl overdose signs

Answer 15

Overdose signs: dyspnea or slow or shallow breathing; slow
heartbeat; severe sleepiness; cold, clammy skin; trouble
walking or talking; or feeling faint, dizzy, or confused

Question 16

Methadone - Indications

Answer 16

† Heroin addiction, severe pain, suppression of opioid

withdrawal symptoms, neuropathic pain?

Question 17

Methadone phamacokinetics and Dynamics

Answer 17

† Long half life: 72 hours
† Dosing decreased after 72 hours to prevent extreme
side effects
† Difficult to determine equlanalgesic conversion

Question 18

Codeine - Indications

Answer 18

† Mild to moderate pain, analgesia, antidiarrheal,

antitussive

Question 19

codeine - phamacokinetics and dynamics

Answer 19

† Administered orally or IV
† Often combined with acetaminophen
† Ethnic differences: Hispanic and Mediterranean ring
countries not able to metabolize to morphine

Question 20

codeine SE

Answer 20

constipation, N&V

Question 21

Hydrocodone - Indications

Answer 21

† Moderate to severe pain, antitusssive

† May be useful short term in acute pain

Question 22

Hydrocodone - P&D

Answer 22

† Half life: 3-4 h
† Duration: 4-8 h
† Often combined with acetaminophen or ibuprofen
(Vicodin or vicoprofen)

Question 23

Oxycodone (Oxycontin, Percocet) Clinical Indications

Answer 23

† Moderate to severe pain

Question 24

Oxycodone Pharmacokinetics and Dynamics

Answer 24

† Oral route only
† Onset 40-60 minutes
† Half life: 2-3h
† Duration 3-6h
† Often combined with acetaminophen, ibuprofen

Question 25

Opioids to Avoid

Answer 25

… Meperidine (Demerol)
† Active metabolite
† Metabolite ½ life 72 h
… Prop yp ox hene
† Active metabolite nonpropoxyphene
† Half life 15 h

Question 26

Opioid Angonist-Antagonists Clinical Indication

Answer 26

moderate to severe pain

Question 27

Opioid Angonist-Antagonists - MOA

Answer 27

MOA: activate 1 type of receptor while blocking

another

Question 28

Opioid Angonist-Antagonists agents

Answer 28

† Buprenorphine
† Butorphenol
† Nalbuphine*
† Pentazocine*

Question 29

Opioid Angonist-Antagonists - ADR

Answer 29

Adverse reactions less common than with true agonists

Question 30

Suboxone

Answer 30

… buprenorphine and naloxone

Question 31

Suboxone - Indications

Answer 31

Clinical indications

† Used to treat opiate addiction

Question 32

Suboxone - SE

Answer 32

Similar side effects and precautions to opiates

Question 33

Suboxone cannont

Answer 33

Cannot stop abruptly, will trigger withdrawal