Lecture 2 - Opiates - Agonists/Antagonists/Contraindications

Question 1

What are the main differences between Buprenorphine and morphine?

(What type of class drug, what effect does it have on mu, kappa receptors, analgesic effectiveness, addition level)

Answer 1

• Partial Agonist at mu receptors
• Weak antagonist at kappa receptors
• equal analgesic to morphine
• no addition

Question 2

What are the main differences between Pentazocine and morphine?

(What type of class drug, what effect does it have on mu, kappa receptors, analgesic effectiveness, addictiveness, severity of nausea/vomiting, uses, potency and administration)

Answer 2

• most frequent used mixed agonist /antagonists
• weak antagonist at mu
• good analgesia via kappa agonist activity
• low addiction
• low nausea/vomiting
• good for chronic pain management
• less potency
• subcutaneous or oral administration

Question 3

What are the main differences between Naltrexone/Naloxone and morphine?

(What type of class drug, what effect does it have on morphine, duration length, any receptor action on its own)

Answer 3

• Pure antagonists
• rapidly, reverses morphine effects
• short duration
• no action on its own

Question 4

What are the main differences between Tramadol and morphine?

What type of class drug, what receptors does it act on, does it have antidepressant actions, toxicities

Answer 4

• Pure antagonist
• weak mu receptor agonist
• inhibits NE & 5-HT uptake (antidepressant)
• low abuse potential
• Toxicities: dizziness, vertigo, CNS stimulation, constipation, pruritis, CI upset, seizures

Question 5

Which partial agonists/pure antagonists are correctly matched up? (Pick 3)

A. Buprenorphine (partial mu agonist, weak kappa antagonist)
B. Buprenorphine (weak kappa antagonist, kappa agonist)
C. Pentazocine (partial mu agonist, weak kappa antagonist)
D. Pentazocine (weak kappa antagonist, kappa agonist)
E. Tramadol (weak mu agonist, weak NE & 5-HT antagonist)

Answer 5

A. Buprenorphine (partial mu agonist, weak kappa antagonist)
D. Pentazocine (weak kappa antagonist, kappa agonist)
E. Tramadol (weak mu agonist, weak NE & 5-HT antagonist)

Question 6

Which drug is useful for chronic pain management?

A. Buprenorphine
B. Pentazocine
C. Naltrexone
D. Tramadol

Answer 6

B. Pentazocine

Question 7

Which drug rapidly reverses effects of opiates?

A. Buprenorphine
B. Pentazocine
C. Naltrexone
D. Tramadol

Answer 7

C. Naltrexone

Question 8

Which drug is has anti-depressant effects?

A. Buprenorphine
B. Pentazocine
C. Naltrexone
D. Tramadol

Answer 8

D. Tramadol

Question 9

Why are the following contraindications to all opiate agonists?

A. Head trauma
B. Chronic respiratory diseases (asthma)
C. Convulsion disorders or CNS stimulants

Answer 9

A. Head trauma - increased vascular dilation leads to increased intracranial pressure
B. Asthma - decreased response leads to hypoxia
C. Convulsion disorders or CNS stimulants (convulsant action enhanced with stimulants)

Question 10

Describe properties of morphine tolerance:

(what two factors does tolerance depend on, analgesia is a tolerance problem in what type of treatment (chronic or acute), what is the tolerance level to miosis and constipation?)

Answer 10

• Tolerance rapidly develops based on dose and schedule
• Analgesia is a tolerance problem in chronic treatment
• Little tolerence to miosis and constipation

Question 11

What are the withdrawl symptoms of morphine?

diarrheal?, increased/decreased CNS activity, Mood, what drug can be give to relieve symptoms

Answer 11

• Diarrhea
• Increased CNS activity
• Aggression
• Anxiety
• Clonidine (alpha 2 agoinst) relieves symptoms
• opiate relieves withdrawl effects

Question 12

Which of the follow is NOT a withdrawl symptom of morphine?

A. Diarrhea
B. Decreased CNS activity
C. Aggression
D. Anxiety

Answer 12

B. Decreased CNS activity

Withdrawl effects should increase CNS Activity