Mixed opioid agonist-antagonists and partial agonists

Question 1

Mixed opioid agonist-antagonists - 4 drugs

Answer 1

Buprenorphine
Butorphanol
Nalbuphine
Pentazocine

Question 2

Mixed opioid agonist-antagonists - MOA

Answer 2

Partial agonist or antagonist activity at μ receptors and κ receptors.

Question 3

Mixed opioid agonist-antagonists - difference from full agonists

Answer 3

Less respiratory depression.
Lower liability for dependence and abuse.
Less constipation.
Cause anxiety, nightmares, psychomotor effects (hallucinations).
Precipitate withdrawal in pt dependent on a full agonist.

Question 4

Mixed opioid agonist-antagonists - Indications

Answer 4

Pre- and postoperative analgesia, obstetric (parenteral).

Moderate to severe pain (oral).

Question 5

Buprenorphine - MOA

Answer 5

Partial agonist at μ-receptors

Question 6

Buprenorphine - indicaitons

Answer 6

Opioid dependence

Question 7

Butorphanol and nalbuphine - MOA

Answer 7

κ opioid receptor agonist. Partial agonist/antagonist at μ-receptors.

Question 8

Pantazocine - MOA

Answer 8

κ opioid receptor agonist. σ receptor activity (mediates psychotomimetic effect of PCP and ketamine)

Question 9

Pantazocine - adverse effects

Answer 9

Severe cardiovascular effects in pts with preexicting cardiovascular disease.