Mixed opioid agonist-antagonists and partial agonists Flashcards Preview

23 Opioids > Mixed opioid agonist-antagonists and partial agonists > Flashcards

Flashcards in Mixed opioid agonist-antagonists and partial agonists Deck (9)
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1

Mixed opioid agonist-antagonists - 4 drugs

Buprenorphine
Butorphanol
Nalbuphine
Pentazocine

2

Mixed opioid agonist-antagonists - MOA

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

3

Mixed opioid agonist-antagonists - difference from full agonists

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.

4

Mixed opioid agonist-antagonists - Indications

Pre- and postoperative analgesia, obstetric (parenteral).
Moderate to severe pain (oral).

5

Buprenorphine - MOA

Partial agonist at μ-receptors

6

Buprenorphine - indicaitons

Opioid dependence

7

Butorphanol and nalbuphine - MOA

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

8

Pantazocine - MOA

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

9

Pantazocine - adverse effects

Severe cardiovascular effects in pts with preexicting cardiovascular disease.