*Opioid Agonist-Antagonists & Antagonists (Exam II) Flashcards
What is the primary indication for opioid agonist-antagonists?
Used if unable to tolerate full agonist
S4
Which receptors that Opioid Agonist-Antagonists binds to and their effects?
µ receptors: partial effect (agonist) or no effect (competitive antagonist)
Κ and δ receptors: partial effect (agonist)
S6
Name the four advantages of Opioid Agonist-Antagonists.
- Analgesia
- Less respiratory depression
- Low dependence potential
- Ceiling effect (prevents ODing)
S6
How potent is Pentazocine?
1/5 as potent as Morphine
S7
What receptors does pentazocine bind to?
What type of activity does it exhibit?
- κ & δ receptor
-Agonist effects with weak antagonist activity
S7
What is Pentazocine antagonized by?
Naloxone
S7
What is the elimination 1/2 time of Pentazocine?
2 - 3 hours
S7
How is Pentazocine excreted?
Glucuronide conjugates in the urine.
S7
What is the chronic pain dose of Pentazocine?
What dose and route would be equivalent to Morphine 10mg?
- 10 - 30mg IV or 50 mg PO
- 20-30mg IM= 10mg Morphine
S8
What is the epidural analgesia duration of Pentazocine?
Shorter duration < Morphine
S8
What are the side effects of Pentazocine?
- sedation
- diaphoresis
- dizziness
- dysphoria (high doses)
- increased HR, BP, PA bp, LVEDP
S8
Which opioid agonist-antagonist crosses the placental barrier causing fetal depression?
Pentazocine
S8
What type of drug is Butorphanol?
Agonist 20x and antagonist 10x to 30x > Pentazocine
S9
What receptors does Butorphanol bind to?
- κ = analgesia & anti-shivering
- μ (low)
- σ (low)
S9
Sigma (σ) receptors are associated with what side effect?
Dysphoria
S9
2 to 3 mg of butorphanol is equivalent to _____ mg of morphine.
10
s9
By what route is butorphanol rapidly and completely absorbed?
Intramuscular
S9
Where is Butorphanol excreted?
Bile > urine
S10
What are the side effects of Butorphanol?
- sedation
- nausea
- diaphoresis
- dysphoria
- depression of ventilation
- withdrawal symptoms occur
- increased BP, PA BP, & C0
S10
What is the caution with Butorphanol?
difficult to use with another opioid agonist
S10
What receptors does Nalbuphine bind to?
How potent is it?
μ receptor agonist that is equipotent to Morphine.
S12
Where is Nalbuphine metabolized?
Liver
S12
What is the elimination 1/2 time of Nalbuphine?
3 to 6 hours
S12
What are the side effects of Nalbuphine?
- sedation
- dysphoria
- withdrawal symptoms
S12
What drug is an excellent choice for cardiac catheterization patients?
Why?
- Nalbuphine
- No increase in BP, pBP, HR or atrial filling.
S12*
Which agonist-antagonist has 50 times greater μ receptor affinity than morphine?
Buprenorphine
S13
Analgesic potency of ____ mg IM of Buprenorphone = 10 mg Morphine?
0.3 mg IM
S13
What is Buprenorphine’s onset?
Duration?
- 30min onset
- 8 hour duration
S13
What is Buprenorphine’s used for?
- Post op
- cancer
- renal colic
- MI
- epidural
S13
Which two drugs have resistance to Naloxone?
- Buprenorphine and Bremazocine.
S13 and S14