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Pharmacology 680 > opioid agonist-antagonist > Flashcards

opioid agonist-antagonist Flashcards

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1
Q

name the 5 agonists/antagonists we need to know

A
  1. Pentazocine (Talwin)
  2. Butorphanol (stadol)
  3. Nalbuphine (Nubain)
  4. Buprenorphine (Buprenex)
  5. Buprenorphine/Naloxone (Suboxone)
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2
Q

reversibly binds
receptor at same site as agonist but does NOT
activate receptor.

A

competitive antagonist

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3
Q

what are the effects from competitive antagonists from?

A

preventing agonists from binding

to and activating the receptor

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4
Q

what does the clinical response of competitive antagonists depend on?

A

the concentration of agonists in the system that the drug has to compete with to bind to receptor site

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5
Q

irreversibly binds

receptor at a separate site from agonists.

A

Non-competitive antagonists

think non-comp = drug does not care about winning receptor

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6
Q

2 important things that Non-competitive antagonists do

A

– Inhibits the full agonist response
Prevents conformational changes in receptor which
are required for receptor activation.

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7
Q

Drug has a high affinity for the receptor but not

so much intrinsic activity

A

Partial agonist

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8
Q

this type of drug binds to a receptor but causes a decrease in receptors response

A

• Partial agonist

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9
Q 
greater effects at the receptor than the defining
receptor agonist (morphine)
A

Superagonist

*fent vs morphine

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10
Q

Opioid Agonists/Antagonists have most Successful use in these type of patients

A

opioid addiction/chronic use population

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11
Q

Opioid Agonists/Antagonists have what effect on morphine and pure agonists?

A

Produce a degree of competitive antagonism

to morphine and pure agonists

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12
Q

What type of pain are opioid agonist/antagonists appropriate for?

A

acute & chronic pain

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13
Q

even tho agonist/antagonists are Synthetic or semi-synthetic analgesics, what drug are they structurally r/t?

A

morphine

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14
Q

what characteristics to ag/ant have on mu receptor (broad)

A

Partial µ agonist producing limited to no effects (less resp depression)

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15
Q

what two receptors do ag/ant effect most?

A

kappa and delta!

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16
Q

what is the cool thing about ag/ant?

A

Reverses opioid overdose while continuing to

provide analgesia

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17
Q

are Opioids that have antagonist effects on µ and к

receptors useful in pain management?

A

Yes

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18
Q

6 Benefits of Opioid Agonists/Antagonists

A
  1. great when pt cant tolerate full agonist
  2. analgesia (k) without resp depression (mu)
  3. used in pt with opioid dependency hx
  4. ceiling effects limit toxicity of drug
  5. no significant elevation of interbiliary pressure
  6. less constipation
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19
Q

because ag/ant do not cause significant elevation of interbiliary pressure, what pts are these good for?

A

Useful in patients with biliary colic

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20
Q

kappa receptors main side effect

A

Psych

dysphoria

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21
Q

will giving morphine after giving an ag/ant work well for analgesia?

A

Subsequent doses of agonist after opioid A/A may NOT provide

adequate analgesia

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22
Q

3 undesirable effects from kappa receptor

A
  • dysphoria, confusion (elderly)
  • no euphoria
  • depression
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23
Q

these ag/ant are typically not appropriate for what patient population?

A

cards because of catecholamine release so increase in BP, CO

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24
Q

in regards to ceiling effect of response with ag/ant:

A

Depression of ventilation (advantage)

– Weak ability to decrease anesthetic requirement, really not great for “balanced” anesthesia plan

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25
what receptor antagonist can lead to withdrawal
mu
26
CNS effects of kappa receptor
``` depression sedation dysphoria hallucinations delirium ```
27
what does the kappa receptor cause in the GU system that other receptors do not?
diuresis due to inhibition of vasopressin
28
Weak antagonist of µ receptors, partial к agonists that does not antagonize resp depression
Pentazocine(Talwin)
29
what 2 meds can be antagonized by narcan
- Talwin (pentazocine) | - nubain (nalbuphine)
30
indications of pentazocine
– Relief of moderate pain | – Chronic pain & increase risk of physical dependence.
31
Antagonist effects of talwin cause
withdrawal in patients | chronically receiving opioids
32
Effects of pentazocine (talwin)
Analgesia, sedation, mild resp.depression
33
CNS side effects of Pentazocine(Talwin)? | *dose dependent
Sedation, dysphoria, diaphoresis, dizziness, dissociation | “weird” feelings, hallucinations, NO mood elevation
34
can pentazocine cross the placenta?
YES! potentially causing fetal depression | P=Placenta
35
cards side effects of Pentazocine(Talwin)
– ↑HR & cardiac workload(catecholamine release) ↑SBP & | pulmonary artery pressure, ↑ myocardial O2 consumption
36
*Butorphanol(Stadol) is More potent agonist & antagonist than Talwin by what amount
Agonists 20x | Antagonists 10-30x greater
37
what ag/ant has more potent analgesia than morphine?
Butorphanol(Stadol)
38
Indications for butorphanol (stadol)
Post-op pain and migraine headaches. – Post op shivering S=S [shivering]
39
Equal doses of Butorphanol(Stadol)?
Analgesia & respiratory depression =10 | mg Morphine or 80-100 mg Demerol.
40
side effects include sedation, nausea, diaphoresis, resp. depression, dissociation, rarely dysphoria
Butorphanol(Stadol)
41
– CV side effects of stadol
: ↑Cardiac Output and cardiac | workload, ↑SBP and pulmonary artery pressure.
42
why does stadol RARELY cause dysphoria?
because there are MULTIPLE kappa receptors
43
Potency comparable to morphine
*Nalbuphine(Nubain)
44
what makes Nalbuphine(Nubain) really cool?
*No ill-effects on CV patients.
45
Nalbuphine(Nubain) is a µ receptor antagonist and к receptors agonist which means (3 points)
– Subsequent morphine dosing less effective – Useful in reversing lingering fentanyl-induced respiratory depressant effects while providing satisfactory analgesia. – Antagonizes pruritus induced by epidural morphine.
46
withdrawal can occur with whats ag/ant?
``` nubain - nalbuphine talwin - pentazocine stadol - butorphanol buprenorphine - buprenex suboxone (least amount) literally all of them ```
47
• Effects of Nalbuphine(Nubain)?
Analgesia, sedation, diaphoresis, headache
48
what receptor agonist effects provide adequate pain relief with less respiratory depression with nubain
kappa
49
Side Effects of nalbuphine - nubain
sedation (33%) resp depression dissociation
50
µ receptor affinity 50x greater than morphine
Buprenorphine(Buprenex)
51
this ag/ant has a Prolonged duration up to 8 hours
Buprenorphine(Buprenex)
52
does narcan work with buprenorphine - buprenex?
Resistant to antagonism
53
Indications for buprenex
– Effective on moderate to severe cancer pain. | – Opioid dependence (really the best)
54
Side effects of Buprenorphine(Buprenex)
Sedation, N/V, diaphoresis, HA, dizziness
55
what drug class does buprenorphine - buprenex interact with?
Benzos | B=B
56
Buprenorphine(Buprenex effect what receptors and in what way
* Partial µ receptor agonist. | * Antagonizes µ and k receptors
57
– partial μ-agonist and full κ-antagonist in a fixed 4:1 | ratio with naloxone
Buprenorphine/Naloxone (Suboxone)
58
Alternative to methadone for addicted patients and why?
Buprenorphine/Naloxone (Suboxone) | – Less resp depression, better safety, less withdrawal
59
in general, pts had a what % decrease in cravings for opioids when taking suboxone
40% - big time
60
suboxone is a analgesic that provides very little pain relief for non-opioid dependent or addicted patients why?
Because suboxone works to reduce hyperalgesia and non-opioid patients don’t have hyperalgesia like opioid patients do.
61
Pain is exaggerated and prolonged in response | to noxious stimuli
Hyperalgesia
62
what two patient populations has suboxone been proven to be effective with
opioid addiction without chronic pain | opioid addiction with chronic pain
63
when pt comes in on suboxone what do you expect their anesthesia care plan to include?
Requires a higher dose of opioid needed to | achieve adequate pain control
64
why does suboxone Requires a higher dose of opioid needed to achieve adequate pain control
• Can block other opioids from activating the | same opioid u receptors
65
• Some recommend replacing suboxone with | other opioids preoperatively for how many days?
3-7 days then | re-initiating suboxone therapy

Pharmacology 680 (19 decks)

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