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5230 > Opiate Agonists/Antagonists > Flashcards

Opiate Agonists/Antagonists Flashcards

1
Q

Endogenous opioid peptides

A

Enkephalins (met- and leu-)
-5 amino acid sequence with met- and leu- group different at the end
B-Endorphins
-99 amino acids
Dynorphins
^All are released in CNS and GI system in response to stress and pain, have tried to commercially produce them but can’t

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2
Q

Biggest group of opiate receptors found in ____

A

GI system

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3
Q

Opioid receptors

A
  • mu receptor (MOP)
  • delta receptor (DOP)
  • kappa receptor (KOP)
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4
Q

Opiate receptors (how they work)

A

Anti-pain neurons with endorphins or enkephalins will run parallel to pain pathway
-Will attach to presynaptic opiate receptors (opioids=agonists to these receptors) on pain nerves to decrease the amount of pain chemical released

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5
Q

Opioid receptor with the most analgesic effect

A

Mu

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6
Q

Opioid receptor with dysphoria effect

A

Kappa, have low abuse potential

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7
Q

Opioid receptor with antishivering effect

A

Kappa

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8
Q

Opioid receptors with miosis effect

A

Miosis=pinpoint pupils

Mu and Kappa

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9
Q

Partial opioid agonists (example, what they do)

A

Ex: Buprenorphine
Act as partial antagonist if given after agonist
If given along acts an as agonist

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10
Q

3 chemical structures of opioids

A 
Phenanthrene alkaloids
-Natural
-Semisynthetic
-Synthetic
Piperidine derivatives
-All synthetic
-Phenylpiperidines (not technically correct but usually they're all referred to as this)
-Anilidopiperidines
Diphenylheptanes
-Methadone
*3 different classes are structurally different, if true allergy a cross allergic reaction should happen between classes
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11
Q

Opioids most likely to stimulate the release of histamine

A

Meperidine (Demerol)
Morphine
Codeine
Semisynthetic phenanthrenes (dilaudid, oxy, etc)

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12
Q

Phenanthrene Alkaloids (common meds we would give)

A 
Naturally occurring
-Morphine
-Codeine
Semisynthetic
-Vicodan
-Dilaudid
-Oxycodone
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13
Q

Piperidine Derivatives (common meds we would give)

A 
Phenylpiperidine: Demerol
Anilidopiperidines
-Fentanyl
-Sufentanil
-Alfentanil
-Remifentanil
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14
Q

Potency (compared to morphine) of

A 
Demerol: 0.1
Fentanyl: 100
Sufentanil: 500-1000
Alfentanil: 10-20
Remifentanil: 100
Dilaudid: 5
Heroin: 2 (but has more euphoria)
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15
Q

Remifentanil metabolism

A

Nonspecific esterase enzymes via hydrolysis (needs to be given as a drip)

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16
Q

Demerol metabolism and contraindication

A

Metabolism
-Metabolized to a toxic metabolite (normaperidine) which is CNS toxic -> seizures
-Don’t use >24 hours or in those with renal disease/elderly, they can’t get rid of the metabolite
Contraindication: Patient taking MAO inhibitors

17
Q

What effects of opioids do you never develop tolerance to

A

Constipation and miosis

18
Q

Do opioids have antitussive effect?

A

Yes, they all suppress cough which helps during emergence

19
Q

Narcotics and muscle rigidity

A

Happens when high potency opioids are administered rapidly
-Especially in older patients when muscle relaxants aren’t used and N2O is given at the same time
Thoracic muscles are rigid, and glottis closure occurs
-Give succinylcholine (it only happens after loss of consciousness, so if it’s happening you know paralytics are OK to give)

20
Q

Opioid effect on biliary pressure

A 
Opioids have vagal effect on SMC sphincters: tighten them
-Including sphincter of odi-biliary tree outlet=biliary pressure buildup
-Dose dependent 
Can treat/reverse with
-atropine or glycopyrrolate
-nitroglycerine
-glucagon
-naloxone
21
Q

Suftenanil use

A

Giving any dose will result in apnea

-Only use for big/long cases where patient will stay intubated postop

22
Q

Opioid effect on ICP

A

Don’t directly increase or decrease it
But, if they cause respiratory depression and CO2 increases, this causes vasodilation and increases ICP
-Doesn’t matter for surgery because we are supporting their respirations

23
Q

Naloxone mechanism of action

A

Competitive mu-opioid receptor antagonist

24
Q

Dosing narcan

A

0.4-2mg increments (start lower 0.4mg after surgery so you can get respiratory effort back but don’t lose all your analgesia)
Max dose: 10mg

25
Q

Narcan onset, peak, duration

A

Onset: 2 minutes
Peak: 5-15 minutes
Duration: 20-60 minutes

5230 (13 decks)

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