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PBT 3 Exam 2 > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

Endogenous neuropeptide transmitters

A

Beta-endorphin
Enkephalin
Dynorphin

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2
Q

Opioid receptor classes

A

Mu
Delta
Kappa

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3
Q

Ligand-receptor matches

A

B-endorphin -> mu
Enkephalin -> mu and delta
dynorphin -> kappa

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4
Q

Intracellular pathway for Opioid receptors

A

coupled to inhibitory G-protein
ligand or drug binds -> alpha unit inhibits cAMP -> this inhibits opening of Ca and Na channels -> leads to hyperpolarization and reduction in AP
Beta unit -> still opens K channels -> K leaves the cell -> hyperpolarizes even more
this leads to inhibition of the neuron

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5
Q

Two locations of action for opioids

A

Brain and spinal cord

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6
Q

Where do opiates work

A

midbrain and brainstem

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7
Q

How do opiates work in the brain

A

disinhibit the descending pathway

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8
Q

GABAergic neuron in the midbrain/brainstem release GABA which inhibits_____

A

NE and 5HT release

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9
Q

NE and 5HT do what

A

inhibit pain (descending pathway)

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10
Q

If you inhibit the GABAergic neuron with an opioid, what will happen

A

inhibit GABA release leads to release of 5HT and NE to activate descending pathway and block/reduce pain

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11
Q

Nociceptive circuitry in the spinal cord

A

Ascending pathway: A-delta and C-fibers release glutamate and substance P -> activate projection neurons -> send pain message to brain
Descending pathway: NE and 5HT released into spinal cord -> bind and activate interneuron -> interneuron makes enkephalin -> inhibits release of glutamate and substance P -> inhibits pain mechanism

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12
Q

Presynaptic terminals of sensory neurons have

A

opioid receptors

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13
Q

what happens if an opioid binds to presynaptic mu or delta receptor

A

release enkephalin -> inhibit release of glutamate and substance P

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14
Q

What activates projection neurons; what inhibits them?

A

activates: glutamate and substance P
inhibits: release of enkephalin

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15
Q

Can opioid agonists activate all receptors

A

Yes, with the exception of fentanyl which shows strong mu preference

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16
Q

Binding preference of opioids

A

mu > delta > kappa

kappa not used much b/c of SE

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17
Q

Morphine and analogs

A

morphine is gold standard

most commonly used

18
Q

Morphine

A

MS contin; Kadian

19
Q

Oxycodone

A

Oxycontin

slightly higher potency 1:1.5 oxy:morphine

20
Q

Hydromorphone

A

Dilaudid
morphine alternative
3-5x more potent than morphine, orally

21
Q

Codeine

A

pro-drug
poor analgesic
can increase analgesic efficacy of NSAIDs

22
Q

Fentanyl

A 
Highly potent mu receptor agonist
80-100x more potent than morphine
HIGH lipid solubility
SHORT duration of action
often transdermal patch or lozenge for chronic/breakthrough pain
23
Q

Fentanyl analogs (3)

A

Alfentanil (Alfenta): ultra-short acting (5-10 min)
Sufentanil (Sufenta): 50-10x more potent than fentanyl
Remifentanil (Ultiva): very very short acting (1-4 min)

24
Q

Tramadol

A

Ultram
weak mu receptor agonist
inhibits 5-HT and NE reputake -> prolongs effects
Alpha-2 agonist

25
Q

Methadone

A

Dolophine
long acting agonist
similar potency to morphine
Often used as maintenance tx for addicts

26
Q

Buprenorphine

A 
Subutex
mu partial agonist
long duration of action
moderate to severe pain
tx of physical dependence on opioids
27
Q

Suboxone

A

buprenorphine/naloxone combo
agonist and antagonist
prevents abuse - if crushed/compromised naloxone release and buprenorphine won’t work

28
Q

Weak opioids

A

codeine

tramadol

29
Q

strong opioids

A

morphine and analogs
fentanyl
methadone
buprenorphine

30
Q

WHO analgesic ladder

A
  1. non-opioid +/- adjuvant
  2. weak opioid for mild to moderate pain +/- non-opioid, +/- adjuvant
  3. strong opioid for moderate to severe pain +/- non-opioid, +/- adjuvant
31
Q

SE of opioids

A 
Nausea
constipation
sedation
respiratory distress -> at high doses
Miosis (OD)
32
Q

why do opioids cause respiratory distress

A

act in brainstem -> pons and medulla involved in modifying respiratory rate

33
Q

What is a peripheral SE and tx opioid use

A

constipation
methylnaltrexone (relistor) OR
alvimpoan (entereg)
opioid receptor antagonists, do not cross BBB

34
Q

SE with long term use

A

tolerance
physical dependence
addiction

35
Q

Hydrocodone + acetaminophen

A

Vicodin, Lortab

Opioid combo tx

36
Q

Hydrocodone + ibuprofen

A

Vicoprofen

Opioid combo tx

37
Q

Oxycodone + acetaminophen

A

Percocet

Opioid combo tx

38
Q

Oxycodone + ibuprofen

A

Combunox

Opioid combo tx

39
Q

Oxycodone + aspirin

A

Percodan

Opioid combo tx

40
Q

Why have opioid combo tx? (2 reasons)

A

1A. Acetaminopen or NSAIDs produce additive/synergistic effect
1B. Thus, a lower opioid dose is needed to achieve the same effect
2. reduction in opioid dose reduces occurrence of SE

PBT 3 Exam 2 (8 decks)

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