L216 Opiods Flashcards

1
Q

Flow of pain

A
Nocireceptors
Adelta and c fibers
Trigeminal ganglion
Trigeminal nuclei (not great spatial)
Thalamas
Limbic system and cerebral cortex
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2
Q
Adelta vs C fibers
Speed
Myelination
Type of pain
Stimuli
A

Adelta: fast, myelinated, sharp initial pain to mechanical stimuli
C fibers: Slow, unmyelinated, dull, aching, burning pain, thermal, mechanical, chemical stimuli

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3
Q

Tissue damage leads to the release of

A
Prostaglandins
Substance P
TNF-alpha
IL 1-Beta
IL-6
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4
Q

TRPV1 responds to this type of stimuli

A

Acid

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5
Q

Hyperalgesia

A

Heightened sense of pain to noxious stimuli

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6
Q

Allodynia

A

Pain resulting from normally painless stimuli

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7
Q

Beta endorphin is an example of this peptide

A

Pro-opiomelanocortin (POMC)

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8
Q

Three important Opioid receptors

A

Mu
Kappa
Delta

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9
Q

Mu, Kappa, Delta common charactersitics

A

G protein coupled receptors
Widely distributed in CNS
Activate G alpha-i

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10
Q

Beta endorphin is a natural agonist of

A

mu opioid receptor

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11
Q

Met-enkephalin and Leu enkephalin are natural agonists of the

A

delta opioid receptor

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12
Q

Dynorphin A
Dynorphin B
alpha/beta neo-endorphin
Are natural agonists of

A

Kappa opioid receptor

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13
Q

Proenkephalin gives off

A

Met enkephalin

Leu ekephalin

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14
Q

Prodynorphin gives off

A

Dyn-A
Dyn-B
alpha-neo-endorphin

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15
Q

Endorphins

A

Endormorphin-1

Endomorephin-2

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16
Q

Pre-synaptic mechanism of opioid receptor activity

A

Gi activation inhibits AC
Causing decrease cAMP
Causing decrease PKA
Cause decrease in Ca entry thru cannels

17
Q

Post synaptic mechanism of opioid receptor activty

A

GbetaGgamma activation
Potassium leaves the cell
Hyperpolarization

18
Q

Natural agonist of mu opiod receptor

A

B-endorphin

19
Q

Physiologically important opiod receptors

A

U1, U2

20
Q

U receptors are found in

A
PAG
Superficial dorsal horn
Nucleus accumbens
Amygdala
cerebral cortex
21
Q

What does Mu do?

A

Suppresses presynaptic transmitter release

22
Q

Mechanism of action of opioids with analgesic action

A

Opiods inhibit release of GABA which would usually inhibit the inhibitory pathway

23
Q

GI effects of opiods

A

constipation

GI spasm

24
Q

Emotional compenent of pain is from

A

Limbic system

25
Q

How is tolerance first manifested in morphine

A

Shortened or diminshed analgesia

26
Q

Morphine is metabolized by _____ into ____ and _____

A

UGT2B7
Morphine 3 glucuronide (inactive)
Morphine 6 glucuronide (better than morphine)

27
Q

UGT2B7 presence

A

brain and liver

28
Q

Codeine metabolism

A

(morphine, M3G, M6G) (5 percent)

codeine 6 glucuronide (80percent)

29
Q

When is codeine more effective than morphine

A

Orally but not intramuscularly