Mechanisms of Analgesia Flashcards

1
Q

These drugs modify transmission of nociceptive signals in the dorsal horn of the signal cord

A

Opioids

Anti-depressant drugs

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2
Q

These drugs activate descending inhibitory controls

A

Opioids

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3
Q

NSAIDS

A
Aspirin
Diclofenac
Ibuprofen
Indomethacin
Naproxen
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4
Q

Weak opiods

A

Codeine
Tramadol
Dextropropoxyphene

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5
Q

Strong opiod

A

Morphine
Hydromorphane
Fentanyl
Heroin

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6
Q

What does the nucleus raphne magnus release?

A

Serotonin (5-HT)

Enkephalins

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7
Q

What does the locus coruleus produce?

A

NA (noradrenergic neurones)

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8
Q

What stimulates the PAG (periaqueductal grey)

A

Electrical stimulation
Opiods

(Excitation by electrical stimulation produces PROFOUND analgesia)

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9
Q

Opiod drugs mimic the activity of what?

A

Enkaphalinergic interneurones

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10
Q

Which type of drug mimics the activity of enkaphalinergic interneurones?

A

Opioids

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11
Q

Opiod action is mediated by which type of receptor?

A

G protein coupled receptor

(couple to Gi/o to produce:

  • inhibition of opening of voltage activated Ca2+ channels
  • opening of K+ channels
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12
Q

Side effect of m opiod receptors

A
Respiratory depression
Constipation
Euphoria
Sedation
Dependence
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13
Q

Side effect of delta opiod receptors

A

Proconvulsant

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14
Q

These opiod receptors contribute to analgesia at the spinal and peripheral level

A

K opiod receptors

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15
Q

Side effect of k opiod receptors

A

Sedation
Dysphoria
Hallucinations

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16
Q

Activation of these receptors produces an anti-opiod effect

A

ORL-1 receptors

17
Q

These opiod receptors are responsible for most of the analgesic action of opiods

A

m receptors

18
Q

What inhibits COX-2?

A

Non-selective NSAIDs and COXIBs

19
Q

What does PGE2 do?

A

Sensitises nociceptive neurones and causes hyperalgesia

20
Q

Why is paracetemol not classes as an NSAID?

A

Lacks anti-inflammatory activity and only WEAKLY inhibits COX

21
Q

What is acetaminophen?

A

Paracetemol

22
Q

Why might paracetemol cause nephrotoxicity?

A

Because of inhibition of COX-2 which is constitutively expressed by the kidney and because of compromisation of renal haemodynamics)

23
Q

Which COX-2 inhibitors are prothrombotic?

A

Rofecoxib, celecoxib (this limits their use)

24
Q

COX-1 produced what which helps protect against the acid environment?

A

PGE2

25
Q

Why do NSAIDS have limited analgesic effect?

A

NSAIDs have limited analgesic efficacy because multiple signalling pathways, several of which do not involve arachidonic acid metabolism, cause nociceptor sensitization