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Neurology Week 5 2018/19 > 8: Mechanism of analgesia > Flashcards

8: Mechanism of analgesia Flashcards

1
Q

Which type of analgesic drug reduces inflammatory pain by dampening down the inflammatory response?

A

NSAIDs

inhibit prostaglandin production by inhibiting COX1/2

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2
Q

How do NSAIDs work?

A

Cycloxygenase inhibitors

Reduce production of prostaglandins

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3
Q

Prostaglandins produce which three effects?

A

Inflammation

Pyrexia (fever)

Pain

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4
Q

Name five non-selective NSAIDs.

A

Aspirin

Ibuprofen

Diclofenac

Naproxen

Indomethacin

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5
Q

How can you tell that an NSAID is COX-2 specific?

A

It will be called something-coxib

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6
Q

What are some side effects of NSAIDs?

A

Peptic ulceration > GI bleeding

Renal toxicity

Cardiovascular problems (COX-2 only)

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7
Q

COX-2 inhibitors (-coxibs) aren’t often used because they contribute to cardiovascular disease - how?

A

Prothrombotic

increase chance of DVT > PE, stroke

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8
Q

Which type of analgesic drug reduces pain by inhibiting nociceptive nerve transmission in the brainstem and posterior horn of the spinal cord?

A

Opioids

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9
Q

Which type of analgesic drug reduces pain by targetting ion channels involved in nerve damage and inflammation?

A

Anti-epileptics

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10
Q

Which type of analgesic drug works by inhibiting serotonin and noradrenaline reuptake?

A

Tricyclic anti-depressants

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11
Q

Which ion channel is blocked by many antiepileptic drugs e.g carbamazepine?

A

Na+

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12
Q

Describe the WHO analgesic ladder.

A

1. Non-opioid +/- adjuvant

2. Weak opioid +/- non-opioid +/- adjuvant

3. Strong opioid +/- non-opioid +/- adjuvant

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13
Q

Is paracetamol an NSAID?

Why (not)?

A

No

NSAIDs are anti-inflammatory, anti-pyrexial and analgesic - paracetamol isn’t anti-inflammatory

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14
Q

What is the difference between pain and nociception?

A

Pain is the experience of suffering

Nociception is the nervous system’s way of conveying pain signals to the brain

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15
Q

What is the Gate Control Theory?

A

Pain is transmitted by SMALL FIBRE sensory nerves

Mostly everything else is transmitted by LARGE FIBRE sensory nerves

if the large fibre nerves are transmitting impulses, inhibitory interneurons stop small fibre impulses (i.e pain impulses) from going any higher

i.e if you’re bombarded with other sensory information, your perception of pain is reduced

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16
Q

In the Gate Control Theory, nerve impulses from large (Aα and Aß fibres) sensory fibres activate the ___ interneurone, stopping the transmission of pain signals.

A

inhibitory interneurone

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17
Q

Which types of nerve fibre are classed as large fibre sensory nerves?

A

A-alpha

A-beta

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18
Q

A-alpha and A-beta fibres are involved in dampening down nociceptive signals in the Gate Control Theory.

Which senses are these fibres responsible for?

A

A-alpha = proprioception

A-beta = skin mechanoreceptors

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19
Q

Which types of nerve fibre are classed as small fibre sensory nerves?

Which sensations do they control?

A

A-delta

C

Pain, temperature, itch

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20
Q
A
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21
Q

Which inhibitory neurotransmitter is involved in the Gate Control Theory?

A

GABA

Glycine

22
Q

Which excitatory neurotransmitter is involved in the Gate Control Theory?

A

Glutamate

23
Q

The Gate Control Theory is an example of (afferent / efferent) pain modulation.

A

afferent

ascending tracts, sensory

24
Q

Pain modulation descending from the brain is known as (afferent / efferent) modulation.

A

efferent

25
Q

Which area of the brainstem has an analgesic effect when stimulated?

Where specifically in the brainstem is it found?

A

Periaqueductal grey matter

Midbrain

26
Q

The periaqueductal grey area of the midbrain is an efferent regulator of pain.

Apart from electrical stimulation, what activates it?

A

Opioids

27
Q

What is the result of activation of the periaqueductal gray matter?

A

Nociceptive signals from the posterior horn are INHIBITED

i.e perception of pain is reduced

because Nucleus raphe magnus and Locus coeruleus are activated

28
Q

What are the body’s endogenous opioids called?

A

Enkephalins

29
Q

When activated by electrical impulses or opioids, the periaqueductal gray area activates two other brain areas.

What are they called?

A

Nucleus raphe magnus

Locus coeruleus

30
Q

Which chemicals are released by the nucleus raphe magnus?

What is the end result of this chemical release?

A

Serotonin (5-HT)

Enkephalins

inhibition of nociceptive transmission, analgesia

31
Q

Which area of the midbrain is involved in pain regulation and can be activated by electrical impulses and opioids?

A

Periaqueductal gray matter

32
Q

Which neurotransmitter is released by the locus caeruleus?

What is the end result of this release?

A

Noradrenaline

Inhibition of nociceptive transmission, analgesia

33
Q

Which areas of the CNS are affected (either excited or inhibited) by opioids?

A

Periaqueductal gray matter in the midbrain

Nucleus raphe magnus in the pons

Relay neurons in the posterior horn of the spinal cord

34
Q

Which type of receptor do opioids act on?

A

G-protein coupled receptors

35
Q

Opioids inhibit

a) Ca2+ channels
b) K+ channels

found on nociceptive neurons (both pre and post-synaptic, a bit confusing).

How does this modulate pain?

A

a) Ca2+ responsible for excitatory neurotransmitter (glutamate) release, so blocking this channel dampens down excitation
b) K+ enters the cell to cause repolarisation and stop an action potential, so blocking this channel prolongs the AP, reducing excitation

36
Q

Which channels are blocked in response to the activation of G-protein coupled opioid receptors?

A

Ca2+

K+

37
Q

Which named opioid receptor is most important in analgesia?

A

Mu (μ) receptor

38
Q

Opioids are highly ___ if used inappropriately.

A

addictive

39
Q

Apart from their addictive potential, what are some side effects of opioids?

A

Respiratory depression > Apnoea

Postural hypotension

N&V, constipation

Confusion, hallucinations

40
Q

What are important

a) respiratory
b) GI
c) neurological
d) cardiovascular

side-effects of opioids like morphine?

A

a) Respiratory depression

b) N&V, constipation

c) Confusion, hallucinations

d) Postural hypotension

41
Q

Which opioid receptor does morphine activate?

A

μ​ receptor

42
Q

How does morphine tend to be administered for

a) acute pain
b) chronic pain?

A

a) IV

b) Oral

43
Q

What is an opiate antagonist used to reverse the effects of opiates like morphine?

A

Naloxone

44
Q

Why must continuous release morphine be prescribed carefully?

A

Can be misused (dissolved and injected to deliver a high dose rapidly)

45
Q

What is diamorphine also known as?

A

Heroin

46
Q

What is heroin also known as?

A

Diamorphine

47
Q

Which strong opioid has a rapid effect when delivered intravenously and is sometimes used for severe post-op pain?

A

Diamorphine (heroin)

48
Q

Which weak opioid is only given orally and is converted to morphine by the liver?

A

Codeine

49
Q

Codeine is given (orally / IV).

A

oral only

50
Q

Which two strong opioids are derivatives of codeine?

A

Oxycodone

Hydrocodone

51
Q

Which opioid is 75-100x more potent than morphine?

What does it tend to be used for?

A

Fentanyl

Maintenance anaesthesia during surgery

52
Q

Which opioid can be given for acute pain and is often used during childbirth?

A

Pethidine

Neurology Week 5 2018/19 (11 decks)

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