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Neurology > Analgesia > Flashcards

Analgesia Flashcards

1
Q

What are the modes of action of analgesics?

A

Act at side of injury to decrease nociceptor sensitization
Suppress nerve conduction by blocking/ inactivating voltage-activated sodium channels
Suppress synaptic transmission of nociceptive signals in the dorsal horn of the spinal cord
Activate or potentiate descending inhibitory controls
Targeting ion channels upregulated in nerve damage

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2
Q

Examples of strong opioids

A 
Morphine
Oxycodone
Hydromorphone
Heroin
Fentanyl
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3
Q

Examples of weak opioids

A

Codeine
Tramadol
Dextropropoxyphene

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4
Q

Examples of NSAIDs

A 
Aspirin
Diclofenac
Ibuprofen 
Indomethacin
Naproxen
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5
Q

What are endogenous peptides?

A

Endorphine which act upon opioid receptors

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6
Q

What mediates the supraspinal antinociception pathway?

A

Descending pathways from the brainstem

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7
Q

Which areas of the brain are involved in pain perception?

A

Cortex
Amygdala
Thalamus
Hypothalamus

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8
Q

What are important brainstem regions in the regulation of pain?

A

Periaqueductal grey area of midbrain around the 4th ventricle
Locus ceruleus of the pons
Nucleus raphe magnus of the medulla

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9
Q

Where will activated PAG neurones project?

A

Nucleus Raphe Magnus (NRM) to excite 5-HT and enkephalinergic neurones which project to the dorsal horn resulting in suppression of nociceptive transmission

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10
Q

Which neurotransmitter will the locus coeruleus utilise in regulation of pain?

A

Noradrenergic neurones which project to the dorsal horn

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11
Q

What are the different types of opioid receptors?

A

Mu
Delta
Kappa

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12
Q

What is the function of Mu?

A

Responsible for the majority of analgesic action of opioids but also the major adverse side effects

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13
Q

What is the function of delta?

A

Contributes to analgesia but also can be a proconvulsanat

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14
Q

What is the function of kappa?

A

Contributes to analgesia at the spinal and peripheral level and activation assoc with sedation, dysphoria and hallucinations

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15
Q

What is the major resp effect of opioids and what is the mechanism?

A

Apnoea

Blunting of medullary resp centre to CO2 involving Mu and delta receptors

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16
Q

What is the major CV effect of opioids and what is the mechanism?

A

Orthostatic hypertension
Reduced sympathetic tone and bradycardia via actions on medulla
Histamine evoked vasodilation
Morphine can cause mast degranulation which can trigger bronchospasm in asthmatics

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17
Q

What is the major GI effects of opioids and what are the modes of action?

A

N+V, constipation, increased intrabiliary pressure
Actions on CTZ
Increased smooth muscle tone, decreased motility via enteric neurones
Involves Mu and Delta receptors

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18
Q

What are the major CNS effects of opioids and what are the modes of action?

A

Confusion, eurphora, dysphoria, hallucinations, dizziness, myoclonus and hyperalgesia
Occurs to different degrees dependent upon the specific opioid drug and receptor subtypes activated

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19
Q

How is morphine metabolised and where?

A

Liver

Glucuronidation at the 3 and 6 hydroxyl positions

20
Q

What is the impact of glucuronidation at the 3 and 6 positions of morphine?

A

3 - inactive drug

6 - active analgesic that is excreted renally

21
Q

What is the difference between morphine and diamorphine?

A

Diamorphine is more lipophilic than morphine

Rapid onset of action (enters CNS)

22
Q

How is codeine metabolised and where?

A

Hepatic metabolism by demethylation to morphine by cytochrome p450

23
Q

What are common side effects of codeine?

A

Anti-diarrhoeal

Antitussive

24
Q

What are the semi-synthetic derivatives of codeine?

A

Oxycodone

Hydrocodone

25
Q

Is fentanyl more or less potent than morphine?

A

75-100x more potent

26
Q

When is fentanyl commonly given?

A

IV to provide analgesia in maintenance anaesthesia

27
Q

When is pethidine used?

A

Acute pain, particularly labour

28
Q

Which drugs can pethidine not be used in conjunction with?

A

MAO inhibitors as will cause excitement, convulsions and hyperthermia

29
Q

What is the mode of action of tramadol?

A

Weak Mu receptor agonist

Analgesic action by potentiation of descending serotonergic and adrenergic systems

30
Q

What condition can you NOT give tramadol?

A

Epilepsy

31
Q

What is the mode of action of methadone?

A

Weak Mu agonist of the phenylheptylamine class with additional actions at other sides in the CNS, including potassium channels, NMDA glutamate receptors and 5-HT receptors

32
Q

What is the mode of action of naloxone?

A

Competitive antagonist at Mu receptors used to reverse opioid toxicity

33
Q

What is important clinically about naloxone?

A

MUST monitor the effect of naloxone carefully, titrating the individual dose, and frequency to that required to reverse opioid toxicity

34
Q

What is the difference between naloxone and naltrexone?

A

Naltrexone has oral availability and a much longer half life

35
Q

What benefits do NSAIDs result in?

A

Analgesic
Antipyretic
Anti-inflammatory

36
Q

What is the mode of action of NSAIDs?

A

Inhibit the synthesis and accumulation of prostaglandins by COX enzymes COX-1 and COX-2

37
Q

What is the difference between COX-1 and COX-2?

A

COX-1 is constitutively active

COX-2 is induced locally at sites of inflammation by various cytokines

38
Q

How do NSAIDs reduce pain and inflammation?

A

Suppress the decrease in activation of threshold of peripheral terminals of nociceptors caused by prostaglandins
Decrease recruitment of leukocytes that produce inflammatory mediators
If cross BBB; suppress the production of pain-producing prostaglandins in the dorsal horn of the spinal cord

39
Q

Why can NSAIDs result in GI damage?

A

PGE2 produced by COX-1 protects against the acid/pepsin environment of the stomach

40
Q

What is neuropathic pain?

A

Trigeminal neuralgia
Diabetic neuropathy
Postherpetic neuralgia
Phantom limb pain

41
Q

What are the treatment options for neuropathic pain?

A

Gabapentin and pregabalin (antiepileptics)
Amitriptyline (antidepressants)
Carbamezapine

42
Q

What is the mode of action of gabapentin/pregabalin in pain modulation?

A

Reduction in surface expression of calcium channels which are upregulated in damaged sensory neurones
Causes a decrease of neurotransmitters such as glutamate and substance P from the central terminal sof nociceptive neurones

43
Q

In what condition is gabapentin frequently used?

A

Migraine prophylaxi

44
Q

In what condition is pregabalin frequently used?

A

Painful diabetic neuropathy

45
Q

What is the mode of action of tricyclics in modulation of pain?

A

Act centrally by decreasing the uptake of NA

46
Q

What is the mode of action of carbamazepine in the modulation of pain?

A

Blocks subtypes of voltage activated Na+ channels that are upregulated in damaged nerve cells

47
Q

In what condition is carbamazepine commonly used?

A

1st line to control pain intensity and frequency of attacks in trigeminal neuralgia

Neurology (48 decks)

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