Analgesic Drugs Flashcards

1
Q

Describe the WHO Pain ladder

A
  1. Strong opioid
  2. Weak opioid
  3. NSAIDs
  4. Paracetamol
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2
Q

What is the difference between an opiate and opioid?

A

Opiate - substances extracted from opium

Opioid - any agent that acts on opioid receptors (including endogenous peptides)

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3
Q

What descending pathway acts to modify pain?

A

Supraspinal antinociception

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4
Q

Describe the supraspinal antinociception pathway

A

Peri-aqueductual grey matter sends signals to the locus ceruleus and nucleus raphe magnus which project to dorsal horn of spinal cord and inhibit nociceptive transmission

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5
Q

What stimulates the peri-aqueductal grey matter?

A

Opioids and electrical stimulation

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6
Q

Where is the PAG?

A

Midbrain

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7
Q

Where is the locus ceruleus?

A

Pons

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8
Q

Where is the nucleus raphe magnus?

A

Medulla

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9
Q

What does the PAG excite?

A

Nucleus raphe magnus

Locus coruleus

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10
Q

What is the effect of PAG excitation of NRM and LC?

A

They excite 5HT and NA neurones which project to the dorsal horn and inhibit nociceptive transmission

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11
Q

Describe the cellular action of opioids

A

Inhibit opening of voltage activated calcium channels to prevent release of neurotransmitter
Opens potassium channels to suppress excitation
Inhibits adenylate cyclase

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12
Q

Name the three opioid receptors

A

MU
Delta
Kappa

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13
Q

What is the effect of opioids on the respiratory system?

A

Apnoea - blinding of medullary resp centre to carbon dioxide

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14
Q

What is the effect of opioids on the cardiovascular system?

A

Orthostatic hypertension - reduced sympathetic tone and bradycardia - histamine evoked vasodilation

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15
Q

What is the effect of opioids on the GI system?

A

Nausea, vomiting, constipation, intrabilary pressure

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16
Q

What is the effect of opioids on the CNS?

A

Confusion, euphoria, dysphoria, hallucinations, dizziness, hyperalgesia

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17
Q

What can morphine cause in asthmatics?

A

Degranulation and bronchospasm

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18
Q

How do most analgesic drugs work?

A

Prolonged activation of opioid receptors

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19
Q

Name opioid agonists

A
Morphine 
Diamorphine 
Coedine 
Fentanyl 
Pethidine 
Buprenophine 
Tramadol 
Methadone
20
Q

Name an opioid antagonist

A

Naloxone

21
Q

When is morphine used?

A

Severe acute pain

Chronic pain

22
Q

Where is morphine broken down?

A

Liver

  • M3G (inactive)
  • M6G (analgesic activity)
23
Q

Name the methods of administration of morphine

A

IV
IM, SC, oral
Epidural or intrathecal

24
Q

What is another name for diamorphine?

A

Heroin

25
Q

How is diamorphine different to morphine?

A

More lipophilic and has a rapid onset of action when administered IV as can enter CNS

26
Q

When is codeine used?

A

Mild/moderate pain - hepatic metabolism to morphine

27
Q

What are the higher potency derivatives of codeine?

A

Oxycodone and hydrocodone

28
Q

In addition to pain relief what are the other effects of codeine?

A

Anti-diarrhoeal

Anti-tussive

29
Q

Describe fentanyl

A

75-100 times more potent than morphine
Given IV to provide analgesia in anaesthetic
Transdermal, IV or sublingual delivery

30
Q

When is pethidine used?

A

Acute pain in labour

Rapid onset

31
Q

What drug can pethidine not be used with?

A

Monoamine oxidase inhibitors

32
Q

When is buprenorphine used?

A

Chronic pain with patient controlled injection systems

33
Q

What is the mechanism of action of tramadol?

A

Weak mu receptor agonist potentiates the descending pathways

34
Q

What disease should tramadol be avoided in?

A

Epilepsy

35
Q

Where does methadone work?

A

Weak mu receptor agonist
Acts on potassium channels
NMDA glutamate receptors
5HT receptors

36
Q

What can methadone be used for?

A

Terminal cancer

Withdrawal

37
Q

What does naloxone do?

A

Competitive antagonist of mu receptors and used to reverse opioid toxicity

38
Q

Where do non-selective NSAIDs work?

A

COX 1 inhibitor

39
Q

Where do selective NSAIDs work?

A

COX2 induced locally at sites of inflammation

40
Q

Name non-selective NSAIDs

A

Aspirin
Ibuprofen
Diclofenac
Naproxen

41
Q

Name selective NSAIDs

A

Etoricoxib
Celecoxib
Inmiracoxib

42
Q

Name drugs that can be used in neuropathic pain

A

Gabapentin
Pregablin
Amitriptyline
Carbamazepine

43
Q

How do gabapentin and pregablin work?

A

Reduce cell surface expression of a subunit of voltage gated calcium channels which are unregulated in damaged neurones

44
Q

What can gabapentin and pregablin be used for?

A

Pregablin - diabetic neuropathy

Gabapentin - migraine

45
Q

How does amitriptyline work?

A

Decrease reuptake of noradrenaline

46
Q

Name a sodium channel blocker

A

Carbamazepine

47
Q

What type of pain can carbamazepine be used for?

A

Trigeminal neuralgia