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Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

What is nociception?

A

Non conscious neural traffic due to trauma or potential trauma to tissue

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2
Q

What is pain?

A

Complex, unpleasant awareness of sensation modified by experience

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3
Q

How is pain signalled?

A 
Nocicpetors stimulated 
Release of substance P + glutamate
Afferent nerve stimulated
Fibres decussate
Action potential ascends
Synapse I thalamus
Project to post-central gyrus
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4
Q

What modulates pain peripherally?

A

Substantia gelatinosa

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5
Q

What modulates pain centrally?

A

Peri aqueductal grey

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6
Q

How is pain felt peripherally?

A

Stimulate AP - lamina 1+5 -> thalamus

Inhibits substantia gelatinosa

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7
Q

How is pain modulated peripherally?

A

‘Rub it’

Aδ stimulate substantia gelatinosa
Inhibits lamina

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8
Q

How is pain felt centrally?

A

Thalamus stimulates cortex

Cortex inhibits peri aqueductal grey

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9
Q

How is pain modulated centrally?

A

Peri aqueductal grey overrides inhibition

Modulated by

  • 5HT
  • endogenous opioids
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10
Q

What are the endogenous opioids?

A

Enkephalins
Dynorphins
B-endorphins

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11
Q

What are the receptors for opioids?

A

GPCRS

  • μ (MOP)
  • δ (DOP)
  • K (KOP)
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12
Q

Where are μ receptors found?

A

Supraspinal

GI tract

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13
Q

What is the effect μ receptor stimulation?

A

Decreased cAMP
Outward flux of potassium
Hyperpolarisation
Substance P release

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14
Q

What endogenous opioids act on μ receptors?

A

Enkephalins

B-endorphins

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15
Q

What happens when μ receptors are stimulated?

A 
Analgesia
Depression 
Euphoria 
Dependence
Respiratory sedation
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16
Q

Where are δ receptors found?

A

Wide distribution

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17
Q

What is the effect of δ receptor stimulation?

A

Decreased cAMP
Influx of calcium
Hyperpolarisation
Substance P release

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18
Q

What endogenous opioids act δ receptors?

A

Enkephalins

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19
Q

What happens when δ receptors are stimulated?

A

Analgesia
Inhibit dopamine
Modulate μ receptors

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20
Q

Where are K receptors found?

A

Spinal cord
Brain
Periphery

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21
Q

What is the effect of K receptor stimulation?

A 
Decreased cAMP 
Efflux of potassium 
Influx of calcium 
Hyperpolarisation 
Substance P release
22
Q

What endogenous opioids act on K receptors?

A

Dynorphins

23
Q

What happens when K receptors are stimulated?

A

Analgesia
Diuresis
Dysphoria

24
Q

What is the WHO analgesic ladder?

A

Simple analgesia
Weak opioid
Strong opioid

25
Q

What is a weak opioid?

A

Codeine

26
Q

What is a strong opioid?

A

Morphine

Fentanyl

27
Q

What is a partial opioid agonist?

A

Buprenorphine

28
Q

What is an opioid antagonist?

A

Naloxone

29
Q

What routes can be used to administer morphine?

A 
PO
IV
IM 
SC
PR
30
Q

What is the mechanism for morphine as an analgesia?

A

Strong affinity for μ receptors

Release of enkephalins + B-endorphins

31
Q

What is the mechanism for morphine as an anti-diarrhoeal?

A

Decreases tone of longitudinal and circular smooth muscle
Reduces peristalsis
Decreases colonic mass movement

32
Q

What are the side effects of morphine?

A

Respiratory depression
Emesis
Histamine release
Constipation

33
Q

What are the indications for fentanyl?

A

Analgesia

Anaesthesia

34
Q

What are the routes of administration for fentanyl?

A 
IV
Epidural 
Transdermal 
Buccal
Intrathecal
35
Q

What is the mechanism of fentanyl?

A

High affinity for μ receptor

36
Q

What are the side effects of fentanyl?

A

Respiratory depression
Constipation
Vomiting

37
Q

What are the indications for codeine?

A

Analgesia
Anti-diarrhoeal
Cough depressant

38
Q

What are the routes of administration for codeine?

A

PO

IM

39
Q

What is the mechanism of codeine?

A

Activation of μ receptors

1/10th potency of morphine

40
Q

What are the side effects of codeine?

A

Constipation

Respiratory depression

41
Q

What are the indications for buprenorphine?

A

Analgesia

Opioid addiction adjunct

42
Q

What are the routes of administration for buprenorphine?

A

Transdermal
IM
Sublingual

43
Q

What is the mechanism of buprenorphine?

A

High affinity for μ receptor

  • low kd
  • partial agonist

Antagonist at K receptor

44
Q

What are side effects of buprenorphine?

A

Respiratory depression
Hypotension
Nausea
Dizziness

45
Q

What is the indication for naloxone?

A

Competitive antagonism of opioid

46
Q

What are the routes of administration for naloxone?

A

IV

IM

47
Q

What is the mechanism of naloxone?

A

Competitively blocks μ recptors

Greater affinity than morphine

48
Q

What are the side effects of naloxone?

A 
Arrhythmias 
Dizziness 
Headache 
Hypertension 
Nausea
49
Q

How does opioid tolerance occur?

A

Body upregulates receptors so higher dose needed to cause an effect

50
Q

What is given to reduce symptoms of opioid withdrawal?

A

Methadone

51
Q

What are the signs of an opioid overdose?

A

Vomiting
Hypotension
Respiratory depression

52
Q

How is an opioid overdose managed?

A

Naloxone

Pharmacology (27 decks)

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