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Biomedical Pharmacology > Lecture 15 - Analgesics > Flashcards

Lecture 15 - Analgesics Flashcards

1
Q

What are the relevant mediators of Nociceptors?

A

Bradykinin 5HT Prostaglandin H+ ions

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2
Q

What are the different stimuli the Nociceptor nerve ending is responsive to?

A

Heat Cold
Pressure Tissue injury

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3
Q

What are nociceptor nerve endings referred to as?

A

Polymodal receptors (respond to more than one type of input)

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4
Q

What does tissue injury induce?

A

Local inflammatory response

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5
Q

What substances can be released to potentiate inflammatory response and have effect on blood vessels and mast cells?

A

Substance P and CGPR

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6
Q

Where are signals conducted?

A

Up the spinal cord and enter CNS via a simple pathway

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7
Q

What does NMDA receptor target?

A

General anaesthetics Target for modulation of nociceptive inputs in CNS

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8
Q

What blocks NMDA receptors?

A

Ketamine

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9
Q

What properties does ketamine have ?

A

Anaesthetic and analgesic properties

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10
Q

Where does glutamate act at?

A

Several receptors e.g. NMDA receptors

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11
Q

Where does ketamine block the NMDA receptor ?

A

Spinal cord

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12
Q

What are the different levels of the brain?

A

Cortex Midbrain Medulla

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13
Q

Where can you induce analgesia in subject?

A

Periaqueductal Grey

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14
Q

What regions can be found further up the cerebral cortex?

A

Locus coeruleus Amygdala Hippocampus

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15
Q

What region can modulate sensitivity to brain?

A

Hippocampus via hypothalamus

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16
Q

What Brain region is involved with regulation of autonomic functions, cardiovascular and respiratory systems?

A

Rostroventral medulla (RVM)

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17
Q

What happens when one senses a painful stimuli?

A

Has significant effect on cardiovascular system (alter heart rate and BP)

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18
Q

What transmitters are important for the descending inhibition?

A

5HT and enkephalins

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19
Q

What is the main site of noradrenergic cell bodies?

A

Locus coeruleus

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20
Q

What mechanisms are involved in the processing of pain?

A

Peripheral and central mechanism

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21
Q

What is most important in nociceptive processing ?

A

TRPV1

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22
Q

What happens when various stimuli activates TRPV1?

A

Subsequent depolarisation and excitation

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23
Q

What is the active component found in chilli?

A

Capsaicin

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24
Q

What happens when we stimulate NACH receptor enough?

A

Desensitisation

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25
Q

What does bradykinin Upon inflammatory response act and do?

A

Act via its own GPCR and increase levels of protein kinase C and phosphorylate the receptor

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26
Q

What does bradykinin do?

A

Modulate the responsiveness of TRP receptor in a positive way

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27
Q

What else modulates TRP?

A

Tyrosine kinase receptor

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28
Q

What does prostaglandin do?

A

Sensitize nociceptive nerve endings by enhancing pain-producing effect of other agents

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29
Q

What activates TRPV1?

A

Capsaicin Temperature and acidity

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30
Q

What is the role of nociception?

A

Cause subsequent peptide release

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31
Q

What does ATP act on to modulate nociceptive Information?

A

Purinergic receptors

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32
Q

What are the 3 isoforms that the cyclooxygenase exhibit?

A

Cox-1, Cox-2 and Cox-3

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33
Q

What are prostaglandin?

A

General inflammatory mediator

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34
Q

What can NSAID be?

A

Non-selective: Aspirin, ibuprofen, Diclofenac Selective: croxibs (Rofecoxib)(COx-2),paracetamol

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35
Q

What does ibuprofen and diclofenac produce?

A

Cardiovascular side effects

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36
Q

Where does paracetamol have an effect upon?

A

COX-3 and effects on prostaglandin seen in CNS only

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37
Q

What increases the descending modulation?

A

Endogenous opioids

38
Q

What nerve fibres are involved in descending inhibition?

A

A delta fibres - small diameter/ myelinated C fibres - unmyelinated

39
Q

What evidence has been provided in ascending and descending modulation Upon nature of pain?

A

Alteration and population of Na+ and K+ - affect speed of transmission and whether there is increase in sensitivity to nociceptive input

40
Q

What is pain associated with?

A

Activity of small diameter afferent fibres which have sensory ending in the peripheral tissues

41
Q

What does afferent fibers innervate?

A

Cells in the dorsal horn which give rise to projection pathways to the thalamus

42
Q

What does thalamus in term of function allow?

A

Sorting of Information

43
Q

What is lamina II (substantial gelatinosa) rich in?

A

Opioid receptors

44
Q

What does the descending inhibitory pathway reduce ?

A

Transmission of pain

45
Q

Apart from being rich in opioid receptors what does periaqueductal gray matter do?

A

Central to pain processing and if stimulated electrically can reproduce analgesia

46
Q

What is enkephalins responsible for?

A

Modulation of pain transmission Subjected feelings of highs and lows

47
Q

What are are examples of Enkephalins?

A

Pentapeptides Leu-enkephalins and Met-enkephalins Endogenous ligands and micro and delta receptors

48
Q

Where are enkephalins distributed and produced?

A

Widely distributed in CNS and synthesised in cell body Processed during axonal transport

49
Q

What are some examples of Endorphins and Dynorphins?

A

B-endorphin and dynorphin A

50
Q

What are the 4 classical receptor classification?

A

Mu, delta, kappa and ORL1 Type

51
Q

Which opioid receptor have been discounted?

A

Sigma receptors

52
Q

Which receptor brings about an analgesic effect?

A

Mu

53
Q

What are opioids known to reduce?

A

Significant respiratory depression

54
Q

What are Morphine?

A

Alkaloid extracted from opium Opiate and dried exudate from seed case of poppy

55
Q

What are the actions of Morphine?

A

Analgesic, Antidiarrhoeal and Antitussive Sedation, suppression of cough, respiratory depression, decreased peristalsis, decreased gastric acid secretion , euphoria, stimulation of CTZ, miosis, Increased tons of sphincter of Oddi, Increased release of prolactin and ADH, proconvulsant In overdose

56
Q

What are side effects of Morphine?

A

If used in analgesic/ drug abuse it can produce sustained constipation Gall bladder conditions

57
Q

What drug is effective in causing cough suppression ?

A

Codeine

58
Q

What happens when mu receptors are stimulated?

A

Reduction in CAMP generation

59
Q

Codeine

A

3-O-methyl Morphine Opiate Metabolised to Morphine. (CYP2D6) Used with NSAIDS

60
Q

DiaMorphine (heroin)

A

Effectively a pro drug and a semi-synthetic. Better oral absorption than morphine Terminally ill patients

61
Q

Where does paracetamol have an effect upon?

A

COX-3 and effects on prostaglandin seen in CNS only

62
Q

What increases the descending modulation?

A

Endogenous opioids

63
Q

What nerve fibres are involved in descending inhibition?

A

A delta fibres - small diameter/ myelinated C fibres - unmyelinated

64
Q

What evidence has been provided in ascending and descending modulation Upon nature of pain?

A

Alteration and population of Na+ and K+ - affect speed of transmission and whether there is increase in sensitivity to nociceptive input

65
Q

What is pain associated with?

A

Activity of small diameter afferent fibres which have sensory ending in the peripheral tissues

66
Q

What does afferent fibers innervate?

A

Cells in the dorsal horn which give rise to projection pathways to the thalamus

67
Q

What does thalamus in term of function allow?

A

Sorting of Information

68
Q

What is lamina II (substantial gelatinosa) rich in?

A

Opioid receptors

69
Q

What does the descending inhibitory pathway reduce ?

A

Transmission of pain

70
Q

Apart from being rich in opioid receptors what does periaqueductal gray matter do?

A

Central to pain processing and if stimulated electrically can reproduce analgesia

71
Q

What is enkephalins responsible for?

A

Modulation of pain transmission Subjected feelings of highs and lows

72
Q

What are are examples of Enkephalins?

A

Pentapeptides Leu-enkephalins and Met-enkephalins Endogenous ligands and micro and delta receptors

73
Q

Where are enkephalins distributed and produced?

A

Widely distributed in CNS and synthesised in cell body Processed during axonal transport

74
Q

What are some examples of Endorphins and Dynorphins?

A

B-endorphin and dynorphin A

75
Q

What are the 4 classical receptor classification?

A

Mu, delta, kappa and ORL1 Type

76
Q

Which opioid receptor have been discounted?

A

Sigma receptors

77
Q

Which receptor brings about an analgesic effect?

A

Mu

78
Q

What are opioids known to reduce?

A

Significant respiratory depression

79
Q

What are Morphine?

A

Alkaloid extracted from opium Opiate and dried exudate from seed case of poppy

80
Q

What are the actions of Morphine?

A

Analgesic, Antidiarrhoeal and Antitussive

81
Q

Pethidine

A

Shorter acting than Morphine Used (im) in obstetrics in 1st stage of labour Safer than a drug like Morphine Norpethidine is a metabolite Interaction with MAOIS

82
Q

Fentanyl

A

Shorter acting than Morphine due to resdistribution (c.f. Thiopental) Used with general anaesthetics Injectable anaesthetics - shorter generation of action

83
Q

Methadone

A

Long acting - used in addicts Used as a substitute for heroine Can be used as analgesic Less like to produce euphoric effects

84
Q

What is an example of partial agonist?

A

Buprenorphine

85
Q

Buprenorphine

A

Produce strong analgesia Limited respiratory depression Long duration of action Reduces heroin euphoria - it reduces Morphine euphoria

86
Q

What is an example of antagonist?

A

Naloxone Naltrexone

87
Q

Naloxone

A

Antagonist at all 3 receptor subtypes Diagnose and reverse opiate overdose Short half life give repeatedly Danger or precipitating withdrawal in addicts Experimental tool Little effect on pain Causes hyperalgesia

88
Q

Naltrexone

A

Longer duration of action

89
Q

What is noradrenaline used in?

A

Treat certain pain conditions

90
Q

What does neuropathic pain conditions cause?

A

Significant nerve damage

91
Q

How do you modulate the effect of central noradrenaline ?

A

Use of tricyclic antidepressant (amitriptyline)

92
Q

What are anticonvulsant that inhibit calcium channel opening?

A

Gabapentin Carbamazepine

Biomedical Pharmacology (19 decks)

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