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Biomedical Pharmacology > Lecture 15 - Analgesics > Flashcards

Lecture 15 - Analgesics Flashcards

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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
What does bradykinin Upon inflammatory response act and do?
Act via its own GPCR and increase levels of protein kinase C and phosphorylate the receptor
26
What does bradykinin do?
Modulate the responsiveness of TRP receptor in a positive way
27
What else modulates TRP?
Tyrosine kinase receptor
28
What does prostaglandin do?
Sensitize nociceptive nerve endings by enhancing pain-producing effect of other agents
29
What activates TRPV1?
Capsaicin Temperature and acidity
30
What is the role of nociception?
Cause subsequent peptide release
31
What does ATP act on to modulate nociceptive Information?
Purinergic receptors
32
What are the 3 isoforms that the cyclooxygenase exhibit?
Cox-1, Cox-2 and Cox-3
33
What are prostaglandin?
General inflammatory mediator
34
What can NSAID be?
Non-selective: Aspirin, ibuprofen, Diclofenac Selective: croxibs (Rofecoxib)(COx-2),paracetamol
35
What does ibuprofen and diclofenac produce?
Cardiovascular side effects
36
Where does paracetamol have an effect upon?
COX-3 and effects on prostaglandin seen in CNS only
37
What increases the descending modulation?
Endogenous opioids
38
What nerve fibres are involved in descending inhibition?
A delta fibres - small diameter/ myelinated C fibres - unmyelinated
39
What evidence has been provided in ascending and descending modulation Upon nature of pain?
Alteration and population of Na+ and K+ - affect speed of transmission and whether there is increase in sensitivity to nociceptive input
40
What is pain associated with?
Activity of small diameter afferent fibres which have sensory ending in the peripheral tissues
41
What does afferent fibers innervate?
Cells in the dorsal horn which give rise to projection pathways to the thalamus
42
What does thalamus in term of function allow?
Sorting of Information
43
What is lamina II (substantial gelatinosa) rich in?
Opioid receptors
44
What does the descending inhibitory pathway reduce ?
Transmission of pain
45
Apart from being rich in opioid receptors what does periaqueductal gray matter do?
Central to pain processing and if stimulated electrically can reproduce analgesia
46
What is enkephalins responsible for?
Modulation of pain transmission Subjected feelings of highs and lows
47
What are are examples of Enkephalins?
Pentapeptides Leu-enkephalins and Met-enkephalins Endogenous ligands and micro and delta receptors
48
Where are enkephalins distributed and produced?
Widely distributed in CNS and synthesised in cell body Processed during axonal transport
49
What are some examples of Endorphins and Dynorphins?
B-endorphin and dynorphin A
50
What are the 4 classical receptor classification?
Mu, delta, kappa and ORL1 Type
51
Which opioid receptor have been discounted?
Sigma receptors
52
Which receptor brings about an analgesic effect?
Mu
53
What are opioids known to reduce?
Significant respiratory depression
54
What are Morphine?
Alkaloid extracted from opium Opiate and dried exudate from seed case of poppy
55
What are the actions of Morphine?
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
What are side effects of Morphine?
If used in analgesic/ drug abuse it can produce sustained constipation Gall bladder conditions
57
What drug is effective in causing cough suppression ?
Codeine
58
What happens when mu receptors are stimulated?
Reduction in CAMP generation
59
Codeine
3-O-methyl Morphine Opiate Metabolised to Morphine. (CYP2D6) Used with NSAIDS
60
DiaMorphine (heroin)
Effectively a pro drug and a semi-synthetic. Better oral absorption than morphine Terminally ill patients
61
Where does paracetamol have an effect upon?
COX-3 and effects on prostaglandin seen in CNS only
62
What increases the descending modulation?
Endogenous opioids
63
What nerve fibres are involved in descending inhibition?
A delta fibres - small diameter/ myelinated C fibres - unmyelinated
64
What evidence has been provided in ascending and descending modulation Upon nature of pain?
Alteration and population of Na+ and K+ - affect speed of transmission and whether there is increase in sensitivity to nociceptive input
65
What is pain associated with?
Activity of small diameter afferent fibres which have sensory ending in the peripheral tissues
66
What does afferent fibers innervate?
Cells in the dorsal horn which give rise to projection pathways to the thalamus
67
What does thalamus in term of function allow?
Sorting of Information
68
What is lamina II (substantial gelatinosa) rich in?
Opioid receptors
69
What does the descending inhibitory pathway reduce ?
Transmission of pain
70
Apart from being rich in opioid receptors what does periaqueductal gray matter do?
Central to pain processing and if stimulated electrically can reproduce analgesia
71
What is enkephalins responsible for?
Modulation of pain transmission Subjected feelings of highs and lows
72
What are are examples of Enkephalins?
Pentapeptides Leu-enkephalins and Met-enkephalins Endogenous ligands and micro and delta receptors
73
Where are enkephalins distributed and produced?
Widely distributed in CNS and synthesised in cell body Processed during axonal transport
74
What are some examples of Endorphins and Dynorphins?
B-endorphin and dynorphin A
75
What are the 4 classical receptor classification?
Mu, delta, kappa and ORL1 Type
76
Which opioid receptor have been discounted?
Sigma receptors
77
Which receptor brings about an analgesic effect?
Mu
78
What are opioids known to reduce?
Significant respiratory depression
79
What are Morphine?
Alkaloid extracted from opium Opiate and dried exudate from seed case of poppy
80
What are the actions of Morphine?
Analgesic, Antidiarrhoeal and Antitussive
81
Pethidine
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
Fentanyl
Shorter acting than Morphine due to resdistribution (c.f. Thiopental) Used with general anaesthetics Injectable anaesthetics - shorter generation of action
83
Methadone
Long acting - used in addicts Used as a substitute for heroine Can be used as analgesic Less like to produce euphoric effects
84
What is an example of partial agonist?
Buprenorphine
85
Buprenorphine
Produce strong analgesia Limited respiratory depression Long duration of action Reduces heroin euphoria - it reduces Morphine euphoria
86
What is an example of antagonist?
Naloxone Naltrexone
87
Naloxone
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
Naltrexone
Longer duration of action
89
What is noradrenaline used in?
Treat certain pain conditions
90
What does neuropathic pain conditions cause?
Significant nerve damage
91
How do you modulate the effect of central noradrenaline ?
Use of tricyclic antidepressant (amitriptyline)
92
What are anticonvulsant that inhibit calcium channel opening?
Gabapentin Carbamazepine

Biomedical Pharmacology (19 decks)

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