Pharmacology of analgesics Flashcards

1
Q

What is the action of NSAIDs?

A

act at the site of injury

block the synthesis of prostaglandins - which decreases sensitivity of nociceptors

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2
Q

What is the action of local anaesthetics?

A

supress nerve conduction by blocking/inactivating voltage activated sodium channels

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3
Q

What is the action of opioids?

A

supress the synaptic transmission of nociceptive signals in the dorsal horn of the spinal cord

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4
Q

What is the action of gabapentin and pregabalin?

A

target ion channels that are upregulated in nerve damage

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5
Q

What is rung 3 of the WHO analgesic ladder?

A

strong opioids - morphine (gold standard), oxycodone, heroin, fentanyl, hydromorphone

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6
Q

What is rung 2 of the WHO analgesic ladder?

A

weak opioids - codeine, tramadol, dextropropoxyphene

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7
Q

What is rung 1 of the WHO analgesic ladder?

A

NSAIDs or Paracetemol

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8
Q

What are the possible combinations of the WHO analgesic ladder?

A

3 + 1
2 + 1
NOT 3 + 2 AS THEY ACT ON THE SAME RECEPTORS

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9
Q

What is supraspinal anticociception?

A

efferent regulation of pain - decending pathway from the brainstem

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10
Q

What are the important regions of the brain that are involved in pain perception and emotion and project to specific brainstem nuclei?

A

the periaqueductal gray - PAG
locus cereleus - LC
nucleus raphe Magnus - NRM

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11
Q

Where is the PAG found?

A

midbrain

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12
Q

Where is the LC found?

A

pons

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13
Q

Where is the NRM found?

A

medulla

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14
Q

What is the process of supraspinal antinociception?

A

PAG is excited by electrical stimulation or opioids
activated PAG neurones project into the NRM cause release of 5-HT and enkephalins
The serogenrgic and enkephalinergic neurones projecting into the dorsal horn excite the LC which releases Na
all of these substances inhibit nociceptive transmission in the dorsal horn of the spinal cord

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15
Q

What are enkephalins?

A

endogenous opioid - occurs naturally

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16
Q

What is the best opioid to use for chronic pain?

A

morphine

17
Q

What is the best opioid to use for rapid IV administration?

A

diamorphine

18
Q

What opioid is only given orally?

A

codine

19
Q

What opioid should not be given with MAO inhibitors - why?

A

Pethidine

overexcites the CNS

20
Q

What opiods are agonists?

A
Morphine
Diamorphine
Codine
Fentanyl
Pethidine
Tramadol 
Methadone
Etorpine
21
Q

What opioids are antagonists?

A

Nalaxone
Naltrexone
Alvimopan
Methylnaltrexone

22
Q

What opioid must be avoided in epileptic patients?

A

Tramadol

23
Q

What opioid has a long half life so can be used to help with withdrawl from strong opioids?

A

Methadone

24
Q

What is Nalaxone used for?

A

to reverse toxicity of opioid overdose

25
Q

What are opioid side effects?

A

apnoea - RESPIRATORY DEPRESSION
addiction - due to short half life
orthostatic hypotension - reduced sympathetic tone
nausea/vomiting/constipation

26
Q

What is a specific side effect of morphine?

A

mast cell degranulation

27
Q

What do NSAIDs inhibit?

A

COX1 and COX2

28
Q

What is a long term side effect of NSAID use?

A

produce GI damage - as PGE2 produced by COX2 protects the stomach environment

29
Q

What conditions does neuropathic pain happen in?

A

trigeminal neuralgia
diabetic neuropathy
post herpetic neuralgia
phantom limb pain

30
Q

What can be used to treat neuropathic pain?

A

Gabapentin and pregabalin
Amitryptyline
Carbamazepine

31
Q

What is the action of Gabapentin and pregabalin in neuropathic pain?

A

reduce the expression of voltage activated Ca channels - which are upregulated in damaged sensory neurons - causing a decrease in neurotransmitters

32
Q

What is gabapentin especially used for?

A

migraines

33
Q

What is pregabalin especially used for?

A

diabetic neuropathy

34
Q

What is the action of Amitryptiline?

A

decrease uptake of noradrenaline

35
Q

What is the action of Carbamazepeine?

A

blocks voltage activated Na channels that are upregulated in damaged nerve cells

36
Q

What is Carbamazepeine used for?

A

trigeminal neuralgia