Pain, nociception and analgesia 3 Flashcards

1
Q

How do analgesics work?

A

They reduce peripheral nociception and sensitisation, they increase descending inhibition of nociception and reduce primary afferent nociceptive transmission and/or central sensitisation.

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2
Q

What does NSAIDS stand for?

A

Non-steroidal anti-inflammatory drugs.

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3
Q

What is used to treat mild pain?

A

Non-opiod NSAIDS, ibuprofen, paracetamol and aspirin.

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4
Q

What is used to treat persisting moderate pain?

A

Low-potency opioids such as codeine, tramadol and buprenorphine.

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5
Q

What is used to treat persisting severe pain?

A

High potency-opiods such as morphine, fentanyl and oxycodone.

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6
Q

What are two opiate drugs?

A

Morphine and heroin.

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7
Q

What are the differences between opiates and synthetic opioids?

A

Opiates are naturally derived from opium whereas synthetic opioids are drugs that bind to opioid receptors.

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8
Q

Give examples of opiates.

A

Morphine and codeine.

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9
Q

Give some examples of synthetic opioids.

A

Heroin, oxycodone, methadone, pethidine, fentanyl, buprenorphine, butorphanol.

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10
Q

What are some unwanted effects of opioids?

A

Respiratory depression, pupil constriction, reduced gastrointestinal motility, sedation, physical dependence and catatonia.

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11
Q

What receptors do strong opiates affect?

A

Mu, delta and kappa.

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12
Q

What are some strong opiates?

A

Morphine, methadone and fentanyl.

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13
Q

What are some weak opiates?

A

Codeine and buprenorphine.

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14
Q

Why is tolerance an issue with opioid drugs?

A

Continued use requires increased doses for an equivalent effect.

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15
Q

What are the different forms of administration of opiates?

A

Pills, intravenous injections, epidural, transfermal patch and lollipop.

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16
Q

What opiates are taken in pills?

A

Morphine and codeine.

17
Q

What opiates are intravenously injected?

A

Morphine, diamorphine and fentanyl.

18
Q

What opiates are taken epidurally?

A

Fentanyl and pethidine

19
Q

What opiates can be taken using a transdermal patch?

A

Fentanyl.

20
Q

What opiates can be taken in a lollipop form?

A

Fentanyl.

21
Q

What are the properties of NSAIDS?

A

Analgesic, anti-inflammatory, anti-pyretic, all the effects are related to decreased prostaglandin synthesis.

22
Q

What are NSAIDs inhibitors of?

A

COX inhibitors.

23
Q

What are some of the disadvantages of NSAIDS?

A

Skin reactions, severe gastric irritation, nausea, vomiting, kidney disorders, cardiovascular effects, bronchospam.

24
Q

What supraspinal effects does morphine have?

A

Pre and postsynaptic reduction of GABA inhibition, increased excitatory output, increased activity of 5HT neurones, increased output from 5HT neurons and increased 5HT inhibition of second order neurons.

25
Q

What spinal analgesic effects does morphine have?

A

Decreased release of glutamate at primary afferent synapses, reduced action potential in primary afferent neurons and direct inhibition of second order afferent neurons.

26
Q

What peripheral analgesic effects does morphine have?

A

Decreased excitability of nociceptor terminals and decreased Ca2+ signalling in nociceptor terminals.

27
Q

What is the most widely used analgesic agent?

A

NSAIDs.

28
Q

Give some examples of NSAIDs.

A

Aspirin, ibuprofen, diclofenac, paracetamol.

29
Q

What pathway does NSAIDs affect?

A

They prevent prostaglandin being synthesised so the prostanoid receptor cannot be activated. This is due to the effect of COX being inhibited - cyclo-oxygenase1/2. The proastanoid receptor is involved in modulation at nociceptors.

30
Q

What effect do prostaglandins have?

A

They do not cause pain themselves but they sensitive bradykinins to increase nociception ?? i think ?? They block potassium efflux, making them more sensitive.

31
Q

Why do NSAIDs have a lot of adverse effects?

A

Both COX-1 and COX-2 are blocked.

32
Q

How can kidney disorders arise with NSAIDs?

A

Paracetamol overdose.

33
Q

What are some specific COX-2 inhibitors?

A

Rofecoxib and celecoxib.

34
Q

What are the benefits of specific COX-2 inhibitors?

A

There are less side effects, but there are cardiovascular complications.

35
Q

What are other analgesic approaches?

A

Tricyclic antidepressants, antiepileptic drugs, glutamate receptor blockers, neurokinin receptor blockers, cannabinoid receptor agonists, vanilloid receptor blockers.

36
Q

How do tricyclic antidepressants and antiepileptic drugs work to treat analgesia?

A

Na/Ca channel blockade - reduce primary afferent transmission.

37
Q

How do glutamate and neurokinin receptor blockers treat analgesia?

A

They block primary afferent transmission but have severe central side effects such as psychosis.

38
Q

How can cannabinoid receptor agonists be used for analgesia?

A

They have central and peripheral nociceptor effects that can be used for neuropathic pain such as MS.

39
Q

How do vanilloid receptor blockers act to treat analgesia?

A

ATP receptor blocker - they block the detection of peripheral noxious signals.