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SL22044 Neuroscience > Pain and analgesics 3 (analgesic drugs) > Flashcards

Pain and analgesics 3 (analgesic drugs) Flashcards

1
Q

What general process is boosted by analgesic drugs?

A

Descending inhibition of nociception

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2
Q

Which processes are inhibited by analgesic drugs?

A

Central sensitisation and peripheral sensitisation

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3
Q

How do nonsteroidal anti-inflammatories cause analgesia?

A

They inhibit the process of peripheral sensitisation

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4
Q

How do opioid analgesics cause analgesia?

A

Boost the descending inhibition of nociception

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5
Q

What do opioids mimic in order to have their analgesic effect?

A

Endogenous opioid agonists

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6
Q

Where do opioids act?

A

On opioid receptors

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7
Q

Examples of opioids?

A

Morphine, heroin, fentanyl, codeine

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8
Q

What are some low potency opioids?

A

Codeine, pethidine, buprenorphine

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9
Q

What is etorphine used for?

A

Veterinary medicine–> large animals

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10
Q

What is naloxone?

A

An opioid receptor antagonist

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11
Q

How does naloxone work?

A

It is a opioid mew delta and kappa antagonist

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12
Q

Which drugs are used for mild pain?

A

NSAIDs (nonsteroidal anti inflammatories)

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13
Q

Examples of NSAIDs?

A

Aspirin, ibuprofen

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14
Q

What are opioids given to people in moderate pain?

A

Codeine, buprenorphine

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15
Q

What are some opioids given to people in severe pain?

A

Morphine, fentanyl

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16
Q

How do the opioid receptors on free nerve endings have an inhibitory effect?

A

When an agonist binds K+ channels open and allow K+ to leave the cell–> hyperpolarisation

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17
Q

Where are supraspinal opioid receptors?

A

PAG and locus coeruleus

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18
Q

Which type of opioid receptor do most analgesics target?

A

Mu

19
Q

Which opioid receptor do morphine, methadone and fentanyl target?

A

Mu

20
Q

Can morphine and fentanyl also target delta and kappa receptors?

A

Yes

21
Q

Main issue with mu opioid receptors?

A

When agonised they can cause respiratory depression

22
Q

Benefit of targeting delta and kappa receptors over mu?

A

They do not cause respiratory depression when agonsied

23
Q

Mood effect of mu receptor being agonised?

A

Euphoria

24
Q

Mood effect of kappa receptor being agonised?

A

dysphoria

24
Q

Effect of kappa receptors being agonised on bodily waste?

A

Diuresis

25
Q

Mood effect of delta receptor being agonised?

A

none

26
Q

Main issue with agonising delta opioid receptors?

A

Proconvulsant

27
Q

Undesirable effects of mu opioid receptor?

A

Constipation, sedation, nausea and vomiting, itching

28
Q

Why does mu opioid receptor agonists being activated cause constipation?

A

They activate mu opioid receptors in the gut

29
Q

Why can methylnaltrexone be taken to prevent constipation but not the analgesic effect of opioids targeting mu receptors?

A

It cant cross the blood brain barrier meaning it can block the opioid receptors in the gut (so no constipation) but cant access the locus coeruleus or PAG

30
Q

What is psychological dependance?

A

Addiction

31
Q

What is physical dependance?

A

When someone stops taking a drug and they have physical withdrawal symptoms

32
Q

Result of increasing potency of mu receptor agonist on side effects?

A

They increase

33
Q

What changes need to be made to the dose of a drug if continued use occurs?

A

The dosage will need to increase

34
Q

What is the main active ingredient in an opium poppy?

A

morphine

35
Q

Main structural difference between morphine and heroin?

A

Heroin has two acetyl groups where morphine has two OH groups

36
Q

What benefit does having two acetyl groups instead of two OH groups give heroin over morphine?

A

It crosses the blood brain barrier more easily

37
Q

What drawback is there of having two acetyl groups instead of two OH in heroin compared to morphine?

A

Makes heroin completely ineffective against the mu opioid receptor (heroin itself is not an opioid receptor agonist)

38
Q

Why does heroin not having the correct structure to be a mu opioid receptor agonist not really matter?

A

There are many enzymes in the brain which can cleave the acetyl groups off

39
Q

What is a pro-drug?

A

A drug that has to be metabolised in order to be its active ingredient

40
Q

Which analgesics are taken in pill form?

A

Morphine, codeine

41
Q

Which analgesics are taken via intravenous injections?

A

morphine, diamorphine, fentalyl

42
Q
A

SL22044 Neuroscience (34 decks)

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