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*5. Neuro > Pharmacology: analgesics - opioids > Flashcards

Pharmacology: analgesics - opioids Flashcards

1
Q

3 types of pain?

A

Nociceptive pain, neuropathic pain, neuroplastic pain

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2
Q

Describe the three types of pain - nociceptive, neuropathic, neuroplastic

A
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3
Q

Nociceptive pain
- Noxious stimuli can lead to the release of which chemicals?
- These chemical bind to sensory fibres (C fibres), and travel to the brain
- Role of higher centres in regulating pain?

A
  • Descending inhibitory pathways can modulate pain signals
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4
Q

7 examples of analgesics?

A

Opioids
Paracetamol
NSAIDs

Antiepileptics
Anti depressants
Cannabinoids
Capsaicin

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5
Q

How might antidepressants treat pain?
Opioids, paracetamol and NSAIDs are good at treating what type of pain?
Wherease antidepressants and antiepileptics are good at treathing which type of pain?

A

Impact serotonin
Nociceptive pain
Neuropathic pain

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6
Q

OPIOIDS
MOA
- They act on ______ receptors in the ______ and ______ _____.
- They are agonists/antagonists for these receptors
- What are the three types of opioid receptors?
- Activation of which of these receptors produce the strongest analgesic effect?

A

Opioid receptors in the brain and spinal cord
Agonists
μ (mu), δ (delta), and κ (kappa)
mu

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7
Q

OPIOIDS
MOA
Mu opioid receptor
- What kind of receptor is it?
- Impacts of activating it (presynaptic and postsynaptic?)
- Overall impacts of this?

A

GPCR

Presynaptic: reduces cAMP, PKA activity, calcium ion influx/availability, NT release.
Postsynaptic: enhances potassium efflux to hyperpolarise the postsynaptic membrane

Reduced nociceptive signalling

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8
Q

OPIOIDS
MOA
Mu receptor
- Activation of mu receptors produces the strongest analgesic effect, however, it’s more likely to result in which 2 ADRs?

A

Respiratory depression
Physical dependence

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9
Q

OPIOIDS
MOA
- In addition to reducing the excitation and transmission of neurons, what is the other mechanism through which opioids work?

A

Activates descending inhibitory pathways (mainly via serotonin)

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10
Q

OPIOIDS
Indications?

A

Moderate-severe (acute) pain
Cough suppressant
Anti-diarrhoeal

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11
Q

OPIOIDS
Are they meant for acute or chronic pain? Why?

A

Acute - evidence shows they’re effective in treating acute pain

Not chronic - evidence doesn’t show superiority to placebo; and have ADRs

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12
Q

What are the traditional opioids?
What are the synthetic opioids?

A

Traditional
- Morphine
- Heroine
- Codeine

Synthetic
- Oxycodone
- Fentanyl
- Tramadol
- Methadone
- Buprenorphine
- Tapentadol

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13
Q

Morphine
- 2 formulations?

A

Oral (fast and slow release)
Injection (more reliable bioavailability)

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14
Q

Heroin (diamorphine)
- Describe its chemical structure, and how does it lead to its function?

A

2x morphine molecules
Makes it lipid soluble –> crosses the BBB more easily –> quicker euphoria

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15
Q

Codeine
- Relationship to morphine?

A

The pro drug of morphine
Hepatic metabolism converts 10% of codeine to morphine (hence, codeine is 10x less potent than morphine)

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16
Q

Oxycodone
- Is it very popular?
- Does it have a shorter or longer half life than morphine?
- Does it have both slow and quick release formulations?

A

Yes
Longer
Yes

17
Q

Fentanyl
- Formulations
- Is it very potent, and is it very restricted?

A

Lozenges, patches, injectables
Yes

18
Q

Tramadol
- Is it a typical or atypical opioid?
- Does it have a short or long half life?

A

Atypical
Short

19
Q

Tramadol
- Why is it called a “dirty drug”?
- Hence, is it often used?

A
20
Q

2 opioids used for opioid replacement (harm reduction?)

A

Methadone
Buprenorphine

21
Q

Methadone
- Is it a weak or strong agonist?
- Is it short or long lasting?

A

Weak
Long lasting

22
Q

Buprenorphine
- Is it an atypical opioid?
- Is it a partial or full agonist?
- Does it have a short or long half life?
- Formulations?
- Effect on respiratory depression?

A

Atypical
Partial agonist
Long half life
Oral film that sticks to the oral mucosa, patches
Has a ceiling effect on respiratory depression (can increase the dose, but resp depression doesn’t continue to increase)

23
Q

Tapentadol
- Is it a typical or atypical opioid/
- MOA?
- What types of pain is it good for?

A

Atypical
Opioid agonist + NA reuptake inhibitor (antidepressant effects)
Nociceptive and/or neuropathic pain

24
Q

CNS ADRs?

A

Physical dependence (especially with chronic use)
Respiratory depression
Dysphoria (often with high dose chronic use)
Sedation
Pupil constriction

25
Q

GI ADRs?

A

Nausea and vomiting
Constipation

26
Q

OPIOIDS
Clinical considerations
- Tolerance: what is the physiological basis of this?

A

Desensitisation and internalisation of opioid receptors –> need to increase the dose to achieve the previous level of effects

27
Q

OPIOIDS
Clinical considerations
- Withdrawal: what is it? What side effects occur?

A

Occurs when you don’t take the drug?
Irritability, weightloss, GI, body shakes

28
Q

OPIOIDS
Clinical considerations
- Dependence: what is it?

A

Psychological dependence - due to activation of the dopaminergic mesolimbic reward system

29
Q

OPIOIDS
What is the opioid receptor antagonist?

A

Naloxone

30
Q

OPIOIDS
Naloxone
- How can it treat opioid overdose?

A

Binds to opioid receptor to displace opioid agonist –> overcome respiratory depression

31
Q

OPIOIDS
Naloxone
- Formulations?

A

Injection, nasal spray

32
Q

OPIOIDS
Naloxone
- Why is the naloxone + oxycodone tablet combination used?

A

When swallowed whole, naloxone doesn’t work - oxycodone works on its own
When crushed and injected, naloxone antagonises oxycodone - don’t get the high.

33
Q

OPIOIDS
Naloxone
- ADR?

A

May induce acute withdrawal symptoms

34
Q

OPIOIDS
2 ways of cutting down?

A

Switching opioid drug
Tapering dose of current opioid

35
Q

OPIOIDS
Switching between opioids
- Define: cross tolerance
- Is there cross tolerance between opioid drugs?
- Implications for dosages when switching?

A

Cross tolerance: take one type of drug and become tolerant to it; when you try a new type of drug, you’ll also be tolerant to it
Not 100%
Don’t give same dose - give 50-75%

*5. Neuro (29 decks)

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