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BMSC2223 Neuropharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

What is the difference between opioids and opiates?

A

Opioids have a morphine-like effect

Opiates have a morphine-like structure

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2
Q

What are the three types of endogenous opioid peptides?

A

Enkephalins
Endorphins
Dynorphins

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3
Q

Describe the synthetic pathway for enkephalins

A

Preproenkephalin
Proenkephalin
Met-enkephalin or Leu-enkephalin

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4
Q

Describe the synthetic pathway for endorphins

A

Preproopiomelanocortin
Proopiomelanocortin
Beta-endorphin

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5
Q

Describe the synthetic pathway for dynoprhins

A

Preprodynorphin
Prodynorphin
Dynorphin

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6
Q

What are the four opioid receptors?

A

Mu
Delta
Kappa
Opioid like receptor

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7
Q

Which systems do opioids act on?

A

Central nervous system
Respiratory system
Gastrointestinal system

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8
Q

What is the action of opioids on the central nervous system?

A

Reduces pain and distress

Induces euphoria

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9
Q

What occurs when opioid receptors are activated?

A

Activation of potassium channels causing hyperpolarisation on the postsynaptic knob
Inhibition of voltage gated calcium channels inhibiting synaptic transmission.

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10
Q

Which nerves do opioids affect?

A

Descending pain pathway

Peripheral nerves

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11
Q

Which regions do opioids have a stimulatory effect on?

A

Nucleus reticularis paragigantocellularis

Periaquaductal grey matter

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12
Q

Which regions do opioids have an inhibitory effect on?

A

Dorsal horn and nociceptive afferents

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13
Q

How do opioids stimulate action in the descending pathway?

A

Inhibition of inhibitory interneurones halting nociceptive transmission

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14
Q

How do opioids reduce the affective component of pain?

A

Action in the limbic system

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15
Q

What are the adverse effects of opioids?

A 
Euphoria
Respiratory depression
Cough reflex inhibition
Nausea and vomiting
Pupil constriction
Decreased gut motility
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16
Q

Which receptors induce euphoria? How can this be counteracted?

A

Mu receptors

Can be counteracted by kappa receptor activation

17
Q

What causes opioid induced- respiratory depression?

A

Mu receptors decreasing sensitivity of respiratory centres on carbon dioxide

18
Q

What effects of opioids are subject to tolerance?

A

Analgesia
Euphoria
Respiratory depression

19
Q

What may cause tolerance?

A

Downregulation of opioid receptors
Uncoupling of receptor from effector proteins
Changes to the effector proteins

20
Q

What causes withdrawal?

A

The opioid causes decrease in cAMP, so adenylate cyclase concentration increases to compensate
When the opioid is withdrawn, the cAMP levels spike so cellular signalling goes into overload

21
Q

Describe the beta arrestin pathway

A

The GPCR is phosphorylated
Beta arrestin binds to GPCR
GPCR is blocked from further signalling
Causes more opioid required for an effect due to less available GPCRs

22
Q

What may influence dependence on opioids?

A

Desire for the drug
Unwillingness to go through withdrawal
Craving euphoria

23
Q

Describe the properties of codeine

A

Much less potent than morphine
Antitussive in subanalgesic dose
Often given in combination with NSAIDs

24
Q

Describe the properties of diamorphine

A

More potent than morphine
More permeable to the blood brain barrier
Much shorter duration of action

25
Q

Describe the properties of pethidine

A

Similar properties to morphine
Causes restlessness
Antimuscarinic
Short duration of action

26
Q

Describe the properties of fentanyl

A

100x more potent than morphine

Fast pharmacokinetics

27
Q

Describe the properties of benzomorphanes

A

Kappa agonist, mu and delta antagonists
Similar to morphine at low doses
Causes hypertension, dysphoria, nightmares and hallucinations at high doses

28
Q

Give an example of a benzomorphane

A

Pentazocine

Cyclazocine

29
Q

Describe the properties of tramadol

A

Weak agonist of mu receptors
Also SNRI properties
Non-addictive

30
Q

Describe the properties of methadone

A

Slow pharmacokinetics

Oral administration rather than IV

31
Q

Why is methadone used to treat addiction

A

It doesn’t result in a drug high but also doesn’t allow for withdrawal due to the slow pharmacokinetics

32
Q

Describe the properties of loperamide and what it treats

A

Poor blood brain barrier permeability
Acts on enteric nervous system
Treats diarrhoea

33
Q

Describe the mechanism of nalaxone and what it treats

A

Competitive antagonist for opioid receptors

Reverses coma and respiratory depression

BMSC2223 Neuropharmacology (6 decks)

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