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PHAR 211 > Opioids > Flashcards

Opioids Flashcards

1
Q

How many Canadians report pain (both acute and chronic)?

A

More than 40% of Canadians report poorly managed pain

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2
Q

What is the definition of pain?

A

An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage

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3
Q

What are the four G-protein coupled opioid receptors found in the human body?

A
  • Mu
  • Kappa
  • Delta
  • Nociceptin
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4
Q

How do opioid receptors modify perception of pain?

A

These receptors are Gi or Go coupled proteins.

When an agonist binds to these proteins, cAMP decreases and Inwardly rectifying K+ channels are inhibited

“Calms down pain signals”

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5
Q

Where are the opiod receptors located?

A

Peripheral, spinal, and brain receptors

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6
Q

What are some examples of endogenous opiods?

A
  • Enkephalin
  • Dynorphin
  • Substance P
  • Endorphin
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7
Q

What are some characteristics of endogenous opioids?

A

They are short peptide molecules

Need to undergo some post-translational modifications and metabolic activity to become active

Released from synaptic vesicles

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8
Q

What is the biggest source country of pharmaceutical grade exogenous opioids?

A

Tasmania, an Australian state

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9
Q

Which opioids undergo both Phase I and II metabolism?

A
  • Codeine (Morphine–>Morphine-6-glucoronide)
  • Hydrocodone (Hydromorphone–>Hydromorphone-6-glucoronide or Norhydrocodone)
  • Oxycodone (Oxymorphone–>Inactive metabolites or Noroxycodone)
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10
Q

What opioids undergo Phase II metabolism only?

A

Morphine (Morphine-6-glucoronide)

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11
Q

What opioids undergo Phase I metabolism only?

A
  • Fentanyl (Norfentanyl)
  • Methadone (inactive metabolites
  • Tramadol (O-desmethyltramadol)
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12
Q

In general, how does Acetaminophen impart an analgesic effect?

A

It is a CNS-selective cyclooxygenase inhibitor

Anandamide reuptake inhibitor (boost endocannabinoid levels)

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13
Q

In general, how do NSAIDs impart an analgesic effect?

A
  • They are COX inhibitors (and subsequently inhibit prostaglandins, which are mediators of pain, inflammation, and fever
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14
Q

In general, how do cannabinoids impart an analgesic effect?

A

Activate CB1 (a G-protein coupled receptor involved in neurotransmission)

Once CB1 is activated by a cannibinoid, it inhibits release of neurotransmitter

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15
Q

What distinguishes endogenous opioids from exogenous opioid drugs?

A

Endogenous opioids are peptides

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16
Q

What is the common mechanism of action for pain relief with opioid and cannabinoids?

A

Both inhibit neurotransmitter release from the pre-synaptic neuron

17
Q

What is the definition of poor metabolizers?

A

At least 2 loss of function alleles

18
Q

What is the difference between normal and extensive metabolizers?

A

They are the same

19
Q

What is the definition of ultra metabolizers?

A

At least 3 copies of functional alleles

20
Q

What are the CYP gene polymorphisms?

A
  • SNP
  • Indels
  • Whole-gene
  • Duplication
  • CNVs
21
Q

For prodrugs or active metabolites, what is the impact of polymorphisms that increase metabolism?

A

Increase drug efficacy and ADRs = reduced safety

22
Q

For active drugs, what is the impact of polymorphisms that reduce metabolism?

A

High drug concentrations and reduced safety

23
Q

For active drugs, what is the impact of polymorphisms that enhance drug metabolism?

A

Reduced efficacy and can be misconstrued as drug-seeking behaviour

24
Q

If an individual is a CYP2D6 poor metabolizer, how is their response to codeine different from a normal metabolizer?

A

Less analgesia than NM

25
Q

If an individual is a CYP2E1 ultra metabolizer, what is their response to codeine?

A

Higher risk of hepatoxicity

26
Q

What drugs do we have guidelines for dose adjustment according to CYP polymorphisms?

A
  • Codeine and CYP2D6
  • Tramadol and CYP2D6
27
Q

What is the interaction between cannabinoids and opioids?

A

The PD effects likely synergistic

They act on nociceptive neurons and can saturate the same CYP enzymes

28
Q

What are the common CYP enzymes involved in opioid metabolism?

A

3A5

3A4

2D6

29
Q

What are the common CYP enzymes involved in cannabinoid metabolism?

A

3A4

2D6

2C9

30
Q

What are the common CYP enzymes involved in NSAID metabolism?

A

3A4

2D6

2C9

31
Q

What is the impact of uncontrolled pain on overall health?

A
  • Can delay healing
  • Decrease appetite
  • Introduce and augment stress
  • Disturb sleep
  • Lead to anxiety and depression
32
Q

What is the goal of pharmacogenomics in opioid therapy?

A
  • Optimize pain relief
  • Prevent adverse effects

Information about pharmacogenomics and clinical factors (age, weight, clearance, DIs) can help acheive personalized pain management

33
Q
A

PHAR 211 (18 decks)

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