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PHAR 211 > Analgesics > Flashcards

Analgesics Flashcards

1
Q

What are the 4 opioid receptor types?

A
  1. Mu
  2. Kappa
  3. Delta
  4. NOP (nociceptin)
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2
Q

What type of receptor are opioid receptors?

A

All of these receptors are Gai/o-coupled, which means that binding of agonist decreases cAMP and inhibits inwardly rectifying K+ channels.

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3
Q

Where do opioids inhibit? (2)

A
  1. Inhibit the release of nociceptive signals peripherally and centrally
  2. Complimentary control with other mechanisms & receptor systems
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4
Q

What are the 4 most common endogenous opioids?

A
  1. Enkephalin
  2. Dynorphin
  3. Substance P
  4. Endorphin
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5
Q

What are endogenous opioids? (3)

A
  1. Short peptide molecules
  2. Coded on genes as “pre-pro” peptides and subject to post-translational modifications
  3. Released from synaptic vesicles
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6
Q

What are exogenous opioids? (2)

A
  1. Aminoalkylindole compounds naturally occurring in nature and synthesized de novo
  2. Drugs and pro-drugs with variable PD and PK depending on drug and excipients
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7
Q

How does acetaminophen work? (3)

A
  1. CNS-selective cyclooxygenase inhibitor
  2. Anandamide reuptake inhibitor (boosts endocannabinoid levels)
  3. TRPV1 agonist
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8
Q

How is acetaminophen metabolized?

A

Via CYP2E1, 3A4; UGTs

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9
Q

What distinguishes endogenous opioids from exogenous opioid drugs?

A

Endogenous opioids are peptides

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10
Q

Opioids and cannabinoids both do what same thing to limit pain perception?

A

Both inhibit neurotransmitter release from the pre-synaptic neuron

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11
Q

How are NSAIDs metabolized?

A

Undergo Phase I metabolism (CYP2C9, 2D6) and are excreted in urine

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12
Q

What are the major effects of mu receptors? (5)

A
  1. Analgesia
  2. Respiratory depression
  3. Sedation
  4. Euphoria
  5. Constipation
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13
Q

What is the main polymorphism seen in mu receptors? What does that lead to?

A
  1. 118 AΔG
  2. Lower analgesic response - greater consumption
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14
Q

What are the major effects of the kappa receptors? (4)

A
  1. Spinal analgesia
  2. Respiratory depression
  3. Sedation
  4. Dysphoria
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15
Q

What is the main polymorphism seen in kappa receptors? What does that lead to?

A

36 GΔT correlated with addictive potential and abuse liability

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16
Q

What are the major effects of delta receptors? (2)

A
  1. Dysphoria
  2. Psychomimetic
17
Q

What is the main polymorphism seen in delta receptors? What does that lead to?

A

2 major SNPs, no effect

18
Q

Explain gene polymorphism in the PTSG gene when it comes to NSAID efficacy. (3)

A
  1. Subjects homozygous GG for PTGS2 SNP2 demonstrated a better response to analgesic effect of rofecoxib compared with ibuprofen administration.
  2. Subjects identified as GC or CC for PTGS2 SNP2 demonstrated a better response to ibuprofen.
  3. PTGS2 polymorphisms influence the expression of PTGS1 and PTGS2 and consequently analgesic effect of NSAIDs.
19
Q

What is a poor metabolizer (PM) defined as?

A

At least 2 loss of function alleles

20
Q

What is an ultra metabolizer (UM) defined as?

A

At least 3 copies of functional alleles

21
Q

Polymorphisms that reduce metabolism may lead to what?

A

High drug concentration and reduced safety

22
Q

Polymorphisms that enhance drug metabolism may lead to what?

A

Will reduce drug efficacy and may be misconstrued as drug-seeking behaviour

23
Q

If drugs are pro-drugs or metabolism produces an active compound, then polymorphisms that increase metabolism will do what?

A

Will increase drug efficacy and ADRS and reduce safety

24
Q

If an individual is a CYP2D6 poor metabolizer they will take codeiene and experience:
a) Greater analgesia than a NM
b) Less analgesia than an NM
c) The same amount of analgesia compared to an NM
d) Far more constipation but no change in analgesia compared to an NM

A

b)

25
Q

If an individual is a CYP2E1 ultrametabolizer for acetaminophen, they are likely to experience?

A

Hepatotoxicity

26
Q

138 patients who underwent open abdominal surgery
received continuous epidural analgesia with fentanyl or
morphine. The distribution of the OPRM1 genotypes for
the 118 A>G SNP was:
1. 41 (29.7%) for AA (normal MOR)
2. 70 (50.7%) for AG (less-functional MOR)
3. 27 (19.6%) for GG (poorly-functional MOR)
What was the result for these patients?

A

The 24-hour postoperative opioid dose requirement was significantly higher in patients with the GG genotype compared to patients with the AG and the AA genotype for the OPRM1 (p <0.05)

27
Q

Pain management is critical in clinical practice because uncontrolled pain can: (5)

A
  1. Delay healing,
  2. Decrease appetite,
  3. Introduce and augment stress,
  4. Disturb sleep,
  5. Lead to anxiety and depression
28
Q

True or False? Personalization of opioid therapy is very common

A

False - not widely practiced

29
Q

What are the 2 drugs and enzymes that are listed as ‘actionable’ when it comes to PK variability?

A
  1. Codeine and CYP2D6
  2. Tramadol and CYP2D6
30
Q

What is the drug and enzyme that is listed as ‘moderately actionable’ when it comes to PK variability?

A

Morphine and OPRM1

31
Q

What are the 4 drugs and enzymes that are listed as ‘further research needed’ when it comes to PK variability?

A
  1. Oxycodone and CYP2D6
  2. Hydromorphone and CYP2D6
  3. Fentanyl and OPRM1
  4. Methadone
32
Q

True or False? It is not practical at this time to test every patient for whom codeine is prescribed

A

True

33
Q

Two patients – both of whom have a history of narcotics use – are prescribed opioid-based medicines to manage their post-surgical in-hospital pain:
- Patient 1 is prescribed fentanyl and they are found to be a CYP3A4 UM.
- Patient 2 is prescribed codeine and they are found to be a CYP2D6 PM.
During follow-up both patients complain that they are not receiving any benefit from their opioids and request a higher dose. You are concerned this is a drug seeking behaviour, but how else might their actions be explained?

A
  1. Fentanyl is the active analgesic form. If ultra-metabolized then there is less of the active form so they will not experience analgesia. Could give them codeine.
  2. Patient 2 has the opposite problem and could be given fentanyl for example.

PHAR 211 (10 decks)

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