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Pharmacology > Opioid Lecture part 1 > Flashcards

Opioid Lecture part 1 Flashcards

1
Q

General indications for Opiates

A
  1. Moderate to severe dental pain that cannot be managed effectively with NSAIDS
  2. Patients for whom NSAIDS are contraindicated
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2
Q

The word Opiates is used to describe what?

A

to describe substances from the white liquid extract derived from the seeds of poppy plant
- Alkaloids found in opium

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3
Q

Opioids can be classified in what 3 ways

A
  1. Mechanism of action (agonists, partial agonists, mixed opioids, antagonists
  2. Chemical structure
  3. Degree of efficacy that they produce
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4
Q

What is the mechanism of action for opioids?

A

They bind to receptors in both CNS and spinal cord. Produce ALTERED perception of pain reaction

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5
Q

How do opioids produce an analgesic effect?

A

Produced by midbrain stimulation due to activation of a pain-modulating circuit
- Projects via the medulla to the spinal cord dorsal horn
Descending pain-modulating circuit

***Opiates produce analgesia by direct action on the CNS

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6
Q

Analgesia system of opioids are mediated by what 3 major components

A
  1. Periaquaductal grey matter (midbrain)
  2. nucleus raphe magnus (medulla)
  3. pain inhibitory neurons (dorsal horns of the spinal cord)
  • These areas are the areas in which the chemical mechanisms of opioid analgesics will take place.
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7
Q

The pain suppression system involves what neurotransmitter and is mediated by what?

A

serotonin as neurotransmitter

- Partially enkephalin-mediated

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8
Q

What activates the pain suppression system pathway?

A
  1. Noxious stimuli
  2. Pain
  3. Psychological factors, including placebo responders
  4. Opioids
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9
Q

Endogenous Opioids act as what?

A

neurotransmitters

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10
Q

3 groups of endogenous substances with opioid-like action

A

endorphins
enkephalins
dynorphins

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11
Q

Endogenous opioids act through three different receptors

A
  1. mu
  2. delta
  3. kappa
  • G protein-coupled receptors
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12
Q

Descending pain-modulating circuit contains high concentrations of what peptides?

A

endogenous opioid peptides

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13
Q

Endogenous opioid peptides are produced where?

A

By the pituitary gland and hypothalamus

  • They are located in the CNS (mainly in limbic system and brainstem areas associated with pain reception)
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14
Q

Beta-Endorphin are expressed where via what receptor?

A

Expressed in cells in the arcuate nucleus of the hypothalamus and in the brainstem
- acts via mu: influences appetite, sexual behavior

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15
Q

Enkephalins are expressed where via what receptor?

A

widely distributed throughout the brain

- acts via mu and delta

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16
Q

Dynorphins are found where and act via what receptor?

A

Found in spinal cord and in many parts of the brain, including the hypothalamus
- acts via kappa

17
Q

Endorphins are derived from what precursor molecules

A
  1. Proenkephalin A - many endorphins
  2. Pro-opiomelanocortin (POMC) - B-endorphin
  3. Proenkephalin B (prodynorphin) - dynorphins
18
Q

Enodorphins are found where?

A

Found in gut (pancreatic islet cells), sympathetic nervous system, adrenal medullary chromatin cells, CNS

19
Q

Beta-endorphins are distributed where?

A

In the brain

20
Q

Endorphins are involved in what physiologic actions

A

Involved in blood pressure regulation, temperature regulation and food intake

21
Q

First isolated Enkephalins compounds

A
  1. Leucine-enkephalin

2. Methionine-enkephalin

22
Q

Do Enkephalins mimic opiate activity? Are they strong or weak analgesics?

A

Mimic opiate activity = weak analgesics

23
Q

What endogenous opioid may be responsible for producing analgesia in placebo responders and acupuncture?

A

Enkephalins

24
Q

Dynorphins are found where?

A

Found in the spinal cord and in many parts of the brain, including the hypothalamus

25
Q

Where are the dense concentrations of opiate binding sites?

A

PAG (periaqueductal gray) and dorsal horn of spinal cord

26
Q

T or F, Opiate receptors that are found in tissues also are involved in analgesia

A

False, NOT involved in analgesia

27
Q

T or F, recognition site of opioid receptors are highly specific. The analgesia produced by endogenous or opioid drugs depends upon their action at specific sites (opioid receptor sites)

A

True

28
Q

5 opioid receptor subtypes

A
  1. Mu
  2. Delta
  3. Kappa
  4. Epsilon
  5. Sigma (no longer classified as opioid receptor)
29
Q

T or F, Binding to receptor subtype on an opioid receptor will cause different responses

A

True

30
Q

Mu 1 and Mu 2 receptor functions

A

Mu1:

  • Supraspinal analgesia
  • Euphoria
  • Physical dependence

Mu2:
- Respiratory depression

31
Q

Drugs that do what exhibit the best analgesic properties

A

Drugs that bind to Mu

32
Q

What must happen for opioid to be physically addicting

A

Must bind to Mu to be physically addicting

33
Q

What is the downside to opioid receptors

A

Always the risk of addiction and risk for respiratory depression

34
Q

Kappa opioid receptor functions

A
  1. Spinal analgesia
  2. Miosis (pinpoint pupils)
  3. Sedation
35
Q

Delta opioid receptor functions

A
  1. Analgesia
  2. Emotion
  3. Seizures
36
Q

Epsilon opioid receptor functions

A
  1. Analgesia
37
Q

Strength of attachment of an opioid drug to its binding site (binding affinity) is proportional to what?

A

Its potency

  • The stronger the affinity, the higher the potency
38
Q

Opioids act by what 3 steps

A
  1. Presynaptic inhibition of production of neurotransmitters C-fiber endings
  2. Postsynaptic suppression of evoked activity in nociceptive path or remove the remaining parts of the regulation of inhibition of nociceptive impulses
  3. Increased transmission of the descending inhibition of spinal nociceptive conduction
39
Q

T or F, Opioids cause depolarization of nerve cells, activation of nerve firing and presynaptic activation of transmitter release?

A

False, Opioids cause HYPERPOLARIZATION of nerve cells, INHIBITION of nerve firing and presynaptic INHIBITION of transmitter release

Pharmacology (24 decks)

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