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SP18: Pharm MT2 > Opioids > Flashcards

Opioids Flashcards

1
Q

T/F: Patients will often be able to identify a specific spot for orofacial pain.

A

False

Not great spatial resolution

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2
Q

What fibers will carry the first onset of quick pain?

A

Myelinated A delta fibers

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3
Q

Which fiber responds with dull aching pain?

A

C fibers (unmyelinated)

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4
Q

How does inflammation stimulate nociceptors?

A

Inflamed tissue releases mediators (prostaglandins, substance P, TNF-a, IL1b, IL-6) which interact with receptors and facilitate pain signals

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5
Q

Tissue injury can lead to sensitization of the pain response through which two methods?

A

Allodynia - response to normally painless stimuli

Hyperalgesia - heightened sense of pain to noxious stimuli

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6
Q

In general, how do opioids intervene to diminish pain?

A

Inhibition at periphery and inhibition of CNS activity

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7
Q

T/F: A single neuron in the CNSa might receive input from hundreds of axons.

A

True

Means a threshold must be reached for the nerve to fire

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8
Q

Which channels do you want to activate to hyperpolarize (inactivate) the neuron?

A

Cl- and K+ channels

Cl- channel will let Cl in the cell
K+ channel will let K+ out of the cell

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9
Q

What are the four types of endogenous opioids?

A
  1. Pro-opiomelanocortin peptides (B-endorphin)
  2. Pro-enkephalin peptides
  3. Prodynorphin peptides (Dyn-A, Dyn-B, a-neo-endorphin
  4. Endomorphins
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10
Q

What are the three types of opioid receptors?

A

Mu, kappa, and delta

Mu is the target of most drugs

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11
Q

What are the common characteristics of opioid receptors?

A

Widely distributed in CNS

GPCR

Activate G(alpha)i - inhibit cAMP production

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12
Q

___________ is the natural agonist of the mu opioid receptor.

A

B-endorphin

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13
Q

_________ and __________ are the natural agonists of the delta receptor.

A

Met-enkephalin and leu-enkephalin

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14
Q

What are the agonists to the kappa receptor?

A

Dyn-A, Dyn-B, and a-neo-endorphin

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15
Q

T/F: The GPCRs that are activated by opioids are blockers of the nerve pain signal.

A

False

Make it more difficult for nerve impulses to be conducted

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16
Q

What is the pathway for opioid activity?

A

Activates G(alpha)i -> inhibits adenylate cyclase -> less cAMP -> inhibits PKA -> less Ca entry

Activates G(beta)G(gamma) -> hyperpolarizes the cell

17
Q

T/F: Opioids can inhibit synaptic transmission if receptors are located pre- or post- synaptically.

A

True

18
Q

T/F: Mu receptors are found in the GI tract.

A

True

Leads to constipation

19
Q

T/F: Mu receptors are mostly presynaptic.

A

True

20
Q

What two nerve pathways are affected by opioids?

A

Inhibit ascending pathway from pain stimuli

Activate descending pathway of pain inhibition

21
Q

How do opioids activate the pain inhibition pathway?

A

Inhibit GABA

GABA normally hyper-polarizes neurons -> inhibition

We are therefor inhibiting the inhibitor leading to activation

22
Q

What are some common clinical effects of opioids?

A

Analgesia, Respiratory depression, constipation, GI spasm, physical dependence

23
Q

What is the most serious acute adverse effect of opioids?

A

Respiratory depression

24
Q

T/F: Morphine produces analgesia without sedation.

A

True

25
Q

T/F: The active form of morphine is injected into the patient.

A

False

Must be glucuronidized to the active form

Most turned to inactive form

26
Q

Where is it suggested that morphine has the greatest effect?

A

LImbic system

27
Q

How is tolerance first manifested in morphine?

A

Shortened or diminished analgesia

28
Q

When is tolerance of morphine normally seen?

A

After 5-7 days of treatment

29
Q

T/F: Morphine-3-glucuronide is the primary and active product of morphine metabolism.

A

False

Primary but inactive

30
Q

Why is morphine not effective taken orally?

A

Gets metabolized into M-3-G (innactive) more quickly

31
Q

What makes codeine different from morphine?

A

Substitution at 3 position makes it more effective taken orally

32
Q

T/F: Fentanyl is often given in patches and is much stronger than morphine.

A

True

33
Q

T/F: Fentanyl is often users for anesthesia.

A

True

34
Q

What are the two major factors leading to the increased strength of fentanyl?

A
  1. It is more lipid soluble

2. Binds tighter to the mu receptor

35
Q

T/F: The problem with fentanyl has to do with its therapeutic index.

A

False

36
Q

Why are fentanyl affects hard to reverse with narcan?

A

Binds so tightly

37
Q

__________ is an injected opioid antagonist.

A

Naloxone

SP18: Pharm MT2 (7 decks)

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