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Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

___ present on trigeminal nerve endings send signals on A-delta and C fibers to ___ ganglion which project to trigeminal nuclei located in the ___. The signal is then sent to the ___ which projects to the cerebral cortex and limbic system, both of which perceive pain.

A

Nociceptors; trigeminal; brainstem; thalamus

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2
Q

What area does not have great spatial resolution?

A

trigeminal nuclei in the brainstem

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3
Q

T/F. Orofacial pain follows a different basic pathway from other pain pathways throughout the body.

A

False, Orofacial pain follows THE SAME basic pathway from other pain pathways throughout the body.

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4
Q

What are the three divisions of the trigeminal nerve?

A

opthalmic (V1), maxillary (V2), mandibular (V3)

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5
Q

T/F. Nociceptors (pain receptors) are distributed throughout the skin, oral mucosa, and tooth pulp.

A

True.

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6
Q

Describe an A-delta fiber.

A

faster, myelinated axons response first to noxious mechanical stimuli. Produce initial sensation of sharp pain

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7
Q

Describe a C fiber.

A

slower, unmyelinated axons respond to thermal, mechanical and chemical assaults. Dull, aching, or burning pain.

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8
Q

T/F. There are 5x more C fibers than A-delta fibers.

A

True.

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9
Q

Nociceptors are ___ sensors. Different nociceptors respond to various noxious stimuli such as ___, ___, mechanical ___, or ___. Their activation leads to local ___ which in turn initiates action potentials.

A

molecular; heat; cold; perburbations; protons; depolarization

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10
Q

Nociceptors express many ___ channels that are modulated by ___ to produce ___. If depolarization is great enough to reach activation ___ or voltage gated sodium channels then an action potential can be initiated.

A

ion; acid; depolarization; threshold

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11
Q

T/F. Nociceptive pain and inflammation are unrelated.

A

False, they go hand-in-hand

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12
Q

___ damage leads to the release of inflammatory ___ from neurons and resident ___ cells that interact with receptors and facilitate the transmission of ___ signals through the nervous system.

A

Tissue; mediators; immune; pain

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13
Q

List some mediators released following tissue damage.

A

prostaglandins, substance P, tumor necrosis factor-alpha, interleukin-16 and -6

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14
Q

What leads to sensitization of the pain response?

A

tissue injury

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15
Q

Define hyperalgesia and allodynia.

A

hyperalgesia: heightened sense of pain to noxious stimuli
allodynia: pain resulting from normally painless stimuli

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16
Q

___ act to inhibit the CNS and in the periphery, ___ ___ inhibit signaling to the CNS and non-steroidal and steroidal anti-inflammatories inhibit at the ___.

A

Opioids; local anesthetics; periphery

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17
Q

What are the four families of endogenous opioids?

A
  1. pro-opimelanocortin peptides: beta-endorphin
  2. pro-enkephalin peptides: met-enkephalin and leu-enkephalin
  3. Prodynorphin peptides: Dyn-A, Dyn-B and alpha-neo-endorphin
  4. Endomorphins: endomorphin-1 and endomorphin-2
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18
Q

What are the 3 important opioid receptors involved in responses to pain?

A

mu
kappa
delta

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19
Q

What do mu, kappa, and delta have in common?

A

They are all GPCR
They are widely distributed in the CNS
They activate G-alpha-i

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20
Q

POMC is made in the ___ and ___ as a ___ amino acid peptide that is processed into _-___, which is the natural agonist of the ___-opioid receptor.

A

pituitary; hypothalamus; 31; B-endorphin; mu

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21
Q

What is the pentapeptide sequence for met-enkephalin? Where is it derived from? Where is it found?

A

tyr-gly-gly-phe-met

derived from pro-enkephalin precursor (5 copies)

adrenal medulla and throughout the CNS

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22
Q

What is the pentapeptide sequence for leu-enkephalin? Where is it derived from? Where is it found?

A

tyr-gly-gly-phe-leu

derived from pro-enkephalin and pro-dynophin

through the CNS

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23
Q

Met-enkephalin and leu-enkephalin are natural agonist against the ___ opioid receptor.

A

delta

24
Q

What does the precursor pro-dynophin form? How many peptides make up each product? where are they found? What are they an agonist against?

A

dynorphin-A (13 aa)
dynorphin-B (13 aa)
alpha/beta neo-endorphin (10 aa - alpha / 9 aa - beta)

Found throughout the CNS

Agonists of kappa opioid receptor

25
Q

What happens when an opioid activates it GPCR?

A
  1. it activates G-alpha-i and dissociates GbetaGgamma
  2. Gi inhibits AC activity
  3. cAMP levels decrease and there is a reduction in PKA
  4. reduction of Ca2+ entry from voltage sensitive Ca2+ channels
26
Q

Activation of the opioid receptor leads to activation of a particular type of ___ channel via ___. This will ___ the cell and make it more difficult to transmit nerve impulses.

A

potassium; GbetaGgamma; hyperpolarization

27
Q

what effect will reduction of Ca2+ and hyperpolarization produce at the synapse?

A

They can inhibit synaptic transmission if located pre- or post-synaptically. Pre-synaptically, opioids will inhibit synaptic tranmission by reducing transmitter release. Post-synaptically, hyperpolarization will diminish generation of an action potential.

28
Q

Which opioid receptor has more adverse effects, such as respiratory depression and constipation?

A

mu receptors

29
Q

Of the three forms of mu receptors, which are the most important?

A

mu-1 and -2

30
Q

T/F. Majority of the mu receptors are located pre-synaptically and most analgesic drugs act on mu receptors.

A

True.

31
Q

Where are mu receptors found through out the body?

A

periaqueductal gray region, superficial dorsal horn of the spinal cord, nucleus accumbens, amygdala, cerebral cortex and GI tract

32
Q

Where is inhibition to the ascending pathway of pain most efficient?

A
  1. inhibit excitatory neurotransmitter release

2. inhibit transmission of impulse

33
Q

In the descending pathway, opioids ___ GABA release and therefore GABA cannot activate the ___ channel and produce hyperpolarization. Therefore, Opioids inhibit the inhibitor, helping to activate the pathway that produces CNS mediated inhibition of pain.

A

inhibit; Cl-

34
Q

What do all opioid analgesics produce?

A 
analgesia
respiratory depression
constipation
GI spasm
physical dependence
35
Q

Morphine is a ___ agonist to the mu receptor and a ___ agonist to the kappa receptor.

A

strong; weak

36
Q

T/F. When morphine is not active it is toxic. This is preferred so that it doesn’t get into the brain.

A

True, when it is activated by glucuronidation in the liver and brain it will become active and be more analgesic

37
Q

T/F. Morphine causes analgesia with sedation.

A

False, without sedation

38
Q

T/F. Morphine is more effective against sharp pains than dull aches.

A

False, it is more effective against dull aches than sharp pain

39
Q

What is the most serious acute adverse effect of the opioids?

A

respiratory depression

40
Q

What is a stage in which an organism no longer responds to a given dosage of drug and requires a higher dose to achieve the same effect?

A

Tolerance, it can manifest first as shortened to diminished analgesia

41
Q

The rate of tolerance development is a function of ___ and frequency of ___. It is generally seen after ___ days of treatment and its ___ effects remain even if tolerance has developed.

A

dose; administration; 5-7; toxic

42
Q

___ is the need for a drug even if the pain is gone. It has physical and psychological components.

A

Dependence

43
Q

Morphine is metabolized by ___ very quickly in the liver and brain into ___ (primary product) and ___ (secondary product).

A

UGT2B7; Morphine-3-glucuronide; morphine-6-glucuronide

44
Q

T/F. Morphine-3-glucuronide is usable.

A

False, it is not used. it cannot cross the BBB and therefore is excreted

45
Q

What can cross the blood-brain barrier? Which is a better agonist for the mu receptor?

A

Morphine and M-6-G

M-6-G

46
Q

T/F. Morphine can be given orally?

A

False, it is not metabolized orally, therefore must be injected

47
Q

Why is codeine more effective orally? Is it more effective than morphine if administered intramuscularly? Does it bind to the mu receptor better than morphine?

A

it has a substitution at the 3 position that renders it more effective orally
No, morphine is more effective intramuscularly
No, it binds poorly to the mu receptor

48
Q

What is codeine initially metabolized into?

A

morphine (5%) and codeine-6-glucuronide (80% - crosses the BBB)

49
Q

What dose of codeine is an oral dose to be given daily with minimum side effects and little dependence?

A

30-60mg

50
Q

T/F. Pain (dental) with an inflammatory component should not be treated without an anti-inflammatory drug.

A

True.

51
Q

What other opioids are methylated at the 3’ position and can be taken orally?

A
  1. dihydrocodeine
  2. oxycodone (percocet)
  3. hydrocodone (vicodin)
52
Q

Which form of hydrocodone or oxycontin has the potential for abuse?

A

controlled release form because there is more drug per pill

53
Q

What are 3 mu opioid receptor antagonists used to treat opioid toxicity/overdose?

A

naloxone (injected and works rapidly)
naltrexone (effective orally and long lasting)
nalmefene (active orally and last longer than naltrexone)

54
Q

Explain mixed agonists-antagonist

A

since activation of all the opioid receptors produce analgesia, it is possible to produce drugs that act on kappa and delta receptors that don’t cause major adverse effects (respiratory depression) or produce dependence.

55
Q

Which opioids are readily used in dentistry?

A

oral administration: codeine, hydrocodone, oxycodone, pentazocine

Pharmacology (13 decks)

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