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Pharmacology > Pain & Opiates > Flashcards

Pain & Opiates Flashcards

1
Q

What 2 elements make up pain?

A
  • Local irritation (stimulation of peripheral nerves)

- Recognition (CNS)

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2
Q

What are the 4 stages of nociception?

A
  1. Transduction/ Nociception
  2. Transmission
  3. Perception
  4. Modulation
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3
Q

What drugs act on the transduction/ nociceptors?

A
  • Local anesthetics

- NSAIDs

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4
Q

What does transmission connect?

A

The PNS and CNS

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5
Q

What tract does pain ascend through the spinal cord?

A
  • Spinothalamic tract
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6
Q

What types of drugs act on the trasmission stage of nociception?

A
  • Local anesthetics
  • Opioids
  • Alpha-2 agonists
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7
Q

Where is pain perceived?

A

CNS/ cerebrum

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8
Q

What drugs act on the perception stage of nociception?

A
  • Opioids

- Alpha-2 agonists

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9
Q

What do the descending tracts of modulation of nociception act on in the spinal cord?

A

The dorsal horn cells

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10
Q

What are nociceptors? (anatomically)

A

Peripheral nerve endings

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11
Q

Where are nociceptors found?

A
  • Skin
  • Muscle
  • Joints
  • Bones
  • Viscera
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12
Q

What is the novel stimulus of nociception?

A

Tissue injury

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13
Q

What do the peripheral nerves of nociceptors synapse on in the transmission phase of nociception?

A
  • 2nd order neurons in the dorsal horn
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14
Q

What neurotransmitters relay pain signals from peripheral nerves to the CNS?

A
  • Glutamate

- Substance P

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15
Q

Are Glutamate and Substance P excitatory or inhibatory?

A

Excitatory

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16
Q

What is the inhibitory neurotransmitters of pain in the CNS?

A
  • GABA

- Serotonin

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17
Q

What structure PERCEIVES pain?

A

The brain

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18
Q

What is involved in perception of pain?

A
  • Integration of all nociceptive impulses and giving meaning to the sensory input
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19
Q

From where in the CNS does descending inhibition originate?

A

Midbrain

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20
Q

What 2 neurotransmitters are involved in the modulation of pain through descending inhibition?

A
  • Serotonin

- Norepinephrine

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21
Q

What non-neurotransmitter also modulates pain through descending inhibition?

A
  • Endogenous opioids
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22
Q

What type of mechanism do endogenous opioids use to reinforce desirable behavior?

A

Positive reinforcement

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23
Q

What activity is most correlated with endogenous opioid release?

A

Sex

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24
Q

What ANS are endogenous opioids related to?

A

Symapthetic

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25
Q

How is pain modulation by opioids achieved?

A
  • Opioid receptor/ activity

- Dynorphins

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26
Q

Is nociceptive pain acute or chronic?

A

Can be either

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27
Q

Is neuropathic pain acute or chronic?

A

Chronic because it can’t be changed or alleviated

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28
Q

What is required for nociceptive pain to occur?

A

All “neural equipment” needs to functioning normally

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29
Q

What 3 factors will affect the choice of analgesia for nociceptive pain?

A
  • Type
  • Duration
  • Intensity
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30
Q

What causes neuropathic pain?

A

Injury to the nervous system

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31
Q

What trauma, illnesses, and disease cause neropathic pain?

A
  • Surgery
  • Diabetes
  • Stroke
  • Chemotherapy
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32
Q

What is allodynia?

A

Interpretation of non-pain stimuli as painful

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33
Q

What is hyperpathia?

A

Exaggerated or prolonged response to painful stimuli

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34
Q

What receptors do opioids act on?

A
  • Mu
  • Delta
  • Kappa
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35
Q

Do opioids act on acute or chronic pain?

A

Both

36
Q

By what 2 methods do stimulation of opiate work?

A
  • Inhibit transmission of pain signals

- Stimulate pain control circuits in spinal cord

37
Q

What are endorphins?

A

Peptides released opioid receptor

38
Q

Where are endorphins produced?

A

In the pituitary and hypothalamus

39
Q

Where are enkephlins produced?

A

Throughout CNS and peripheral nerve endings

40
Q

Where are dynorphins produced?

A

Nerve endings

41
Q

Which peptide is selective for mu receptors?

A

Endorphins

42
Q

Which peptide is selective for delta receptors?

A

Enkephlins

43
Q

Which peptide is selective for kappa receptors?

A

Dynorphins

44
Q

How do synthetic opioids work?

A

Bind to opioid receptors, and activate them

45
Q

Describe how opioids work on both pre and post-synaptic receptors.

A
  • Opioid restricts amount of Ca++ entering pre-synaptic nerve slowing the release of neurotransmitter
  • Opioid increases permeability of K+ in post-synaptic neuron causing hyperpolarization
46
Q

What are the 4 clinical effects of mu opiate receptors?

A
  • Euphoria
  • Physical dependence
  • Respiratory depression
  • Supraspinal analgesia
47
Q

What are the 4 clinical effects of kappa opiate receptors?

A
  • Miosis (constriction of pupil)
  • Sedation
  • Spinal analgesia
  • Respiratory depression
48
Q

What are the 4 clinical effects of sigma opiate receptors?

A
  • Dysphoria
  • Hallucinations
  • Respiratory stimulation
  • Vasomotor stimulation
49
Q

What are the 9 additional pharamacological effects of opioids in addition to pain control?

A
  • Anti-tussive
  • Alterations in smooth muscle tone
  • Inhibition of parasympathetic stimulation (constipation)
  • Decreased urine formation (stimulates release of ADH)
  • Miosis
  • Mood alteration
  • Respiratory depression
  • Nausea/ emetic effect (stimulation of CTZ)
  • Direct release of histamines (hives, itching, flushing)
50
Q

What is typically used to treat the nausea associated with opioids? How does this drug work?

A
  • Zophran

- Blocks CTZ and sensation

51
Q

What are the 3 categories opioids are classified by?

A
  1. Source
  2. Potency
  3. Special features
52
Q

What are the 2 natural occurring opiates?

A
  • Morphine

- Codeine

53
Q

Which of the 2 naturally occurring opiates are stronger for pain control?

A

Morphine

54
Q

What does codeine have a high potency as?

A

An anti-tussive

55
Q

Do morphine and codeine have strong PO effects?

A

Morphine: Poor
Codeine: Strong

56
Q

Which natural occurring opiate releases histamine? Why?

A
  • Morphine

- It is a base

57
Q

What are the 3 semisynthetic narcotics?

A
  • Heroin
  • Dihydromorphone (Dilaudid)
  • Oxycodone (OxyConin, Percocet)
58
Q

What C:P ratio?

A

Central to Peripheral effects

59
Q

What is the most prevalent street narcotic?

A

Heroin

60
Q

What is the significance of acetyl groups in heroin?

A

Facilitates passage through blood-brain barrier

61
Q

What semisynthetic narcotic has an excellent C:P ratio?

A

Dihydromorphone/ Dilaudid

62
Q

Which semisynthetic narcotic is used in over 40 products in which it is combined with non-narcotics?

A

Oxycodone

63
Q

Is oxycodone long or short-acting?

A

Short

64
Q

What is the synthetic narcotic?

A

Methadone (Dolophine)

65
Q

Is methadone stronger or weaker than morphine?

A

Equal

66
Q

How long is the half-life of methadone?

A

Extremely long

67
Q

Why is methadone so effect in preventing withdrawl symptoms?

A
  • Accumulates if taken daily

- Maintains steady plasma concentration that is easy to maintain in plateau

68
Q

Besides maintenance and weaning programs, what is the other use of methadone?

A

Chronic pain treatment

69
Q

What is meant by equianalgesic dose?

A

Equivalence of drug for analgesic effect compared to morphine

70
Q

Is an equianalgesic dose of 0.1 or 100 stronger?

A

0.1

71
Q

What is tolerance?

A

A drug loses effectiveness over time and increased dosage is required to produce therapeutic effect

72
Q

What is physical dependence?

A

Dependence on a drug to maintain a normal homeostasis of the body

73
Q

What is drug withdrawl?

A

Set of symptoms consistant with stoppage of a drug that produces physical dependence

74
Q

What are some symptoms of opiate withdrawl?

A
  • Excessive yawning
  • Tearing
  • Runny nose
  • Restlessness
  • Increased pain sensitivity
  • Nausea
  • Vomiting
  • Diarrhea
  • Cramps
  • Muscle aches
  • Sweating
  • Dysphoric mood
  • Goose bumps
  • Sweating
75
Q

When are opioid antagonists used?

A

To treat overdose

76
Q

What are 3 common opioid antagonists?

A
  • Naloxone
  • Naltrexone (trexan, vivitrol)
  • Nalmefene
77
Q

What is antagonist precipitated withdrawal?

A

Withdrawl effects onset rapidly when drug is administered

78
Q

What is the mechanism of action of naloxone?

A
  • Competitive blocking of mu and kappa receptors
79
Q

What drug administration route are naltrexone and nalmefene effective through?

A

PO

80
Q

How is naloxone administered?

A
  • Parenterally
81
Q

Does naloxone have quick or slow action?

A

Very quick

82
Q

Do naltrexone and nalmefene long or short-acting?

A

Long-acting

83
Q

What are naltrexone and nalmefene used to treat?

A
  • Prevent addicts from getting high on street narcotics

- Reduce craving, relapse, and drinking in alcohol troubled persons

84
Q

Why do patients overdosing on heroin need to be monitored after administration of naloxone?

A

The half-life of heroin is longer than naloxone

85
Q

What populations should be carefully monitored when given opioids?

A

Patients with a history of addiction

Pharmacology (9 decks)

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