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MSK/Derm > SM 236/240: Pharmacology > Flashcards

SM 236/240: Pharmacology Flashcards

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1
Q

What is pain?

A

Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage

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2
Q

What are the most common drugs involved in prescription overdose?

A

Prescription opioids, including: Oxycodone, Methadone, and Hydrocodone

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3
Q

What race is most impacted by opioid overdose death?

A

Caucasians

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4
Q

What are pain systems?

A

Peripheral neurons with nociceptors or central neuronal relay pathways

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5
Q

What are nociceptors?

A

Peripheral pain sensors

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6
Q

How do pain systems alter pain perception?

A

Pain systems impose excitatory or inhibitory influences on nociceptive information throughout many levels of the neuraxis

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7
Q

Where can nociception occur?

A

Skin, Muscle, Joints, Viscera, Dura

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8
Q

What are the two types of pain fibers?

A

A-delta and C fibers

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9
Q

How do A-delta and C pain fibers compare?

A

A-delta is fast, C is slow

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10
Q

How do fibers explain “double pain”?

A

After a traumatic injury, A-delta fibers produce initial sharp pain while C pain fibers produce later dull, throbbing pain

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11
Q

What molecules initiate pain?

A

Central: Glutamate and Substance P

Peripheral: Bradykinin

Both: Prostaglandins

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12
Q

What are the central pain initiators?

A

Glutamate and Substance P

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13
Q

What are the peripheral pain initiators?

A

Bradykinin

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14
Q

What molecules can initiate pain both centrally and peripherally?

A

Prostaglandins

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15
Q

What are the pain inhibitor molecules?

A

Serotonin, Norepi, Endorphins, Enkephalisn, Dynorphin

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16
Q

Describe the general pain pathway:

A

Pain is detected by the Nociceptor

Pain travels up sensory axon through the Dorsal Horn of a Spinal Cord neuron via Substance P/Glutamate

Pain signal is amplified

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17
Q

What is the anterolateral pathway?

A

The pathway that conveys pain and temperature, as well as crude touch

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18
Q

What is the posterior column pathway?

A

The pathway that covneys proprioception, vibration, and fine touch

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19
Q

Where does the anterolateral pathway cross over in the spinal cord?

A

At the level a signal, such as pain, is received

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20
Q

Where does the posterior column pathway cross over in the spinal cord?

A

At the Medulla Oblongata, a higher level than where the pain is received,

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21
Q

Which pathway does pain use?

A

The Anterolateral Pathway

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22
Q

What is gate control theory?

A

Idea that you can “shake off” pain with non-painful stimuli distracting you from painful stimuli

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23
Q

What is the Periaqueductal gray?

A

An area that inhibits pain transmission in the dorsal horn via relay to the rostral ventral medulla

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24
Q

What are the “ascending” and “descending” pain pathway sand how do they relate to Opioids?

A

Pain is detected and travels to brain via Ascending pathways

Pain is inhibited by central neurons using Descending pathways

Opioids inhibit Ascending pathways and activate Descending pathways to inhibit pain

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25
Q

How do Opioids activate the Descending pain inhibition pathway?

A

Double negative: normally, GABA neurons inhibit the pain-inhibiting neurons of the Descending pathway

Opioids inhibit GABA neurons to disinhibit pain inhibition, potentiating the Descending pathway

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26
Q

What are the Opioid receptors and how many genes code for them?

A

3 receptor: Mu, Kappa, and Delta

All coded for by the same gene with varied splicing

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27
Q

How does the same gene give rise to Mu, Kappa, and Delta Opioid receptors?

A

Subtypes come from splice variants

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28
Q

Describe the Mu Opioid receptor?

A

Mu for Morphine

Causes Analgesia/Euphoria, Dependence, Respiratory Depression and Miosis

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29
Q

Describe the Kappa Opioid receptor?

A

Mild analgesia, less respiratory depression than Mu , and psychomimetic effects

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30
Q

How do the Mu and Kappa Opioid receptors compare?

A

Mu causes stronger analgesia and respiratory depression than Kappa

Kappa also has psychomimetic effects

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31
Q

Describe the Delta Opioid receptor?

A

Function unknown

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32
Q

Where are Opioid receptors expressed?

A

Brain, spinal cord, gut

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33
Q

Where are Opiod receptors located in the brain and with what function?

A

Thalamus = detect pains sensation
Amygdala = emotional aspect of pain
Area Postrema = nausea from pain
Brainstem Ventilation Nuclei = assist breathing
Periaqueductal Gray = Inhibit pain transmission
Substantia Gelatinosa = nociceptor connecting to SC

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34
Q

Which area of the brain is responsible for detecting pain sensations?

A

The Thalamus

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35
Q

Which area of the brain encodes the emotional aspect of pain?

A

Amygdala

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36
Q

Which area of the pain is responsible for the nausea caused by Opioids?

A

Area Postrema

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37
Q

Which part of the brain is responsible for respiratory depression caused by Opioids?

A

Brainstem Ventilation Nuclei

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38
Q

What is the term for where a nociceptor axon first interfaces with the spinal cord?

A

Substantia Gelatinosa

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39
Q

What type of protein are Opioid receptors?

A

GPCR’s

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40
Q

Describe the signalling changes caused by Opioid binding to Opioid receptors?

A

Inhibit cAMP
Increase K efflux and decease Ca influx = hyperpolarize
Decrease nociceptive transmission

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41
Q

What effect do Opioids have on motor and touch fibers?

A

They don’t

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42
Q

Why are Opioids able to disinhibit pain inhibitory neurons?

A

GABAnergic interneurons that inhibit pain inhibitory neurons have Opioid receptors, which can bind Opiods and inhibit the interneuron, potentiating the Pain inhibitory neuron

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43
Q

What is an Opiate?

A

A drug derived from Opium

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44
Q

What is an Opioid?

A

All drugs, natural and synthetic, that bind to Opioid receptors

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45
Q

What is a Narcotic?

A

Any substance that induces sleep, actors on opioid receptors, or any illicit substance

46
Q

What are the 3 broad ways to categorize Opioids?

A

Naturally occurring
Semisynthetic
Synthetic

47
Q

What are examples of naturally occurring Opioids?

A

Morphine and Codeine

48
Q

What are examples of semisynthetic Opioids?

A

Heroin

49
Q

What are examples of synthetic Opioids?

A

Methadone and Fentanyl

50
Q

What are the weak Opioids?

A

Codeine and Hydrocodone

51
Q

What are the strong Opioids?

A

Everything other than Codeine and Hydrocodone

52
Q

What are Opioid Agonists?

A

Mu receptor agonists:

Morphine and Hydromorphone

53
Q

What are Opioid Antagonists?

A

Mu receptor antagonists:

Naloxone, Naltrexone

54
Q

What are Opioid Agonist/Antagonists?

A

Medications that activate Kappa and inhibit Mu, to provide some pain relief and minimize side effects

Ex: Butorphanol

55
Q

What are Opioid Partial Agonists?

A

Buprenomorphine, causes high affinity partial Mu agonism

56
Q

Which Opioid receptor mediates Analgesia in an Agonist/Antagonist medication?

A

Analgesia and Kappa mediated

57
Q

Which Opioid receptor is inhibited in an Agonist/Antagonist medication?

A

Mu is weakly antagonized

58
Q

What are the pros and cons of Agonist/Antagonist Opioids?

A

Less GI side effects and respiratory depression due to weak Mu inhibition, but have a ceiling effect and can trigger withdrawal

59
Q

When should an Agonist/Antagonist Opioid never be used?

A

Never use them on an Opioid tolerant patient because they can trigger withdrawal and psychosis

60
Q

Describe how the binding of Buprenomorphine leads it’s effects?

A

Buprenomorphine is a high affinity partial Mu agonist

Has a ceiling on agonism and binds with such high affinity that other Opioids and even Naloxone cannot bind

Makes reversal following OD difficullt

61
Q

What is the current use of Buprenomorphine?

A

Opioid maintenance

62
Q

How does lipophilicity relate to Opioid use?

A

Lipophilicity sets the efficacy with which an Opioid crosses the BBB

High Lipophilicity = fast onset and short duration
Low Lipophilicity = slow onset and long duration

63
Q

What are the high lipohilicity Opioids?

A

Fentanyl, Meperidine

64
Q

What are the low lipophilicity Opioids?

A

Morphine, Hydromorphone

65
Q

What are the neurologic effects of Opioids?

A

Analgesia

66
Q

What is Analgesia?

A

Pain relief at the supra spinal and spinal cord level not reliably associated with a loss of consciousness

67
Q

Does Analgesia cause a loss of consciousness?

A

Nope

68
Q

Is Analgesia better at controlling Nociceptive Pain or Neuropathic Pain?

A

Nociceptive Pain

69
Q

How do Nociceptive and Neuropathic Pain compare?

A

Nociceptive Pain is due to pain caused by nociceptor stimulation

Neuropathic pain is pain caused by damaged neural structures

Analgesics work better on Nociceptive pain

70
Q

What is Miosis?

A

Pinpoint pupils associated with Opioid agonist OD

71
Q

Which Opioid agonists cause Mioisis?

A

All of them

72
Q

How long does it take to build up tolerance against Mioisis?

A

There is no tolerance, even in addicts, making it useful for diagnosis of Opioid OD

73
Q

What is the major cause of Opioid mortality and how can it be avoided?

A

Opioid induced respiratory depression is a major cause of death

Best way to avoid this is to hold the Opioid if a patient is sedated

74
Q

What receptor mediates Opioid respiratory mortality?

A

Mu receptors bind Opioids and cause respiratory depression leading to death

75
Q

What effect do Opioids have on the respiratory system other than respiratory depression?

A

Opioids inhibit the ventilatory response to hypercapnia, preventing tachypnea and causes respiratory depression

76
Q

Why are Opioids used for anxiety?

A

Anxiety causes hyperventilation while Opioids slow the respiratory drive

77
Q

Can Opioids be used in patients with Cardiac problems?

A

For the most part, yes, since Opioid don’t have much of an effect on the heart

78
Q

What are the GI effects of Opioids?

A

Opioids can slow peristalsis due to enteric Opioid receptors, and lead to Nausea or vomiting

79
Q

What Opioid effects can tolerance develop toward?

A

Tolerance can emerge to: Euphoria, sedation, analgesia, respiratory depression and Nausea/vomiting

80
Q

What Opioid effects can tolerance not develop toward?

A

Tolerance never emerges to Miosis or Constipation

81
Q

How do Tolerance and Dependence vary?

A

A patient is dependent when the body is physically dependent on a drug for normal function

Tolerance refers to acclimatization of the body toward the drug’s effects

82
Q

What are the symptoms of Opioid withdrawal?

A

Sympathettic overdrive:

Anxiety, Insomnia, HTN, Tachycardia, and Hyperventilation

83
Q

Can you die from Withdrawal?

A

Nope, but it feels miserable

84
Q

What are the signs of Opioid Overdose?

A

Respiratory depression/arrest, Sedation/Unresponsive, Miosis/pinpoint pupils

85
Q

What should be done if you suspect an Opioid OD?

A

Supportive ventilation + Naloxone

86
Q

Describe the hydrophilicity/phobicity, duration, and MoA of Morphine?

A 
Hydrophilic = delayed transport across BBB = delayed onset
Duration = 4-5 hours
MoA = histamine release (risk of hypotension)
87
Q

Describe the metabolism of Morphine?

A

Morphine is converted into Morphine-3-Glucoronide and Morphine-6-Glucororide in the Liver for excretion in the Kidney

88
Q

Why shouldn’t you give someone with renal failure Morphine?

A

Morphine is gloconidated and excreted in the Kidneys, and renal failure impairs excretion

89
Q

What is the significance of the metabolites of Morphine?

A

Morphine is glucoronidated into M3G and M6G

M6G is a minor metabolite and 10-100x more potent than Morphine and is believed to cause the Analgesic effects

M3G can cause myoclonus/twitches and seizures

90
Q

Describe the PK/PD of Oxycodone?

A

High bioavailability compared to Morphine

Analgesia via Oxycodone itself, but can be metabolized in small amounts into the more potent Oxymorphone

91
Q

What is Oxymorphone?

A

A metabolite of Oxycodone that is a rare byproduct but much more potent

92
Q

What is Codeine?

A

A prodrug with low Mu affinity, and 10% is metabolized to Morphine that in some patients cannot be metabolized

93
Q

How is Hydrocodone administered in the US?

A

Always combined with Acetamniophen

Both prodrug and metabolites are potentially efficacious

94
Q

How does Hydromorphone compare to Morphine?

A

Both are Hydrophilic with similar duration of Analgesia

Hydromorphine has a better side effect profile and is more potent

95
Q

How is Hydromorphone metabolized?

A

Hydromorphone is metabolzied in the Liver to H3G, which lacks analgesic effects

96
Q

Describe the binding of Fentanyl?

A

Fentanyl is highly lipophilic with high affinity for the Mu receptor with a fast onset and short duration

97
Q

Which is more potent, Fentanyl or Morphine?

A

Fentanyl is 100x more potent than Morphine

98
Q

When is Fentanyl used and why?

A

Because it has a fast onset and short duration, it is used in the OR and ICU for analgesia via IV

99
Q

Why is Fentanyl given transdermally?

A

The transdermal patch causes a SubQ deposit of Fentanyl for slow sustained release, prolonging it’s otherwise shortlived effects and duration

Also helps prevent abuse

100
Q

Can you give Transdermal Fentanyl to patients with GI issues?

A

Yes, this is ideal because it doesn’t need to be absorbed by GI

101
Q

What is Merperidine?

A

A lipophilic drug with very rapid onset, albeit less potent than Morphine at binding Mu

102
Q

How does Merperidine work outside of Mu agonismW?

A

Serotonin Reuptake Inhibitor

103
Q

What is the metabolite of Merperidine?

A

Normeperidine, which has a long half-life as it is not cleared by the kidneys and can cause CNS hyperactivity

104
Q

Why should you not give Merperidine to patients with renal failure?

A

Merperidine is metabolized into Normeperidine, which is not cleared by the Kidneys effectively, and can therefore reach very toxic conc. that leads to seizures

105
Q

What is Tramadol?

A

A prodrug that has Mu receptor agonism as well as blocking the reuptake of Serotonin and Norepi, to treat mild/moderate pain

106
Q

What is Naloxone?

A

An Opioid competitive antagonist with a short duration that temporarily reverses the effects of Opioid pills

107
Q

How must Naloxone administered?

A

Only via IV

108
Q

How do the density of Opioid receptors vary within patients?

A

Every patient has a different distribution of Opioid receptors throughout their body

109
Q

Why do different Opioids have varying effects on patients?

A

Not only do patients have a different distribution of Opioids in each patient, but they also have different affinities for an Opioid ligand based on their subtype and splice variation, leading to different effects in different patients

110
Q

What should you do if an Opioid has harsh side effects and poor analgesia?

A

Switch Opioids, just don’t go too high

MSK/Derm (46 decks)

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