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Nurs 575 Anesthesia Pharmacology > Week 2 > Flashcards

Week 2 Flashcards

opioid analgesics part 1

1
Q

What drug class(es) work on Transduction?

A
  • NSAIDs
  • Local Anesthetics
  • Steroids
  • Antihistamines
  • Opioids

Apex Unit 5, Pharmacology 2 - Opioids & Non-Opioid Analgesics - 1. Pain Overview

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2
Q

What drug class(es) works on Transmission?

A
  • Local Anesthetics

Apex Unit 5, Pharmacology 2 - Opioids & Non-Opioid Analgesics - 1. Pain Overview

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3
Q

What drug class(es) work on Modulation

A
  • Neuraxial Opioids
  • NMDA Antagonists
  • a2 agonists
  • Cholinesterase Inhibitors
  • SSRIs
  • SNRIs

NH lists NSAIDs, but the explanation is kind of roundabout/indirect

Apex Unit 5, Pharmacology 2 - Opioids & Non-Opioid Analgesics - 1. Pain Overview

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4
Q

What drug class(es) work on Perception of pain?

A
  • General Anesthetics
  • a2 agonists
  • Opioids

Apex Unit 5, Pharmacology 2 - Opioids & Non-Opioid Analgesics - 1. Pain Overview

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5
Q

What endogenous ligands target the mu receptor?

A
  • Endomorphin 1
  • Endomorphin 2
  • B-endorphin
  • maybe enkephalins??

Nagelhout Ch. 11, pg 140, Table 11.2

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6
Q

What endogenous ligands target the Delt receptor?

A

Enkephalins

  • Enkephalins
  • maybe B-endorphin??

Nagelhout Ch. 11, pg 140, Table 11.2

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7
Q

What ligands target the kappa receptor ?

A

Dynorphins

  • Dynorphin A
  • Dynorphin B
  • α-neoendorphin

Nagelhout Ch. 11, pg 140, Table 11.2

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8
Q

What ligands target the nociceptin orphanin FQ peptide receptor (NOP)?

A

Nociceptin

  • Nociceptin/orphanin FQ (N/OFQ)

Nagelhout Ch. 11, pg 140, Table 11.2

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9
Q

What do opioids do to receptors on pre-synaptic neurons?

A
  • They bind with G-Protein Coupled Receptors (GPCR)
  • Which inhibits Adenylate cyclase
  • Which inhibits conversion of ATP to cyclic adenosine monophosphate (cAMP)
  • Closes Ca+2 gates channels
  • Inhibits Neurotransmitter release (NE, Substance P, Acetylcholine, dopamine)

Apex Unit 5, Pharmacology 2 - Opioids & Non-Opioid Analgesics - 2. Opioid Receptors & Nagelhout Ch. 11, pg 141, Fig. 11.2

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10
Q

What do opioids do to receptors on post-synaptic neurons?

A
  • They bind with G-Protein Coupled Receptors (GPCR)
  • Which inhibits Adenylate cyclase
  • Which inhibits conversion of ATP to cyclic adenosine monophosphate (cAMP)
  • Opens G protein coupled inwardly rectifying K+ (GIRK) channels
  • Hyperpolarizes the post-synaptic neuron, preventing propagation of action potentials

Apex Unit 5, Pharmacology 2 - Opioids & Non-Opioid Analgesics - 2. Opioid Receptors & Nagelhout Ch. 11, pg 139

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11
Q

What are the differences in analgesia between Mu, kappa, and delta receptors?

A
  • All provide Supraspinal and Spinal Analgesia
  • Delta modulates Mu activity

Nagelhout Ch. 11, pg 140, Table 11.1
Stoelting’s Ch. 7, pg. 219, Table 7.2

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12
Q

What are the differences in CV effects between Mu, kappa, and Delta receptors?

A

Mu-1 = Brady

Nagelhout Ch. 11, pg 140, Table 11.1
Stoelting’s Ch. 7, pg. 219, Table 7.2

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13
Q

What are the differences in respiratory effects between Mu, Kappa, and Delta receptors?

A
  • Mu2 and Delta = depression
  • Kappa= “possible depression”

same Kappa, same

Nagelhout Ch. 11, pg 140, Table 11.1
Stoelting’s Ch. 7, pg. 219, Table 7.2

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14
Q

What are the differences in CNS effects between Mu, Kappa, and Delta receptors?

A
  • Mu - Sedation, Euphoria, Prolactin Release, Hypothermia
  • Kapa - Sedation, Dysphoria, Hallucinations, Delirium
  • Delta - Nada

Nagelhout Ch. 11, pg 140, Table 11.1
Stoelting’s Ch. 7, pg. 219, Table 7.2

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15
Q

What are the differences in pupillary effects between Mu, Kappa, and Delta receptors?

A
  • Mu - Miosis
  • Kappa - Miosis
  • Delta - Nada

Nagelhout Ch. 11, pg 140, Table 11.1
Stoelting’s Ch. 7, pg. 219, Table 7.2

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16
Q

What are the differences in GI effects between Mu, Kappa, Delta receptors?

A
  • Mu- N/V, increased biliary pressure & decreased peristalsis, marked
  • Kappa - Nope
  • delta - minimal

Nagelhout Ch. 11, pg 140, Table 11.1
Stoelting’s Ch. 7, pg. 219, Table 7.2

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17
Q

What are the differences in GU effects between Mu, Kappa, and Delta receptors?

A
  • Mu - Urinary Retention
  • Kappa - Diuresis (inhibits vasopressin)
  • Delta - Urinary Retention

Nagelhout Ch. 11, pg 140, Table 11.1
Stoelting’s Ch. 7, pg. 219, Table 7.2

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18
Q

Which opioid receptors induce pruritis?

A
  • Mu & Kappa

Nagelhout Ch. 11, pg 140, Table 11.1

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19
Q

Which opioid receptors have anti-shivering effects?

A

Kappa

Nagelhout Ch. 11, pg 140, Table 11.1

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20
Q

What effects do Mu-1 and Mu-2 receptors share?

A
  • Analgesia
  • Bradycardia

Apex Unit 5, Pharmacology 2 - Opioids & Non-Opioid Analgesics - 2. Opioid Receptors
Stoelting’s Ch. 7, pg. 219, Table 7.2

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21
Q

How do the effects of Mu-1 and Mu-2 receptors differ?

A

Mu-1 - Euphoria, Low Abuse Potential, Miosis, Hypothermia, Urinary Retention
Mu-2 - Respiratory Depression, Constipation, Physical Dependence (2 lungs, #2 = crap, PD = 2 words?)

Apex Unit 5, Pharmacology 2 - Opioids & Non-Opioid Analgesics - 2. Opioid Receptors
Stoelting’s Ch. 7, pg. 219, Table 7.2

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22
Q

What’s Meperidine’s relative potency compared to Morphine?

A

0.1 or 1/10 the potency of Morphine

Stoelting’s Ch. 7, pg. 229

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23
Q

What’s Fentanyl’s relative potency compared to Morphine?

A
  • 75 - 125x
  • APEX says 100x

Stoelting’s Ch. 7, pg. 231

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24
Q

What is Sufentanil’s relative potency?

A
  • 500 - 1000x Morphine
  • Book says 5-10x fentanyl

Stoelting’s Ch. 7, pg. 235

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25
Q

What’s Alfentanil’s relative potency?

A

10x Morphine
* Book compares to Fentanyl, which is about 1/10 or 0.1

Stoelting’s Ch. 7, pg. 236

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26
Q

What’s Remifentanil’s relative potency?

A

100x Morphine
* Same as Fentanyl

Stoelting’s Ch. 7, pg. 237

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27
Q

What is Hydromorphone’s relative potency?

A

5x Morphine
7x if you ask APEX

Stoelting’s Ch. 7, pg. 240

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28
Q

Morphine and Codeine are classified as what derivative?

A
  • Phenanthrene
  • Naturally occuring

Stoelting’s Ch. 7, pg. 217

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29
Q

Which drugs are Morphine derivatives

A
  • Hydromorphone
  • Heroin
  • Naloxone & Naltrexone <-oxymorphone <-Hydromorphone

Stoelting’s Ch. 7, pg. 217, pg. 240
Nagelhout Ch. 11, pg. 148-149

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30
Q

Which drugs are Phenylpiperdine derivatives?

A
  • Meperidine
  • Fentanyl
  • Sufentanil
  • Remifentanil
  • Alfentanil

Stoelting’s Ch. 7, pg. 217

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31
Q

Which opioid(s) are NOT biotransformed in the liver?

A
  • Remifentanil- biotransformed by tissue & plasma esterases

Nagelhout Ch. 11, pg. 148
Stoelting’s Ch. 7, pg. 238

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32
Q

Which opioids have active metabolites?

A

The M’s
* Morphine (M6G)
* Meperidine (Normeperidine - neurotoxic)
* HydroMorphone (according to APEX -> H3G, not Nagelhout/Stoelting)
* & stupid Codeine (Technically becomes morphine)

Stoelting’s Ch. 7, pg. 228, 229, 240

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33
Q

Supraspinal analgesia occurs through activation of opioid receptors in the ____________

A
  • medulla
  • midbrain
  • “other areas”

Nagelhout, pg. 138

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34
Q

What are the 3 endogenous substances that are opiate receptor agonists?

A
  • enkephalins
  • endorphins
  • dynorphins

Nagelhout, pg. 138

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35
Q

Which of the opioids are naturally occuring?

A
  • Morphine
  • Codeine

Nagelhout, pg. 139, Table 11.1

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36
Q

Name several semisynthetic opioid agonists

A
  • oxycodone
  • hydrocodone
  • oxymorphone
  • hydromorphone

Nagelhout, pg. 139, Table 11.1

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37
Q

What are the two semisynthetic opioid antagonists?

A
  • naloxone
  • naltrexone

Nagelhout, pg. 139, Table 11.1

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38
Q

Name several synthetic opioids

A
  • All of the “ils/yls” - Fent, alfent, sufent, remi
  • Meperidine
  • Nalbuphine
  • Methadone

Nagelhout, pg. 139, Table 11.1

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39
Q

What are the three classes of opiate receptors?

A
  • mu, μ
  • kappa, κ
  • delta, δ

Nagelhout, pg. 139

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40
Q

Name the primary endogenous ligand for the opiate receptors:

  • mu, μ -
  • kappa, κ -
  • delta, δ -
A
  • mu, μ - endorphins & endomorphins
  • kappa, κ - dynorphins
  • delta, δ - enkephalins

Nagelhout, pg. 140

41
Q

Opioid receptors are g protein-coupled receptors with the intracellular action of decreasing ___________ production, reducing the influx of __________ ions

A
  • cAMP
  • calcium

Nagelhout, pg. 139

42
Q

Explain how activation of opioid receptors relates to intracellular potassium concentrations

A
  • activation of opioid receptors leads to opening of G protein-coupled inwardly rectifying (GIRK) channels
  • this allows efflux of potassium from the cell and hyperpolarization
  • hyperpolarization prevents the propagation of action potentials

Nagelhout, pg. 139

43
Q

Stimulation of the _________ receptor produces most of the classic clinical actions of the opioid agonists

A
  • mu, μ

Nagelhout, pg. 139

44
Q

The _________ receptor serves to modulate activity of the mu receptors

A
  • delta, δ

Nagelhout, pg. 139

45
Q

When small doses of opioids are used, the effects are usually terminated by _____________ rather than metabolism

A
  • redistribution (from central to peripheral compartment

Nagelhout, pg. 140

46
Q

The analgesic effects of opioids come from their ability to directily inhibit ascending transmission of nociceptive information and activate ________________ from the midbrain/rostral ventromedulla

A
  • pain control pathways that descend

Nagelhout, pg. 142

47
Q

Dysphoria appears more prominent with drugs that have strong ___________ receptor effects or when opioids are taken in the absence of ___________

A
  • kappa, κ
  • pain

Nagelhout, pg. 142

48
Q

Opiates are not anesthetics, so _________ is a concern when even high doses are used

A
  • awareness under anesthesia

Nagelhout, pg. 142

49
Q

Acute and chronic tolerance can occur with opiates, and cross-tolerance among μ-agonists will occur. Usually a decrease in ____________ is noted first, followed eventually by __________

A
  • duration
  • decrease in effect

Nagelhout, pg. 142

50
Q

All opiate agonists produce a dose-dependent depression of respirations via effects on ________ and ________ receptors in the brainstem respiratory centers

A
  • mu, μ
  • delta, δ

Nagelhout, pg. 142

51
Q

What is the mechanism for opiate-induced respiratory depression?

A
  • shift to the right in the CO2 response curve
  • reduced responsiveness to increasing carbon dioxide levels - higher PCO2 required to maintain adequate respiration

Nagelhout, pg. 142

52
Q

___________ is affected first, and a classic “narcotized” patient will take slow _______ breaths

A
  • respiratory rate
  • deep

usually a decreased rate with increased tidal volume is observed - Dr. C

53
Q

Pinpoint pupils, AKA _________, is a prominent action of opioids - minimal tolerance develops to this effect

A
  • miosis

Nagelhout, pg. 142

54
Q

True or false:

The cough suppressant effect of opiates also causes a loss of protective glottal reflexes

A
  • False - they are not effected
55
Q

Because of their depressant effect on the cough center in the medulla, the clinical use of opiates can help patients better tolerate _____________ and ______________

A
  • airway devices
  • ventilators

Nagelhout, pg. 143

56
Q

Opioids elicit nausea and vomiting by stimulating the __________ in the area postrema of the medulla - a ___________ component is also probable because the incidence is much higher in ambulatory patients

A
  • chemoreceptor trigger zone
  • vestibular

Nagelhout, pg. 143

57
Q

When opiates are used as part of the anesthetic plan, there is a(n) ____________ incidence of postoperative nausea and vomiting

A
  • increased

Nagelhout, pg. 143

58
Q

Much of the hypotension produced by morphine, codeine, and meperidine is attributed to __________ release

A
  • histamine

hypotension minimal in healthy pts - especially when supine/normovolemic

Nagelhout, pg. 143

59
Q

Histmaine release is absent in which opioids?

A
  • fentanyl
  • sufentanil
  • alfentanil
  • remifentanil

Nagelhout, pg. 143

60
Q

Opioids decrease tone at the bladder detrusor muscle and constrict the ___________, producing an antidiuretic effect

A
  • urinary sphincter

Nagelhout, pg. 143

61
Q

Administration of opioids with which anesthetic gas may increase the frequency of muscluar rigidity?

A
  • Nitrous oxide

Nagelhout, pg. 143

62
Q

Activation of which opioid receptor results in diuresis? What is the mechanism?

A
  • kappa, κ
  • inhibition of vasopressin release
63
Q

Muscular rigidity caused by large intravenous doses of opioids is easily reduced by the administration of ____________ or ______________

A
  • NMBA
  • naloxone

Nagelhout, pg. 144

64
Q

True or false:

Only histamine releasing opiates (morphine, codeine, meperidine) cause pruritus

A
  • False - the mechanism for pruritus appears to be through central mu receptors and NOT local histamine release

Nagelhout, pg. 144

65
Q

Pruritus is especially prominent in which route of opiate administration?

A
  • neuraxial

Nagelhout, pg. 144

66
Q

Which medication should be used as first-line treatment for opioid-induced pruritus?

A
  • Nalbuphine - it is superior to placebo, diphenhydramine, naloxone or propofol

agents like naloxone or naltrexone may also work but reverse analgesia

Nagelhout, pg. 144

67
Q

The __________ opioid receptor is responsible for effects on GI function - name those effects

A
  • Mu, μ
  • decreased gastric motility → prolonged gastric emptying time
  • decreased intestinal propulsive activity → constipation/postop ileus
  • reduced secretory activity through GI system

Nagelhout, pg. 144

68
Q

Opioids produce a dose-dependent ________ in biliary duct pressure and sphincter of Oddi tone

A
  • increase

questionable whether this has clinical relevance

Nagelhout, pg. 144

69
Q

Opiates reduce the ________ to surgery by inhibiting release of ___________ from the pituitary

A
  • stress response
  • corticotropin

Nagelhout, pg. 144

70
Q

What actions do opioids have on body temperature? How do they exert these actions?

A
  • Slightly decreased body temperature
  • Inhibit release of thyroid stimulating hormone → decreased basal metabolic rate
  • Resetting of temperature set point in hypothalamus

Nagelhout, pg. 144

71
Q

The analgesic response to neuraxial opioid administration is especially related to which opioid receptor subtype?

A
  • kappa, κ

located in the substantia gelatinosa

Nagelhout, pg. 144

72
Q

Side effects with spinal administration of opioids are similar to systemic administration, except that ________ and __________ occur with much greater frequency

A
  • urinary retention
  • pruritus

Nagelhout, pg. 144

73
Q

_________ is the most common serious complication associated with intrathecally and epidurally administered opioids

A
  • Respiratory depression

Nagelhout, pg. 144

74
Q

Why does neuraxial morphine cause both an early phase and late phase of respiratory depression?

A
  • Rapid systemic absorption (similar to parenteral dosing)
  • Rostral flow of CSF and delivery of morphine to the brainstem respiratory centers 8-12 hrs later

Nagelhout, pg. 144

75
Q

Do hydrophilic or lipophilic opioids have a smaller area of distribution along the length of the spinal cord? Why?

A
  • lipophilic
  • they are rapidly absorbed into the spinal tissues before spreading

lipophilic drugs also have a faster onset, but shorter duration

Nagelhout, pg. 145

76
Q

Name several advantages of continuous opioid infusion when compared with intermittent bolus

A

Nagelhout, pg. 145

77
Q

Why is sedation not a good indicator of appropriate analgesia with the administration of IV morphine?

A
  • IV morphine causes sedation before it causes analgesia

Nagelhout, pg. 147

78
Q

True or false:

When administered intrathecally, morphine has the shortest duration of action of the specific opioids

79
Q

Why is morphine contraindicated in a patient with renal failure?

A
  • It has an active metabolite, M6G, which may cause a more prolonged effect

Nagelhout, pg. 147

80
Q

_________ is a weak opioid with good antitussive activity - about 10% is metabolized to morphine

A
  • Codeine

Nagelhout, pg. 147

81
Q

________ is a drug derived from morphine with a similar pharmacokinetic profile, but is 5-7 times more potent

A

Hydromorphone

Nagelhout, pg. 147

82
Q

Methadone is a synthetic opioid often indicated for ___________ because it produces less euphoria when compared to other common opioids

A
  • opioid abstinence syndromes
  • opioid use disorders

Nagelhout, pg. 147

83
Q

_________ is a synthetic opioid agonist that is effective in reducing shivering - this appears to result from _________ receptor stimulation

A
  • meperidine
  • kappa

BUT, it is technically classified as mu receptor agonist

Nagelhout, pg. 147

84
Q

Meperidine is structurally similar to __________ and has similar antispasmodic effects

A
  • atropine

Nagelhout, pg. 147

85
Q

What are the major neurologic concerns with the active metabolite of meperidine (normeperidine)?

A
  • Lowering of seizure threshold → seizures
  • CNS excitability → tremors, muscle twitches

Nagelhout, pg. 147

86
Q

___________ is the most widely used opioid analgesic in anesthesia

A
  • Fentanyl

Nagelhout, pg. 147

87
Q

The action of a single dose of fentanyl is terminated by _______________ and has a duration of approximately ___________

A
  • redistribution (not metabolism/elimination)
  • 20-40 minutes

Nagelhout, pg. 147

88
Q

Fentanyl undergoes a significant first-pass uptake in the __________ with temporary accumlation before release

89
Q

Metabolism of ___________ by plasma and tissue esterases lends itself to ultrashort duration and titratability

A
  • remifentanil

Nagelhout, pg. 148

90
Q

Due to the high potential for respiratory depression, muscle rigidity, and bradycardia (per Dr. C), bolus dosing of __________ in the preoperative of postoperative period is not recommended

A
  • remifentanil

Nagelhout, pg. 148

91
Q

Why is remifentanil not administered epidurally or intrathecally?

A
  • potential for neurotoxicity related to glycine use in powder preparations

Nagelhout, pg. 148

92
Q

____________ is the most potent of the parenterally administered opioids

A
  • Sufentanil

Nagelhout, pg. 148

93
Q

Buprenorphine is a partial opioid agonist that, when used neuraxially, has a lower incidence of _________ and __________

A
  • pruritis
  • nausea

Dr. C, the man himself

94
Q

Which drug has the ability to reverse opioid induced respiratory depression and pruritis while retaining analgesic properties?

A
  • Nalbuphine

Nagelhout, pg. 148

95
Q

Nalbuphine provides an agonist effect at the __________ receptors, and an antagonist effect at the __________ receptors, with an analgesic response equal to that of ___________

A
  • kappa
  • mu
  • morphine

Nagelhout, pg. 148

96
Q

_________ and _________ are pure opioid antagonsits

A
  • Naloxone
  • Naltrexone

Nagelhout, pg. 148-149

97
Q

The following are drugs commonly used orally for treating acute pain:
_____________ is approximately twice as potent as oral morphine
____________ is similar in potency to oral morphine

A
  • oxycodone
  • hydrocodone

morphine 10 mg = hydrocodone 5-10 mg

Stoeltings, pg. 240

98
Q

When physical dependence is established, discontinuation of the opioid agonist produces a typical withdrawal abstinence syndrome - this usually requires _________ days with morphine but begins to occur within 48 hours of continuous medication usage

A
  • 25 days

Stoeltings, pg. 225

99
Q

While __________ has a more rapid onset than fentanyl, it has a much shorter duration of action, and its popularity in current practice is limited

A
  • Alfentanil

Nurs 575 Anesthesia Pharmacology (9 decks)

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