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(Steele) Anesthesia Pharm Grayson (Spring 2023) > Opioids Agonists (Exam II) > Flashcards

Opioids Agonists (Exam II) Flashcards

1
Q

What are opioids effects on the CO₂ medullary center?

A
  • Opioids inhibit the CO₂ medullary center.
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2
Q

Three opiates from Papaver somniferum (Opion)

A

Morphine - 1803
Codeine - 1832
Papaverine - 1848

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3
Q

Differentiate opioids from narcotics.

A
  • Opioids = all exogenous substances that bind to endogenous opioid receptors.
  • Narcotic = any substance that can produce physical dependence (stupor)
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4
Q

What two types of opioid chemical structures are there?

A
  • Phenanthrenes
  • Benzylisoquinolines
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5
Q

Which drugs are Phenanthrenes?
Which drugs are benzylisoquinolines?

A
  • Phenanthrenes: Morphine & codeine, and Thebaine
  • Benzylisoquinoline: Papaverine and Noscapine
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6
Q

What is papaverine mostly used for?

A

Treating intra-arterial barbiturate administration (dilates the highly constricted artery).

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7
Q

What portions of the brain are the source of descending inhibitory signals?

A
  • Hypothalamus
  • PAG
  • RVM
  • Locus Coeruleus
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8
Q

What endogenous substances have the same effect as or use the same receptors as opioids?

A

Endorphins, Enkephalins, and Dynorphines.

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9
Q

Presynaptic inhibition of what neurotransmitters occurs with opioid administration?

A
  • ACh
  • Dopamine
  • NE
  • Substance P
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10
Q

How do opioids modulate pain at the cellular level?

A
  • ↑ pK⁺ (hyperpolarization)
  • Ca⁺⁺ channel inactivation
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11
Q

Where are opioid receptors located in the brain?

A
  • PAG
  • Locus Ceruleus
  • RVM (rostral ventral medulla)
  • Hypothalamus
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12
Q

Where is the primary site of opioid receptors in the spinal cord?

A

Substantia gelatinosa (aka Laminae 2)

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13
Q

Where is/are opioid receptors found outside the CNS?

A
  • Sensory neurons & immune cells
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14
Q

What are the four (most important) types of opioid receptors?

A
  • Μu1 (μ₁)
  • Μu2 (μ₂)
  • Κappa (κ)
  • Delta (δ)
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15
Q

Which opioid receptor(s) is/are responsible for respiratory depression & physical dependence?

A
  • Μu2 and δ (delta)
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16
Q

Which receptors are responsible for constipation?

A
  • Μu2 primarily
  • δ (less)
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17
Q

Which receptors can cause urinary retention?
Are there any receptors that cause diuresis when bound?

A
  • Retention: Μu1 and δ
  • Diuresis: κappa
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18
Q

All opioid receptors induce analgesia at both the brain the spinal cord. T/F?

A
  • False. Μu2 receptors only cause at analgesia at the spinal cord level.
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19
Q

What opioid receptors have low abuse potential when bound?

A

Μu1 and κ

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20
Q

Which opioid receptor is responsible for euphoria, bradycardia, hypothermia when bound?

A

Mu1

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21
Q

An agonist binding to Mu1 and Kappa receptors result in

A

Low abuse potential
Miosis

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22
Q

What agonists bind to the four opioid receptors?

A
  • Mu1 & Mu2 = endorphins, morphine, synthetics opioids.
  • κ = dynorphins.
  • δ = enkephalins.
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23
Q

What 3 meds are antagonists of all 4 major opioid receptors?

A

Naloxone
Naltrexone
Nalmefene

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24
Q

What does this graph show?

A

That if you add nitrous or a benzodiazepine (diazepam) with an opioid like fentanyl –> depression in MAP and SVR

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25
Q

Describe the adverse side effects of opioids on the cardiovascular system.

A
  • ↓BP from ↓SNS tone - orthostatic hypotension and syncope
  • ↓HR or histamine release = ↓BP
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26
Q

What possible cardiovascular benefits do opioids provide?

A
  • Myocardial ischemia protection (won’t cause myocardial depression)
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27
Q

What are the respiratory effects of opioids?
What would symptoms of overdose be?

A
  • Depressed CNS response to CO₂ causing a right shift of PaCO₂ (↑)
  • Overdose = apnea, miosis, ↓RR, coma.
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28
Q

What drug would treat opioid ventilatory depression but not reverse analgesia?
How?

A
  • Physostigmine would by increasing CNS ACh levels.
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29
Q

What is normal PaO₂?
What shift in PaO₂ would be seen with metabolic acidosis?
What shift in PaO₂ would be seen with general anesthesia?

A
  • Normal PaO₂ is 80 mmHg
  • Left shift
  • Right shift
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30
Q

What would cause a leftward shift in PaO₂?
What would cause a rightward shift?

A
  • Leftward: Metabolic acidosis (to breathe off all that CO₂)
  • Rightward: sleep → opiates → anesthesia
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31
Q

What level of PaCO2 do we want to avoid?

A

PaCO2 of 60 (CO2 narcosis)

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32
Q

Why should caution be used when administering opioids to head trauma patients?

A
  • Opioids ↓CBF and possibly ICP

Myoclonus (with large doses)

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33
Q

What musculoskeletal abnormality occurs with opioid administration?
What makes this condition worse or severe?
How is it treated?

A
  • Skeletal chest wall and abdominal muscle rigidity.
  • Mechanical ventilation
  • Muscle relaxants and/or naloxone
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34
Q

What are sphincter of Oddi spasms?
Which drugs can cause this?

A
  • Biliary smooth muscle spasm
  • Fentanyl (99%), Morphine (53%), and Meperidine (61%).

I think maybe all opioids can cause this but these are the primary culprits

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35
Q

What drugs should be used for ERCP cases?

A
  • Non-opioids (multimodal approach w/ NSAIDs, gabapentin, etc.)

To avoid the Sphinctre of Oddi spasms

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36
Q

How are opioid-induced sphincter of Oddi spasm’s treated?

A
  • Naloxone (will differentiate between Oddi spasm or angina)
  • Glucagon (2mg IV given incrementally, ,don’t give all 2 mg at once) and causes no opioid antagonism.
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37
Q

Treatment of Oddi spasms per TWU reference guide

A

Glucagon 2 mg IV
Naloxone 40 mcg IV
Atropine 0.2 mg IV
NTG 50 mcg IV

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38
Q

How do opioids effect N/V?

A

They directly stimulate the Chemoreceptor trigger zone (CTZ)
- increases GI secretions and results in delayed emptying

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39
Q

Opioid side effects
GU:
Cutaneous:
Placenta:

A

GU: Urinary urgency
Cutaneous: histamine release –> flushed face, neck, upper chest
Placenta: Neonate depression, dependence (chronic)

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40
Q

How long does it take (generally) to develop tolerance to opioids?
What causes tolerance?

A
  • 2-3 weeks
  • Morphine: 25 days
  • Downregulation
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41
Q

T/F: Cross tolerance can happen with all opioids.

A

True

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42
Q

Initial symptoms of opioid withdrawal: (5)

A

Yawning
diaphoresis
lacrimation
coryza
restlessness

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43
Q

opioid withdrawal symptoms after 72hrs:

A

72 hrs: ABD cramps, N/V, diarrhea

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44
Q

Which two drugs have the same shortest Onset, Peak intensity, and Duration of withdrawal symptoms?

A

Fentanyl
Meperidine

onset: 2-6 hrs
Peak intensity: 6-12 hrs
Duration: 4-5 days

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45
Q

Which two drugs have the same medium Onset, Peak intensity, and Duration of withdrawal symptoms?

A

Morphine
Heroine

onset: 6-18 hrs
Peak intensity: 36-72 hrs
Duration: 7-10 days

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46
Q

Which drug has the longest Onset, Peak intensity, and Duration of withdrawal symptoms?

A

Methadone

24-48 hrs
3-21 days
6-7 weeks

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47
Q

What is the dosage of morphine?
Duration?

A
  • 1 - 10 mg IV Intraop
  • 5 - 20 mg post op
  • Duration: 4-5 hours
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48
Q

When does morphine peak?

A
  • IV Peak: 15 - 30 minutes
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49
Q

Onset of morphine

A

10-20 min

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50
Q

Morphine works on the ____ more then the other fibers

A

Unmyelinated C-fibers

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51
Q

Fentanyl
Intraop dose:
Onset:
Duration:

A

Intraop dose: 1.5-3 mcg/kg
Onset: 30-60 sec
Duration: 1-1.5 hrs

52
Q

Sufentanil
Intraop dose:
Onset:
Duration:
Infusion dose:

A

Intraop dose: 0.3-1 mcg/kg
Onset: 30-60 sec
Duration: 1-1.5 hr
Infusion dose: 0.5-1 mcg/kg/hr

53
Q

Remifentanil
Intraop dose:
Onset:
Duration:
Infusion:

A

Intraop dose: Load: 0.5 - 1 mcg/kg over 1 min
Onset: 30-60 sec
Duration: 6-8 min
Infusion: 0.125 - 0.375 mcg/kg/min

54
Q

Meperidine
Post op dose:
Onset:
Duration:

A

Post op dose: 12.5 mg (shivering)
Onset: 5 - 15 min
Duration: 2 - 4 hrs

55
Q

Naloxone
Intraop OR Post op dose:
Onset:
Duration:

A

Intraop OR Post op dose: 40 - 80 mcg
Onset: 1 - 5 min
Duration: 30 min

56
Q

Hydromorphone
Intraop, Post op:
Onset:
Duration:

A

Intraop, Post op: 1 - 4 mg, 1.5 - 4 mg
Onset: 5 - 15 min
Duration: 2 - 4 hrs

57
Q

What is the gold standard of opioids?
What god is it named after?

A

Morphine
Greek god of morpheus (1806)

58
Q

Which opioid does not have first pass in the lungs?

59
Q

How is morphine metabolized?
What is the active metabolite and its significance?

A
  • Glucuronidation in the kidneys.
  • Morphine-6-glucuronide = comprises only 5-25% of morphine metabolites but is an active anaglesic causing late resp depression.
60
Q

What would occur with morphine overdose in a renal failure patient?

A
  • Prolonged ventilatory depression
61
Q

Morphine analgesic potencey and slower speed of offset with ____

A

women more than men

62
Q

Elimination half-time is longer if morphine contains the ____

Take extra caution in giving this type to pts with _____

A

morphine-3-glucuronide

renal dysfunction

63
Q

What receptors does meperidine agonize?

A
  • μ and κ receptors
  • α2 receptors as well
64
Q

What are the analogues of meperidine?
What other drugs does meperidine have a similar organic structure to?

A
  • Fentanyl & it’s derivatives
  • Lidocaine (tertiary amine, ester group, and lipophilic phenyl group) & Atropine
65
Q

How potent is Meperidine?
How long does it last?

A
  • 10% as potent as morphine
  • Duration: 2-4 hours
66
Q

What is the primary indication for meperidine?
What dose is used?

A
  • Post-operative shivering
  • 12.5 mg IV
67
Q

When should meperidine not be used?

A
  • Bronchoscopies (promotes coughing)
  • diarrhea
  • cough suppressant
68
Q

meperidine metabolism is by

A

Hepatic 1st pass = 80%
90% hepatic –> normeperidine

69
Q

T/F: Withdrawal symptoms develop more rapidly with morphine than with Meperidine.

70
Q

Demerol is ____ protein bound

A

60%

Caution in the elderly

71
Q

Meperidine elimination half time

A

3-5 hours
35 hours with renal failure pt

72
Q

How potent is fentanyl?

A
  • 75 - 125 x morphine.
73
Q

What is the blood-brain equilibration of fentanyl?
What does this mean?

A
  • 6.4 minutes
  • Potent with rapid onset and ↑ lipid solubility.
74
Q

What percent of fentanyl is subject to lung first-pass effect?
What does this mean?

A
  • 75%
  • Drug is taken up into lung tissue and possibly subjected to breakdown via pulmonary esterases.
75
Q

Where is fentanyl metabolized?
What is its principal metabolite?

A
  • Liver via CYP3A
  • Norfentanyl
76
Q

The following definition is known as ____

“Drug gets retained/accumulated and removed/cleared/metabolized at a specific location in the body that result in a reduced concentration of the active drug upon reaching its site of action”

A

First pass effect

77
Q

How does fentanyl dosing change for the elderly or liver patients?

A

No change in elderly or cirrhotic patients.

according to the book. He said gives less in elderly

78
Q

Describe what the graph below is showing.

A

Fentanyl has the greatest context-sensitive half-time of any of the fentanyl derivatives.

79
Q

What is the reason for the context-sensitive half time of fentanyl?

A

d/t the saturation of inactive tissue –> return to plasma replaces those metabolized

80
Q

What is the analgesia dosage of fentanyl?
Induction dose?

A
  • Analgesia: 1 - 2 μg/kg IV
  • Induction: 1.5 - 3 μg/kg IV 5 min prior to induction
81
Q

dose of fentanyl with inhaled anesthetics as an adjunct

A

2 - 20 µg/kg IV

82
Q

Dose of fentanyl if ONLY giving it SOLO for surgical anesthesia:

A

50 - 150 mcg/kg IV

83
Q

1mg of PO fentanyl = ____ mg of IV morphine

84
Q

What is the intrathecal dosage of fentanyl?

85
Q

What is the adult oral dose of fentanyl?
Pediatric?

A
  • Adult: 5 - 20 mcg/kg
  • Peds: 15 - 20 mcg/kg
86
Q

What is the transdermal dose of fentanyl?

A
  • 75 - 100 μg (18 hours steady state)
87
Q

What cardiovascular side effects should be known about fentanyl?
What CNS side effects should be known?

A
  • ↓BP & ↓CO
  • Can cause seizures
  • depressed carotid sinus baroreceptor reflex (graph)
  • Can cause muscle or chest wall rigidity (Sufentanil does as well)
88
Q

Does fentanyl increase or decrease ICP?

A

Increase by 6 - 9 mmHg

89
Q

How much more potent is sufentanil than fentanyl?

A
  • 5-12 times more potent.
90
Q

How much of sufentanil is subject to first pass effects?

A
  • 60% lung first-pass
91
Q

How much of sufentanil is protein bound? What protein is it bound to?
Vd compared to fentanyl?

A

92.5% α-1 acid glycoprotein bound.

Smaller Vd than fentanyl

92
Q

What is the analgesia dose of sufentanil?

A
  • Analgesia: 0.1 - 0.4 μg/kg IV
93
Q

What is the induction dose of sufentanil?

A

18.9 mcg/kg IV

What an odd number

I don’t think that this is right, a quick google search shows completely different numbers.

94
Q

What is the potency of alfentanil?
What is its onset?

A
  • 20% as potent as fentanyl
  • Onset: 1.4 min (faster than all derivatives except remifentanil)
95
Q

Is Alfentanil more or less lipid soluble than fentanyl?

A

Less lipid solube
- 90% nonionized at normal pH –> lower lipid solubility

96
Q

What is the alfentanil induction dose?
What about laryngoscopy dose?
What about maintenance?

A
  • Induction alone: 150 - 300 mcg /kg IV
  • with Laryngoscopy: 15 - 30 mcg/kg IV
  • Maintenance: 25 - 150 mcg/kg/hr with inhaled anesthetics
97
Q

What drug can cause acute dystonia when given to a Parkinson’s patient?

A

Alfentanil

98
Q

Which drug is 15 - 20 times as potent as Alfentanil?

A

Remifentanil

99
Q

What receptor affinity does remifentanil have?
How potent is it?

A

μ opioid agonist that is equipotent to fentanyl

with less context sensitve half time than fent

100
Q

What is remifentanil’s structure and why is it important?

A

Ester Structure = hydrolyzed by plasma & tissue esterases.

  • Rapid onset & recovery (15 min offset)
  • Very titratable
  • No accumulation
101
Q

What drug was said to be a great choice for carotid procedures in lecture? (carotid endarterectomy)

A

Remifentanil

102
Q

Answer the following characteristics of remifentanil below:
Clearance:
Peak effect:

A
  • Clearance: 3-L/min (8x faster than alfentanil)
  • Peak or Blood/brain equilibration: 1.1 min (fastest fentanyl derivative) (Table 7.4)
103
Q

What is the induction dose of remifentanil?

A
  • 0.5 - 1 mcg/kg IV over 1 min
104
Q

How is remifentanil dosed by weight?

105
Q

Remifentanil can cause ______ ______ of ventilation with propofol

A

Synergistic depression

106
Q

What is the maintenance dosing of remifentanil?

A
  • 0.005 - 2 μg/kg/min IV
107
Q

Remifentanil side effects: (5)

A
  • Seizure like activity
  • N/V
  • Depression of ventilation
  • Decreased BP and HR
  • Hyperalgesia d/t previous large dose opioid use and tolerance
108
Q

How potent is hydromorphone?
What dose should be given?
What benefits does hydromorphone have over morphine?

A
  • 5x more potent than morphine
  • 0.5mg → 1-4 mg total
  • No histamine release & no active metabolites.
109
Q

Before stopping Remifentanil, give a

A

longer acting opioid

110
Q

Why is codeine not given IV?

A
  • Induced hypotension via histamine release.
111
Q

What is the dose of codeine for cough suppression?
Analgesia?

A
  • Cough: 15mg
  • Analgesia: 60mg (= about 5mg morphine)
112
Q

Which opioid is most cleared?

A
  • Remifentanil (3-4L/min)
113
Q

Which opioid(s) is/are the most protein bound?
Which is the least?

A
  • Sufentanil, alfentanil, & remifentanil
  • Least = morphine
114
Q

Which opioid is the highest percent non-ionized at pH of 7.4?

A
  • Alfentanil (89%)
115
Q

Morphine tends to relieve _____ type pain more than _____ type pain.

A

Dull: sharp

116
Q

Other opioid agonists: (6)

A

Oxymorphone
oxycodone
methadone - (used in opioid withdrawal and chronic pain)
Propoxyphene
Tramadol - Interacts with coumadin
Heroin

117
Q

What is the most important factor to consider when determining onset of action? (table 7.4)

A

Effect-Site
(blood/brain equilibration time in min.)

118
Q

which opioid has the largest partition coefficient?

A

Sufentanil (1,727)

119
Q

which opioid has the smallest partition coefficient?

A

Morphine (1)

120
Q

which opioid has the fastest clearance?

A

Remifentanil

121
Q

which opioid has the slowest clearance?

A

Alfentanil (238 mL/min)

122
Q

which opioid has the smallest volume of distribution?

A

Alfentanil (27L)

123
Q

which opioid has the largest Vd?

A

Fentanyl (335L)

124
Q

which opioid has the shortest context sensitive half-time?

A

Remifentanil

125
Q

which opioid has the slowest Effect-site time?

A

Fentanyl (6.8 min or 6.4 min)

(Steele) Anesthesia Pharm Grayson (Spring 2023) (20 decks)

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