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KM (Spring 2024) COPY of Anesthesia Pharm (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

Differentiate opioids from narcotics.

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

S7

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3
Q

What two types of opioid chemical structures are there?

A
  • Phenanthrenes
  • Benzylisoquinolines

S8

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4
Q

What types of drugs are Phenanthrenes?

A

Morphine & codeine

S8

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5
Q

What types of drugs are Benzylisoquinolines?

A

Papaverine

S8

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6
Q

What is Papaverine mostly used for?

A

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

S8

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7
Q

What portions of the brain are the source of Descending Inhibitory Signals?

A
  • Thalamus
  • PAG
  • Locus Coeruleus

S9

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8
Q

What endogenous substances have the same effect on receptors as Opioids?

A

Endorphins, Enkephalins, and Dynorphines.

S10

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9
Q

Presynaptic inhibition of what neurotransmitters occurs with Opioid administration?

A
  • Substance P
  • ACh
  • NE
  • Dopamine

S10

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10
Q

How do Opioids modulate pain at the cellular level?

A
  • ↑ K⁺ conductance (hyperpolarization)
  • Ca⁺⁺ channel inactivation

S10

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11
Q

Where are Opioid receptors located in the brain?

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

S11

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12
Q

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

A

Substantia gelatinosa (aka Laminae 2)

where local anesthetics work

S11

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13
Q

Where is/are Opioid receptors found outside the CNS?

A

Sensory neurons & immune cells

S11

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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)

S12

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15
Q

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

A
  • Μu2
  • δ

S12

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16
Q

Which receptors are responsible for constipation?

A
  • Μu2 (primarily)
  • δ (less)

S12

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17
Q

Which receptors can cause urinary retention?

A
  • Μu1
  • δ (delta)

S12

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18
Q

Are there any receptors that cause diuresis when bound?

A

κ (Kappa)

S12

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19
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.

S12

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20
Q

What opioid receptors have low abuse potential when bound?

A

Μu1 and κ

S12

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21
Q

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

A

Mu1

S12

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22
Q

What agonists bind to the four opioid receptors?

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

S12

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23
Q

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

A
  • ↓SNS tone = ↓BP, VR, and CO & Orthostatic hypotension and sycope
  • ↓HR + histamine release = ↓BP

+ N2O or Benzo = CV depression

S12

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24
Q

What possible cardiovascular benefits do Opioids provide?

A

Myocardial ischemia protection
(won’t cause myocardial depression)

S13

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25
Q

What are the respiratory effects of Opioids?

A
  • Depressed CNS response to CO₂ causing a right shift of PaCO₂ (↑)

S14

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26
Q

What are the syptoms of Opioid overdose?

A

- apnea
- miosis
- hypoventilation
- coma

S14

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27
Q

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

A

Physostigmine would by increasing CNS levels of ACh

S14

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28
Q

What is normal PaO₂?

A

Normal PaO₂ is 80 mmHg

S15

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29
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 (need higher CO2 to make them breath)

S15

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30
Q

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

A

Opioids ↓CBF and possibly ↓ICP

S16

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31
Q

What can happen when large doses of Opioid is given?

A

Myoclonus

S16

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32
Q

What musculoskeletal abnormality occurs with Opioid administration?
What makes this condition worse?
How is it treated?

A

-Skeletal chest wall and abdominal muscle rigidity

  • Mechanical ventilation makes it worse
  • treat with Muscle relaxants and/or naloxone

S16

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33
Q

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

A
  • Biliary smooth muscle spasm

caused by:
- Fentanyl (99%),
- Morphine (53%)
- Meperidine (61%).

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

S17

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34
Q

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

A
  • Naloxone
  • Glucagon (2mg IV given incrementally) and causes no opioid antagonism.
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35
Q

What drugs should be used for ERCP cases?

A
  • Non-opioids (multimodal approach w/ NSAIDs, gabapentin, etc.)
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36
Q

What is the side effect on GU with Opioids?

A

urinary urgency

S19

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37
Q

What are the effects on cutaneous with Opioid?

A

flushed face, neck, & upper chest
d/t Histamine release

S19

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38
Q

What are the side effects on the placenta with Opioids?

A
  • neonate depression
  • dependence (chronic)

S19

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39
Q

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

A
  • 2-3 weeks
  • 25 days with Morphine
  • Downregulation (↓ opioid receptors) causes tolerance

S20

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40
Q

What negative change can develop between all opioids?

A

Cross-tolerance

S20

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41
Q

Morphine is ____ standard with opioids

A

Gold standard

S27

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42
Q

What effects does Morphine have?

A
  • Analgesia
  • euphoria
  • sedation,
  • diminished ability to concentrate
  • nausea
  • feeling of body warmth
  • heaviness of extremities,
  • dryness of the mouth
  • pruritis.

S27

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43
Q

What areas of the body does Morphine relieve?

A
  • visceral
  • skeletal muscles
  • joints and integumental dull > sharp
  • intermittent pain

S27

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44
Q

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

A

Dull: sharp

S27

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45
Q

What is the dosage of Morphine?

A

1 - 10 mg IV

S22/28

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46
Q

What is the onset of Morphine?

A

10 - 20 mins

S28

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47
Q

What is the IM and IV peak of Morphine?

A

IM: 45 to 90 mins

IV: 15-30 mins

S28

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48
Q

What is the duration of Morphine?

A

4-5 hours

S28

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49
Q

What are the first past effects of Morphine in the liver and lungs?

A
  • PO Hepatic 1st Pass: 25%.
  • No first pass uptake in lungs

S28

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50
Q

Where does Morphine accumulate rapidly?

A
  • kidneys
  • liver
  • skeletal muscles

S28

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51
Q

How is Morphine metabolized?
What are the metabolites and their significance?

A
  • Glucuronidation in the liver

metabolites:
- Morphine-6-glucuronide = (5-25%) but is an active anaglesic causing late resp depression.

  • Morphine-3-glucuronide (75% to 95%) but inactive

S29

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52
Q

What is the elimination 1/2 time of Morphine?

A

longer with morphine-3-glucuronide

S30

53
Q

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

A

Prolonged ventilatory depression.

54
Q

Which gender has more analgesic potency and slower speed of offset with Morphine?

A

Women

S30

55
Q

What receptors does Meperidine agonize?

A
  • μ and κ receptors
  • α2 receptors as well

S31

56
Q

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

A

-Analogues: Fentanyl & it’s derivatives

  • structure similarity: Lidocaine & Atropine

S31

57
Q

How potent is Meperidine?
How long does it last?

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

S32

58
Q

What is the dose and primary indication for Meperidine?

A

12.5 mg IV for Post-operative shivering

S32/33

59
Q

What are the effects of Meperidine?

A
  • sedation
  • euphoria
  • N/V
  • depression of ventilation

S32

60
Q

What is the metabolism and how much is protein bound of Meperidine?

A

90 % hepatic metabolism
–> Normeperidine

60 % protein bound (consider with elderly)

S32

61
Q

What is the elimination profile of Meperidine?

A

Elimination: Renal (acidic urine can speed elimination)

Elimination 1/2 time: 3 to 5 hours (35 hours with renal failure)

S32

62
Q

What are the toxic effecs of Meperidine?

A
  • delirium (confusion, hallucinations)
  • myoclonus
  • seizures

S32

63
Q

When should Meperidine not be used?

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

S33

64
Q

What are the side effects of Meperidine?

A
  • tachycardia
  • mydriasis with dry mouth
  • (-) inotropy
  • serotonin syndrome (MAOIs & TCAs)
  • impaired ventilation
  • crosses placenta
65
Q

True or False: Meperidine develops withdrawal symptoms more rapidly than Morphine?

A

True

S33

66
Q

How potent is fentanyl?

A
  • 75 - 125 x Morphine.

S34

67
Q

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

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

S34

68
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.

S34

69
Q

What organs are reservoirs and affect the drug’s pharmacokinetics’ dispositional phase?

A

Lungs

S35

70
Q

What is removal of endogenous compounds form the pulmonary arterial blood?

A

Pulmonary Uptake/Extraction

S35

71
Q

What is the term for 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

Lung First-Pass

S35

72
Q

Where is fentanyl metabolized?
What is its principal metabolite?

A
  • Liver via CYP3A
  • Norfentanyl is the principal metabolite

S 36

73
Q

Where is Fentanyl excreted?

A

Kidneys

S36

74
Q

What is the Vd of Fentanyl?

A

Large Vd

IV ( < 5 mins 80% is gone)
–> highly vascular tissues
–> inactive tissue sites

S36

75
Q

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

A

No change in elderly or cirrhotic patients.

S36

76
Q

Describe what the graph below is showing.

A

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

d/t saturation of inactive tissue

S37

77
Q

What is the analgesia dosage of Fentanyl?

A

1 - 2 μg/kg IV

S38

78
Q

What is the induction dose of Fentanyl?

A

1.5 - 3 μg/kg IV

S38

79
Q

What is the dose of Fentanyl with inhaled anesthetics?

A

2 to 20 µg/kg IV

  • Direct laryngoscopy during intubation
  • Sudden changes in surgical stimulation level

S38

80
Q

What is the surgical anesthesia dose of Fentanyl?

A

50 to 150 µg/kg IV

S39

81
Q

What is the intrathecal dosage of Fentanyl?

A

25 mcg

S39

82
Q

What is the adult oral dose of Fentanyl?
Pediatric?

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

S39

83
Q

1mg of PO Fentanyl = ____ mg of IV Morphine

A

5

S39

84
Q

What is the transdermal dose of Fentanyl?

A

75 - 100 μg (18 hours steady state)

S39

85
Q

What cardiovascular side effects should be known about Fentanyl?

A
  • no histamine release
  • depress carotid sinus baroreceptor reflex
  • no significant bradycardia
  • ↓BP & ↓CO

S40

86
Q

What CNS side effects of Fentanyl should be known?

A
  • Can cause seizures
  • modestly increase ICP (6-9 mmHg)

S41

87
Q

What are synergism effects of Fentanyl?

A
  • Potentiate Benzodiazepines
  • Decrease dose requirements with Propofol

S41

88
Q

How much more potent is Sufentanil than Fentanyl?

A

5-12 times more potent.

S42

89
Q

How much of Sufentanil is subject to first pass effects?

A

60% lung first-pass

S42

90
Q

How much of Sufentanil is protein bound? What protein is it bound to?

A

92.5% α-1 acid glycoprotein bound.

S42

91
Q

What is the metabolism and excretion of Sufentanil?

A

Metabolism: hepatic

Excretion: renal and fecal (caution in chronic renal failure)

S42

92
Q

What is the context-sensitive half-time and Vd of Sufentanil?

A
  • Context-sensitive half-time: shorter
  • larger Vd > alfentanil

S42

93
Q

What is the analgesia dose of Sufentanil?

A

0.1 - 0.4 μg/kg IV

S43

94
Q

What is the induction dose of sufentanil?

A

18.9 mcg/kg IV

S43

95
Q

What is the intraop dose of Sufentanil?

A

0.3 to 1 µg/kg IV

S43

96
Q

What is the infusion dose of Sufentanil?

A

0.5 to 1 µg/kg/hr IV

S43

97
Q

What are the side effects of Sufentanil?

A
  • Bradycardia (↓ C.O.)
  • Rigidity chest wall and abdominal muscles)

S43

98
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)

S44

99
Q

What are the pharmacokinetics of Alfentanil?

A
  • Cirrhosis: prolongs elimination half-time
  • 90% nonionized at normal pH –> lower lipid solubility
  • Higher protein binding
  • Metabolite: Noralfentanil (Hepatic P450 3A4)

S44

100
Q

What is the Alfentanil induction dose?

A

Induction: 150 - 300 mcg /kg IV

S45

101
Q

What is laryngoscopy dose of Alfentanil?

A

15 - 30 mcg/kg IV (90 seconds prior)

S45

102
Q

What about is the maintenance dose of Alfentanil?

A

25 - 150 mcg/kg/hr with inhaled anesthetics

S45

103
Q

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

A

Alfentanil

S45

104
Q

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

A

μ opioid agonist that is equipotent to fentanyl

S46

105
Q

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

A

Ester Structure = hydrolyzed by plasma & tissue esterases.

  • Rapid onset & recovery
  • rapid titratable effect
  • No accumulation
  • rapid recovery when discontinued

S46

106
Q

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

A

Remifentanil

107
Q

What is the clearance of Remfentanil?

A

3-L/min
(8x faster than Alfentanil)

S47

108
Q

What is the peak effect of Remifentanil?

A

30 - 60 seconds

S47

109
Q

Where is Remifentanil excreted?

A

kidneys

(unchanged by renal or hepatic disease)

S47

110
Q

What is the elimination half-time of Remifentanil?

A

6.3 minutes

S47

111
Q

What is the induction dose of Remifentanil?

A

0.5 to 1 µg/kg IV over 30-60 seconds

S48

112
Q

What is the maintenance dosing of Remifentanil?

A
  • 0.005 - 2 μg/kg/min IV

S48

113
Q

What do you need to give before stopping Remifentanil?

A

give longer-acting opioid

S48

114
Q

What use is not recommended for Remifentanil?

A

spinal or epidural use

S48

115
Q

What are the side effects of Remifentanil?

A
  • Seizure-like activity
  • N/V
  • Depression of ventilation
  • Decreased BP and HR
  • Hyperalgesia d/t
    -Previous acute exposure to large opioid doses
    -Tolerance

S49

116
Q

How potent is Hydromorphone?
What benefits does hydromorphone have over morphine?

A
  • 5x more potent than morphine
  • No histamine release & no active metabolites.

S50

117
Q

What is the dose of Hydromorphone?

A

0.5mg → 1-4 mg total

Redose every 4 hours

S50

118
Q

Why is codeine not given IV?

A

Induced hypotension via histamine release.

119
Q

What is the elimination 1/2 time of Codeine?

A

3 to 3.5 hours

S51

120
Q

Where is Codeine metabolized?

A

Liver

S51

121
Q

What are the side effects of Codeine?

A
  • physical dependence
  • minimal sedation
  • N/V
  • constipation
  • dizziness

S51

122
Q

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

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

S51

123
Q

Which opioid is most cleared?

A

Remifentanil (3-4L/min)

S53

124
Q

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

A
  • most = Sufentanil, alfentanil, & remifentanil
  • least = morphine

S53

125
Q

Which opioid is the highest percent non-ionized?

A

Alfentanil

S53

126
Q

What are the other Opioid Agonists?

A
  • Oxymorphone
  • Oxycodone
  • Hydrocodone
  • Methadone
  • Propoxyphene
  • Tramadol
  • Heroin

S52

127
Q

Which Opioid Agonist is used in opioid withdrawal & chronic pain?

A

Methadone

S52

128
Q

What are the drug facts about Tramadol?

A
  • 5 -10x less (Morphine)
  • µ with weak κ & δ
  • PO: 3 mg/kg
  • Interacts with Coumadin

S52

129
Q

What are drug facts of Heroin?

A
  • More rapid onset
  • less N/V
  • great potential for dependency

S52

KM (Spring 2024) COPY of Anesthesia Pharm (Spring 2023) (103 decks)

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