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Anes Pharm (Spring 2025) Grayson Mixed > 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)
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3
Q

What two types of opioid chemical structures are there?

A
  • Phenanthrenes
  • Benzylisoquinolines
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4
Q

What types of drugs are Phenanthrenes?
What types of drugs are benzylisoquinolines?

A
  • Phenanthrenes: Morphine, Codeine, Thebaine
  • Benzylisoquinoline: Papaverine, Noscapine
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5
Q

What is papaverine mostly used for?

A

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

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6
Q

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

A
  • Thalamus
  • PAG
  • Locus Coeruleus
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7
Q

What endogenous substances have the same effect as opioids?

A

Endorphins, Enkephalins, and Dynorphines.

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8
Q

Presynaptic inhibition of what neurotransmitters occurs with opioid administration?

A
  • ACh
  • Dopamine
  • NE
  • Substance P
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9
Q

How do opioids modulate pain at the cellular level?

A
  • ↑ pK⁺ (hyperpolarization)
  • Ca⁺⁺ channel inactivation
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10
Q

Where are opioid receptors located in the brain?

A
  • PAG
  • Locus Ceruleus
  • RVM (rostral ventral medulla)
  • Hypothalamus
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11
Q

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

A

Interneurons and primary afferent neurons of the substantia gelatinosa (aka Laminae 2)

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12
Q

Where is/are opioid receptors found outside the CNS?

A
  • Sensory neurons & immune cells

Intraarticular morphine after knee surgery.

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13
Q

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

A
  • Μu1 (μ₁)
  • Μu2 (μ₂)
  • Κappa (κ)
  • Delta (δ)
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14
Q

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

A
  • Μu2 and δ
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15
Q

Which receptors are responsible for constipation?

A
  • Μu2 primarily
  • δ (less)

Μu2 (μ₂) receptors in the stomach cause peristalsis

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16
Q

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

A
  • Retention: Μu1 and δ
  • Diuresis: κ
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17
Q

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

A
  • False. Μu2 receptors only cause analgesia at the spinal cord level.
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18
Q

What opioid receptors have low abuse potential when bound?

A

Μu1 and κ

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19
Q

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

A

Μu1

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20
Q

What agonists bind to the four opioid receptors?
What about antagonists?

A
  • Mu1 & Mu2 = endorphins, morphine, synthetic opioids.
  • κ = dynorphins.
  • δ = enkephalins.
  • All receptors bound by same antagonists: Naloxone, Naltrexone, and Nalmefene
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21
Q

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

A
  • ↓CO, venous return, and BP D/T ↓SNS tone
  • ↓HR + histamine release = ↓BP\
  • Adding N20 or benzo = CV depression (CO & BP)

Orthostatic hypotension likely, as well as syncope

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22
Q

What possible cardiovascular benefits do opioids provide?

A
  • Myocardial ischemia protection (won’t cause myocardial depression) unless given with nitrous or benzo
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23
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 (↑PaCO2 at rest)
  • Cough suppression seen in Codeine and Dextromethorphan (no analgesia)
  • Overdose = apnea, miosis, ↓RR, coma.

Caution: Provocation of reflex coughing d/t pre-induction dose

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24
Q

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

A
  • Physostigmine would by increasing CNS ACh levels.

This will effectively antagonize ventilatory depression but not reverse analgesia like narcan.

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25
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, opiate use, and even sleeping?

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

Anything that would cause an increase in PaCO 2 at rest will cause a rightward shift

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26
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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27
Q

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

A
  • Opioids ↓CBF and possibly ICP

Myoclonus can occur with large doses

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28
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 (wooden chest syndrome).
  • Mechanical ventilation
  • Muscle relaxants and/or naloxone

Rigid chest is typically caused with rapid administration of opiates such as fentanyl.

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29
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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30
Q

What drugs should be used for ERCP cases?

A
  • Non-opioids (multimodal approach w/ NSAIDs, gabapentin, etc.)
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31
Q

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

A

Usually one of these:
- Glucagon (2mg IV given incrementally) and causes no opioid antagonism.
- Naloxone 40mcg IV
- Atropine 0.2mg IV
- Nalbuphine 10mg IV
- NTG 50mcg IV

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32
Q

What are some common GU side effects to opiates?
How about cutaneous or placental?

A
  • GU: urinary urgency
  • Cutaneous: histamine release leads to flushed face, neck, & upper chest.
  • Placenta: neonate depression and dependence (chronic use)
33
Q

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

A
  • 2-3 weeks (morphine is 25 days)
  • Downregulation of opioid receptors

Cross tolerance can develop between all opioids

34
Q

What is the dosage of morphine?
When does it peak?
How long does it last?

A
  • 1 - 10 mg IV
  • Peak: 15 - 30 minutes (IV) 45-90 minutes (IM)
  • Duration: 4-5 hours
35
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.
36
Q

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

A
  • Prolonged ventilatory depression.
37
Q

What receptors does meperidine agonize?

A
  • μ and κ receptors
  • α2 receptors as well
38
Q

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

A
  • Fentanyl & it’s derivatives
  • Lidocaine & Atropine
39
Q

How potent is Meperidine?
How long does it last?

A
  • 10% (1/10th) as potent as morphine
  • Duration: 2-4 hours
40
Q

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

A
  • Post-operative shivering
  • 12.5mg IV
41
Q

When should meperidine not be used?

A
  • Bronchoscopies (promotes coughing)
42
Q

How potent is fentanyl? (compared to morphine)

A
  • 75 - 125 x morphine.
43
Q

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

A
  • 6.4 minutes
  • Potent with rapid onset and ↑ lipid solubility.
44
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.
45
Q

Where is fentanyl metabolized?
What is its principal metabolite?

A
  • Liver via CYP3A
  • Norfentanil
46
Q

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

A

No change in elderly or cirrhotic patients.
- Caution with morphine use in renal and elderly patients b/c metabolites stick around longer in renal disease. Serum plasma concentrations increase with age.

47
Q

Describe what the graph below is showing.

A

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

Context-sensitive half-time describes the time it takes for the plasma concentration of a drug to decrease by 50% after an infusion is stopped.

48
Q

What is the analgesia dosage of fentanyl?
Induction dose?

A
  • Analgesia: 1 - 2 μg/kg IV
  • Induction: 1.5 - 3 μg/kg IV (5min prior)
49
Q

What Fentanyl dose is used as an adjunct with inhaled anesthetics?

A

2 - 20 μg/kg IV
Used in cases of :
- Direct laryngoscopy during intubation
- Sudden changes in surgical stimulation level

50
Q

1mg of PO fentanyl = ____ mg of IV morphine

A

5

IV fentanyl is 75-125x as potent as morphine.

51
Q

What is the intrathecal dosage of fentanyl?

52
Q

What is the adult oral dose of fentanyl (transmucosal)?
Pediatric (rapid dissolving film/lozenges)?

A
  • Adult: 5 - 20 mcg/kg
  • Peds (2-8yr olds): 15 - 20 mcg/kg 45min prior
53
Q

What is the transdermal dose of fentanyl?

A
  • 75 - 100 μg (18 hours steady state)
54
Q

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

A
  • ↓BP & ↓CO (depressed carotid sinus baroreceptor reflex)
  • Can cause seizures (doses>30 μg/kg IV) & modestly increase ICP (6-9mmHg).
55
Q

How much more potent is sufentanil than fentanyl?

A
  • 5-12 times more potent.
56
Q

How much of sufentanil is subject to first pass effects?

A
  • 60% lung first-pass
57
Q

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

A

92.5% α-1 acid glycoprotein bound.

58
Q

What is the analgesia dose of sufentanil?

A
  • Analgesia: 0.1 - 0.4 μg/kg IV
59
Q

What is the induction dose of sufentanil?

A

18.9 mcg/kg IV

What an odd number but it is referenced directly in the text.

60
Q

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

A
  • 20% (1/5th) as potent as fentanyl
  • Onset: 1.4 min (faster than all derivatives except remifentanil)
61
Q

What is the alfentanil induction dose?
What about laryngoscopy dose and when should it be given?
What about maintenance?

A
  • Induction Alone: 150 - 300 mcg /kg IV
  • Laryngoscopy (give 90sec prior): 15 - 30 mcg/kg IV
  • Maintenance: 25 - 150 mcg/kg/hr with inhaled anesthetics
62
Q

Considering Alfentanil’s pharmacokinetics, would you give it to a cirrhotic patient? Does alfentanil have any metabolites?

A
  • Yes but remember that Cirrhosis patients result in a longer elimination half-time
  • Metabolite: noralfentanil (hepatic P450 3A4)

  • Higher protein binding: same with sufentanil
  • 90% nonionized at normal pH –> lower lipid solubility
63
Q

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

A

Alfentanil

64
Q

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

A

μ opioid agonist that is equipotent to fentanyl

65
Q

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

A

Ester Structure = hydrolyzed by plasma & tissue esterases.

  • Rapid onset & recovery (15min)
  • Very titratable
  • No accumulation
66
Q

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

A

Remifentanil

67
Q

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

A
  • Clearance: 3-L/min (8x faster than alfentanil)
  • Peak: 1.1 min (fastest fentanyl derivative)
68
Q

What is the induction dose of remifentanil?

A
  • 0.5-1 mcg/kg IV over 30-60sec
69
Q

What is the maintenance dosing of remifentanil?

A

0.25-1μg/kg IV
OR
- 0.005 - 2 μg/kg/min IV

70
Q

What is the recommended spinal dose for Remifentanil?

A

Trick question, Remifentanil is NOT recommended for spinal or epidural use :)

71
Q

What are the primary S/E of Remifentanil?

72
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.
73
Q

Why is codeine not given IV?

A
  • Induced hypotension via histamine release.
74
Q

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

A
  • Cough: 15mg
  • Analgesia: 60mg (= about 5mg morphine)
75
Q

Which opioid is most cleared?

A
  • Remifentanil (3-4L/min)
76
Q

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

A
  • Sufentanil, alfentanil, & remifentanil
  • Least = morphine
77
Q

Which opioid is the highest percent non-ionized?

A
  • Alfentanil
78
Q

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

A

Dull: sharp

Anes Pharm (Spring 2025) Grayson Mixed (20 decks)

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