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GI II Exam 1. > Lecture 6 - Treatment of Nausea and Vomiting > Flashcards

Lecture 6 - Treatment of Nausea and Vomiting Flashcards

1
Q

Serotonin (5-HT3) Receptor Antagonists have which suffix?

A

-setron

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2
Q

List the 4 Serotonin (5-HT3) Receptor Antagonists used as antiemetics.

A
  • Dolasetron
  • Granisetron
  • Ondansetron
  • Palonosetron
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3
Q

What is the most worrisome adverse effect of using the Serotonin (5-HT3) Receptor Antagonists?

Caution must be taken in which patients?

A
  • Dose-dependent QT prolonation and Torsade’s
  • Pts already on QT prolonging agents (i.e., anti-arrhythmics) or in those w/ electrolyte imbalances (i.e., hypokalemia or hypomagnesemia)
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4
Q

Which Serotonin (5-HT3) Receptor Antagonists used as antiemetics have longer half-lives?

Useful in which patients?

A
  • Palonosetron

- Sustained-release formula of Granisetron (SQ)

  • Effective for delayed-CINV as a SINGLE dose
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5
Q

Which 2 classes of drugs have the potential for adverse interactions when given with Serotonin (5-HT3) Receptor Antagonists as antiemetics?

A

1) QT-prolonging agents
2) Antiarrhythmics

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6
Q

Which Neurokinin (NK1) Receptor Antagonist is the only one given up to 3 hours before anesthesia induction for prophylaxis of post-operative N/V?

A

Aprepitant

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7
Q

The Neurokinin (NK1) Receptor Antagonists used as antiemetics end in which suffix?

A

-pitant

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8
Q

List the 5 Neurokinin (NK1) Receptor Antagonists used as antiemetics?

A
  • Aprepitant
  • Fosaprepitant (pro-drug)
  • Netupitant
  • Fosnetupitant (pro-drug)
  • Rolapitant
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9
Q

Which 2 Neurokinin (NK1) Receptor Antagonists used as antiemetics are used as combo-only?

Which drug are they combined with?

A
  1. Netupitant
  2. Fosnetupitant
    - Combo w/ Palonosetron (5-HT3 receptor antagonist)
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10
Q

Which NT typically binds Neurokinin (NK1) Receptor?

A

Substance P

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11
Q

Which Histamine (H1) receptor antagonist is used for pregnancy induced N/V?

In combo with?

A

Doxylamine w/ pyridoxine (B6)

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12
Q

Which 2 Histamine (H1) receptor antagonists are only used for motion sickness/vertigo?

A
  1. Meclizine
  2. Cyclizine
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13
Q

Histamine (H1) receptor antagonists also have which type of properties (i.e., bind another receptor) at which level in the brain?

A
  • Anticholinergic
  • At level of chemoreceptor trigger zone (CTZ)
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14
Q

What are some of the adverse effects of Histamine (H1), Dopamine (D2), and Muscarinic (M1) receptor antagonists used as antiemetics?

A
  • Classic anticholinergic effects!
  • Drowsiness (CNS depression)
  • Dry mouth
  • Constipation + Urinary retention
  • Blurred vision
  • Decreased BP
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15
Q

Which drug interactions must you be careful with when using Histamine (H1) receptor antagonists?

A

Other agents that induce anticholinergic-related effects (cumulative)

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16
Q

Which anti-emetic/class can be used in pts with Diabetic Gastroparesis/Dysmotility to enhance GI motility and also increase LES tone?

How does it do this?

A
  • Metoclopramide (D2 receptor antagonist)
  • Stimulates ACh actions in GI

*No impact on GI secretions*

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17
Q

Scopolamine acts on which receptor?

A

M1 receptor antagonist

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18
Q

What is Scopolamine most commonly used for and how is this drug given?

A
  • Motion sickness
  • Transdermal patch (worn for 72 hours)
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19
Q

What are the 2 cannabinoid receptor agonists used as anti-emetics?

A
  • Dronabinol (C-III)
  • Nabilone (C-II)
20
Q

How potent are Cannabinoid Receptor Agonists and when are they used clinically as antiemetics?

A
  • Strong antiemetic effects
  • Reserved for treatment-resistant CINV
21
Q

For a high-emetogenic chemotherapy regimen, what is the standard 3-drug treatment used for anti-emetic effects?

A
  1. NK1 receptor antagonist (any)
  2. 5-HT3 receptor antagonist (any)
  3. Corticosteroid (Dexamethasone)
22
Q

When should the 3-drug anti-emetic regimen given alongside a high-emetogenic chemotherapy?

A
  • Give day of (prior to) chemotherapy (for acute N/V)
  • And for 3 days after chemotherapy (for delayed N/V)
23
Q

If the 3-drug anti-emetic regimen is not working for someone on a high-emetogenic chemotherapy tx, which drug should be added to increase it to a 4-drug regimen?

May also give what for treatment-resistance?

A

- Olanzapine (D2 antagonist) –> increase to 4-drug regimen

- Cannabinoid if treatment-resistance

24
Q

Therapy for which type of N/V possibly seen during a high-, moderate-, low-, or minimal-emetogenic chemotherapy regimens should be given to ALL patients?

A

Breakthrough N/V = occuring in between scheduled doses

25
Q

For a moderate-emetogenic chemotherapy regimen, what is the standard 2-drug treatment used for anti-emetic effects?

A
  1. 5-HT3 receptor antagonist
  2. Corticosteroid (Dexamethasone)
26
Q

When should the 2-drug anti-emetic regimen be given alongside a moderate-emetogenic chemotherapy?

A
  • Give day of (prior to) chemotherapy (for acute N/V)
  • For 2 days after chemotherapy (for delayed N/V)
27
Q

For pregnancy-induced N/V which 3 drugs should you try first (not in combo)?

A
  1. Vitamin B6 or
  2. Histamine Antagonist (w/ Vit. B6) = Doxylamine w/ B6; or
  3. 5-HT3 Antagonist
28
Q

Which drugs, if necessary, may be added to the standard 2-drug anti-emetic regimen in a patient undergoing a moderate-emetogenic chemotherapy treatment?

A
  • May add NK1 antagonist or olanzapine, if necessary (increase to 3-drug regimen)
  • May add cannabinoid in treatment-resistance (increase to 4-drug regimen after going up to 3-drug regimen)
29
Q

For a low-emetogenic chemotherapy regimen, what is the standard 1-drug treatment used for anti-emetic effects?

A
  1. Corticosteroid (Dexamethasone) OR
  2. 5-HT3 receptor antagonist OR
  3. Metoclopramide (D2 receptor antagonist) OR
  4. Prochlorperazine (D2 receptor antagonist)
30
Q

When should the 1-drug anti-emetic regimen be given to someone on a low-emetogenic chemotherapy regimen?

A

Given day of (prior to) chemotherapy (for acute N/V)

31
Q

What is the recommendation for giving anti-emetics to someone receiving a minimal-emetogenic chemotherapy treatment?

A

- No routine prophylaxis therapy recommended

  • Provide therapy for breakthrough N/V for all patients
  • Provide therapy for anticipatory N/V, as needed
32
Q

Based on the NCCN guidelines, what is the general principle of treating breakthrough N/V associated with chemotherapy?

A

Add one agent from a different drug class to the current regimen

33
Q

Which 3 anti-emetic drugs can be used for Motion Sickness?

A
  1. Scopolamine (patch) or
  2. Dimenhydrinate (H1 receptor antagonist) or
  3. Meclizine (H1 receptor antagonist)
34
Q

Which 2 anti-emetics can be used for Vertigo?

A
  1. Meclizine (H1 receptor antagonist)
  2. Cyclizine (H1 receptor antagonist)
35
Q

Which two NK1 receptor antagonists have moderate-major active metabolites, and longer half-lives?

A
  1. Netupitant
  2. Rolapitant
36
Q

Which H1 receptor antagonist used as an anti-emetic is metabolized to the active metabolite, cetirizine, and can be given as an IM injection?

A

Hydroxyzine

37
Q

IV administration of which H1 receptor antagonist as an anti-emetic requires dilution and a lower dose (than oral)?

A

Promethazine

38
Q

What are the four D2 receptor antagonists used as anti-emetics?

A
  1. Chlorpromazine
  2. Perphenazine
  3. Prochlorperazine
  4. Metoclopramide
39
Q

Which 3 classes of drugs used as anti-emetics also have anticholinergic properties?

A
  1. Histamine (H1) receptor antagonists
  2. Dopamine (D2) receptor antagonists
  3. Muscarinic (M1) receptor antagonists
40
Q

Which 3 drug-drug interactions must you consider when using Dopamine (D2) receptor antagonists as anti-emetics?

A
  1. Other agents that induce anticholinergic-related side effects (cumulative)
  2. Antiarrhythmics (esp. QT-prolonging agents)
  3. Anti-Hypertensives
41
Q

Which drug class used as anti-emetics are scheduled drugs and have limits on quantity/refills?

A

Cannabinoids receptor agonists (i.e., Dronabinol and Nabilone)

42
Q

Cannabinoid receptor agonists act through which kind of receptor?

Results in?

A
  • GPCR
  • Decreased excitability of neurons
  • Minimize 5-HT3 release from vagal afferent terminals
43
Q

Which cannabinoid receptor agonist has a large first-pass effect and is metabolized to one active metabolite?

A

Dronabinol

44
Q

Which drug-drug interactions must you consider when giving cannabinoid receptor agonists as anti-emetics?

A
  • Other CNS depressants
  • Cardiovascular agents
  • Sympathomimetic’s
45
Q

Which 5-HT3 receptors antagonist used for N/V comes in a PO/IV, transdermal (cutaneous) patch, and extended release SQ injection?

A

Granisetron

GI II Exam 1. (25 decks)

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