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Gastrointestinal II Exam #1 > Anti-emetic and Anti-nausea Drugs > Flashcards

Anti-emetic and Anti-nausea Drugs Flashcards

1
Q

What suffix of drugs are serotonin (5-HT3) receptor antagonists?

A

-setron

Dolastron
Granisetron
Ondansetron
Palanosetron

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2
Q

How effective are serotonin (5-HT3) receptor antagonists?

What were they initially developed for?

What is the MOA?

A

Strong anti-emetic agents

Developed for chemo-induced N/V (CINV)

Block serotonin type-3 at vagal n. terminals and blocks transmission to CTZ. Also blocks serotonin release from intestinal enterochromaffin cells.

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3
Q

What are some therapeutic uses for serotonin (5-HT3) receptor antagonists? (4)

A

CINV
Radiation induced NV (RINV)
Post-op NV (PONV)
NV of pregnancy (NVP)

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4
Q

What are some adverse effects of serotonin (5-HT3) receptor antagonists? (3)

Which one is most worrisome?

A

CNS (HA)
GI (constipation/vomiting) - Serotonin syndrome
Dose-dependent QT prolongation (Torsades) - most worrisome

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5
Q

Which serotonin (5-HT3) receptor antagonists have long half-lives?

A

Palonostron

Sustained-release formulation of Granisetron (SQ)

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6
Q

What are 2 drug interactions in serotonin (5-HT3) receptor antagonists?

A

QT-prolonging agents

Anti-arrhythmics

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7
Q

What suffix of drugs are neurokinin (NK1) receptor antagonists?

A

-pitant

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8
Q

Which 2 neurokinin (NK1) receptor antagonists are used only in combo with Palonostron?

A

Netupitant

Fosnetupitant

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9
Q

What is the strength of neurokinin (NK1) receptor antagonists?

What is the MOA?

A

Moderate anti-emetic agents

Blocks neurokinin1 (supstance P) receptors in CTZ/VC

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10
Q

What are 2 therapeutic uses of neurokinin (NK1) receptor antagonists?

A

Chemo-induced NV (CINV) - most effective when used with glucocorticosteroid and 5-HT3 antagonist

Prophylaxis of post-op NV (PONV) - only Aprepitant

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11
Q

What suffices of drugs are histamine (H1) receptor antagonists?

A
  • amine
  • inate
  • zine
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12
Q

What is Doxylamine given with?

A

Pyridoxine (B6)

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13
Q

What is the strength of histamine (H1) receptor antagonists?

What is the MOA?
What properties do some of these agents exhibit?

A

Weak anti-emetic drugs

Blockade of H1 receptor in VC and vestibular system.
Agents exhibit varying levels of central anticholinergic properties at level of CTZ.

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14
Q

What are some therapeutic uses of histamine (H1) receptor antagonists?

A

Mild NV
PONV
NVP (doxylamine/B6)
Motion sickness

Add on to CINV and RINV

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15
Q

What are the side effects of histamine (H1) receptor antagonists?

A

Classic anti-cholinergic effects: drowsiness, dry mouth, constipation, urine retention, blurred vision, etc.

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16
Q

What are drug interactions with histamine (H1) receptor antagonists?

A

Other agents that also induce anticholinergic effects

17
Q

What are the 2 types of drugs that are dopamine (D2) receptor antagonists?

A

Phenothiazines: Chlorpromazine, Perphenazine, Prochlorperazine

Metoclopramide

18
Q

What is the strength of dopamine (D2) receptor antagonists?

What is the MOA?
What unique MOA does Metoclopramide have?

A

Weak to moderate

Block D2 receptors in CTZ

Metclopramide can also stimule ACh actions in GI and enhance motility and increase LES tone.

19
Q

What are some therapeutic uses for dopamine (D2) receptor antagonists?

A 
Mild NV
Gastroparesis/dysmotility (metoclopramide)
PONV
NVP
CINV
RINV
20
Q

What are the adverse effects of dopamine (D2) receptor antagonists?

A

Classic anti-cholinergic effects: drowsiness, dry mouth, constipation, urine retention, blurred vision, etc.

21
Q

What are the major drug interactions for dopamine receptor antagonists? (3)

A

Other agents that induce anticholinergic-related side effects

Anti-arrhythmics

Anti-hypertensives

22
Q

What is the MOA of Scopolamine?

A

Muscarinic (M1) receptor antagonist

23
Q

What is the strength muscarinic receptor blockers?

What’s it used for mostly?

How long is the patch worn for?

What kind of properties does it have?

A

Weak

Motion sickness

72 hrs.

Significant anti-cholinergic properties

24
Q

What are the side effects of muscarinic receptor blockers?

What is a common drug interaction?

A

Classic anti-cholinergic effects

Only agents that also induce anti-cholinergic related side effects

25
Q

What are the 2 cannabinoid receptor agonists?

A

Dronabinol

Nabilone

26
Q

What is the strength of cannabinoid receptor agonists?

What are they reserved for?

What is the MOA?

A

Strong

Treatment-resistant CINV

Decreases excitability of neurons

27
Q

What are some side effects of cannabinoid receptor agonists?

A 
Euphoria/irritability
Vertigo
Sedation
Dry mouth
Impaired memory
28
Q

What are some drug interactions of cannabinoid receptor agonists? (3)

A

CNS depressants
Cardiovascular agents
Sympathomimetics

29
Q

Post-chemo

When does acute NV occur?

When does chronic NV occur?

When does anticipatory NV occur?

What should proper therapy focus on?

A

Acute - <24 hrs after chemo

Chronic - >24 hrs after chemo

Anticipatory - before chemo given

Focus on prevention!

30
Q

What is the high-emetic regimen? (3-drug regimen)

What can be given if the pt. does not respond?

When is it given?

A

NK1 receptor antagonist
5-HT3 receptor antagonist
Corticosteroid (Dexamethasone)

Can give a 4th drug: D2 antagonist or cannabinoid

Prior to chemo and for 3 days

31
Q

What is the moderate-emetogenic regimen? (2-drug regimen)

What can be given if the pt. does not respond?

When is it given?

A

5-HT3 receptor antagonist (Palanos/Granis SQ)
Corticosteroid (Dexamethasone)

May add NK1 (3 drug regimen), may add cannabinoid (4 drug)

Prior to chemo and for 2 days

32
Q

What is the low-emetogenic regimen? (1-drug regimen)

When is it given?

A

One of: Corticosteroids, 5-HT3 receptor antagonist, Metoclopramide or Prochlorperazine

Given prior to chemo only

33
Q

What are 3 drug options to treat motion sickness?

A

Scopolamine
Dimenhydrinate
Meclizine

34
Q

What are 2 drug options to treat vertigo?

A

Meclizine

Cyclizine

35
Q

What drug will treat diabetic gastroparesis (dysmotility)?

A

Metoclopramide

36
Q

What type of therapy should be given in PINV?

A

Stepped-therapy

  1. Vit B6 or H1 antagonist (w/ Vit B6) or 5-HT3 antagonist
  2. D2 antagonist
  3. Steroid or a different D2 antagonist

Gastrointestinal II Exam #1 (19 decks)

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