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GI Week 1 > Anti-nausea and Anti-emetic Drugs > Flashcards

Anti-nausea and Anti-emetic Drugs Flashcards

1
Q

Dolasetron, Granisetron, Ondansetron, and Palonosetron make up what class of medication?

A

Serotonin 5-HT3 receptor antagonists

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2
Q

The 5-HT3 receptor antagonists block the receptors at what nerve terminal?

It also blocks serotonin-receptor activation after serotonin release
from what cells?

A

1) Vagal nerve terminal

2) Intestinal enterochromaffin cells

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3
Q

What is the most worrisome adverse effect of Serotonin 5-HT3 receptor antagonists?

Which specific drug has the highest risk for this and is no longer recommended for CINV prophylaxis?

A

1) Dose-dependent QT prolongation (Torsades)

2) Dolasetron

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4
Q

All Serotonin 5-HT3 receptor antagonists have short half lives except?

This makes it effective for?

What is the dosage for these drugs?

A

1) Palonosetron and Granisetron
2) Delayed-CINV
3) Single dose

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5
Q

Aprepitant, Fosaprepitant, Netupitant, Fosnetupitant, and Rolapitant make up what class of medication?

A

Neurokinin (NK1) Receptor Antagonists

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6
Q

What does the prefix Fos- denote?

A

It is a prodrug

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7
Q

Neurokinin-1 is also known as?

A

Substance P

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8
Q

Which antiemetic class has the widest range of therapeutic uses?

A

5-HT3 receptor antagonists

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9
Q

What is the main therapeutic use for NK1 Receptor Antagonists?

It is most effective when used in combination with?

A

1) Chemotherapy induced N/V (CINV)

2) Glucocorticosteroid and 5-HT3 antagonist

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10
Q

What is the only NK1 Receptor Antagonists that is used for prophylaxis of post-operative N/V (PONV)?

In what population of patients is it given?

A

1) Aprepitant

2) Patient with history of PONV

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11
Q

Which NK1 Receptor Antagonists have moderate to major active metabolites and longer half-lives?

A

Netupitant/Rolapitant

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12
Q

Diphenhydramine, Dimenhydrinate, Doxylamine, Hydroxyzine, Promethazine, Meclizine and Cyclizine make up what class of medication?

A

Histamine (H1) Receptor Antagonists

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13
Q

What antihistamine is the initial therapy for N/V of Pregnancy (NVP)?

What vitamin is it paired with?

A

1) Doxylamine

2) Pyridoxine (vit B6)

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14
Q

H1 receptor antagonists exhibit what adverse effects?

A

Anticholinergic effects such as:

  • Drowsiness (CNS depression)
  • Dry mouth
  • Constipation
  • Urinary Retention
  • Blurred vision
  • Decrease BP
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15
Q

Which H1 receptor antagonists are used for motion sickness/vertigo?

A

Meclizine and cyclizine

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16
Q

What are H1 receptor antagonists generally useful for?

A

PONV

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17
Q

The phenothiazines: “Chlorpromazine, Perphenazine, and Prochlorperazine”, along with Metoclopramide make up what class of medication?

A

Dopamine (D2) Receptor Antagonists

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18
Q

Which D2 Receptor Antagonists stimulates ACh actions in GI?

What does this cause?

What population is often prescribed this?

A

1) Metoclopramide
2) Enhance GI motility (dysmotility use) and increases lower esophageal sphincter tone
3) Diabetic patients with gastroparesis/dysmotility issues

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19
Q

D2 receptor antagonists exhibit what adverse effects?

A

Anticholinergic effects such as:

  • Drowsiness (CNS depression)
  • Dry mouth
  • Constipation
  • Urinary Retention
  • Blurred vision
  • Decrease BP
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20
Q

Scopolamine makes up what class of medication?

A

Muscarine (M1) receptor antagonists

21
Q

How is scopolamine prescribed and for how long?

A

As a patch worn for 72 hours

22
Q

What is scopolamine most commonly utilized for?

What can it also be utilized for?

A

1) Motion sickness

2) End-of-life care for excessive secretions

23
Q

M1 receptor antagonists exhibit what adverse effects?

A

Anticholinergic effects such as:

  • Drowsiness (CNS depression)
  • Dry mouth
  • Constipation
  • Urinary Retention
  • Blurred vision
24
Q

Dronabinol and Nabilone make up what class of medication?

A

Cannabinoid Receptor Agonist

25
Q

What are cannabinoids?

A

Synthetic preparations of cannabinol (delta-9-THC)

26
Q

Why are there limits on quantity/refill of cannabinoids?

A

Because they are FDA-scheduled medications (C-II for Nabilone and C-III for Dronabinol)

27
Q

What is the therapeutic use for cannabinoids?

A

Treatment-resistant CINV

28
Q

Cannabinoids exert signal transduction effects through G-protein-coupled
receptors resulting in?

A

Decreased excitability of neurons

29
Q

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

Which is metabolized to several active metabolites?

While both have a short-time to onset of activity and long duration of action (24-36 hours) which requires fewer doses/day?

A

1) Dronabinol
2) Nabilone
3) Nabilone

30
Q

What drug-drug interactions do you want to be cautious of when prescribing cannabinoids?

A

1) Other CNS depressants
2) Cardiovascular agents
3) Sympathomimetics

31
Q

1) What is the strength of 5-HT3 receptor antagonists as antiemetic agents?
2) Strength of NK1 receptor antagonists?
3) Strength of H1 receptor antagonists?
4) Strength of D2 receptor antagonists?
5) Strength of M1 receptor antagonists?
6) Strength of cannabinoid receptor agonist?

A

1) Strong
2) Moderate
3) Weak
4) Weak to moderate
5) Weak
6) Strong

32
Q

What is the list of Serotonin (5-HT3) Receptor Antagonists?

A

1) Dolasetron
2) Granisetron
3) Ondansetron
4) Palonosetron

33
Q

What is the list of Neurokinin (NK1) Receptor Antagonists?

A

1) Aprepitant
2) Fosaprepitant
3) Netupitant
4) Fosnetupitant
5) Rolapitant

34
Q

What is the list of Histamine (H1) Receptor Antagonists?

A

1) Diphenhydramine
2) Dimenhydrinate
3) Hydroxyzine
4) Promethazine
5) Meclizine
6) Cyclizine
7) Doxylamine

35
Q

What is the list of Dopamine (D2) Receptor Antagonists?

A

1) Phenothiazines:
- Chlorpromazine
- Perphenazine
- Prochlorperazine
2) Metoclopramide

36
Q

What is the list of Muscarinic (M1) Receptor Antagonists?

A

Scopolamine

37
Q

What is the list of Cannabinoid Receptor Agonist?

A

1) Dronabinol

2) Nabilone

38
Q

What is acute CINV defined as?

What is chronic CINV?

What is anticipatory CINV?

A

1) Occurs <24 hours after chemo given
2) Occurs >24 hours after chemo given
3) Occurs before chemo given, customarily in nontreatment-naïve patients

39
Q

What corticosteroid is often used in combination with anti-emetogenic drugs?

A

Dexamethasone

40
Q

Describe a high-emetogenic regimen for CINV

A

3-drug regimen:

1) NK1 receptor antagonist
2) 5HT3 receptor antagonist
3) Dexamethasone

41
Q

What does the treatment plan look like for a high-emetogenic regimen for CINV?

A

Give treatment regimen day of (prior to) chemotherapy (for acute N/V) and for 3 days after chemotherapy (for delayed N/V)

42
Q

Describe a moderate-emetogenic regimen for CINV

A

2-drug regimen:

1) 5HT3 receptor antagonist
2) Dexamethasone

43
Q

What does the treatment plan look like for a moderate-emetogenic regimen for CINV?

A

Give treatment regimen day of (prior to) chemotherapy (for acute N/V) and for 2 days after chemotherapy (for delayed N/V)

44
Q

What options do you have if the treatment plan for a high-emetogenic regimen is not working?

A

Add D2 antagonist or add cannabinoid (increase to 4-drug regimen)

45
Q

Describe a low-emetogenic regimen for CINV

A

1-drug regimen:

1) 5HT3 receptor antagonist

OR

2) Dexamethasone

OR

3) Either metoclopramide or prochlorperazine but both options above are more likely

46
Q

What does the treatment plan look like for a low-emetogenic regimen for CINV?

A

Give treatment regimen day of (prior to) chemotherapy (for acute N/V)

47
Q

Scopolamine (patch), Dimenhydrinate, or Meclizine can be used to treat?

A

Motion sickness

48
Q

Meclizine or cyclizine can be used to treat?

A

Vertigo

49
Q

Metoclopramide can be used to treat?

A

Diabetic Gastroparesis

GI Week 1 (6 decks)

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