[Pharm] Treatment of Nausea and Vomiting

Question 1

Due to the diversity of receptors in the brain and GI tract that stimulate N/V, what is the best way to combat N/V?

Answer 1

Combinations of agents w/ different MOAs

Question 2

What are the (6) major receptors involved in N/V?

Answer 2

Serotonin (5-HT3)

Neurokinin (NK1)

Histamine (H1)

Dopamine (D2)

Muscarinic (M1)

Cannabinoid

Question 3

What are the (5) antagonist category drugs for treating N/V?

Answer 3

Serotonin receptor antagonists

Neurokinin receptor antagonists

Histamine receptor antagonists

Dopamine receptor antagonists

Muscarinic receptor antagonists

Question 4

What is the (1) agonist drug class used to treat N/V?

Answer 4

Cannabinoid receptor agonist

Question 5

All the drugs within the serotonin receptor antagonists end in…

Answer 5

-Setron

Question 6

What are the (5) serotonin receptor antagonists?

Answer 6

Dolasetron

Granisetron

Ondansetron

Palonosetron

Alosetron

Question 7

What is the ONLY serotonin receptor antagonist that is only indicated for IBS-D?

Answer 7

Alosetron

Question 8

What is the MOA of serotonin receptor antagonists?

Answer 8

Blcok serotonin type-3 receptors at the vagal nerve terminals

Blocks signal transmission to chemoreceptor trigger zone

Question 9

What are the most common AE of serotonin receptor antagonists?

Answer 9

• CNS (headache)
• GI (constipation/Diarrhea)
• Serotonin syndrome

-Dose-dependent QT prolongation (Torsades)

Question 10

What are the major drug interactions with serotonin receptor antagonists?

Answer 10

QT prolonging agents

Antiarrhythmics

Question 11

All of the serotonin receptor antagonists have short half lives EXCEPT for…

Answer 11

Palonosetron

and

Sustained release formulation of Granisetron

Question 12

What do all neurokinin receptor antagonists end with? (suffix)

Answer 12

-PITANT

Aprepitant

Fosaprepitant

Netupitant

Fosnetupitant

Rolapitant

Question 13

What are neurokinin receptor antagonists used for?

Answer 13

Chemotherapy induced N/V

Prophylaxis of post operative N/V

Question 14

When are neurokinin receptor antagonists most effective?

Answer 14

When used in combination with a glucocorticosteroid and 5-HT3 antagonist

Question 15

What are the AE of neurokinin receptor antagonists?

Answer 15

GI (dyspepsia/constipation/diarrhea)

CNS (dizziness/fatigue/somnolence)

Question 16

What is the one histamine receptor antagonist that has the SPECIFIC indication for use as nausea/vomiting in pregnancy?

Answer 16

Doxylamine

Question 17

What are the (7) histamine receptor antagonists?

Answer 17

Diphenhydramine

Doxylamine

Dimenhydrinate

Hydroxyzine

Promethazine

Meclizine

Cyclizine

Question 18

What is one of the major issues with using histamine receptor antagonists?

Answer 18

Anticholinergic properties

Question 19

What is typically used for pts with motion sickness/vertigo?

Answer 19

Meclizine

Cyclizine

Question 20

What are the common AE of histamine receptor antagonists?

Answer 20

Classic anticholinergic effects

• Drowsiness
• Dry mouth
• Constipation
• Urinary retention
• Blurred vision

Question 21

What is the major family of dopamine receptor antagonists?

Answer 21

Phenothiazines

-azine

Question 22

What are the 3 phenothiazines?

Answer 22

Chlorpromazine

Perphenazine

Prochlorperazine

Question 23

What is the “other” dopamine receptor antagonist?

Answer 23

Metoclopramide

Question 24

What is a unique dual action of metoclopramide?

Answer 24

In addition to suppressing N/V, it also stimulates ACh actions in GI which enhances GI motility

Question 25

What are the AE of **dopamine receptor antagonists?**

Answer 25

Classic Anticholinergic effects - Drowsiness - Dry mouth - Constipation - Urinary retention - Blurred vision

Question 26

What is the **muscarinic receptor blocker?**

Answer 26

Scopolamine

Question 27

What is **scopolamine** typically used for?

Answer 27

Motion sickness

Question 28

AE of **scopolamine?**

Answer 28

Classic Anticholinergic effects - Drowsiness - Dry mouth - Constipation - Urinary retention - Blurred vision

Question 29

What are the two **cannabinoid receptor agonists?**

Answer 29

Dronabinol Nabilone

Question 30

Who are **cannabinoids** typically indicated for?

Answer 30

Treatment resistent chemotherapy induced n/v

Question 31

How many active metabolites? Dronabinol Nabilone

Answer 31

Dronabinol = ONE active metabolite Nabilone = SEVERAL active metabolites

Question 32

# Define: Acute N/V Chronic N/V Anticipatory N/V

Answer 32

Acute N/V = occurs \<24 hours after chemo given Chronic N/V = occurs \>24 hours after chemo given Anticipatory N/V = occurs **before** chemo given

Question 33

Proper therapy focuses on \_\_\_\_\_\_\_

Answer 33

Proper therapy focuses on **prevention**

Question 34

For **HIGH Emetogenic potential**, what is the drug regimen you'd prescribe?

Answer 34

1. NK1 receptor antagonist 2. 5-HT3 receptor antagonist 3. Corticosteroid (Dexamethasone)

Question 35

For **HIGH Emetogenic potential**, how many drugs, and how many days do you prescribe?

Answer 35

3

Question 36

For **MODERATE** emetogenic regimen, what drugs would you prescribe?

Answer 36

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

Question 37

For **MODERATE** emetogenic regimen, how many drugs, and how many days to you give drugs?

Answer 37

2

Question 38

For **LOW** emetogenic regimen, what do you prescribe?

Answer 38

1 drug regimen **Corticosteroid (Dexamethasone)** OR **5-HT3 receptor antagonist**

Question 39

Drug you'd prescribe: Motion sickness

Answer 39

Scopolamine or Dimenhydrinate or Meclizine

Question 40

Drug you'd prescribe: Vertigo

Answer 40

Meclizine or Cyclizine

Question 41

Drug you'd prescribe: Diabetic gastroparesis

Answer 41

Metoclopramide

Question 42

Drug you'd prescribe: Pregnancy-induced N/V

Answer 42

1. VItamin B6 OR Histamine Antagonist 2. Dopamine Antagonist 3. Steroid OR different dopamine antagonist