GI 1 (Vomiting)

Question 1

Acute Chemotherapy/Cytotoxic Drug Induced Vomiting
- Pharmacology

Answer 1

5-HT/5HT3 Receptor Signaling (0-24 hrs)

Question 2

Delayed Chemotherapy/Cytotoxic Drug Induced Vomiting
- Pharmacology

Answer 2

SP/NK1 Receptor Signaling (>24 hrs)

Question 3

Ondansetron
- Drug Class?

Answer 3

5-HT(3) Receptor Antagonists

Question 4

Granisetron
- Drug Class?

Answer 4

5-HT(3) Receptor Antagonists

Question 5

Alosetron
- Drug Class?

Answer 5

5-HT(3) Receptor Antagonists
- Ischemic Colitis

Question 6

Palonosetron
- Drug Class?

Answer 6

5-HT(3) Receptor Antagonists

Question 7

5-HT(3) Receptor
- Mechanism of Action

Answer 7

Ligand Gated Ion Channel

Antagonist targets CTZ and blocks 5-HT(3) receptors from sensitizing spinal sensory neurons and blocks vagal signaling of nausea
- Slows down intestinal movement and secretions

Question 8

Chlorpromazine
- Drug Class?

Answer 8

Dopamine Receptor 2 (D2) Antagonist
- Sedation

Question 9

Perphenazine
- Drug Class?

Answer 9

Dopamine Receptor 2 (D2) Antagonist

Question 10

Prochlorperazine
- Drug Class?

Answer 10

Dopamine Receptor 2 (D2) Antagonist

Question 11

Trifluoperazine
- Drug Class?

Answer 11

Dopamine Receptor 2 (D2) Antagonist

Question 12

Dopamine Receptor 2 (D2)
- MOA

Answer 12

G-Protein Coupled Receptor (Gq)
- Causes activation of PLC leading to an increase of IP3 and DAG levels
D2 Antagonist Targets D2 Receptors in CTZ and prevents activation

Question 13

Dopamine Receptor 2 (D2)
- Adverse Effects

Answer 13

Involuntary Movements:
- Extrapyramidal Syndrome
- Dystonia
- Tardive Dyskinesia

Hyperprolactinemia (D2 is supposed to inhibit prolactin)
- Excessive lactation
- Men lactate

Question 14

Metoclopramide
- Drug Class?

Answer 14

Dopamine Receptor 2 (D2) Antagonist
- Acts primarily on CTZ
- Also acts on GI (Increases Motility)
- Blocks Histamine and Muscarinic Receptors too

Question 15

Metoclopramide
- Adverse Effects

Answer 15

Involuntary Movement:
- Spasmodic Torticollis (Neck)
- Oculogyric Crises (Eye)

Hyperprolactinemia

Question 16

Domperidone
- Drug Class?

Answer 16

Dopamine Receptor 2 (D2) Antagonist
- Does not penetrate BBB, less CNS effect
- Risk of cardiac arrest

Question 17

Haloperidol

Answer 17

D2 Receptor Antagonists
- Treats Acute Chemotherapy Emesis

Question 18

Droperidol

Answer 18

D2 Receptor Antagonists
- Treats Acute Chemotherapy Emesis

Question 19

Levomepromazine

Answer 19

D2 Receptor Antagonists
- Treats Acute Chemotherapy Emesis

Question 20

Cinnarizine
- Drug Class?

Answer 20

Histamine H1 Receptor Antagonist

Question 21

Cyclizine
- Drug Class?

Answer 21

Histamine H1 Receptor Antagonist

Question 22

Promethazine
- Drug Class?

Answer 22

Histamine H1 Receptor Antagonist

Question 23

Histamine H1 Receptor
- MOA

Answer 23

G-Protein Coupled Receptor (Gq)
- H1 Antagonist manages motion sickness and pregnancy morning sickness
- Does not act on CTZ

Adverse Effects:
- Drowsiness

Question 24

Hyoscine (Scopolamine)
- Drug Class?

Answer 24

Muscarinic Receptor Antagonist

Question 25

Muscarinic Antagonist - Treats? - Adverse?

Answer 25

M Antagonist is used to prevent and treat motion sickness - Adverse Effects --> Dry mouth / Blurred vision --> Drowsiness

Question 26

Aprepitant - Drug Class?

Answer 26

Substance P Antagonist (Neurokinin-1 Receptors) - Targets CTZ for delayed chemotherapy emesis

Question 27

Fosaprepitant - Drug Class?

Answer 27

Inactive Prodrug for Substance P Antagonist (Neurokinin-1 Receptors)

Question 28

Nabilone - Drug Class?

Answer 28

Synthetic Cannabinol - Treats vomiting - Can be reversed by naloxone through opioid receptors

Question 29

Dexamethasone - Drug Class?

Answer 29

Glucocorticoid - Last Resort Treatment - High doses are used to prevent vomiting caused by cytotoxic drugs