Anti-Nausea/Emetic Pharm

Question 1

Receptors Associated with Nausea and Vomiting (5)

Answer 1

Serotonin Type 3 (5HT3)
Histamine Type 1 (H1)
Muscarininc Type 1 (M1)
Dopamine Type 2 (D2)
Neurokinin-1 (NK1, aka Substance P)

Question 2

Serotonin Receptor Antagonists

Examples (5) and MOA (2)

Answer 2

Dolasetron
Granisetron
Ondansetron
Palonosetron

Block 5-HT3 receptors at Vagus N to decrease signaling to CTZ in medulla

Question 3

Serotonin Antagonists

Uses (4), Adverse Effects (2), Contraindications

Answer 3

Chemotherapy, Radiation, Post-Operative, Pregnancy

Serotonin Syndrome
Dose Dependent QT elongation (Torsade’s)

Use of QT prolonging drugs (anti-arrhythmics)

Question 4

Neurokinin-1 Receptor Antagonists

Examples (5) and MOA (2)

Answer 4

Aprepitant
Fosaprepitant
Netupitant
Fosnetupitant
Rolapitant

Blocks NK1 receptors in CTZ and VC

Question 5

Neurokinin-1 Receptor Antagonists

Uses (2) and Adverse Effects (2)

Answer 5

CINV - combo therapy with corticosteroid and 5-HT3A
PONV - Aprepitant used for prophylaxis

Minor GI and CNS symptoms

Question 6

Histamine Receptor Antagonists

Examples (7) and MOA (2)

Answer 6

Diphenhydramine
Dimenhydrinate
Hydroxyzine
Promethazine
Meclizine
Cyclizine
Doxylamine

Blocks H1-R in VC and vestibular system
Has minor anti-cholinergic effects

Question 7

Histamine Antagonists

Uses (2) and Adverse Effects (5)

Answer 7

Doxylamine used with Vit B6 for pregnancy
Meclizine/Cyclizine used for vertigo/motion sickness

Classic Anti-Cholinergic Effects:
Drowsy
Blurry vision
Dry mouth
Constipation
Urinary retention

Question 8

Dopamine Receptor Antagonists

Examples (4) and MOA (3)

Answer 8

Chlorpromazine
Perphenazine
Prochlorperazine
Metoclopramide

Blocks D2R in CTZ
Anticholinergic effects
Metoclopramide stimulates Ach in GI

Question 9

Dopamine Antagonists

Uses (2) and Adverse Effects (5)

Answer 9

Metoclopramide used for GI dysmotility (gastroparesis)
Used in combo with other anti-emetics

Classic Anti-Cholinergic Effects:
Drowsy
Blurry vision
Dry mouth
Constipation
Urinary retention

Question 10

Scopolamine

Drug Class, MOA (2), Indication, Delivery and Adverse (5)

Answer 10

Muscarinic Type 1 Receptor Antagonist
Blocks M1R in VC and vestibular centers

Indicated for motion sickness
72 hour transdermal patch

Classic Anti-Cholinergic Effects:
Drowsy
Blurry vision
Dry mouth
Constipation
Urinary retention

Question 11

Cannabinoids

Examples (2), MOA (2), Indication, Adverse?, Interactions (3)

Answer 11

Dronabinol
Nabilone

Stimulation of CB1/CB2 receptors
Decreases excitability of 5-HT3 receptors

Only for treatment-resistant CINV

Get stoned

CNS Depressants
Cardioactive agents
Sympathomimetics

Question 12

Treatment of Highly Emetic Chemotherapy Agents

Drugs (3), Timing and Additional Options (2)

Answer 12

Neurokinin-1 Antagonist
Serotonin Antagonist
Dexamethasone

Give drugs prior to chemo and 3 days after

Olanzapine of Cannabinoid

Question 13

Treatment of Moderately Emetic Chemotherapy Agents

Drugs (2), Timing and Additional Options (3)

Answer 13

Serotonin Antagonist
Dexamethasone

Give drugs prior to and 2 days after chemo

Neurokinin Antagonist or Olanzapine
Cannabinoid if still ineffective

Question 14

Treatment of Mildly Emetic Chemotherapy Agents

Drugs (4), Timing and Additional Option

Answer 14

Give ONE of the Following:
Dexamethasone
Serotonin Antagonist
Metoclopramide
Prochlorperazine

Give drug day of prior to chemo

Add second drug of different class if need be

Question 15

Drugs for Motion Sickness (3)

Answer 15

Scopolamine
Dimenhydrinate
Meclizine

Question 16

Drugs for Vertigo (2)

Answer 16

Meclizine

Cyclizine

Question 17

Treatment for Pregnancy Induced N/V

3 Steps

Answer 17

1st Line is Doxylamine and Vit B6 (pyridoxine)
Then Dopamine Antagonist
Then Steroid or other Dopamine Antagonist

Can start with Serotonin Antagonist as well