[Pharm] Treatment of Nausea and Vomiting Flashcards
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?
Combinations of agents w/ different MOAs
What are the (6) major receptors involved in N/V?
Serotonin (5-HT3)
Neurokinin (NK1)
Histamine (H1)
Dopamine (D2)
Muscarinic (M1)
Cannabinoid
What are the (5) antagonist category drugs for treating N/V?
Serotonin receptor antagonists
Neurokinin receptor antagonists
Histamine receptor antagonists
Dopamine receptor antagonists
Muscarinic receptor antagonists
What is the (1) agonist drug class used to treat N/V?
Cannabinoid receptor agonist
All the drugs within the serotonin receptor antagonists end in…
-Setron
What are the (5) serotonin receptor antagonists?
Dolasetron
Granisetron
Ondansetron
Palonosetron
Alosetron
What is the ONLY serotonin receptor antagonist that is only indicated for IBS-D?
Alosetron
What is the MOA of serotonin receptor antagonists?
Blcok serotonin type-3 receptors at the vagal nerve terminals
Blocks signal transmission to chemoreceptor trigger zone
What are the most common AE of serotonin receptor antagonists?
- CNS (headache)
- GI (constipation/Diarrhea)
- Serotonin syndrome
-Dose-dependent QT prolongation (Torsades)
What are the major drug interactions with serotonin receptor antagonists?
QT prolonging agents
Antiarrhythmics
All of the serotonin receptor antagonists have short half lives EXCEPT for…
Palonosetron
and
Sustained release formulation of Granisetron
What do all neurokinin receptor antagonists end with? (suffix)
-PITANT
Aprepitant
Fosaprepitant
Netupitant
Fosnetupitant
Rolapitant
What are neurokinin receptor antagonists used for?
Chemotherapy induced N/V
Prophylaxis of post operative N/V
When are neurokinin receptor antagonists most effective?
When used in combination with a glucocorticosteroid and 5-HT3 antagonist
What are the AE of neurokinin receptor antagonists?
GI (dyspepsia/constipation/diarrhea)
CNS (dizziness/fatigue/somnolence)
What is the one histamine receptor antagonist that has the SPECIFIC indication for use as nausea/vomiting in pregnancy?
Doxylamine
What are the (7) histamine receptor antagonists?
Diphenhydramine
Doxylamine
Dimenhydrinate
Hydroxyzine
Promethazine
Meclizine
Cyclizine
What is one of the major issues with using histamine receptor antagonists?
Anticholinergic properties
What is typically used for pts with motion sickness/vertigo?
Meclizine
Cyclizine
What are the common AE of histamine receptor antagonists?
Classic anticholinergic effects
- Drowsiness
- Dry mouth
- Constipation
- Urinary retention
- Blurred vision
What is the major family of dopamine receptor antagonists?
Phenothiazines
-azine
What are the 3 phenothiazines?
Chlorpromazine
Perphenazine
Prochlorperazine
What is the “other” dopamine receptor antagonist?
Metoclopramide
What is a unique dual action of metoclopramide?
In addition to suppressing N/V, it also stimulates ACh actions in GI which enhances GI motility
What are the AE of dopamine receptor antagonists?
Classic Anticholinergic effects
- Drowsiness
- Dry mouth
- Constipation
- Urinary retention
- Blurred vision
What is the muscarinic receptor blocker?
Scopolamine
What is scopolamine typically used for?
Motion sickness
AE of scopolamine?
Classic Anticholinergic effects
- Drowsiness
- Dry mouth
- Constipation
- Urinary retention
- Blurred vision
What are the two cannabinoid receptor agonists?
Dronabinol
Nabilone
Who are cannabinoids typically indicated for?
Treatment resistent chemotherapy induced n/v
How many active metabolites?
Dronabinol
Nabilone
Dronabinol = ONE active metabolite
Nabilone = SEVERAL active metabolites
Define:
Acute N/V
Chronic N/V
Anticipatory N/V
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
Proper therapy focuses on _______
Proper therapy focuses on prevention
For HIGH Emetogenic potential, what is the drug regimen you’d prescribe?
- NK1 receptor antagonist
- 5-HT3 receptor antagonist
- Corticosteroid (Dexamethasone)
For HIGH Emetogenic potential, how many drugs, and how many days do you prescribe?
3
For MODERATE emetogenic regimen, what drugs would you prescribe?
- 5-HT3 receptor antagonist
- Corticosteroid (Dexamethasone)
For MODERATE emetogenic regimen, how many drugs, and how many days to you give drugs?
2
For LOW emetogenic regimen, what do you prescribe?
1 drug regimen
Corticosteroid (Dexamethasone) OR 5-HT3 receptor antagonist
Drug you’d prescribe:
Motion sickness
Scopolamine
or
Dimenhydrinate
or
Meclizine
Drug you’d prescribe:
Vertigo
Meclizine
or
Cyclizine
Drug you’d prescribe:
Diabetic gastroparesis
Metoclopramide
Drug you’d prescribe:
Pregnancy-induced N/V
- VItamin B6 OR Histamine Antagonist
- Dopamine Antagonist
- Steroid OR different dopamine antagonist