[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