N&V pharmacological agents - AB Flashcards
2 major sites where chemo triggers emesis
- vagus nerve
- CTZ
Why is 5-HT3 important in emesis?
What does it have to do with the GI tract?
5-HT receptors are located in the intestinal lining. Once their enterochromaffin cells are irritated by toxins, 5-HT will be released and activate the 5-HT receptors. The CTZ is then activated and the emetic center is stimulated, triggering emesis.
What is the blood-brain barrier and how is it relevant to CINV?
The blood-brain barrier is our body’s natural defense system against unwanted substances entering the CNS from the blood. The CTZ is located outside the blood-brain barrier, and is therefore unprotected.
MOA:
- metoclopramide
- ondansetron
- dual D2/5-HT3 receptor blocker
2. 5-HT3 receptor antagonist
Aprepitant targets _________________ receptor
Substance P (NK1)