10. Antiemetics Flashcards
Which agents act on the vestibular nuclei?
Muscarinic receptor antagonists
H1 receptor antagonists
Name a muscarinic receptor antagonist
Hyoscine hydrobromide
How do muscarinic receptor antagonists work?
Competitive blockade of muscarinic acetylcholine receptors
- in vestibular nuclei
- also at CTZ
- but also at many other parts of the body
What are muscarinic receptor antagonists good for?
People who cant take tablets
Motion sickness
Bowel obstruction
What are the side effects of hyoscine hydrobromide?
Sedation
Memory problems
Glaucoma
Dry mouth and constipation
How do H1 receptor antagonists work?
Act on vestibular nuclei
Inhibits histaminergic signals from the vestibular system to CTZ in medulla
What are H1 receptor antagonists good for?
Motion sickness Morning sickness (promethazine)
Who cannot use cyclizine?
Little old ladies and children
Name some H1 receptor antagonists
Cyclizine Levomepromazine Cinnirazine Promethazine Diphenhydramine
What are side effects of H1 receptor antagonists?
Sedation
Excitation
Dry mouth, constipation, urinalysis retention, cardiac toxicity
Which drugs act on visceral afferents in the gut?
5HT3 receptor antagonists
D2 receptor antagonists
How does 5HT3 receptor an antagonist work?
Peripherally - reduces GI motility, reduces GI secretions
Centrally - act to inhibit the CTZ
Name some 5HT3 receptor antagonists?
Ondansetron
Granisetron
Palonosetron
What are the side effects of 5HT3 receptor antagonists?
Uncommon Constipation Headache Elevated liver enzymes Long QT syndrome
Name some D2 receptor antagonists
Metoclopramide
Domperidone