Antiemetics Flashcards
Where does the signal to vomit come from?
What events happen in order to vomit?
Vomiting centre in medulla
- Nausea, Salivation, Sweating
- Retrograde peristalsis
- Deep inspiration
- Closure of glottis
- Ab muscles contract
- Lower oesophageal sphincter relaxes
List 4 things that can trigger the Chemoreceptor Trigger Zone (CTZ) and lead to vomiting?
- Sensory afferents via midbrain
- Vestibular nuclei
- Visceral afferents from gut
- Direct triggers
Where is the CTZ?
In the Area Postrema, on the floor of the 4th ventricle
List 2 types of Antiemetic agent acting on the Vestibular Nuclei
What are they usually used for?
- Muscarinic receptor antagonists
- H1 receptor antagonists
- Treating motion sickness
What kind of drug is Hyoscine hydrobromide?
This drug’s targets are where?
A muscarinic receptor antagonist
(mAChRs are the targets)
- Vestibular nuclei
- CTZ
- All over body as part of ParaS system
List 5 ADRs of Muscarinic receptor antagonists
- Sedation
- Memory problems
- Glaucoma
- Dry mouth
- Constipation
List 3 people who Hyoscine hydrobromide would be good for?
- Bowel obstruction
- Motion sickness
- People who can’t take tablets
The following drugs are what kind of drug?
- Cyclizine
- Levomepromazine
- Cinnirazine
- Promethazine
- Dipenhydramine
H1 receptor antagonists
Where do H1 receptor antagonists work?
- Vestibular nuclei
- CTZ (inhibition of histaminergic signals from vestibular system)
Lit 4 ADRs of H1 receptor antagonists
- Sedation
- Excitation
- Cardiac toxicity
- Antimuscarinic (Dry mouth, constipation, urinary retention)
For what patient groups are H1 receptor antagonists good and not good?
Give examples
Good for;
- Motion sickness
- Promethazine (Morning sickness in pregnancy)
Not good for;
- Cyclizine: Elderly women and children (makes them disoriented and confused)
List 2 types of Antiemetic agent acting on the Visceral afferents from the gut
- 5HT3 (Serotonin) antagonists
- SOME D2 receptor antagonists
Where is most of the body’s Serotonin found and what cells is it made by?
What does Serotonin do here?
- 95% found in gut, made by ECL cells
- Regulates appetite
- In response to ParaS stimulation, excites Enteric neurones-> Increased gut secretions and motility (except stomach motility)
What do 5HT3 Receptor Antagonists do Peripherally and Centrally?
Who are these drugs good for?
Peripherally;
- Reduced GI motility and secretions
Centrally;
- Inhibits CTZ
Almost everyone, often 1st line treatment
What kind of drugs are Ondansetron, Granisetron and Palonosetron?
List 5 ADRs of these drugs
5HT3 receptor antagonists
Uncommon;
- Constipation
- Headache
- Elevated liver enzymes
- Long QT Syndrome
- Extra-pyramidal effects (Dystonia, Parkinsonism)
What kind of drugs are Metoclopramide and Domperidone?
What are 2 ADRs of this class of drugs?
D2 Receptor Antagonists
- Galactorrhea (via PRL release)
- Extra-pyramidal effects (Parkinsonism, Dystonia)
How does Metoclopramide work?
- Increases ACh at mAChRs in gut-> Increased gastric emptying via;
- Increased tone at LOS so it closes
- Increased tone & amplitude of gastric contractions
- Decreased tone of Pylorus so it opens
- Increases GI peristalsis
Suggest 2 patient groups who Metoclopramide is good for?
- GORD
- Ileus (Peristalsis stops, similar presentation to bowel obstruction)
How does Domperidone work?
List 1 patent group who its for
List 2 ADRs
- Similar mechanism to Metoclopramide
- Good for improving lactation in breastfeeding mothers (due to its ADR)
- Galactorrhea
- Sudden cardiac death (Long QT, VTach)