Session 11 Antiemetics And Antidiarrhoeals Flashcards
What is vomiting?
Involuntary, forceful expulsion of gastric contents through the mouth
Describe how vomiting occurs
Vomiting centre in medulla —> vomit
- Nausea, salivation and sweating
- Retrograde peristalsis
- Deep inspiration
- Closure of glottis
- Abdominal muscles contract
- Lower oesophageal sphincter relaxes
What makes the vomiting centre ‘go’?
Sensory afferents via midbrain
Direct Triggers (needles etc)
Vestibular nuclei
Visceral afferents from gut
What agents (drugs) act on the vestibular nuclei?
Muscarinic receptor antagonists
H1 receptor antagonist
What is an example of a muscarinic receptor antagonist?
Hyoscine hydrobromide
Muscarinic receptor antagonists MoA?
Competitive blockade of muscarinic acetylcholine receptors in the vestibular nuclei and at the CTZone
Good uses of muscarinic receptor antagonists?
For people who cant take tablets
Motion sickness
Bowel obstruction
Side effects of muscarinic receptor antagonists?
Sedation
Memory problems
Glaucoma
Dry mouth and constipation
How do H1 receptor antagonists work?
Centrally
- acts on the vestibular nuclei
- inhibits histaminergic signals from the vestibular system to the CTZ in medulla
What are H1 receptor antagonists good for?
Motion sickness - long plane journeys
Promethazine = morning sickness in pregnancy
Names of some H1 receptor antagonists?
Cyclizine Levomepromazine Cinnirazine Promethazine Diphenhydramine
Side effects of H1 receptor antagonists?
Sedation
Excitation
Antimuscarinic - dry mouth, constipation, urinary retention
Cardiac toxicity (long QT interval)
What are the two agents that act on visceral afferents in the gut?
5HT3 receptor antagonist
D2 receptor antagonists
What cell type produces serotonin? (5-HT)
Enterochromaffin cells
What does serotonin do in response to parasympathetic stimulation?
Excites enteric neurones
- smooth muscle contraction increases motility (except in stomach)
- increases gut secretions
- regulates appetite
How do 5HT3 receptor antagonists work
A) peripherally
B) centrally
Peripherally
* reduced GI motility and reduces GI secretions
Centrally
* acts to inhibit to CTZ
Good for: almost everyone (1st line treatment most of the time)
Examples of names of 5 HT3 receptor antagonists?
Ondansetron
Granesitron
Palonosetron
Side effects of 5 HT3 receptor antagonists?
Uncommon!
Constipation Headache Elevated liver enzymes Long QT syndrome Extra-pyramidal effects (dystonia, Parkinsonism)