Antiemetics and Antidiarrhoeals Flashcards
What is vomiting?
Involuntary, forecul expulsion of gastric contents through the mouth
What is regurgitation?
The effortless bringing back up of food (not made it to the stomach)
What steps happen in the GI tract during vomiting?
What area of the brain causes vomiting. Where is this located?
Chemoreceptor trigger zone (CTZ)
In the floor of the 4th ventricle on the blood side of the blood brain barrier
What things act on the chemoreceptor trigger zone to cause vomiting?
- Direct triggers e.g. drugs, hormones
- Info from vestibular nuclei e.g. during motion sickness, vertigo
- Visceral afferents from gut i.e. vagus nerve
- Sensory afferents via midbrain e.g. sights and smells
What type of antiemetic drugs can act on the vestibular nuclei?
- Muscarininic receptor antagonists
- H1 receptor antagonists
What type of anti-emetics act on the visceral afferents from the gut?
- 5HT3 antagonists
- D2 receptor antagonists
What anti-emetic drugs act directly on the chemoreceptor trigger zone?
- D2 receptor antaogonists
- 5HT3 antagonists
- Muscarinic receptor antagonists
- H1 receptor antagonists
- Corticosteroids
- Cannabinoids
- NK1 receptor antagonists
Give an example of a muscarinic receptor antagonist
Hyoscine hydrobromide
(tablet or transdermal)
How to muscarinic receptor antagonists work?
Competitively block muscarining Acetylcholine receptors
In the vestibular nuclei and the CTZ
ACh receptors part of parasympathetic nervous system
Which patients are muscarinic receptor antagonists good for?
- People who can’t take tablets- patch form
- Motion sickness
- Bowel obstruction- patch form
What are some of the side effects of muscarinic receptor antaogonists?
- Sedation
- Memory problems
- Glaucoma
- Dry mouth and constipation
Name the most commonly used H1 receptor antagonist
Cyclizine
How do H1 receptor antagonists work?
- Act on vestibular nuclei
- Inhibit histaminergic signals from vestibular system to CTZ in the medulla
Which patients are H1 receptor antagonists good for?
- Motion sickness- long plane journey (sedative effect helps sleep)
- Promethazine is good for morning sickness in pregnancy
Which patients should you avoid using cyclizine in?
- Old ladies
- Children
What are some of the side effects of H1 receptor antagonists?
- Sedation
- Excitation
- Antimuscarinic effects- dry mouth, consitpation, urinary retention
- Cardiac toxicity (long QT interval)
Which cells in gut produce 5HT?
Enterochromaffin cells
What causes 5HT release in the gut? What are the effects of its release?
- In response to parasympathetic stimulation
- Serotonin excites enteric neurones causing:
- Smooth muscle contraction (increasing motility)
- Increased gut secretions
- Regulates appetite
What are the effets of 5-HT3 receptor antagonists?
Peripherally:
- reduces gut motility
- reduces GI secretions
Centrally
- Acts to inhibit the CTZ
Name the most commonly prescribed 5HT3 antagonist?
Ondansetron