Pharmacology: Drugs Affecting Gut Motility Flashcards
What is the myogenic control of gut motility?
There are smooth muscle subunits linked by gap junctions
The interstitial cells of Cajal act as pacemaker cells to cause slow action potentials in the smooth muscle cells.
What is the neural control of gut motility?
Intrinsic control: the enteric NS
Extrinsic control:
- distension of the anus causes intestinal inhibition
- the gastrocolic and dueodenalcolic reflexes stimulate motility after material enters the stomach or duodenum
Outline the mechanical mechanism of vomiting
The pyloric sphincter closes and the cardia and the oesophagus relax.
The abdominal wall and diaphragm contract and propel the gastric contents.
The soft palate elevates causing the glottis to close to prevent entry of the vomit into the airways.
What are some causes of vomiting?
- pregnancy
- medications
- toxins
- pain
- irradiation
- smell
- raised ICP
- stretching and inflammation of the stomach
- rotational movement
List the classifications of anti-emesis drugs
- Dopamine (D2) receptor antagonists
- Serotonin receptor antagonists
- anti-muscarinics
- Histamine (H1) receptor antagonists
- Cannabinoids
- Benzodiazepines
How does domperidone (a D2 antagonist) work?
What are its indications?
Acts on the postrema on the floor of the 4th ventricle to inhibit vomiting. Also acts on the stomach to increase the rate of gastric emptying.
It is used for acute nausea and vomiting, esp caused by L-DOPA or dopamine agonists
How does ondansteron (a serotonin antagonist) work?
What are its indications?
5HT in the gut causes vagal stimulation. Works on the postrema on the floor of the 4th ventricle and opposes vagal nerves in the GIT.
It is used in high doses in radiation sickness and chemo. Anti-emetic effects can be enhanced by a single dose of corticosteroid.
How does metoclopramide work?
What are the indications?
Its a D2 antagonist. Also has GI ant-cholinergic effeects and blocks vagal stimulation of the GI tract.
Used for GI causes of N+V, migraine, post-operatively
What is the route of administration of domperidone?
What are some of the ADRs?
Given orally or PR - undergoes extensive first pass metabolism
ADR - stimulates prolactin release so can cause galactorrhoea, dystonia can happen but is rare
What are the routes of administration of ondansteron?
What are the ADRs?
Can be given IM, IV or orally.
ADRs inc headaches, constipation and flushing when given IV
What are the routes of administration of metoclopramide?
What are the ADRs?
Can be given oral, IV or IM. Short half life so given 3x daily
ADRs include extra-pyramidal reactions eg dystonia so must be avoided in parkinsons disease. Can cause galactorrhoea
How does hyoscine work?
When is it used?
It is a direct antagonist of muscarinic cholinergic receptors.
Used to treat motion sickness (half life around 2 hours)
What are the routes of administration of hyoscine?
What are the ADRs?
Usually given as a patch but can be oral if tolerance to transdermal route.
ADRs are systemic anticholinergic effects such as bradycardia
How does cyclizine work?
What are its indications?
A H1 antagonist with additional anti-muscarinic effects
Most common drug used for acute N+V
What are the routes of administration of cyclizine?
What are the ADRs?
Oral, IV or IM
ADRs - can cross the BBB so has a sedative effect. Can cause QT prolongation so contraindicated in myocardial ischaemia