GI drugs Flashcards
What type of therapy should anti-emetics be considered as?
Symptomatic, NOT therapeutic (may encourage eating, minimise damage due to physical damage)
- always need to resolve the underlying problem
Give 3 situations where anti-emetic therapy would be contra-indicated
- GI infection: prolong infection esp bacterial
- GI obstruction: some anti-emetics ^motility -> perforation
- GI toxicity: antiemetics may prevent the patient from eliminating the toxin (though usually they have already eliminated in 1st couple of vomits by the time they present - at this stage you are treating the secondary inflammation and damage caused by the substance)
Give 6 inputs to the vomiting centre?
- CRTZ (area within brain with no BBB)
- higher CNS (smell, fear, pain)
- vestibular (motion sickness, inner ear infection)
- Peripheral receptors (gut esp duodenum - inflam, toxic damage, abdo organs, peritoneum)
- toxins
- nucleus tractus solitarius (integrating centre)
What is the vomiting centre?
series of nuclei in medulla
Where does the most common (first vet licensced) anti-emetic drug act?
Nucleus tractus solitarius NK1-Rs (final common pathway)
- Maropitant
How do cats and dogs differ in importance of receptors in emesis?
- D2-Rs in CRTZ more important in dogs
> apomorphine [not a morphine derivative] D2 ag is a potent EMETIC in the dog but not the cat.
> Metclopramide (DA-ag) more effective in dogs
> Histamine is a potent emetic in the dog but not the cat - A2-Rs in CRTZ more important in cats
> xylazine more potent emetic in cats (side effect of sedative_
> prochlorperazine (a2 blocker) more effective in cats
When are emetics indicated?
Poison ingestion (providing not caustic)
Do all animals have a vomiting centre?
NO
some may not have the anatomical features to vomit as well, separate reason
What is the “shock organ” in the cat v the dog? ie. how do severe allergic reactions manifest?
Cat: respiratory signs
Dog: liver -> GI signs, vomiting
Give 6 classes of anti-emetic drugs
- NK1 antagonists
- metoclopramide (multiple Rs)
- phenothiazines
- antihistamines
- 5HT3 antagonists
- anticholinergics (have issues)
What was the first anti-emetic to be licensed for vet use? What is its trade name? What is it indicated for?
Maropitant - Cerenia Indicated for > acute gastroenteritis > cytotoxic induced vomiting > motion sickness (higher dose required)
What is the mechanism of action of maropitan?
Selective antagonist of supbstance P at NK1-R
- final common pathway involved in activating vomiting reflex in CNS
- effective against stimulation from peripheral and central stimuli
What is the mechanism of action of metoclopramide?
- D2 antagonist
- 5HT3 antagonist
> Acts on CRTZ and peripheral receptors
Peripheral pro-cholinergic effect (^GI motility)
What is metoclopramide indicated for?
- Various emesis-inducing disorders which involve central/peripheral actiation of vomiting
- cancer chemotherapy (not as effective as maropitan)
- gastroesophageal reflux (endoscopy etc)
- decreased gastric emptying (inflam GI disorders, ulcers, neoplasia, autonomic neuropathy with diabetes mellitis, pyloric stenosis, postop gastric volvulus patients, hypokaleamia, abnormal gastric motility)
What is the action of the phenothiazines?
Antagonise
- a1 a2 (vomiting centre)
- D2 (CRTZ and peripheral Rs)
- H1 H2 (CRTZ)
- muscarinic cholinergic (CRTZ)
What does a1 antagonism cause as a side effect?
Dramatic blood pressure decrease
Give an example of a phenothiazine
Acepromazine (ACP) - sedative/tranq
What are phenothiazines indicated for use in?
Central or peripheral causes of vomiting BUT not vet registered so should use maropitan/metoclopramide