GIT pharmacology Flashcards
List some GIT pathophysiologies that may need pharmacological treatment
Antiulcer
Vomiting
Constipation
Diarrhoea
Motility issues
List some neurotransmitters that are involved in GIT function
Acetylcholine
Noradrenaline
Histamine (H1, H2)
Opioids
Dopaminergic
Serotonin (5HT3)
List some hormones that are involved in GIT function
Gastrin (stomach)
Secretion (duodenum)
Cholecystokinin (regulates fat)
Ghrelin
Motilin
Vasoactive intestinal peptide
Gastric inhibitory peptide
List some causes of gastric ulceration
NSAID use
Uraemia
Liver disease
Stress
Increased production of HCl (e.g. mast cell tumor)
Hypotension
Helicobacter
List some normal protective mechanisms of the GIT
Mucous layer with high levels of bicarbonates
High cell turnover
Tight junctions
Highly vascularised
Prostaglandins (mucous secretion, blood flow, acid inhibition)
List some classes of antiulcer drugs and gastroprotectants
Proton pump inhibitors
Antihistamines
Gastroprotectants
Non-systemic antacids
List a proton pump inhibitor
Omeprazole
What is the mechanism of action of omeprazole?
Proton pump inhibitors (antiulcer/gastroprotectant)
Irreversible inhibition of H+/K+ ATPase proton pump on parietal cells: weak bases accumulate in acidic environment around proton pump to selectively inhibit active cells
List some antihistamines that may be useful as an antiulcer/gastroprotectant drug
Ranitidine
Cimetidine
What is the mechanism of action of ranitidine?
Antihistamine
What is the mechanism of action of Cimetidine?
Antihistamine
List two gastroprotectants
Misoprostal
Sucralfate
Which class of drugs does misoprostal belong to?
Gastroprotectants
What class of drugs does sucralfate belong to?
Gastroprotectants
What are the effects of omeprazole?
Inhibits the final step of acid secretion, increasing both basal and food-stimulated gastic acid secretions
(more effective than antacids and H2-antagonists)
What are the preparations of omeprazole
Enteric coated tablets/capsules to aid absorption
What are the adverse effects/drug interactions of omeprazole?
Well tolerated
Some inhibition of cytochrome P450
What are the mechanisms of action of antihistamine as antiulcer/gastroprotectant drugs?
H2 receptor antagonist
What are the effects of antihistamines as GIT drugs?
Decrease 90% basal and 60% food-stimulated acid secretion
More effective than antacids, but not as effective as PPIs
Lasts 12-24 hours
What are the adverse effects of cimetidine, ranitidine?
Cutaneous eruptions (cats)
gynaecomastia and sexual dysfunction (humans)
Cimetidine inhibits cytochrome p450 - many potential drug interactions
What is the mechanism of action of misoprostal?
Prostaglandin E1 analogue
What are the effects of misoprostal?
Protects GI mucosa by increasing mucous secrtion and bicarbonate and decreasing secretion of gastric acid (useful for NSAID induced ulcers)
What are the adverse effects of misoprostal
Induces parturition, diarrhoea, vomiting
(CAUTION pregnant vets)
What is the mechanism of sucralfate?
Sucrose octasulfate and aluminium hydroxide dissociate in stomach
Acid polymerises sucrose octasulfate (sticky coating covers ulcers)
What is the indication for sucralfate
symptomatic treatment of gastric ulceration
What are the adverse effects of sucralfate
Minor; constipation?
What are some of the preparations of non-systemic antacids
Aluminum hydroxide, calcium carbonate or magnesium compounds
What are the adverse effects of non-systemic antacids
May result in rebound acid secretion if not continually administered
Define vomiting
An active process involving forceful, reflexive ejection of contents from stomach and/or small intestine
Define regurgitation
Passive process (gravity or passive changes in thoracic/abdominal pressures) resulting in retrograde expulsion of material from the oesophagus/pharynx/oral cavity/nasal cavity
List some classes of antiemetic drugs
Dopamine antagonists
Metochlopramide
Serotonin antagonists
NK1 antagonists
Antihistamines
Anticholinergics
Phenothiazines
What is the mechanism of action of domperidone?
Dopamine antagonist in chemosensory trigger zone and GIT + adrenergic antagonist in stomach
List an antiemetic dopamine antagonist
Domperidone
What is the mechanism of metoclopramide?
Dopamine and serotonin antagonist centrally
Peripheral cholinergic effect
What are the indications for metoclopramide?
Promotes gastric emptying (prokinetic)
Indicated for use in reflux, chemotherapy, decreased gastric emptying, emesis
What are the precautions when using metoclopramide?
Caution with GI haemorrhage, obstruction, perforation
List a serotonin antagonist anti-emetic
Ondansetron
What is the mechanism of action of ondansetron?
Antagnosies 5HT3 receptors in the chemosensory trigger zone and visceral afferent nerves