gastrointestinal pharmacology Flashcards
clinical indications of gastric problems
- H.pylori
- peptic ulceration
- reflux oesophagitis
- gastrin producing tumours (zollinger-Ellison syndrome)
- NSAIDs induced ulceration
main receptors in parietal cells
- histamine II receptor
- muscarinic III receptor
- cholescystokinin II receptors
examples of drugs of proton pump inhibitors (PPIs)
- omeprazole
- esomeprazole
- lansoprazole
mechanism of action of proton pump inhibitors (PPIs)
- irreversibly inhibit the H/K ATPase
- accumulates in canaliculi of parietal cells
- specific inhibition of acid secretion (H2 and M3 antagonism)
- inhibit both basal and stimulated acid secretion
pharmacokinetics effects of PPIs
- inhibitory effect on acid secretion can increase bioavailability
- single dose can inhibit about 2-3 days
- half life ~ 1 hour
unwanted effects of PPIs especially omeprazole
- inhibits 2C family of CYP450
- decreased metabolism of warfarin, carbamazepine, phenytoin
- long term increased gastrin production cause gastric neoplasia
- headache
- diarrhoea
- rashes
examples of drugs of histamine H2 receptor antagonists
- cimetidine
- ranitidine
- famotidine
mechanism action of HH2 receptor antagonists
- competitively inhibit HH2 receptors
- inhibits histamine, gastrin, and Ach-stimulated acid secretion
- decrease both basal and food-stimulated acid secretion by 70%
- promote healing of gastric and duodenal ulcers
unwanted effects of HH2 receptors antagonists
- gynaecomastia
- decreased sexual function
- inhibits CYP450
- potentiate action of oral anticoagulant and TCA
examples of antacids
- magnesium hydroxide/salt
- sodium bicarbonate
- aluminium hydroxide
mechanism of action of antacids
neutralise acidity (removal of H+ ion)
adverse effects of antacids
- sodium bicarbonate causes alkalosis and bloating
- Mg hydroxide causes diarrhoea
- Al hydroxide causes constipation
- combination of Mg and Al preserves bowel function
mechanism of action of bismuth chelate
- combine with regimens to treat H.pylori
- prevent adherence it to the mucosa
- inhibit its bacterial proteolytic enzymes
mechanism of action of sucraflate
- inhibit action of pepsin
- stimulate secretion of mucus, bicarbonate, prostaglandin
misoprolol?
- PGE1 analogues
- prevent gastric damage by NSAIDs
- inhibits basal secretion of gastric acid
- increase secretion of mucus and bicarbonate
first line therapy for H.pylori
- PPIs + amoxicillin + clarithromycin or
2. PPIs + amoxicillin followed by PPI + clarithromycin + metronidazole
second line therapy for H.pylori
PPI + levofloxacin + amoxicillin
third line therapy for H.pylori
PPI + amoxicillin + metronidazole + tetracycline
quadruple therapy
PPI + levofloxacin + amoxicillin + bismuth
examples of bulk laxatives
- fibre (bran)
- ispaghula husk
mechanism of action of bulk laxatives
- increase weight and watery stool
- decreased abdominal pain
- improved stool consistency
- well-tolerated
- onset delayed
examples of osmotic laxatives
- lactulose
- sorbitol
- polyethene glycol
mechanism of action of osmotic laxatives
- relief of constipation
- attract and retain water in intestinal lumen
- lead to soft stools and improved propulsion
adverse effects of lactulose (osmotic laxatives)
- bloating
- nausea
- cramping
- diarrhoea