GI pharmacology - Full summary Flashcards
What are some examples of Histamine H2 antagonists?
Ranitidine
Cimetidine
Famotidine
Nizatidine
How does histamine affect HCl production?
Histamine binds to H2 receptors, which activates adenylyl cyclase
This converts AMP to cAMP
cAMP increases production of proton pumps, which increases secretion of HCl
How do anti (H2) histamines work?
They block H2 receptors on parietal cells and thus prevent the action histamine, as it increases HCl production
Anti (H2) histamines therefore decrease HCl production
What conditions are anti-histamines (H2) indicated in?
Benign gastric acid ulceration
NSAID associated ulceration
How can tolerance form against anti-histamines (H2)?
After 4 weeks, down regulation of the histamine pathway can cause up regulation of the acetylcholine and gastrin pathways, therefore increasing HCl secretion
What are some examples of muscarinic (M3) antagonists used in control of stomach acid production?
Solifenacin
Darifenacin
How do antacids work?
They work as a buffering system
They contain salt based compounds such as NaHCO3 and CaCO3, which dissociate and buffer the H+ ions of the HCl, therefore decreasing the acidity of the stomach acid
What are some gastrointestinal side effects of NSAIDs?
Gastric bleeding
Ulceration
Abdominal discomfort
How can NSAIDs cause increased stomach acid production?
NSAIDs prevent the production of prostaglandins, which increases histamine levels and decreases mucosal protection of the stomach lining
What is misoprostol?
This is a chemical analogue of prostaglandin E1
In what conditions is misoprostol indicated?
prophylaxis of NSAID induced ulcers
What are some side effects of misoprostol?
Abdominal pain
Diarrhoea
Induces uterine contractions and labour
What are some examples of proton pump inhibitors?
Lansoprazole
Omeprazole
Pantoprazole
Esomeprazole
How do proton pump inhibitors work?
They irreversibly antagonise the H+/H+ ATPase which allows for the secretion of Cl- ions into the gastrointestinal lumen
What is a possible side effect of PPI use?
Increased susceptibility to GI tract infection