GI Drugs Flashcards
What are the four common medical conditions affecting the gut
- Gastric/peptic ulcers
- Gastroesophegeal Reflux Disorder (GERD)
- Diarrhea
- Constipation
What four things fall under gastric/peptic ulcers
- excessive hydrochloric acid secretion
- helicobacter pylori infection
- NSAID toxicity
- Inadequate mucosal defense against gastric acid.
What are the excessive HCl secretion therapies
- Proton Pump Inhibitors (PPIs)
- H2 (histamine) receptor blockers
- Antacids- treat symptoms only
What is the suffix of proton pump inhibitors
“-prazole”
-starts with a P so recognize them as proton pump inhibitors
What are the 4 proton pump inhibitors
- esomeprazole
- omeprazole
- lansoprazole
- pantoprazole
what is the #3 highest selling drug in America
Esomeprazole –> Nexium
What is the indication for esomeprazole
- GERD
- Gastric ulcer prophylaxis
- Hypersecretory disorders
- H. pylori infection
What is the MOA of esomeprazole
irreversibly inhibits gastric parietal cell H+ K+ ATPase, thereby inhibiting gastric acid secretion.
which receptors usually aid in the secretion of gastric acid
- acetylcholine: activation leads to activation downstream of the proton pump.
- histamine: drives the pump
- prostraglandins: offer cytoprotective benefit.
- gastrin
What are common AE of esomeprazole
- headache
- constipation
- diarrhea
- xerostomia
- flatulence
what are serious AE of esomeprazole
- SJS
2. TEN
what are drug interactions of esomeprazole
- impaired absorption of azole antifungals and certain antiviral agents.
- azole antifungals
- CAIs: exacerbation of hypomagnesemia
what do esomeprazole’s depend on for their absorption? low or high pH?
low pH
what are the H2 receptor blockers?
- Cimetidine
- Ranitidine
- Famotidine
- Nizatidine
what is the suffix of H2 receptor blockers?
“tidine”
what is the indication of cimetidine
- GERD
- Peptic ulcer
- Dyspepsia (indigestion)
what is the MOA of cimetidine
selective antagonism of gastric parietal cell H2 receptors (act more like inverse agonists though)
what role do the Gs and Gi receptors play?
they are membrane proteins that mediate the stimulatory or inhibitory effect of receptor coupling to adenylyl cyclase
what are common AE of cimetidine
- headache
2. dizziness
what are serious AE of cimetidine
- food and drug allergies
- blood dycrasias
- psychosis, depression
- reversible impotence, gymecomastia (enlargement of a mans breasts)
what are drug interactions of cimetidine
- impaired absorption of azole antifungals & certain antiviral agents
- impaired metabolism of caffeine affecting NSAIDS w/ caffeine
- impaired metabolism of cyclosporine! (know this cause its usually the other way around)
