GI Flashcards
Drugs categories that affect gastric secretion?
Antacids
H2RAs
PPIs
Protectants
When are drugs affecting gastric treatment used?
Dyspepsia (indigestion) Gastric/duodenal ulcers GERD Barrett's Esophagus Hypersecretory states (Zollinger-Ellison)
What are the steps that lead to gastric acid release?
Dietary peptides in lumen bind to G cells
G cells produce gastrin
Gastrin stimulates ECL cells to make histamine
Histamine binds to parietal cells
Parietal cells produce H+ ions that go into the stomach
What inhibits gastric acid production? (molecule and cell that makes it)
Somatastatin released by D cells in response to stomach acid
Ulcers: A failure of _____ _____
mucosal protection
_____ maintains the mucosal layer
prostaglandins
Parietal cells have what pump for acid production?
H/K/ATPase (proton pump)
What do NSAIDs inhibit?
PGE production –> decreased mucous production
What controls histamine release by ECL cells (besides gastrin)
ENS - by releasing acetylcholine
Does chloride move out of parietal cells with or against its gradient?
Against
How do antacids work?
They neutralize acids
What are the antacids?
Sodium bicarb
Calcium bicarb
Aluminum hydroxide
Magnesium hydroxide
Side effects: Sodium bicarb
systemic alkalosis, fluid retention
Side effects: calcium bicarb
hypercalcemia, nephrolithiasis, milk-alkali syndrome
Side effects: aluminum hydroxide
Constipation, hypophosphatemia
Side effects: Magnesium hydroxide
Diarrhea, hypermagnesemia
AlternaGEL
Aluminum hydroxide
Tums
Calcium carbonate
Maalox/Mylanta
Aluminum hydroxide & mag hydroxide
Rolaids
Calcium bicarb & mag hydroxide
Alka-Seltzer
ASA & NaHCO3 (for hangovers)
Gaviscon
Sodium alginate + antacids (weak base)
What does Gaviscon do?
Prevent reflux and effective in GERD
What are the dosage forms of commercial antacids?
chewable tablets
Liquid suspension
What’s the first-gen H2RA?
Cimetidine
H2RAs reduce gastric acid secretion in response to what?
Histamine, gastrin, acetylcholine (things upstream of histamine)
Cons of cimetidine?
DRUG INTERACTIONS
CNS effects (esp elderly)
Antiandrogen
Thrombocytopenia
What’s the benefit of cimetidine?
Clears up warts
What CYPs does cimetidine inhibit?
2C6 and 2D9
2nd gen H2RAs?
Ranitidine
Nizatidine
Famotidine
2nd gen h2RAs have longer or shorter half-life?
Loner –> daily dosing
2nd gen H2RA more or less potent?
More
Where do PPIs work?
Directly on proton pump in parietal cell
What’s vanoprazan?
Potassium-competitive acid blocker (NOT PPI - acts on transmembrane region)
What are the PPIs?
-Oprazole's Esomeprazole Omeprazole Lansoprazole Pantoprazole Rabeprazole
T/F: PPIs are prodrugs
True - activated by acid in parietal cells
PPIs should be taken when?
In the morning
PPIs are reversible/irreversible?
Irreversible
PPIs have a short/long half life?
Short - but long effect b/c they irreversibly inhibit PPIs until protein is turned over
Side effect of PPIs?
Hypergastrinemia –> hypsecretion upon drug withdrawal
Why does hypergastrinemia occur?
B/c PPIs are inhibiting negative feedback of acid onto G cells, which causes lots of gastrin to be produced
How do PPIs react w/ PP?
Disulfide bond - via sulfur
How long do PPIs take for full effect?
1-4 days
ADEs of PPIs?
Nausea CYP2C19 interactions (w/ omeprazole) Increased infection Vit B12 deficiency Decreased Ca absorption/increased bone fractures
Do PPIs decrease acid more or less than H2RAs?
More