B5-048 GI Pharmacology Flashcards
most common secretory disorders
acid-peptic disease
GERD
most common motility disorders
vomiting
diarrhea
constipation
list the mediator, receptors, and antagonist for the neural pathway
mediator: Ach
receptor: muscarinic
antagonist: anti-muscarinic
list the mediator, receptors, and antagonist for the endocrine pathway
mediator: gastrin
receptor: CCKB
antagonist: H2 blocker
list the mediator, receptors, and antagonist for the paracrine pathway
mediator: histamin
receptor: H2
antagonist: H2 blocker
classes that inhibit gastric acid secretion
2
proton pump inhibitors
H2-antagonists
class that neutralizes gastric acid secretion
antacids
irreversibly inhibit the parietal cell proton pump
benzimidazole
PPI
proton pump inhibitors are […] that are […] at a neutral pH
prodrugs
inactive
- activated by acid, but unstable at low pH
- enteric coating only dissolves at alkaline pH
PPIs
how do PPIs maintain efficacy even with chronic use?
parietal intracellular canaliculi are upstream from the proton pump
remains acidic even when proton pump is inhibited
-prazole
proton pump inhibitor
most effective drug for suppressing gastric acid secretion
supresses 90-95%
proton pump inhibitors
with prolonged use, diarrhea occurs due to GIT bacterial overgrowth from removal of natural acidic barrier
PPIs
inhibition of gastric acid secretion persists after withdrawal of drug due to irreversible inhibition
PPIs
-tidine
H2 receptor antagonists
reversible block of H2 receptors leading to decreased H+ secretion by parietal cells
H2 antagonists
- OTC preparations that block acid secretion for about 6 hrs
- only inhibits 60-70% of acid secretion
H2 receptor antagonist
especially effective againsts nocturnal acid secretion
H2 receptor antagonists
largely driven by histamine
relative potency of H2 receptor antagonists
famotidine > nizatidine = ranitidine > cimetidine
block H2 receptors selectively to reduce gastric acid and pepsin secretion
H2 receptor antagonists
20% failure in ulcer patients who smoke and elderly
H2 receptor antagonists
should not be used in combination with PPI
H2 receptor antagonists
reduce efficacy
most common side effects of H2 receptor antagonists
diarrhea
headache
fatigue
myalgias
constipation
bradycardia
mental changes like confusion, hallucinations, and agitation may occur with IV infusion of […] in elderly or renal/hepatic dysfunction
H2 receptor antagonists
- endocrine side effects due to androgen receptor binding
- gynecomastia, impotence, galactorrhea
cimetidine
interferes with cytochrome P450 pathways
cimetidine
antacids
3
- aluminum hydroxide
- calcium carbonate
- aluminum hyroxide/magnesium hydroxide
weak bases that neutralize gastric HCl to form salt and water
antacids
popular due to low cost and rapid action but may cause rebound acid oversecretion
antacids
rebound acid secretion
antacids
why are magnesium and aluminum typically combined in an antacid preparation?
mag causes diarrhea
aluminum causes constipation
offset each other
- establish protective coating on peptic ulcers
- limit exposure to acid/pepsin
musocal protective agents
binds selectively to necrotic ulcer tissue and acts as a barrier
sucralfate
mucosal protective agent
common side effect of sucralfate
constipation
requires acid pH for activation so should not be given with PPIs, H2 antagonists, or antacids
sucralfate
methyl analog of PGE1
misoprostol
muscoal protective agent
binds to PG receptors on parietal cells to inhibit acid secretion
misoprostol
used to prevent NSAID induced ulcers
misoprostol
most common adverse effects of misoprostol
diarrhea
abdominal pain
may cause abortion by stimulating uterine contractions
misoprostol
- protective coating of ulcers
- antibacterial against H pylori
bismuth subsalicylate (pepto)
mucosal protective agent
will darken tongue and stools as side effect
bismuth subsalicylate
gram negative bacterium causing inflammatory gastritis that contribute to peptic ulcers
H. pylori