GI Drugs Flashcards
Histamine binds H2 receptors on the _____ cell which increases the intracellular concentration of ________ to stimulate the _______
parietal cell
cAMP
stimulates proton pump (H+/K+ ATPasae)
What substance decreases cAMP production and therefore reduces proton pump activity? It also increases mucous and bicarb production…
PGE3
What drug can be used with NSAID administration to protect against ulcers?
misoprostol (PG analog)
Tritec is the h. pylori triple therapy that includes…
ranitidine, bismuth citrate + clarithromycin
Helidec is the h. pylori quadruple therapy that includes…
metro, amoxicillin, tetracycline, clarithromycin
_______ increases gastric motility and may cause diarrhea…
magnesium
antacid
________ relaxes smooth muscle and may cause constipation…
alumininium
These drugs neutralize HCl to form salts and water.
antacids
Antacids are commonly hydroxides of what 4 compounds?
aluminium
magnesium
sodium bicarb
calcium
Mg antacids are well tolerated, but can be a problem/toxicity in the presence of what condition?
renal impairment
Two main uses for antacids…
Sx relief
GERD Adjunct
sodium bicarb should be avoided with what condition?
CHF
How do antacids cause drug interactions?
alter rate of dissolution/absorption
complex formation
delayed gastric emptying
When are H2 receptor blockers most effective?
overnight
H2 receptor blockers are effective at treating which condition?
PUD
H2 receptor blockers can be considered an adjunct in what 2 conditions?
GERD
Zollinger-Ellison
Which GI drug is given pre-op to reduce stomach acidity in case of aspiration?
H2 receptor blockers
Why are H2 receptor blockers given in allergic rxns?
reduce vasodilation
Duration of H2 blockers
12 hours
H2 blockers have low S/E profile… but which one has an anti-androgen effect?
cimetidine
cimetidine inhibits…
CYP3A4
DOC for GERD.
PPIs
PPIs cause reversible or irreversible inhibition at the parietal cell?
irreversible (covalent bonding)
how long before 80% inhibition of acid secretion with PPIs?
2-5 days
How long do PPIs last? why?
24-48 hours
requires synth of new pumps
T or F… all PPIs are prodrugs converted to active form (Sulfenamide) by acid…
true
Recommended dosing regimen for PPIs
take in morning on empty stomach 30 min before 1st meal
PPIs are generally well tolerated, but what are two SEs that may occur?
PNA
Abd. Colic/GI sxs
chronic PPI use can cause decreases in… (3)
Calcium
Magnesium
B12
long term PPI use can cause what 2 diseases?
CKD
osteoporosis
________ inhibits CYP2C19, decreasing metabolism of phenytoin, diazepam, warfarin and conversion of clopidogrel to active compound.
omeprazole
C/I for misoprostol…
pregnancy, or could become pregnant
What is a cytoprotective agent used to protect the gastric mucosa?
misoprostol
This is a D2 receptor antagonist, which enhances ACh release on M3 receptors in the GI tract
metoclopramide