GI Pharmacology Flashcards
mylanta
class: neutralizing antacid
- fast acting, short t1/2
- immediate relief
use:
- GERD
mx:
- 2 strong bases:
- - Al(OH)3
- - Mg(OH)2
- +1 antiflatulant
- - simethicone
reversible H2 inhibitors (inverse agonists)
use:
- GERD
- duodenal or gastric ulcer
- hypersecretion of gastric acid
mx:
- reversible competitive antagonist to H2 receptors
- H2 binds histamine, which increases acid production when bound to this receptor
pk:
- onset: 30-60 min
- duration: 6-12 h
AEs:
- diarrhea
- dizziness
- rash
- headache
e. g.:
- cimetidine
- famotidine (Pepcid)
- nizatidine
nizatidine
reversible H2 antagonist
GERD
cimetidine
reversible H2 antagonist
GERD
special note:
- CYP450 antagonist: 1A2, 2C9, 2D6, 3A4
- –> drug-drug interactions
famotidine
reversible H2 antagonist
GERD
proton pump inhibitors (PPIs)
use:
- GERD
- peptic ulcer disease and H. pylori
- Zollinger-Ellison syx (rare pancreatic tumor)
- idiopathic hyper-H+
- upper GI prophylaxis w/ LT NSAID use
mx:
- irreversible H+/K+-ATPase antagonist
- block H+ secretion
PK:
- prodrugs converted by acid
- ion trapping in canalicula on parietal cells
- local accumulation
- enteric-coated: don’t dissolve until SI
- t1/2 1-2 h
- duration: 36 ~ 72 h
- onset: 2-5 days for full effect
- CYP2C19 metabolism
AEs:
- few
- some concerns about unjustified long-term use
e. g.: -prazole
- omeprazole (Prilosec)
- esomeprazole (Nexium)
-prazole
PPI
GERD - long term
omeprazole
PPI
GERD
Prilosec
esomeprazole
PPI
GERD
Nexium
EC drugs
enteric-coated
bypasses stomach
GI effects of NSAIDs
COX1 inhibitors
mucosal injury to upper GI
peptic ulcer disease
possible hemorrhage
worst: aspirin
best: celecoxib
misoprostol
use:
- NSAID injury prophylaxis and tx
mx:
- prostaglandin E1 agonist
- stimulates mucus and bicarb secretion in GI
- weak antagonist of acid
AEs:
- often poorly tolerated
- diarrhea
- abdominal pain
sucralfate
use:
- NSAID injury prophylaxis and tx
- anti-ulcer
mx:
- Al salt, basic
- preferentially neutralizes + proteins near ulcers
- stimulates mucosal repair via x-linking
Scopalamine
Dramamine
Class: anti-cholinergic antiemetic
Mx:
- blocks M1 receptors in area postrema to prevent nausea
Uses:
- nausea
- motion sickness
Sfx/AEs
- drowsiness
- dizziness
- xerosterma (dry mouth)
prochlorperazine
Class: D2 (dopamine) antagonist - same class as many antipsychotics
Mx:
- blocks dopamine 2 receptors in area postrema to prevent nausea
Uses:
- general antiemetic
Sfx/AEs:
- extrapyramidal effects (e.g. twitching)
- neuroleptic malignant syx (serious, treatable: high fever, muscle stiffness
- drowsiness
diphenhydramine (as a GI drug)
class: antihistamine antiemetic
mx:
- blocks H1 receptors in area postrema to prevent nausea
uses
- general antiemetic
- non-GI
Sfx/AEs:
- drowsiness
- constipation
- xerostomia (dry mouth)
- urinary retention
- high risk in >65 y/o
ondansetron
Zofran
class: 5HT3 antagonist antiemetic
mx:
- blocks 5HT3 receptors in area postrema to prevent nausea
uses:
- general antiemetic
- chemo
- pregnancy
Sfx/AEs:
- constipation
- QT prolongation
- headache
metaclopramide
class: mixed 5HT3 ANTagonist/5HT4 AGonist, D2 antagonist
mx:
- see above
- CNS
uses:
- antiemetic
- reflux esophagitis
- promotility (for gastroparesis and pre-op)
- migraine
Sfx/AEs
- drowsiness
- dystonia (spasm)
- tardive dyskinesia (involuntary repetitive body movements)
- limited to ~3 mo use
loperamide
class: opioid AGonist, non-absorbed
mx:
- slows intestinal motility
- decreases secretion
- via opioid receptor effects
uses:
- non-bloody diarrhea
- acute, nonspecific diarrhea
- IBD chronic diarrhea
Sfx/AEs
- minimal as not absorbed
- constipation
- c/i in bloody diarrhea
eluxadoline
class: mixed opioid agonist/antagonist
mx:
- slow motility
- decrease pain
- via opioid receptor effects
uses:
- diarrhea
- abdominal pain
- IBS-D only
Sfx/AEs
- constipation
- nausea
- sphincter of Oddi spasm –> pancreatitis, hepatic enzyme elevation