GI Pharm Flashcards
cytoprotectants
- bismuth subsalicylate
- sucralfate
- misoprostol (protect from NSAIDs)
antacids
- aluminum hydroxide
- magnesium hydroxide
- calcium carbonate
- sodium bicarbonate
H2-receptor antagonists
- cimetidine
- ranitidine
- famotidine
- nizatidine
PPIs
Omeprazole Lansoprazole Rabeprazole Pantoprazole Esomeprazole Dexlansoprazole
antacids AE
- diarrhea
- constipation
- abd distension
cautions: kidney insufficiency, drug interactions (chelation w/ fluoroquinolone, tetracyclines)
antacids MOA
work locally within the GI lumen to neutralize acid
quick relief of symptoms, but duration of action short (a few hours)
bismuth compounds
- bind to base of ulcers
- promote mucin and bicarb production
- antibacterial effects
bismuth subsalicylate
AE
(pepto-bismol)
- constipation
- darkening of of tongue/stool
- avoid if aspirin allergy
- drug interactions
sucralfate
sulfated polysaccharide + AlOH3
- drug (-) pref binds damaged GI mucosa (+)
- activ by acidic envio
- lasts up to 6 hr
- low bioavailability
uses: acid-peptic ulcer disease (adjunctive or alt agent), stress ulcer prophylaxis
sucralfate AE
- constipation*
- accumulation to Al3+
- drug interactions
sucralfate use in kidney insufficiency is dangerous why
accumulation of Al 3+ can occur
misoprostol
prostaglandin E analog
- stim secretion of mucin and bicarb
- inc mucosal BF
- suppresses acid production in parietal cell by binding to EP3 receptor
PROTECT FROM NSAIDs
misoprostol
AE
- diarrhea
- inc uterine contractility (termination/induction)
H2 antagonists
- compete w/ histamine for binding to H2 receptors on parietal cells
- more potent, longer-lasting effects than traditional antacids
H2 antagonist uses
- uncomplicated GERD
- gastric and duodenal ulcers
- stress ulcer prophylaxis
H2A should be dose adjusted for
kidney insufficiency
H2A adverse effects
- diarrhea
- constipation
- drowsiness
- fatigue
- HA
- BM suppression (rare)
- drug interactions (changes pH, interferes w/ drugs req acidic envio)
- CNS w/ high doses (confusion, delirium, hallucinations/slurred speech)
- cimetidine (gynecomastia/galactorrhea)
gynecomastia (men)
galactorrhea (women)
cimetidine (H2A)
H2A drug interactions
drugs req an acidic environment (atazanavir, itraconazole)
cimetidine (H2A) =inhibitor of CYP-450 (phenytoin, theophylline, warfarin)
PPI
MOA
IRREVERSIBLY bind to and inactivate H/K-ATPASE
- prodrugs, req activation in acidic envio
- parent cpd=unstable in acid
- enteric coated formulations usu req
PPI
pharmacokinetics
plasma half life 1-2hr
onset 2-4 days
duration of effect 24-48 hr
PPI
uses
- gastric and duodenal ulcers
- GERF
- Barret’s esophagus
- Zollinger-Ellison syndrome
PPI
AE
- nausea, diarrhea, abd pain, constipation
- altered B12/Ca/Mg absorption
- rash, myopathy, arthralgia, HA
- ECL hyperplasia
- infec, fractures?
anti-platelet + PPI = interaction?
clopidogrel (prodrug) –> active form includes 2 steps req p450 enz (2C19) which is inhibited by PPI
H. pylori tx
multiple antimicrobials + high dose acid suppressive therapy
"triple therapy" exp. -clarithromycin -amoxicillin -PPI
tx duration=10-14d of abx, then continue PPI 2 more wks at lower dose
AE: nausea, diarrhea, taste disturb, allergic rxn
prokinetic for constipation
cholinergic agents
bethanchol
prokinetic for constipation
serotonin receptor modulators
metoclopramide
cisapride
prokinetic for constipation
DA receptor modulators
metoclopramide
domperidone
prokinetic for constipation
motilin-like agents
erythromycin
black box warning of metoclopramide
extrapyramidal symptoms (tardive dyskinesia, parkinsonian type features)
bulk-forming agents for constipation
MOA
not absorbed systemically
MOA: source of fiber enhances stool mass
bulk-forming agents for constipation
AE
- bloating/abd pain (AVOID if suspect obstruction)
- drug interactions
bulk-forming agents for constipation (natural)
psyllium
bulk-forming agents for constipation (semi-synthetic)
methylcellulose
polycarbophil
softeners/surfactants MOA
lowers surface tension of stool
softeners/surfactants
AE
- impaired absorption of fat soluble agents
- oil leakage
- lipid pneumonitis
softeners/surfactants exp
decussate
mineral oil
osmotic agents for constipation MOA
osmotically-mediated water retention stimulates peristalsis
osmotic agents for constipation AE
abd discomfort
flatulence
caution w/saline based osmotic agents if CVD disease present
osmotic agents for constipation
saline-based
Mg citrate
Phosphate salts
osmotic agents for constipation
sugar/alcohol-based
- lactulose, sorbitol, mannitol
- glycerin (suppositories/enemas)
osmotic agents for constipation
other
polyethylene glycol solutions
stimulant laxatives
MOA
produce migrating colonic contractions
stimulant for constipation concerns/toxicities
- avoid overuse
- phenolphthalei/danthron-containing products banned
stimulant for constipation
exps
- diphenylmethanes (bisacodyl)
- anthraquinones (aloe, cascara, SENNA)
- castor oil
Senna is a
stimulant laxative
guanylate cyclase agonists 2 actions
- suppress afferent pain fibers
2. activate CTFR (inc GI secretion)
5HT4 receptor agonists for constipation
- tegaserod (IBS, F>40y/o)
- prucalopride
inc serotonin, promotes motility
peripherally acting mu-opioid receptor antagonists for constipation
- methylnaltrexone
- naloxegol
- alvimopan
- naldemedine
bulk-forming agents used for diarrhea
- bismuth subsalicylate
- cholestyramine
anti motility agents for diarrhea
opioid derivatives
- loperamide
- diphenoxylate + atropine
- eluxadoline
slow intestinal transit by binding as agonists at opioid receptors thru GI tract
alosetron
5HT3 receptor antagonist
- for women
- when primary sx=diarrhea
- AE: potential for severe GI side effects
RIfaximin
rifampin-derived antibiotic
-precise MOA unclear, poss changes in bacterial content
octreotide
- peptide analog of naturally occurring SST that inhibits secretion of serotonin/gastrin/VIP/insulin
- splanchnic VASOCONSTRICTION
use: secretory diarrhea, variceal bleeding
parenteral route
AE: nausea, bloating, injection site reactions
Clonidine
◦ A centrally acting alpha-2 receptor agonist that reduces sympathetic outjow.
◦ Side effects include hypotension and rebound hypertension if abruptly discontinued.
◦ Other side effects include sedation and dry mouth.
type 2 chloride channel agonists
activates chloride channels within GI tract increasing intestinal fluid secretion
exp. Lubiprostone