- bismuth subsalicylate - sucralfate - misoprostol (protect from NSAIDs)

- aluminum hydroxide - magnesium hydroxide - calcium carbonate - sodium bicarbonate

- 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

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

- constipation - accumulation to Al3+ - drug interactions

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

- diarrhea - inc uterine contractility (termination/induction)

- compete w/ histamine for binding to H2 receptors on parietal cells - more potent, longer-lasting effects than traditional antacids

- uncomplicated GERD - gastric and duodenal ulcers - stress ulcer prophylaxis

- 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)

IRREVERSIBLY bind to and inactivate H/K-ATPASE - prodrugs, req activation in acidic envio - parent cpd=unstable in acid - enteric coated formulations usu req

- gastric and duodenal ulcers - GERF - Barret's esophagus - Zollinger-Ellison syndrome

- nausea, diarrhea, abd pain, constipation - altered B12/Ca/Mg absorption - rash, myopathy, arthralgia, HA - ECL hyperplasia - infec, fractures?

GI Pharm Flashcards by Alegra Mendez

cytoprotectants

bismuth subsalicylate
sucralfate
misoprostol (protect from NSAIDs)

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antacids

aluminum hydroxide
magnesium hydroxide
calcium carbonate
sodium bicarbonate

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H2-receptor antagonists

cimetidine
ranitidine
famotidine
nizatidine

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PPIs

Omeprazole 
Lansoprazole
Rabeprazole
Pantoprazole
Esomeprazole
Dexlansoprazole

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antacids AE

diarrhea
constipation
abd distension

cautions: kidney insufficiency, drug interactions (chelation w/ fluoroquinolone, tetracyclines)

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antacids MOA

work locally within the GI lumen to neutralize acid

quick relief of symptoms, but duration of action short (a few hours)

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bismuth compounds

bind to base of ulcers
promote mucin and bicarb production
antibacterial effects

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bismuth subsalicylate

(pepto-bismol)

constipation
darkening of of tongue/stool
avoid if aspirin allergy
drug interactions

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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

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sucralfate AE

constipation*
accumulation to Al3+
drug interactions

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sucralfate use in kidney insufficiency is dangerous why

accumulation of Al 3+ can occur

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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

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misoprostol

diarrhea

- inc uterine contractility (termination/induction)

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H2 antagonists

compete w/ histamine for binding to H2 receptors on parietal cells
more potent, longer-lasting effects than traditional antacids

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H2 antagonist uses

uncomplicated GERD
gastric and duodenal ulcers
stress ulcer prophylaxis

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H2A should be dose adjusted for

kidney insufficiency

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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)

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gynecomastia (men)

galactorrhea (women)

cimetidine (H2A)

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H2A drug interactions

drugs req an acidic environment (atazanavir, itraconazole)

cimetidine (H2A) =inhibitor of CYP-450 (phenytoin, theophylline, warfarin)

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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

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PPI

pharmacokinetics

plasma half life 1-2hr

onset 2-4 days

duration of effect 24-48 hr

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PPI

uses

gastric and duodenal ulcers
GERF
Barret’s esophagus
Zollinger-Ellison syndrome

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PPI

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

1. 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