mucosal protective agent Binds selectively to necrotic ulcer tissue and acts as a barier Polymerizes to produce a viscous gel that adheres to the epi cells Effective in healing duodenal ulcers AE Constipation = most common Requires acidic pH for activation - don’t give with antacids, H2 antagonists or PPIs

mucosal protective agent Misoprostol - Methyl analog of PGE1 Binds to PG receptors on parietal cells to inhibit acid secretion NSAIDs inhibit production of PG - but you can replace the PG in the stomach to stop the ulcers from forming Use Prevent NSAIDs ulcers from forming AE Diarrhea and abdominal pain May cause abortion by stimulating uterine contractions

osmotic laxatives - saline laxatives - nondigestible sugars and alcohols Glycerin - Trihydroxy alcohol that acts as a lubricant and osmotic agent Lactulose, sorbitol, mannitol - non absorbable sugars Saline laxatives - non absorbable salts containing magnesium cations (mag citrate) or phosphate anions (sodium phosphate) Have a very bitter taste - people commonly add to fuit juices Avoid in patients with Renal insufficiency - theses patients already have issues with water balance Heart disease Electrolyte imbalance Diuretic drug co treatment

stimulant or irritant laxatives Bisacodyl Enteric coated tablets taken at bedtime to take effect next morning Don’t chew = break the capsule

stimulant or irritant laxatives Anthraquinones like: aloe, cascara sagrada, or senna Poorly absorbed in small intestine and require activation in the colon (laxative effects 6-12 hours later) Long term use can cuase melanomic pigmentation of colonic mucosa and cathartic colon (colon dilated and ahaustral)

stimulant or irritant laxatives (castor oil) Local irritant -\> increases intestinal secretion and motility Now seldom used due to unpleasant taste and toxic potential

GI Flashcards by Matt Zabel

esomeprazole, omeprazole, inasoprazole, dexlansoprazole, pantoprazole, rabeprazole

PPI

Benzimidazole compounds irreversibly inhibit parietal cell proton pump (H/K ATPase)
- The inhibition persists after stoping the drug (because its an irreversible inhibitor) - have to wait for new pumps to be made
They are pro drugs that are inactive at neutral pH (need acid to be active)
- Take with meals = food -> more gastric secretion
- These drugs are unstable at low pH - enteric coating (only disolves in alkaline pH) to get past stomach - absorbed in intestines -> carried in circulation to parietal cells where it acts
- The drug acts at the intracellular canaliculi which is upstream from the proton pump (this is how it stays chornically active even when it shuts down gastric acid secretion ) (it still needs acidic envionrment to work)
Drugs
- Esomeprazole, omeprazole, lansoprazole, dexlansoprazole, pantroprazole, rabeprazole
Curretnly the most effective drugs for suppressing gastric acid secretion because gastric response to all stimuli is inhibited\
Can give a single daily dose
AE
- GI effects (nausea, colic, flatulence, constipation, diarrhea)
- CNS effects (headaches, dizziness, somnolence)
- Skin rashes
- With prolonged use diarrhea often occurs due to GIT bacterial overgrowth from removal of natural acid barrier
- Hypergastrinemia can happen
Hepatic metabolism with negligible renal clearance
Uses
- Promote peptic ulcer healing and prevent recurrence
- Effective in patienst unresponsive to H2 antagonists
- More effective than H2 antagonists for GERD or NSAID induced peptic ulcers

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cimetidine, famotidine, nizatidine, ranitidine

H2 receptor antagonists

All are over the counter structural histamine analogs -> block H2 receptors selectivlty to reduce gastric acid and pepsin secretion
- Doesn’t affect H/K ATPase, H1 or any other receptors
- Best at inhibiting nocturnal secretion (largely driven by histamine)
AE
- Diarrhea, headaches, fatigue, myalgias, constipation, bradycardia
- Don’t give to pregannt women or nursing women - they can cross placenta and get into milk
- Mental changes: confusion, hallucinations and agitation may occur with IV administration in patents who are old or have renal or hepatic dysfunction
- Cimetidine can cuase gynecomastia or impotence in men
  - Cimetidine inhibits dihydrotestosterone to androgen receptors
  - Can also interfere with CYP 450 pathways for other drugs
- They stop formation of protons at the canaliculi of parietal cells = less activation of PPDs
Uses
- All equally effective for healing and preventing recurrence of PUD
- Given once a day at bed time
- We have better drugs so they are used less now
- Can be combined with antibiotics and bismuth for treatment of H pylori

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aluminum hydroxide

antacid

Aluminum hydroxide, calcium carbonate, combination aluminum hydroxide and magnesium hydroxide
AE
- Aluminum hydroxide - produces constipation
  *

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magnesium hydroxide

antacid

produces diarrhea

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calcium carbonate

tums and others - antacids

doesnt really cuase constipation or diarrhea

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combination aluminum hydroxide and magnesium hydroxide

antacid

aluminum cuases constipation and the magnesium cuases diarrhea - put them together - they cancel eachother out

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sucralfate

mucosal protective agent

Binds selectively to necrotic ulcer tissue and acts as a barier
- Polymerizes to produce a viscous gel that adheres to the epi cells
- Effective in healing duodenal ulcers
AE
- Constipation = most common
Requires acidic pH for activation - don’t give with antacids, H2 antagonists or PPIs

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misoprostol

mucosal protective agent

Misoprostol - Methyl analog of PGE1
- Binds to PG receptors on parietal cells to inhibit acid secretion
  - NSAIDs inhibit production of PG - but you can replace the PG in the stomach to stop the ulcers from forming
- Use
  - Prevent NSAIDs ulcers from forming
- AE
  - Diarrhea and abdominal pain
- May cause abortion by stimulating uterine contractions

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bismuth subsalicylate

peto-bismol

Bismuth subsalicylate (pepto bismol) - colloidal bismuth
- Protective coating of ulcers - precipitates out in the stomach forming a lining on the stomach
  - The precipitate is black - can turn your tongue black
- Antibacteiral agaisnt H pylori

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how to treat H pylori

clarithromycin

amoxicillin

PPI

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glycerin

osmotic laxatives - saline laxatives - nondigestible sugars and alcohols

Glycerin -
- Trihydroxy alcohol that acts as a lubricant and osmotic agent
Lactulose, sorbitol, mannitol - non absorbable sugars
Saline laxatives - non absorbable salts containing magnesium cations (mag citrate) or phosphate anions (sodium phosphate)
- Have a very bitter taste - people commonly add to fuit juices
- Avoid in patients with
  - Renal insufficiency - theses patients already have issues with water balance
  - Heart disease
  - Electrolyte imbalance
  - Diuretic drug co treatment

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lactulose

osmotic laxatives - saline laxatives - nondigestible sugars and alcohols

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sorbitol

osmotic laxatives - saline laxatives - nondigestible sugars and alcohols

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minnitol-polyethylene glycol

osmotic laxatives - saline laxatives - nondigestible sugars and alcohols

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(PEG) - electrolyte solutions

Poorly absorbed and retain added water by osmotic pressure
Mixtures of: sodium sulfate, sodium bicarbonate, sodium chloride, potassium chloride in isotonic solution
Used in colonoscopy preparation - drink 3-4 liters over 3-4 hours to produce watery diarrhea and remove solid wastes

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bisacodyl

stimulant or irritant laxatives

Bisacodyl
- Enteric coated tablets taken at bedtime to take effect next morning
  - Don’t chew = break the capsule

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cascara sagrada

stimulant or irritant laxatives

Anthraquinones like: aloe, cascara sagrada, or senna
- Poorly absorbed in small intestine and require activation in the colon (laxative effects 6-12 hours later)
- Long term use can cuase melanomic pigmentation of colonic mucosa and cathartic colon (colon dilated and ahaustral)

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senna

stimulant or irritant laxatives

Anthraquinones like: aloe, cascara sagrada, or senna
- Poorly absorbed in small intestine and require activation in the colon (laxative effects 6-12 hours later)
- Long term use can cuase melanomic pigmentation of colonic mucosa and cathartic colon (colon dilated and ahaustral)

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ricinoleic acid

stimulant or irritant laxatives (castor oil)

Local irritant -> increases intestinal secretion and motility
Now seldom used due to unpleasant taste and toxic potential

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methylcellulose

bulk forming laxatives

contain lots of soluble fiber and other stuff to give you more material in feces

Methylcellulose, lactulose and polycarbophil

Still have to keep hydrated - need water to move everything along

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lactulose

bulk forming laxatives

contain lots of soluble fiber and other stuff to give you more material in feces

Methylcellulose, lactulose and polycarbophil

Still have to keep hydrated - need water to move everything along

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polycarbophil

bulk forming laxatives

contain lots of soluble fiber and other stuff to give you more material in feces

Methylcellulose, lactulose and polycarbophil

Still have to keep hydrated - need water to move everything along

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mineral oil

stool softener

Agents that soften stools and facilitate expulsion
Given orally or rectally
Include: mineral oil, glycerin suppositories, docusate sodium
Docusate is often prescribed to prevent straining in hospitalized patienst
- Also can be given with opiates to prevent constipation

glycerin suppositories

stool softener

Agents that soften stools and facilitate expulsion
Given orally or rectally
Include: mineral oil, glycerin suppositories, docusate sodium
Docusate is often prescribed to prevent straining in hospitalized patienst
- Also can be given with opiates to prevent constipation

docusate

stool softener * Agents that soften stools and facilitate expulsion * Given orally or rectally * Include: mineral oil, glycerin suppositories, docusate sodium * Docusate is often prescribed to prevent straining in hospitalized patienst * Also can be given with opiates to prevent constipation

loperamide

antidiarrheal drug * Loperamide, difenoxin and diphenoxylate - these are basically non effective opioids - give constipation but don’t relieve pain * Act on intestinal opioid receptors -\> inhibit ACH release -\> decreases motility * Loperamide * Effective agasint travelers diarrhea - but need to discontinue if improvemnet doesn’t happen in 48 hours * Can get rebound constipation

diphenoxylate

difenoxin

bismuth - subsalicylate

antidiarrheal drug (petobismol) * nhibits intestinal secretions * Management of infectious diarrhea

kaolin/pectin

antidiarrheal drug * Kaolin (chalk)/pectin (polymerizing agent) * When you eat this it forms harder stools (because of the chalk)

octreotide

antidiarrheal drug * Somatostatin/octreotide - endogenous hormones = reduce motility * Inhibits secretion of: gastrin, cholecystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, VIP, and 5-HT * Slows motility and inhibits gallbladder contraction * Reduces portal and splanchnic blood flow * Used more in chronic cases of diarhea (more serious drugs)

dimenhydrinate

histamine H1 antagonist * Histamine H1 antagoinists * First generation H1 blockers * Produce sedation and antimuscarnic activity * Prevents motion sickness * Drugs: dimenhydrinate, diphenhydramine, cyclizine, meclizine

meclizine

diphenhydramine

cyclizine

metoclopramide

D2 antagonists

trimethobenzamide

D2 antagonist

ondansetron, granisetron, dolasetron

HT3 antagonists * * Currently used for nausea and vomiting during cancer chemo

aprepitant, foaprepitant, rolapitant

NK-1 antagonists

chlorpromazine

phenothiazine - antiemetic

prochloorperazine

phenothiazine - antiemetic

lorazepam

benzodiazepine - antiemetic

alprazolam

benzodiazepine - antiemetic

tetrahydrocannabinol

marijuana derivative

dronabinol

marijuana derivative

pancrelipase

pancreastic enzyme replacment * Pancreatic enzyme supplements * Exocrine pancreastic insufficiency caused by cystic fibrosis, chronic pancreastitis, or pancreastic resection * Can lead to steatorrhea, azotorrhea, vitamin malabsorption and weight loss * Supplements * Pancreatin * Pancrelipase * Administed with each meal and snack - need the enzymes to digest the food * High purine content of extracts can lead to hyperuricosuria and renal stones

amitriptyline or desipramine

IBS treatment * Tricyclic antidepressants * Low doses of amitriptyline or desipramine * Treatment of abdominal pain

dicyclomine or hyoscyamine

IBS treatment * Antispasmodics * Anticholinergic (dicyclomine, hydroscyamine)

tegaserod

IBS treatment * 5-HT4 partial agonist * Tegaserod * Emergency treatment only (IBS with constipation) where no alternative exists * Serious cardiovascular events can occur

alosetron

* 5-HT3 antagonist * Alosetron * This is if conventional therapy failed * Diarrhea predominant IBS * Serious cardiovascular events can occur IBS treatment

eluxadoline

IBS treatment * kappa opioid agonist/ delat opioid antagonist * Eluxadoline * Diarrhea predominant IBS * Reduces neuronal drive on peristalsis * Spasm in sphincter of oddi can result in pancreatitis

rifaximin

IBS treatment * Antibiotic * Rifaximin * Diarrhea predominant IBS * Synthetic antibiotic similar to rifampin * May alter bacterial content of GI tract

orlistat

antiobesity GI lipase inhibitor reduces absorption of fats since triglycerides are not split tox: flatulence, steatorrhea, fecal incontinence

sibutramine

antiobesity SERT and NET inhibitor reduces appetitie Tox: cardiovascular - tachy, hypertension

rimonabant

antiobesity CB1 receptor antagonists (canabanoid receptor antag - bascially anti weed) reduces appetitie TOX: depression, anxiety, nausea