GI Flashcards

1
Q

esomeprazole, omeprazole, inasoprazole, dexlansoprazole, pantoprazole, rabeprazole

A

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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2
Q

cimetidine, famotidine, nizatidine, ranitidine

A

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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3
Q

aluminum hydroxide

A

antacid

  • Aluminum hydroxide, calcium carbonate, combination aluminum hydroxide and magnesium hydroxide
  • AE
    • Aluminum hydroxide - produces constipation
      *
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4
Q

magnesium hydroxide

A

antacid

produces diarrhea

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5
Q

calcium carbonate

A

tums and others - antacids

doesnt really cuase constipation or diarrhea

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6
Q

combination aluminum hydroxide and magnesium hydroxide

A

antacid

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

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7
Q

sucralfate

A

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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8
Q

misoprostol

A

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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9
Q

bismuth subsalicylate

A

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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10
Q

how to treat H pylori

A

clarithromycin

amoxicillin

PPI

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11
Q

glycerin

A

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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12
Q

lactulose

A

osmotic laxatives - saline laxatives - nondigestible sugars and alcohols

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13
Q

sorbitol

A

osmotic laxatives - saline laxatives - nondigestible sugars and alcohols

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14
Q

minnitol-polyethylene glycol

A

osmotic laxatives - saline laxatives - nondigestible sugars and alcohols

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15
Q

(PEG) - electrolyte solutions

A
  • 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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16
Q

bisacodyl

A

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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17
Q

cascara sagrada

A

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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18
Q

senna

A

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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19
Q

ricinoleic acid

A

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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20
Q

methylcellulose

A

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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21
Q

lactulose

A

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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22
Q

polycarbophil

A

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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23
Q

mineral oil

A

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
24
Q

glycerin suppositories

A

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
25
Q

docusate

A

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
26
Q

loperamide

A

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
27
Q

diphenoxylate

A

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
28
Q

difenoxin

A

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
29
Q

bismuth - subsalicylate

A

antidiarrheal drug (petobismol)

  • nhibits intestinal secretions
  • Management of infectious diarrhea
30
Q

kaolin/pectin

A

antidiarrheal drug

  • Kaolin (chalk)/pectin (polymerizing agent)
    • When you eat this it forms harder stools (because of the chalk)
31
Q

octreotide

A

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)
32
Q

dimenhydrinate

A

histamine H1 antagonist

  • Histamine H1 antagoinists
    • First generation H1 blockers
    • Produce sedation and antimuscarnic activity
    • Prevents motion sickness
    • Drugs: dimenhydrinate, diphenhydramine, cyclizine, meclizine
33
Q

meclizine

A

histamine H1 antagonist

  • Histamine H1 antagoinists
    • First generation H1 blockers
    • Produce sedation and antimuscarnic activity
    • Prevents motion sickness
    • Drugs: dimenhydrinate, diphenhydramine, cyclizine, meclizine
34
Q

diphenhydramine

A

histamine H1 antagonist

  • Histamine H1 antagoinists
    • First generation H1 blockers
    • Produce sedation and antimuscarnic activity
    • Prevents motion sickness
    • Drugs: dimenhydrinate, diphenhydramine, cyclizine, meclizine
35
Q

cyclizine

A

histamine H1 antagonist

  • Histamine H1 antagoinists
    • First generation H1 blockers
    • Produce sedation and antimuscarnic activity
    • Prevents motion sickness
    • Drugs: dimenhydrinate, diphenhydramine, cyclizine, meclizine
36
Q

metoclopramide

A

D2 antagonists

37
Q

trimethobenzamide

A

D2 antagonist

38
Q

ondansetron, granisetron, dolasetron

A

HT3 antagonists

    • Currently used for nausea and vomiting during cancer chemo
39
Q

aprepitant, foaprepitant, rolapitant

A

NK-1 antagonists

40
Q

chlorpromazine

A

phenothiazine - antiemetic

41
Q

prochloorperazine

A

phenothiazine - antiemetic

42
Q

lorazepam

A

benzodiazepine - antiemetic

43
Q

alprazolam

A

benzodiazepine - antiemetic

44
Q

tetrahydrocannabinol

A

marijuana derivative

45
Q

dronabinol

A

marijuana derivative

46
Q

pancrelipase

A

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
47
Q

amitriptyline or desipramine

A

IBS treatment

  • Tricyclic antidepressants
    • Low doses of amitriptyline or desipramine
    • Treatment of abdominal pain
48
Q

dicyclomine or hyoscyamine

A

IBS treatment

  • Antispasmodics
    • Anticholinergic (dicyclomine, hydroscyamine)
49
Q

tegaserod

A

IBS treatment

  • 5-HT4 partial agonist
    • Tegaserod
    • Emergency treatment only (IBS with constipation) where no alternative exists
    • Serious cardiovascular events can occur
50
Q

alosetron

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

IBS treatment

51
Q

eluxadoline

A

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
52
Q

rifaximin

A

IBS treatment

  • Antibiotic
    • Rifaximin
      • Diarrhea predominant IBS
      • Synthetic antibiotic similar to rifampin
      • May alter bacterial content of GI tract
53
Q

orlistat

A

antiobesity

GI lipase inhibitor

reduces absorption of fats since triglycerides are not split

tox: flatulence, steatorrhea, fecal incontinence

54
Q

sibutramine

A

antiobesity

SERT and NET inhibitor

reduces appetitie

Tox: cardiovascular - tachy, hypertension

55
Q

rimonabant

A

antiobesity

CB1 receptor antagonists (canabanoid receptor antag - bascially anti weed)

reduces appetitie

TOX: depression, anxiety, nausea