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IC > Drugs to Treat GI Disorders > Flashcards

Drugs to Treat GI Disorders Flashcards

1
Q

________ drugs are relatively weak inhibitors of acid secretion b/c they act at only one site (M3 receptor mediated by acetylcholine), used as adjuncts to other therapies

A

anti-muscarinic

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2
Q
  • family of peptide hormones formed by gastric mucosal cells
  • stimulates gastric motility, HCl and pepsin secretion
  • no direct antagonists
A

gastrin

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3
Q
  • reduce gastrin secretion

- block histamine induced cAMP and proton pump activation

A

H2 antagonists

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4
Q
  • irreversibly inhibit the parietal cell H/K ATPase
  • all prodrugs that are inactive at neutral pH, activation requires acid environment (take w/ meals so food can stimulate acid secretion)
  • unstable at low pH –> have enteric coated granules that dissolve only at alkaline pH
  • prodrug absorbed in intestines, carried to circulation to parietal cells, accumulates in secretory canaliculi
  • activated at acid pH and bind sulfhydryl groups on H/K ATPase
A

proton pump inhibitors

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5
Q

PPIs retain efficacy with chronic use b/c intracellular canaliculi are ________ from the proton pump target at the luminal membrane

A

upstream

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6
Q
  • prazoles

- currently most effective drugs for suppressing gastric acid secretion b/c gastric response to all stimuli is inhibited

A

PPIs

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7
Q

adverse effects of this drug:

  • GI effects: colic, flatulence, constipation, diarrhea
  • CNS
  • skin rash
  • prolonged use - diarrhea due to GIT bacteria overgrowth from removal of natural acid barrier
  • hepatic metabolism
A

PPIs adverse effects

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8
Q

cimetidine, famotidine, nizatadine, ranitidine

A

H2 receptor antagonists

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9
Q
  • OTC preps that inhibit acid secretion for <6 hours
  • block H2 receptors selectively to reduce gastric acid and pepsin secretion without affecting H/K ATPase, H1, or other receptors
  • effective against noctural secretion which is largely driven by histamine
A

H2 receptor antagonists (-dines)

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10
Q

side effects of this drug

  • extremely safe, minor and infrequent adverse effects
  • don’t give to pregnant or nursing women
  • diarrhea, headaches, fatigue, myalgias, constipation, bradycardia
  • confusion, hallucinations, agitation with IV admin in hepatic dysfunction
A

H2 receptor antagonists

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11
Q
  • this drug causes gynecomastia or impotence in men, galactorrhea in women
  • endocrine effects b/c it inhibits binding of dihydrotestosterone to androgen receptors, inhibits estradiol metabolism, increases serum prolactin
  • interferes with CYP450 paths
A

cimetidine (H2 receptor antagonist)

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12
Q
  • all equally effective for healing and preventing recurrence of PUD
  • given 1X daily at bedtime to suppress nocturnal acid secretion
  • use declined following PPIs
A

H2 antagonists (-dines)

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13
Q
  • 20% failure in ulcer patients who smoke and in the elderly
  • don’t use in combo with PPIs, reduce efficacy by reducing acid activation
  • combined with abx and bismuth for treatment of Hpylori
A

uses of H2 antagonists

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14
Q
  • aluminum hydroxide
  • calcium carbonate
  • combo aluminum hydroxide and magnesium hydroxide
A

antacids

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15
Q
  • act by reducing gastric acidity, inactivating pepsin
  • weak bases that neutralize gastric HCl to form salt and water, may interfere with absorption of other drugs
  • may provide mucosal protection by stimulating PG synthesis
A

antacids

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16
Q
  • aluminum or magnesium hydroxide
  • single dose given 1 hr after eating neutralizes for 2 hours
  • side effects: diarrhea for magnesium, constipation for aluminum
  • used as needed to relieve pain in esophagitis, peptic ulcer, and GERD
  • not recommended for treatment of active peptic ulcers
A

antacids

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17
Q
  • protective coating on peptic ulcers, limits exposure to acid and pepsin
  • sucralfate binds selectively to necrotic ulcer tissue and acts as barrier
A

mucosal protective agents

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18
Q
  • polymerizes to produce viscous gel that adheres strongly to epithelial cells and ulcer craters in acid environment
  • effective in healing duodenal ulcers
  • side effect: constipation
  • requires acid pH for activation, don’t give with antacids/H2 antagonist/PPI
A

sucralfate

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19
Q
  • methyl analog of PGE1
  • binds PG receptors on parietal cells to inhibit acid secretion
  • because NSAIDS inhibit PG formation, it’s used to prevent NSAID induced ulcers
  • adverse: diarrhea, abdominal pain
  • may cause abortion by stimulating uterine contractions
A

misoprostol

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20
Q
  • colloidal bismuth
  • protective coating of ulcers, antibacterial against Hpylori
  • darken tongue and stool
A

bismuth subsalicylate (pepto bismol)

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21
Q

antibiotic regimen for Hpylori?

A

clarithromycin + amoxicillin + PPI

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22
Q
  • nonabsorbable salts containing magnesium cations (magnesium citrate) or phosphate anions (sodium phosphate)
  • act by osmotic force to hold water inside intestines –> distended intestines –> stimulate peristalsis
  • intensely bitter taste masked by citrus
  • avoid in renal insufficiency, heart disease, electrolye imbalance, diuretic co treatment
A

saline laxatives

23
Q

-trihydroxy alcohol that acts in the rectum as lubricant and hygroscopic agent –> water retention –> stimulate peristalsis

A

glycerin

24
Q
  • nonabsorbable sugars

- hydrolyzed to organic acids - acidify luminal contents - draw water into lumen - increase colonic propulsive motility

A

lactulose, sorbitol, mannitol

25
Q
  • poorly absorbed, retain added water by their high osmotic pressure
  • colonoscopy prep, drink 3-4 liters over 3-4 hours to produce watery diarrhea and remove solid wastes
A

PEG-electrolyte solutions

26
Q
  • act directly on enterocytes, enteric neurons, and muscle

- induce low grade intestinal inflammation, water and electrolytes accumulate, increase intestinal motility

A

stimulant or irritant laxatives

27
Q
  • a diphenylmethane derivative, available as enteric coated tablets taken at bedtime to take effect next morning
  • swallow to avoid activation in stomach
A

bisacodyl

28
Q
  • stimulant/irritant laxative
  • poorly absorbed in small intestine and require activation in colon with effects 6-12 hours later
  • long term use: melanomic pigmentation of colon, cathartic colon (dilated, ahaustral)
A

anthraquinones - aloe, cascara sagrada, senna

29
Q

-stimulant/irritant: increases intestinal secretion and motility, seldom used due to unpleasant taste and toxic potential

A

castor oil (ricinoleic acid)

30
Q

methylcellulose, lactulose, polycarbophil

A

bulk forming laxatives

31
Q

mineral oil, glycerin suppositories, docusate sodium

A

stool softeners - facilitate expulsion

32
Q

often prescribed to prevent straining in hospitalized patients

A

docusate

33
Q

loperamide, diphenoxylate, difenozin, bismuth salicylate, kaolin/pectin

A

antidiarrheal drugs

34
Q

act on intestinal opioid receptors - inhibit Ach release - decrease motility (peristalsis)

A

loperamide, difenoxin, diphenoxylate

35
Q
  • 40-50X more effective than morphine for diarrhea, does not cross BBB
  • relief of acute nonspecific diarrhea
  • effective against traveler’s diarrhea
  • more effective than diphenoxylate
A

loperamide

36
Q
  • act by absorbing compounds and presumably binding potential intestinal toxins
  • antidiarrheal
A

kaolin and pectin

37
Q

-antidiarrheal that inhibits intestinal secretions, management of infectious diarrhea

A

bismuth salicylate

38
Q
  • antidiarrheal: inhibits secretion of gastrin, cholecystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, VIP, 5-HT
  • reduces intestinal fluid and pancreatic secretion
  • slows GI motility and inhibits gallbladder contraction
  • reduces portal and splanchnic bloodflow
A

somatostatin/octreotide

39
Q
  • first generation H1 blockers
  • produce sedation and antimuscarinic activity
  • prevent motion sickness
  • dimenhydrinate, diphenhydramine, cyclizine, meclizine
A

anti-emetics: histamine H1 antagonists

40
Q

metoclopramide, trimethobenzamide

A

D2 antagonists (anti-emetic)

41
Q

ondansetron, granisetron, dolasetron

A

5-HT3 antagonists, chemotherapy anti-emetics

42
Q

aprepitant, fosaprepitant, rolapitant

A

NK-1 antagonists, anti-emetic

43
Q

chorpromazine, prochlorperazine

A

phenothiazines, anti-emetic

44
Q

THC, dronabinol

A

marijuana derivatives - anti-emetic

45
Q
  • low doses of amitriptyline or desipiramine

- treatment of abdominal pain

A

tricyclic antidepressants - treat IBS

46
Q

anticholinergics (dicyclomine, hyoscyamine)

A

antispasmodics - IBS treatment

47
Q
  • tegaserod
  • emergency treatment only
  • CV effects
A

5-HT4 partial agonist, IBS treatment

48
Q
  • 5HT3 antagonist, for IBS treatment
  • diarrhea prominent IBS
  • serious CV events can occur
A

alosetron

49
Q
  • diarrhea prominent IBS treament
  • opioid agonist/antagonist
  • reduces neuronal drive on peristalsis
  • spasm in sphincter of Oddi can cause pancreatitis
A

eluxadoline

50
Q
  • diarrhea prominent IBS treatment
  • synthetic antibiotic similar to rifampin
  • may alter bacterial content of GI tract
A

rifaximin

51
Q
  • pancreatic insufficiency can lead to steatorrhea, azotorrhea, vitamin malabsorption, weight loss
  • enzyme supplements _______ and _______ treat enzyme insufficiency
  • administer with each meal and snack
  • can lead to hyperuricosuria and renal stones
A

pancreatin, pancrelipase

52
Q
  • antiobesity
  • targets gut, GI lipase inhibitor
  • reduces absorption of fats since triglycerides not split
  • toxicity: flatulence, steatorrhea, fecal incontinence
A

orlistat

53
Q
  • target CNS, SERT and NET inhibitor
  • reduces appetite
  • CV effects: tachycardia, hypertension
A

sibutramine

54
Q

targets CNS, a CB1 receptor antagonist, reduces appetite

-toxicity: depression, anxiety, nausea

A

rimonabant

IC (29 decks)

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