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IC > Drugs for GI Disorders > Flashcards

Drugs for GI Disorders Flashcards

1
Q

The most common secretory disorder in GI tract is

A

acid- peptic disease

  • peptic ulcer disease
  • GERD (50%)
  • hypersecretory states (Zollinger ellison syndrome)
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2
Q

Goals of treating acid-peptic disease

A

Relieve pain, promote healing, prevent recurrence

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3
Q

Anti ulcer drugs act to

A

neutralize gastric acid, reduce secretion, enhance mucosal defenses

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4
Q

Anti muscarinic drugs for gastric acid secretion

A

weak inhibitors of acid secretion because they act at one site
-Ach mediator acting on muscarinic receptors
Use with other therapies

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5
Q

Gastrin blockage

A

-peptide hormones formed by mucosal cells
Stimulates gastric motility, HCL, and pepsin secretion

Acts towards gastrin- cholecystokinin B and is an H2 blocker

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6
Q

H2 antagonists (general)

A

reduce gastrin secretion by blocking histamine induced inc cAMP and proton pump activation (Gastric acid secretion)

On parietal cell

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7
Q

PPI

A

-end with -prazole (omeprazole, esomeprazole, etc.)

Benzimidazole cpds irreversibly inhibit parietal cell proton pump, H/K/ATPase

Prodrugs which are inactive at neutral pH- requires acidic environment in canaliculi (don’t give with antacids)

Metabolized in liver

More effective than H2 antagonists or NSAID induced peptic ulcers

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8
Q

AE of PPI

A

GI effects because no longer having acidic environment to prevent food and microbes from entering small bowel

Diarrhea with prolonged use due to GIT bacterial overgrowth

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9
Q

Activation of PPI

A

Prodrugs which after passing through stomach, enteric coating dissolve and the pro drug is absorbed in the intestines and then carried to parietal cell, where drug accumulates in secretory canaliculi.
Here, the activated drug binds to sulfyhdryl groups on H/K ATPase

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10
Q

H2 antagonists-

A

-end with tidine (famotidine > nizatidine = ranitidine > cimetidine)

histamine (H2) receptor antagonists to reduce gastric acid and pepsin secretion (particularly useful at bedtime)- does not inhibit other receptors or channels

inhibit acid secretion for <6 hrs when OTC and inhibits 60-70% for 24 hours when prescription

decline use because of ppi

do not use in combo with ppis because reduce acid secretion in parietal cells so ppi won’t get activated

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11
Q

H2 Antagonist AE

A
  • safe
  • not to be given to pregnant women bc they cross placenta and secreted into breast milk
  • diarrhea, headaches, bradycardia, fatigue
  • confusion and agitation with IV admin in pts who are elderly
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12
Q

Cimetidine

A

H2 receptor antagonist which causes gynecomastia or impotence in men and galactorrhea in women because endocrine effects (cimetidine inh binding of dihydrotestosterone to androgen receptors)
interferes with cyp 450 pathways

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13
Q

Antacids

A
  • aluminum hydroxide, calcium carbonate, combination aluminum hydroxide and magnesium hydroxide (aluminum will lead to constipation, magnesium will lead to diarrhea, calcium is constipating)
  • weak bases that neutralize gastric Hcl
  • used as needed to relieve pain in esophagitis, peptic ulcer, and GERD

can cause cation absorption and systemic alkalosis in renal pts

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14
Q

Do not use antacids if you are a

A

renal pt- can cause cation absorption and systemic alkalosis in renal pts

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15
Q

-Sucralfate (aluminum sucrose sulfate)

A
  • Mucosal protective agent
  • protective coating on peptic ulcers

require’s acidic environment to be activated

AE: constipation
few other adverse effects

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16
Q

Misoprostol

A

Mucosal protective agent

methyl analog of PGE1
Binds to PG receptors on parietal cells to inhibit acid secretion

Used for long term NSAID use because NSAIDs inhibit PG formation, misoprostal will prevent NSAID induced ulcers

AE: diarrhea, abd pain, abortion by stimulating uterine contractions

17
Q

Bismuth subsalicylate (Pepto Bismol)

A 
mucosal protective agents
protective coating of ulcers
antibacterial against H pylori
-OTC for dyspepsia and acute diarrhea 
-minimal AE because not absorbed but will darken tongue and stools
18
Q

H pylori

A

gram neg bacterium, causes inflammatory gastritis that may lead to peptic ulcers

triple therapy for 10-14 days: calrithromycin, amoxicillin, ppi (allergic to penicillin- use metronidazole)

19
Q

Laxatives

A

Used to promote defecation and treat constipation

  • often abused by patients with eating disorders
  • usually unnecessary as constipation can be resolved by inc water and fiber content, appropriate bowel habits, imrproved physical activity, attention to psychosocial and emotions
20
Q

Saline laxatives

A

-Osmotically active
Nonabsorbable salts containing mangesium cations or phosphate anions
-act as osmotic force to hold water inside intestines–> distended intestines–> stimulate peristalsis
-avoid in renal insufficiency, heart disease, electrolyte imbalance, diuretic co treatment

21
Q

Nondigestible sugars and alcohols

A

osmotically active laxative
-glycerin acts in rectum as lubricant–> water retention–> stimulate peristalsis

lactulose, sorbitol, mannitol are nonabsorbable sugars–> hydrolyzed to organic acids–> acidify lumen–> draw water in–> increase motility

22
Q

Polyethylene glycol electrolyte solutions

A

osmotically active laxative

  • poorly absorbed and retain added water by high osmotic pressure
  • colonoscopy prep
23
Q

Stimulant or Irritant Laxatives

A

Act on enterocytes, enteric neurons, muscle induce low grade intestinal inflammation–> water and electrolytes accumulate–> inc intestinal motility

  • Diphylmethane derivatives- bisacodyl (unchewed pill taken at bedtime), phenolphthalein (withdrawn due to carcinogenicity)
  • anthraquinones like aloe, cascara sagrada or senna- poorly absorbed in SI and require activation in colon with lax effects later; long term use causes melanomic pigmentation of colonic mucosa and cathartic colon (dilated and ahaustral)
  • Ricinoleic acid (castor oil) -local irritant, unpleasant taste, toxic potential
24
Q

Bulk forming laxatives

A

dietary supplements add bulk and hold water to intestinal contents

  • methylcellulose, lactulose, polycarbophil
  • must take with lots of water
25
Q

Stool softeners

A

soften stool, facilitate expulsion

  • oral or rectal
  • mineral oil, glycerin suppositories, docusate sodium
  • docusate often prescribed to prevent straining in hospitalized pts or those on opioids
26
Q

Antidiarrheal

A
  • usually self limiting
  • loperamide, diphenoxylate, difenoxin (low efficacy opioids only producing SE of constipation- remove ACh and para tone on GI), bismuth subsacicylate (inh intestinal secretions- manage infxs diarrhea), kaolin/pectin (absorbing cpds and bind potential intestinal toxins), somatostatin/octreotide
27
Q

Loperamide

A
  • Antidiarrheal drugs
  • opioid, inhibits ACh release–> decrease motility, does not cross BBB
  • quickly (3-5) hrs for relief of acute, non specific diarrhea (Traveler’s diarrhea) (may exacerbate diarrhea due to criters)
  • may result in rebound constipation

-more effective than diphynoxylate

28
Q

Somatostatin/Octreotide

A

-inhibits secretin of gastrin, cholesystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, VIP, 5-HT

  • reduces intestinal fluid and pancreatic secretion
  • slows GI motility and inh gall bladder contraction
  • reduces portal and splanchnic bloow flow
29
Q

H1 antagonists

A

anti-emetics
first gen h1 blockers
prevents motion sickness by producing sedation and antimuscarinic activity

-dimenhydrinate, diphenhydramine, cyclizine, meclizine

30
Q

Dopamine D2 antagonists

A

Metoclopramide, trimethobenzamide

anti-emetics

31
Q

5HT3 antagonists

A

odansetron, granisetron, dolasetron

used for nausea and vomiting during cancer chemotherapy

32
Q

NK1 antagonists

A

aprepitant, fosaprepitant, rolapitant

anti emetic

33
Q

Phenothiazines

A

anti-emetic

Chlorpromazine, prochlorperazine

34
Q

Benzodiazepines

A

anxiety drugs used for anti-emetics

lorazepam, alprazolam

35
Q

Marijuana derivatives

A

Tetrahydrocannabinol (THC) or dronabinol

anti emetic with unknown underlying mechanism

AE: inc SYM activity- laughing, paranoid reactions, thinking abnormalities

36
Q

Tx of IBS

A

tricyclic antidepressants-amitriptyline or desipramine

Antispasmodics- anticholinergics (dicylomine, hyoscyamine)

5-HT4 partial agonist- tegaserod (emergency tx only for IBS with constipation), CV events can occur

5HT3 antagonist- alosetron for diarrhea predominant IBS, CV events can occur

opioid agonist- eluxadoline (diarrhea predominant ibs)

Antibiotic- rifaximin- dirrhea predominant IBS (may alter bacterial content of GI tract)

37
Q

Pancreatic enzyme supplements

A

For pancreatic insufficiency caused by CF, chronic pancreatitis, resection
-can lead to steatorrhea, vit malabsorption, weight loss

-pancreatin, pancrelipase administered with each meal and snack
can lead to hyperuricosuria and renal stones

38
Q

Antiobesity drugs

A

Orlistate- gi lipase inhibitor

Sibutramine- CNS, reduces appetite

RImonabant- CNS (peripheral?), reduces appetite, opposite of weed

IC (31 decks)

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