GI Pharm Flashcards

1
Q

cytoprotectants

A
  • bismuth subsalicylate
  • sucralfate
  • misoprostol
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2
Q

antacids

A
  • aluminum hydroxide
  • magnesium hydroxide
  • calcium carbonate
  • sodium bicarbonate
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3
Q

H2-receptor antagonists

A
  • cimetidine
  • ranitidine
  • famotidine
  • nizatidine
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4
Q

PPIs

A
Omeprazole 
Lansoprazole
Rabeprazole
Pantoprazole
Esomeprazole
Dexlansoprazole
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5
Q

antacids AE

A
  • diarrhea (Mg)
  • constipation (Al)
  • abd distension (Ca)

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

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6
Q

antacids MOA

A

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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7
Q

bismuth compounds

A
  • bind to base of ulcers
  • promote mucin and bicarb production
  • antibacterial effects
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8
Q

bismuth subsalicylate

AE

A

(pepto-bismol)

  • constipation
  • darkening of of tongue/stool
  • avoid if aspirin allergy
  • drug interactions
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9
Q

sucralfate

A

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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10
Q

sucralfate AE

A
  • constipation*
  • accumulation to Al3+
  • drug interactions
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11
Q

sucralfate use in kidney insufficiency is dangerous why

A

accumulation of Al 3+ can occur

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12
Q

misoprostol

A

prevention of ulcers w/ NSAID use

prostaglandin E analog

  • stim secretion of mucin and bicarb
  • inc mucosal BF
  • suppresses acid production in parietal cell by binding to EP3 receptor
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13
Q

misoprostol

AE

A
  • diarrhea

- inc uterine contractility (termination/induction)

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14
Q

H2 antagonists

A
  • compete w/ histamine for binding to H2 receptors on parietal cells
  • more potent, longer-lasting effects than traditional antacids
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15
Q

H2 antagonist uses

A
  • uncomplicated GERD
  • gastric and duodenal ulcers
  • stress ulcer prophylaxis
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16
Q

H2A should be dose adjusted for

A

kidney insufficiency

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17
Q

H2A adverse effects

A
  • 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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18
Q

gynecomastia (men)

galactorrhea (women)

A

cimetidine (H2A)

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19
Q

H2A drug interactions

A

drugs req an acidic environment (atazanavir, itraconazole)

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

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20
Q

PPI

MOA

A

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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21
Q

PPI

pharmacokinetics

A

plasma half life 1-2hr

onset 2-4 days

duration of effect 24-48 hr

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22
Q

PPI

uses

A
  • gastric and duodenal ulcers
  • GERF
  • Barret’s esophagus
  • Zollinger-Ellison syndrome
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23
Q

PPI

AE

A
  • nausea, diarrhea, abd pain, constipation
  • altered B12/Ca/Mg absorption
  • rash, myopathy, arthralgia, HA
  • ECL hyperplasia
  • infec, fractures?
24
Q

anti-platelet + PPI = interaction?

A

clopidogrel (prodrug) –> active form includes 2 steps req p450 enz (2C19) which is inhibited by PPI

25
Q

H. pylori tx

A

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

26
Q

prokinetic for constipation

cholinergic agents

A

bethanchol

27
Q

prokinetic for constipation

serotonin receptor modulators

A

metoclopramide

cisapride

28
Q

prokinetic for constipation

DA receptor modulators

A

metoclopramide

domperidone

29
Q

prokinetic for constipation

motilin-like agents

A

erythromycin

30
Q

black box warning of metoclopramide

A

extrapyramidal symptoms (tardive dyskinesia, parkinsonian type features)

31
Q

bulk-forming agents for constipation

MOA

A

not absorbed systemically

MOA: source of fiber enhances stool mass

32
Q

bulk-forming agents for constipation

AE

A
  • bloating/abd pain (AVOID if suspect obstruction)

- drug interactions

33
Q

bulk-forming agents for constipation (natural)

A

psyllium

34
Q

bulk-forming agents for constipation (semi-synthetic)

A

methylcellulose

polycarbophil

35
Q

softeners/surfactants MOA

A

lowers surface tension of stool

36
Q

softeners/surfactants

AE

A
  • impaired absorption of fat soluble agents
  • oil leakage
  • lipid pneumonitis
37
Q

softeners/surfactants exp

A

decussate

mineral oil

38
Q

osmotic agents for constipation MOA

A

osmotically-mediated water retention stimulates peristalsis

39
Q

osmotic agents for constipation AE

A

abd discomfort
flatulence

caution w/saline based osmotic agents if CVD disease present

40
Q

osmotic agents for constipation

saline-based

A

Mg citrate

Phosphate salts

41
Q

osmotic agents for constipation

sugar/alcohol-based

A
  • lactulose, sorbitol, mannitol

- glycerin (suppositories/enemas)

42
Q

osmotic agents for constipation

other

A

polyethylene glycol solutions

43
Q

stimulant laxatives

MOA

A

produce migrating colonic contractions

44
Q

stimulant for constipation concerns/toxicities

A
  • avoid overuse

- phenolphthalei/danthron-containing products banned

45
Q

stimulant for constipation

exps

A
  • diphenylmethanes (bisacodyl)
  • anthraquinones (aloe, cascara, SENNA)
  • castor oil
46
Q

Senna is a

A

stimulant laxative

47
Q

guanylate cyclase agonists 2 actions

A
  1. suppress afferent pain fibers

2. activate CTFR (inc GI secretion)

48
Q

5HT4 receptor agonists for constipation

A
  • tegaserod (IBS, F>40y/o)
  • prucalopride

inc serotonin, promotes motility

49
Q

peripherally acting mu-opioid receptor antagonists for constipation

A
  • methylnaltrexone
  • naloxegol
  • alvimopan
  • naldemedine
50
Q

bulk-forming agents used for diarrhea

A
  • bismuth subsalicylate

- cholestyramine

51
Q

anti motility agents for diarrhea

opioid derivatives

A
  • loperamide
  • diphenoxylate + atropine
  • eluxadoline

slow intestinal transit by binding as agonists at opioid receptors thru GI tract

52
Q

alosetron

A

5HT3 receptor antagonist

  • for women
  • when primary sx=diarrhea
  • AE: potential for severe GI side effects
53
Q

RIfaximin

A

rifampin-derived antibiotic

-precise MOA unclear, poss changes in bacterial content

54
Q

octreotide

A
  • 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

55
Q

Clonidine

A

◦ 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.

56
Q

type 2 chloride channel agonists

A

activates chloride channels within GI tract increasing intestinal fluid secretion

exp. Lubiprostone