GI Pharmacology Flashcards

1
Q

mylanta

A

class: neutralizing antacid
- fast acting, short t1/2
- immediate relief

use:
- GERD

mx:
- 2 strong bases:
- - Al(OH)3
- - Mg(OH)2
- +1 antiflatulant
- - simethicone

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2
Q

reversible H2 inhibitors (inverse agonists)

A

use:

  • GERD
  • duodenal or gastric ulcer
  • hypersecretion of gastric acid

mx:

  • reversible competitive antagonist to H2 receptors
  • H2 binds histamine, which increases acid production when bound to this receptor

pk:

  • onset: 30-60 min
  • duration: 6-12 h

AEs:

  • diarrhea
  • dizziness
  • rash
  • headache

e. g.:
- cimetidine
- famotidine (Pepcid)
- nizatidine

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3
Q

nizatidine

A

reversible H2 antagonist

GERD

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4
Q

cimetidine

A

reversible H2 antagonist
GERD

special note:

  • CYP450 antagonist: 1A2, 2C9, 2D6, 3A4
  • –> drug-drug interactions
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5
Q

famotidine

A

reversible H2 antagonist

GERD

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6
Q

proton pump inhibitors (PPIs)

A

use:
- GERD
- peptic ulcer disease and H. pylori
- Zollinger-Ellison syx (rare pancreatic tumor)
- idiopathic hyper-H+
- upper GI prophylaxis w/ LT NSAID use

mx:

  • irreversible H+/K+-ATPase antagonist
  • block H+ secretion

PK:

  • prodrugs converted by acid
  • ion trapping in canalicula on parietal cells
  • local accumulation
  • enteric-coated: don’t dissolve until SI
  • t1/2 1-2 h
  • duration: 36 ~ 72 h
  • onset: 2-5 days for full effect
  • CYP2C19 metabolism

AEs:

  • few
  • some concerns about unjustified long-term use

e. g.: -prazole
- omeprazole (Prilosec)
- esomeprazole (Nexium)

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7
Q

-prazole

A

PPI

GERD - long term

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8
Q

omeprazole

A

PPI
GERD
Prilosec

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9
Q

esomeprazole

A

PPI
GERD
Nexium

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10
Q

EC drugs

A

enteric-coated

bypasses stomach

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11
Q

GI effects of NSAIDs

A

COX1 inhibitors
mucosal injury to upper GI
peptic ulcer disease
possible hemorrhage

worst: aspirin
best: celecoxib

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12
Q

misoprostol

A

use:
- NSAID injury prophylaxis and tx

mx:

  • prostaglandin E1 agonist
  • stimulates mucus and bicarb secretion in GI
  • weak antagonist of acid

AEs:

  • often poorly tolerated
  • diarrhea
  • abdominal pain
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13
Q

sucralfate

A

use:

  • NSAID injury prophylaxis and tx
  • anti-ulcer

mx:
- Al salt, basic
- preferentially neutralizes + proteins near ulcers
- stimulates mucosal repair via x-linking

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14
Q

Scopalamine

A

Dramamine

Class: anti-cholinergic antiemetic

Mx:
- blocks M1 receptors in area postrema to prevent nausea

Uses:

  • nausea
  • motion sickness

Sfx/AEs

  • drowsiness
  • dizziness
  • xerosterma (dry mouth)
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15
Q

prochlorperazine

A
Class: D2 (dopamine) antagonist
- same class as many antipsychotics 

Mx:
- blocks dopamine 2 receptors in area postrema to prevent nausea

Uses:
- general antiemetic

Sfx/AEs:

  • extrapyramidal effects (e.g. twitching)
  • neuroleptic malignant syx (serious, treatable: high fever, muscle stiffness
  • drowsiness
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16
Q

diphenhydramine (as a GI drug)

A

class: antihistamine antiemetic

mx:
- blocks H1 receptors in area postrema to prevent nausea

uses

  • general antiemetic
  • non-GI

Sfx/AEs:

  • drowsiness
  • constipation
  • xerostomia (dry mouth)
  • urinary retention
  • high risk in >65 y/o
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17
Q

ondansetron

A

Zofran

class: 5HT3 antagonist antiemetic

mx:
- blocks 5HT3 receptors in area postrema to prevent nausea

uses:

  • general antiemetic
  • chemo
  • pregnancy

Sfx/AEs:

  • constipation
  • QT prolongation
  • headache
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18
Q

metaclopramide

A

class: mixed 5HT3 ANTagonist/5HT4 AGonist, D2 antagonist

mx:

  • see above
  • CNS

uses:

  • antiemetic
  • reflux esophagitis
  • promotility (for gastroparesis and pre-op)
  • migraine

Sfx/AEs

  • drowsiness
  • dystonia (spasm)
  • tardive dyskinesia (involuntary repetitive body movements)
  • limited to ~3 mo use
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19
Q

loperamide

A

class: opioid AGonist, non-absorbed

mx:

  • slows intestinal motility
  • decreases secretion
  • via opioid receptor effects

uses:

  • non-bloody diarrhea
  • acute, nonspecific diarrhea
  • IBD chronic diarrhea

Sfx/AEs

  • minimal as not absorbed
  • constipation
  • c/i in bloody diarrhea
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20
Q

eluxadoline

A

class: mixed opioid agonist/antagonist

mx:

  • slow motility
  • decrease pain
  • via opioid receptor effects

uses:

  • diarrhea
  • abdominal pain
  • IBS-D only

Sfx/AEs

  • constipation
  • nausea
  • sphincter of Oddi spasm –> pancreatitis, hepatic enzyme elevation
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21
Q

octreotide

A

class: somatostatin analog

mx:

  • decreases endocrine and exocrine secretions
  • decreases blood flow
  • reduces GI motility
  • inhibits secretion of many GI regulatory factors

uses:

  • carcinoid secretory diarrhea
  • gastrinoma secretory diarrhea
  • VIPoma secretory diarrhea
  • chemo-induced diarrhea
  • sx of intestinal tumors
  • sx of variceal bleeding

sfx:

  • abdominal cramps
  • nausea
22
Q

atropine (GI effects)

A

class: muscarinic antagonist

mx:

  • decreased GI motility
  • decreased salivation

uses:
- prevent respiratory secretions before anesthesia

Sfx/AEs:

  • dry eye and mouh
  • urinary retention
  • tachycardia
  • c/i glaucoma
  • c/i prostatic hyperplasia
23
Q

antacids

A

class: acid-base neutralizers

e. g.
- Al(OH)3
- Mg(OH)2
- CaCO3
- NaHCO3

uses:
- mild intermittent GERD

Sfx/AEs

  • Al: constipation
  • Mg: diarrhea
24
Q

simethicone

A

class: antiflatulant

mx:

  • surfactant
  • decreases foaming of gas
  • allows for non-flatus passing of gas

uses:

  • flatulance
  • belching
25
Q

aprepitant

A

class: NK-1 receptor ANTagonist antiemetic

mx:
- blocks substance P:NK-1 at chemotrigger zone (CTZ), which receives inputs from drugs and hormones

uses:

  • chemo nausea and vomiting
  • postoperative nausea and vomiting

Sfx/AEs:

  • asthenia (weakness, low energy)
  • diarrhea
26
Q

dexamethasone (GI effects)

A

class: glucocorticoid

mx:

  • anti-inflammatory
  • multiple effects at area postrema
  • direct action at solitary tract nucleus

uses:

  • chemo and radiation nausea and vomiting
  • postoperative nausea and vomiting

Sfx/AEs:

  • minimal w/ single dose
  • irritability, insomnia, fluid retention, weakness, delayed wound healing, hyperglycemia
27
Q

olanzapine (GI effects)

A

class: atypical antipsychotic

mx:
- D2, 5-HT2A, H1, and muscarinic receptors at area postrema to reduce nausea

uses:

  • off-label for chemo nausea and vomiting
  • psych

SFx/AEs:

  • low bp
  • drowsiness
  • extrapyramidal sx
  • others
28
Q

neostigmine (GI effects)

A

class: carbamate-type peripheral ACh-ase inhibitor

mx:
- periphery only ACh-ase inhibitor

uses:

  • increases gastric motility
  • non-GI

SFx/AEs:

  • bowel cramps
  • diarrhea
29
Q

erythromycin

A

class: macrolide abx; also motilin AGonist

mx:

  • motilin receptor AGonist
  • increases GI motility
  • direct and indirect neurotransmitter effects

uses:

  • gastroparesis
  • abx: respiratory and soft-tissue

AEs:
- GI upset

30
Q

diphenoxylate

A

class: opioid antidiarrheal

mx:

  • inhibits GI motility, slows propulsion
  • no other opiate effects

uses:

  • acute, nonspecific diarrhea
  • IBD chronic diarrhea

SFx/AEs

  • at high doses, antimuscarinic effects
  • atropine added to prevent drug misuse
31
Q

PAMORAs

A

class: peripherally acting mu-opioid receptor ANTagonists

e. g.:
- methylnaltrexone
- naloxegol
- naldemedine

mx:

  • does not cross bbb
  • antagonizes mu receptors in periphery only

uses:
- opioid-induced constipation

SFx/AEs

  • abdominal pain w/ methylnaltrexone and naloxegol
  • diarrhea w/ naldemedine
32
Q

methylnaltrexone

A

PAMORA

opioid-induced constiption

33
Q

naloxegol

A

PAMORA

opioid-induced constipation

34
Q

nalemedine

A

PAMORA

opioid-induced constipation

35
Q

linaclotide

A

class: guanylate cyclase-C AGonist

mx:
- secretory laxative
- pro-motility
- GCC activation –> cAMP –> CFTR –> Cl- and HCO3- & increased transit rates

uses:
- CIC and IBS-C

SFx/AEs:
- diarrhea

36
Q

lubiprostone

A

class: chloride channel activator

mx:

  • secretory laxative
  • prostaglandin E1 derived bicyclic fatty acid
  • specifically activates chloride channel on GI epithelium

uses:

  • CIC and IBS-C
  • opioid-induced constipation

SFx/AEs:

  • nausea
  • headache
  • diarrhea
37
Q

plecatinide

A

Trulance

class: guanylate cyclase-C AGonist

mx:

  • secretory laxative
  • pro-motility
  • minimal absorption d/t pH dependent binding
  • GCC activation –> cAMP –> CFTR activation –> Cl- and HCO3- secretion

uses:
- CIC and IBS-C

SFx/AEs

  • stomach bloating or tenderness
  • gas
  • diarrhea
38
Q

prucalopride

A

class: 5HT4 prokinetic AGonist

mx:

  • increased gastric emptying
  • increased small bowel, colonic transit

uses:
- CIC

SFx/AEs

  • headache
  • nausea
  • diarrhea
39
Q

cisplatin

A

platinum-based chemo

colon cancer among others

40
Q

pemetrexed

A

antimetabolite chemo

41
Q

docetaxel

A

taxane chemo

42
Q

bevacizumab

A

anti-VEGF

colon cancer among others

43
Q

osimertinib

A

EGFR inhibitor

44
Q

lorlatinib

A

ALK (tyrosine kinase) inhibitor

45
Q

capmatinib

A

MET (tyrosine kinase) inhibitor

46
Q

sotarasib

A

KRAS G12C (tyrosine kinase) inhibitor

47
Q

trastuzumab deruxtecan

A

not yet approved
HER2 antagonist
Ab-drug conjugate (ADC)

48
Q

pembrolizumab

A

PD-1 inhibitor

49
Q

atezolizumab

A

PD-L1 inhibitor

50
Q

durvalumab

A

PD-L1 inhibitor