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Flashcards in GI Drugs Deck (49):
1

Calcium Carbonate

Antacid

⁃ High ANC
⁃ Rapid Onset / Long Acting
⁃ Releases CO2

⁃ AE:
⁃ Hypercalcemia
⁃ Nephrolithiasis
⁃ Milk-Alkali Syndrome

2

Sodium Bicarbonate

Antacid

⁃ High ANC
⁃ Rapid Onset/ Short Acting
⁃ Releases CO2

⁃ AE:
⁃ Systemic Alkalosis
⁃ Fluid Retention

3

Aluminum Hydroxide

Antacid

⁃ Low ANC
⁃ Slow onset/ Long acting
⁃ Binds Pepsin

⁃ AE:
⁃ Constipation
⁃ Hypophosphatemia
⁃ Decreases Bioavailability of other drugs due to binding

Note: Mix with Milk of Magnesia to balance the constipation AE. 

4

Magnesium Hydroxide

Antacid

⁃ High ANC

⁃ Rapid Onset/ Long Acting

 

⁃ AE:
⁃ Diarrhea
⁃ Hypermagnesemia in Renal patients

5

Bismuth Subsalicylate

Cytoprotective

⁃ Cytoprotection mechanism unknown
⁃ Antisecretory
⁃ Anti-inflammatory
⁃ Antimicrobial

⁃ AE:
⁃ Black Stool
⁃ Neurological Injury via Bismuth absorption

6

Cimetidine

H2 Receptor Antagonist

RX:

  • PUD
  • GERD
  • ZE
  • Erosive Esophagitis

AE:

Gynacomastia

Impotence

 

Inhibits:

  • CYP1A2, 2C9, 2D6, 3A4

7

Ranitidine

H2 Antagonist

8

Famotidine

H2 Antagonist

 

No CYP interaction; Longest Half life; high bioavailability

9

Omeprazole

PPI

Rx:

  • GERD
  • Erosive Esophagitis
  • PUD (Hpylori, NSAIDS induced)
  • Dyspepsia
  • Prevention of Stress Ulcers in ICU (IV use)
  • ZE

MOA:

  • Inhibits HKATPase of PArietal Cell Irreversibly
  • Prodrug

AE:

  • Hepatic Liver Induction (Clopidogrel, Warfarin, Methotrexate, Tacrolimus)
  • CDIFF infection risk
  • Osteoporosis
  • Hypomagnesemia
  • B12 Deficiency

 

10

Esomeprazole

PPI

IV and PO

Less AE than Omeprazole

11

Lansoprazole

PPI

PO and IV

OTC

12

Misoprostol

Cytoprotective

Rx:

  • Prevent NSAID induced Ulcers
  • Available in combination with NSAIDS

MOA:

  • Increase Mucus and bicarb secretion from superficial epithelial cells
  • Decrease Acid secretion
  • Maintain Submucosal Flow

AE:

  • Diarrhea
  • Colic
  • CONTRAINDICATED in Pregnancy

13

Sucralfate

Cytoprotective

Rx:

  • Ulcer Healing
  • (Can be given with NSAIDS)

Note: Rarely used

MOA:

  • Forms Viscous gel in Acid
  • Binds to inflamed tissue
  • Protects ulcer from acid
  • Inhibits absorption of other drugs

AE:

  • Constipation

14

Bismuth Subsalicylate

Cytoprotective

MOA:

  • Unknown mechanism
  • Anti-secretory
  • Anti-inflammatory
  • Anti-microbial
  • Anti-diarrheal

AE:

  • Neurological Injury due to Bismuth absorption
  • Black Stool

15

Propantheline

Antimuscarinic

Quaternary Amine

Rx:

⁃ PUD
⁃ Hypermotility

16

Dicyclomine

Antimuscarinic

Tertiary Amine

Rx:

⁃ peptic disease
⁃ Hypermotility

17

Amitriptyline

Antidiarrheal 

Anticholinergic/ Antispasmotic

Rx:

IBD

18

Glycopyrrolate

 

Quaternary Antimuscarinic

Rx:

Treat Ulcers

19

Hyoscyamine

Antimuscarinic

Rx:

Gastric Spasms

Ulcers

 

*Not used much anymore; used to be used to increase LES. 

20

Cisapride

Prokinetic

⁃ 5HT4 agonist
⁃ Was widely used in GERd to contract LES.
⁃ Available for Compassionate use only
⁃ can be found on internet though

⁃ AE:
⁃ Cardiac arrhythmia
⁃ Long QT
 

 

21

Metoclopramide

Prokinetic

MOA:⁃

 -5HT4 agonist

⁃ 5HT3 antagonist (CNS and Vagus)

⁃ D2 antagonist
⁃ Enhances actions of ACh

 

RX:

GERD

Increase LES

Gastroparesis

Antiemetic in cancer Rx

 

AE:

⁃ Extrapyramidal effects from D2 antagonism.
⁃ Parkinson like- short term, reversible.
⁃ Long term use results in irreversible Tardive dyskinesia
⁃ Galactorrhea

Contra:

GI obstruction

Bleeding/ Perforation

22

Erythromycin

Prokinetic

⁃ Motilin like activity
⁃ Short term use for Gastroparesis Rx
⁃ Tolerance develops

23

Domperidone

Prokinetic

D2 receptor antagonist

Fewer CNS and CV side effects

Available through Investigator IND and in Canada

24

Bethanechol

Prokinetic

Muscarinic Agonist

Not hydrolyzed by acetylcholinesterase and therefore long half life

⁃ formerly used for GERD Rx
⁃ Widespread cholinergic AEs

 

25

Neostigmine

Prokinetic

AChE inhibitor

Stimulates nicotinic and muscarinic receptors

No CNS effects

 

Rx:

⁃ formerly used for GERD Rx
⁃ Widespread cholinergic AEs

26

Alosetron

Antidiarrheal

MOA:

⁃ Selective 5HT3 Antagonist

⁃ Reduces lower abdominal pain and discomfort, cramps, urgency, diarrhea

Use:
⁃ Severe diarrhea dominant IBS in women who have not responded to other therapy.

AE:
⁃ Constipation
⁃ Can be severe
⁃ Ischemic colitis (can be fatal)

 

27

Loperamide

Antidiarrheal

Opioid

MOA:

Acts on mu opioid receptor

Slows down the GI for more H2O absorption. 

Rx:

IBD Diarrhea

28

Bismuth Subsalicylate

Cytoprotective

MOA:

Unknown mechanism
Anti-secretory
Anti-inflammatory
Anti-microbial
Anti-diarrheal
AE:

Neurological Injury due to Bismuth absorption
Black Stool

29

Psyllium

Laxatives

Mild Stool softener 

Dietary Fiber

30

Magnesium Hydroxide

Laxative (and antacid) 

Intense 

MOA:

Mg++ draws fluid into the intestine via osmosis

Mg++ stimulates the release of CCK which results in increased water, electrolytes, and motility in the lumen. 

 

AE:

Hypermagnesemia

31

Polyethylene Glycol

Laxative

Intense

Osmotic laxative

Use:

Bowel Prep before Surgery

32

Bisacodyl

Laxative

Moderate

Stimulates the CNS to increase NaCl and Fluid secretion; colonic stimulation mainly  

33

Lubiprostone

Rx:

Chronic constipation of unknown cause and IBS

 

MOA:

Acts on GI epithelial chloride channels to release Cl- and subsequently stimulate fluid secretion to soften the stool 

 

 

34

Linaclotide

Prokinetic

MOA:

Guanylate cyclase agonist, increases cGMP

Stimulates chloride and bicarb secretion via activation of Cystic fibrosis regulator channel. 

Increases GI transit time and reduces abdominal pain- 1x daily before 1st meal

 

Rx:

IBS with constipation or idiopathic constipation

AE:

Diarrhea with pain (Can be life threatening)

GERD

35

Sodium Phosphate

Laxative

Fast

Rx:

Not really used; used to be used for colonoscopy prep. 

 

AE:

Phosphate nephropathy in renal patients

36

Tegaserod

Prokinetic

MOA:

⁃ 5HT4 partial agonist
⁃ Approved for emergency use for severe constipation in IBS.
⁃ Available from FDA only for emergencies

⁃ AE:
⁃ Withdrawn from market
⁃ Serious Cardiac AEs
 

37

Sulfasalazine

IBD Drug (First Line Rx for UC)

Inflammatory Mediator modulation via LOC pathway

Prodrug converted to 5ASA

MOA:

Inhibits Nf-kappaB and inhibits formation of inflammatory cytokines

Inhibits NK cells

38

Mesalamine

5-ASA (Active form of Sulfasalazine)

 

Thus, sulfasalazine metabolite

39

Budesonide

Glucocorticoid

Rectal suppository available if there is rectal or sigmoid disease

Large 1st pass effect

 

RX:

IBD

40

Hydrocortisone

Rx:

IBD

 

41

Adalimumab

IgG antibody

Anti-TNF

SubQ

 

Rx:

Crohn's Disease

42

Infliximab

IgG

IV

Crohn's disease

43

Azathioprine

Immunomodulator

Prodrug of 6 Mercaptopurine

Rx: IBD

MOA:

Purine analogue- inhibits nucleotide synthesis 

⁃ Azathioprine and 6MP
⁃ Used to induce and maintain remission in UC and Crohn's.

⁃ PO or IV daily for 6mos
⁃ AE:
⁃ Nausea
⁃ Vomiting
⁃ Bone Marrow depression
Hepatotoxicity

 

44

Methotrexate

⁃ Inhibition of dihydrofolate reductase

⁃ Low dose, once weekly for 8-12 weeks

Rx:

Crohn's disease

MOA:

Blocks purine synthesis

⁃ AE:
⁃ Uncommon at low doses
⁃ Bone marrow suppression
⁃ Anemia
⁃ Alopecia
⁃ Mucositis
⁃ Reno-hepatic toxicity potential

Note: Do not use with PPI

45

Cholestyramine

Bile salt binder

Lowers Cholesterol

Used to prevent diarrhea in Cronh's disease

 

AE:

gallstone formation

46

N-Acetylcysteine

Acetaminophen antidote

MOA:

Binds to NAPQI via the donation of a sulfhydril group

47

Ursodiol

Reduces the rate of cholesterol absorption by the GI

 

Breaks down Micelles containing cholesterol

48

Pancrelipase

synthetic mixture of pancreatic enzymes:

Lipase

Amylase

Chymotrypsin

49

Cimetidine

H2 Receptor Antagonist

RX:

  • PUD
  • GERD
  • ZE
  • Erosive Esophagitis

AE:

-Hepatic Enzyme Inhibition

-Antiandrogenic

-Gynecomastia (inhibits estradiol metabolism)

-Caution in renal pts