GI Drugs Flashcards

1
Q

Calcium Carbonate

A

Antacid

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

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

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2
Q

Sodium Bicarbonate

A

Antacid

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

⁃ AE:
⁃ Systemic Alkalosis
⁃ Fluid Retention

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3
Q

Aluminum Hydroxide

A

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.

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4
Q

Magnesium Hydroxide

A

Antacid

⁃ High ANC

⁃ Rapid Onset/ Long Acting

⁃ AE:
⁃ Diarrhea
⁃ Hypermagnesemia in Renal patients

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5
Q

Bismuth Subsalicylate

A

Cytoprotective

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

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

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6
Q

Cimetidine

A

H2 Receptor Antagonist

RX:

  • PUD
  • GERD
  • ZE
  • Erosive Esophagitis

AE:

Gynacomastia

Impotence

Inhibits:

  • CYP1A2, 2C9, 2D6, 3A4
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7
Q

Ranitidine

A

H2 Antagonist

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8
Q

Famotidine

A

H2 Antagonist

No CYP interaction; Longest Half life; high bioavailability

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9
Q

Omeprazole

A

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
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10
Q

Esomeprazole

A

PPI

IV and PO

Less AE than Omeprazole

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11
Q

Lansoprazole

A

PPI

PO and IV

OTC

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12
Q

Misoprostol

A

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
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13
Q

Sucralfate

A

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
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14
Q

Bismuth Subsalicylate

A

Cytoprotective

MOA:

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

AE:

  • Neurological Injury due to Bismuth absorption
  • Black Stool
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15
Q

Propantheline

A

Antimuscarinic

Quaternary Amine

Rx:

⁃ PUD
⁃ Hypermotility

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16
Q

Dicyclomine

A

Antimuscarinic

Tertiary Amine

Rx:

⁃ peptic disease
⁃ Hypermotility

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17
Q

Amitriptyline

A

Antidiarrheal

Anticholinergic/ Antispasmotic

Rx:

IBD

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18
Q

Glycopyrrolate

A

Quaternary Antimuscarinic

Rx:

Treat Ulcers

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19
Q

Hyoscyamine

A

Antimuscarinic

Rx:

Gastric Spasms

Ulcers

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

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20
Q

Cisapride

A

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
Q

Metoclopramide

A

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
Q

Erythromycin

A

Prokinetic

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

23
Q

Domperidone

A

Prokinetic

D2 receptor antagonist

Fewer CNS and CV side effects

Available through Investigator IND and in Canada

24
Q

Bethanechol

A

Prokinetic

Muscarinic Agonist

Not hydrolyzed by acetylcholinesterase and therefore long half life

⁃ formerly used for GERD Rx
⁃ Widespread cholinergic AEs

25
Q

Neostigmine

A

Prokinetic

AChE inhibitor

Stimulates nicotinic and muscarinic receptors

No CNS effects

Rx:

⁃ formerly used for GERD Rx
⁃ Widespread cholinergic AEs

26
Q

Alosetron

A

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
Q

Loperamide

A

Antidiarrheal

Opioid

MOA:

Acts on mu opioid receptor

Slows down the GI for more H2O absorption.

Rx:

IBD Diarrhea

28
Q

Bismuth Subsalicylate

A

Cytoprotective

MOA:

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

Neurological Injury due to Bismuth absorption
Black Stool

29
Q

Psyllium

A

Laxatives

Mild Stool softener

Dietary Fiber

30
Q

Magnesium Hydroxide

A

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
Q

Polyethylene Glycol

A

Laxative

Intense

Osmotic laxative

Use:

Bowel Prep before Surgery

32
Q

Bisacodyl

A

Laxative

Moderate

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

33
Q

Lubiprostone

A

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
Q

Linaclotide

A

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
Q

Sodium Phosphate

A

Laxative

Fast

Rx:

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

AE:

Phosphate nephropathy in renal patients

36
Q

Tegaserod

A

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
Q

Sulfasalazine

A

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
Q

Mesalamine

A

5-ASA (Active form of Sulfasalazine)

Thus, sulfasalazine metabolite

39
Q

Budesonide

A

Glucocorticoid

Rectal suppository available if there is rectal or sigmoid disease

Large 1st pass effect

RX:

IBD

40
Q

Hydrocortisone

A

Rx:

IBD

41
Q

Adalimumab

A

IgG antibody

Anti-TNF

SubQ

Rx:

Crohn’s Disease

42
Q

Infliximab

A

IgG

IV

Crohn’s disease

43
Q

Azathioprine

A

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
Q

Methotrexate

A

⁃ 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
Q

Cholestyramine

A

Bile salt binder

Lowers Cholesterol

Used to prevent diarrhea in Cronh’s disease

AE:

gallstone formation

46
Q

N-Acetylcysteine

A

Acetaminophen antidote

MOA:

Binds to NAPQI via the donation of a sulfhydril group

47
Q

Ursodiol

A

Reduces the rate of cholesterol absorption by the GI

Breaks down Micelles containing cholesterol

48
Q

Pancrelipase

A

synthetic mixture of pancreatic enzymes:

Lipase

Amylase

Chymotrypsin

49
Q

Cimetidine

A

H2 Receptor Antagonist

RX:

  • PUD
  • GERD
  • ZE
  • Erosive Esophagitis

AE:

  • Hepatic Enzyme Inhibition
  • Antiandrogenic
  • Gynecomastia (inhibits estradiol metabolism)
  • Caution in renal pts