Agents for Peptic Ulcer Disease & GERD (Segars) Flashcards

1
Q

What are the classes of Anti-ulcer drugs discussed in class?

A

H2 Receptor Antagonists

Proton Pump inhibitors

Surface Acting Agents

PGE1 Analogs

Bismuth Compounds

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

List the H2 Receptor Antagonists discussed in class

A

Cimetidine

Famotidine

Nizatidine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is the MOA of Histamine H2 receptor antagonist

A

They reversibly inhibit H2 receptors on the baso-lateral membrane of parietal cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the general adverse effects of H2 Receptor Antagonists

A

Primarily GI-related

Some CNS- related

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What rare side effects are seen in H2 Receptor Antagonists which are more likely seen with long-term and high dosing

A

Gyencomastia in men

Galactorrhea in women

Blood dyscrasias such as neutropenia & thrombocytopenia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What H2 Receptor Antagonists causes gynecomastia/galactorrhea & what is it’s MOA

A

Cimetidine

Decreases testosterone binding to androgen receptor causing a weak anti-androgen effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

_____, an H2 Receptor Antagonist, has A LOT of drug-drug interactions and is the prototypical inhibitor of several ______

A

Cimetidine

CYP450

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are the relative contraindications of H2 Receptor Antagonists

A

Pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What proton pump inhibitors were discussed

A

Lansoprazole

Dexlansoprazole

Omeprazole

Esomepraazole

Pantoprazole

Rabeprazole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is the MOA of Proton Pump Inhibitors (PPI’s)

A

They covalently bind to sulfhydryl groups of H+/K+ ATPase at parietal cell secretory sites, thereby inhibiting gastric acid secretion by irreversibly inhibitng functioning -ase pumps

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are the general & rare adverse effects of Proton Pump Inhibitors

A

General: Primary GI related & Some CNS related

Rare: Clostridioides/Clostridium difficile associated diarrhea (CDAD)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the prototypical PPI for CYP450 inhibition

A

Omeprazole

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is the relative contraindications for PPI

A

Pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What surface acting agents were discussed

A

Sucralfate

SUrface - SUcralfate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is the MOA of Sucralfate

A

Undergoes cross-linking from interaction with stomach acid, creating a viscous, sticky polymer which adheres to epithelial cells around ulcer’s crater & prevents acid access to ulcer sites

Band-aid drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are the indications, relative contraindications and adverse effects of sucralfate

A

Indications - Any ulcers

Relative contraindications - Severe renal failure (avoid aluminum)

Adverse Effects - Constipation (Al(OH)3)

17
Q

How are drug interactions avoided in sucralfate

A

Taken 4x daily (QID) for active ulcers 2 hours before meals

18
Q

What are the PGE1 Analogs discussed

A

Misoprostol

19
Q

What is the MOA of Misoprostol

A

Acts like a prostaglandin by binding to parietal cells and reducing acid production & also binding to superficial epithelial cells and promoting bicarbonate and mucous production

20
Q

What is the indications for Misoprostol

A

Prevention of NSAID-induced gastric ulceration in patients at high risk of ulcerations and complications

Patients who can’t come off NSAID so you give them misprostol

21
Q

What are the off label use of misoprostol

A
  1. W/ or w/o mifepristone (pregnancy termination)
  2. Alone for cervical ripening
  3. Post-partum hemorrhaging
22
Q

What are the adverse effects and contraindications of Misoprostol

A

Adverse Effects - Primarily GI related & Some CNS related

Contraindications - Pregnancy & Inflammatory Bowel Disease

23
Q

What were the Bismuth Compounds discussed

A

Bismuth Subsalicylate

24
Q

What is the MOA of Subalicylate

A

Originally developed as an anti-diarrheal agent and has antimicrobial actions so it can treat H. pylori

25
Q

What are the adverse effects of Subsalicylate

A

Constipation (anti-diarrheal actions)

Black/Dark (regularly-formed) stools

26
Q

What are the drug interactions of subsalicylate and how do you avoid it

A

A lot

Take 2 hours after other medications

27
Q

What are the relative and absolute contraindications of subsalicylate

A

Relative - Antiplatelets/anticoagulants & severe renal failure

Absolute - GI bleeding & salicylate hypersensitivity