Anti- Ulcer Drugs

Question 1

What receptors are Proton Pump Inhibitors capable of blocking?

Answer 1

H2, CCK2 and M3 receptors

-Parietal Cells (responsible for H+ secretion) bind EP3 receptors.
EP3 blockers are also PPIs

Question 2

Calcium Carbonate, Mg2+ and AL(OH)3 ?

Answer 2

Buffering Agents

*Neutralize Acids

Question 3

The downside of Buffering Agents?

Answer 3

-Simple to use, but not strong enough for many people.

Question 4

Cimetidine:

Answer 4

Reversible H2 antagonist
-CYP450 inhibitor

Generally well tolerated, but can lead to Gynecomastia & Galactorrhea (excessive production of milk)

Question 5

Omeprazole:

Answer 5

Irreversible Proton Pump Inhibitor
–>POTENT acid suppression when used correctly.
(Narrow window for use)
-Generally well tolerated for short term use.
-Concerns over long- term use, including Hypergastrinemia (Gastrin binds CCK2 receptor) and Osteoporosis.

Question 6

Pirenzapine:

Answer 6

-Anti- cholinergic
(Reduces acid secretions by blocking the M3 receptor)
*Rarely used due to poor efficacy and several adverse effects.

Question 7

Do Gastrin antagonists exist?

Answer 7

Yes, they are currently being developed.

Question 8

Misoprostol:

Answer 8

Prostaglandin Analogue

• Looks like a PG and therefore can bind PG- receptors.
• Promote secretion of mucus and bicarbonate/ inhibits acid secretion.

Adverse Effects include Diarrhea, Abdominal Cramping & Teratogenic

Question 9

Sucralfate (Aluminum Hydroxide & Sucrose Sulfate)

Answer 9

*Coating agent
-Forms a paste over the ulcerated area, and stimulates mucus and bicarbonate secretion.
(Must be taken 4x a day with a meal)
-Acts locally

Side Effects include Constipation (due to aluminum)

Question 10

Bismuth Subsalicylate:

Answer 10

Pepto Bismol

• Forms a protective barrier on the ulcerated area (coating agent)
• Enhances mucus/ bicarbonate secretion
• INHIBITS the growth of H. pylori & its adherence to the mucosa

Question 11

What are the 2 main causes of GI Ulceration?

Answer 11

H. pylori and NSAIDS (ASA)

Question 12

H. pylori:

Answer 12

• Produces inflammatory changes in the mucosa
• Impairs mucosal defence
• Increase H+ secretion

Question 13

What is H. pylori typically eradicated?

Answer 13

-Combination of PPI and antibiotics

(Common antibiotics include amoxicillin, clarithromycin, tetracycline, metronidazole)
-Bismuth is often include in this regimen, as well as a PPI (ex. Omeprazole)

Question 14

True or False: Resistance is a common problem with the treatment of Ulcers.

Answer 14

True.

Question 15

NSAIDS causing ulceration:

Answer 15

• Irritation of NSAIDS can be minimized with food, but taking MSAIDS with food does not decrease the risk of developing an ulcer.
• -How can GI side effects be reduced?
• ->Take with food, take with Misoprostol (PG analogue), or take with a PPI (protective role- however, long term use leads to concerns)

Question 16

True or False: If someone is at a high risk of developing an ulcer and needs to take aspirin, you should also prescribe them a PPI.

Answer 16

True.