PPIs

Question 1

What can an increase in acid lead to?

Answer 1

Indigestion
Heartburn

Question 2

What are some acid-related diseases?

Answer 2

GORD
PUD
H.Pylori

Question 3

What are some therapies used to control acid?

Answer 3

• Antacids
• H2RAs
• PPIs

Question 4

Give some examples of H2RAs.

Answer 4

• Cimetidine
• Famotidine
• Ranitidine

Question 5

Give some examples of PPIs.

Answer 5

• Lansoprazole
• Omeprazole
• Esomeprazole

Question 6

What is the chemistry behind how proton pump inhibitors work?

Answer 6

Covalently bond to cysteine residues of the proton pump causing degradation.
-> proton pump can reform for acid to be produced again

Question 7

How does proton pump inhibitors get to the site of action?

Answer 7

Pro drugs
-> Absorbed in the intestines and enter systemic circulation. Enter parietal cells, where they are activated when they come in contact with the acid.

Question 8

What property allows proton pump inhibitors to remain in the gastric lumen and not move back into parietal cells?

Answer 8

They are ionised.
-> become protonated

Question 9

Is the binding of proton pump inhibitors reversible or irreversible?

Answer 9

Irreversible
-> Will require regeneration of new pump

Question 10

What are the 3 functional regions of PPIs?

Answer 10

• Pyridyl
• Methylsulfinyl
• Benzimidazole