Proton pump inhibitors are the drugs or agents which are used for the prevention and treatment of acid-related conditions such as:
•GERD
•Peptic Ulcers
•Zollinger-Ellison syndrome
•H. Pyroli infection
They show their action by inhibiting the proton pump which are essential for the exchange of hydrogen and potassium ions and hence responsible for the acid secretion.
The drugs belonging to this class are:
Omeprazole, Rabeprazole, Lansoprazole, Pantoprazole etc
The duration of action the proton pump inhibitors is for three days.
For that we'll first discuss the mechanism of proton pumps in t
The proton pumps can be stimulated by three receptors which are
CCK 2 receptor
H2 receptor
Muscarinic receptor or M receptor
G cells are responsible for the production of gastrin & when these gastrin binds with the CCK2 receptor. Then it will directly stimulate the proton pump.
Enterochromaffin cells are responsible for the production of histamine. When these histamine binds with the H2 receptor. It activates this G protein coupled receptor. It will lead to the formation of cyclic AMP from the ATP in the presence of adenylyl cyclase.
This cyclic AMP will stimulate protein kinase A.
This will further lead to the entry of Calcium inside the cell which is responsible for the stimulation of proton pumps.
Acetylcholine are released by the parasympathetic system.
When these acetylcholine binds to the muscarinic receptor. Then this will activate this another G protein coupled receptor which is attached with phospholipase C. This will lead to formation of Inositol phosphate and diaceylglycerate from the Phosphatidylinositol 4,5-bisphosphate.
Inositol phosphate and diaceylglycerate will increase the intracellular calcium levels.
Inositol phosphate will increase the calcium intracellulary from the sarcoplasmic reticulum.
While diaceylglycerate will increase the entry of calcium inside the cell from L type calcium channels.
This increased intracellular calcium levels will stimulate the proton pump.
And this will further lead to the exchange of K and H ions and hence it will secrete HCl.
Thus proton pump can be stimulated by these three receptors.
And can lead to increased secretion of acid and can cause peptic Ulcers.
To prevent this proton pump inhibitors are given.
Examples are Omeprazole, Rabeprazole etc
The major advantage of proton pump inhibitors over the other drugs is that it is directly inhibiting the proton pump and thus giving releif.
In Zollinger-Ellison syndrome which is caused due to gastrin which is released by G cells. We can't give other drugs like antihistamines will not work in that case because it can't block the Cholecystokinin receptor. Similarly we can't give anticholinergic drug in that case.
So this was about the mechanism of proton pump inhibitors.
The most common side effects of proton pump inhibitors are:
•Headache
•Diarrhea
•Constipation
•Abdominal pain
•Flatulence
•Fever
•Vomiting
•Nausea
•Rashes
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Proton pump inhibitors and their mechanism of action
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