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Gastrin
Histamine Ac. Ch
H
K+
Cl-
HCo3
Proton
Pump
Gastric Lumen
H2 blockers (1976)
X
X
Proton Pump inhibitors
P-CABs
Vonoprazan in 2015 
X
Ionic binding
Covalent
Parietal Cell
pCABs PPI
Active drug Pro-drug, rapid 1st pass metabolism
Stable in acid Unstable in acid
Fast onset of action Needs 4-5 days to reach maximal
effect
Resting and active pumps
No food effect
Needs active proton pump,
must before meals
Reversible binding to proton pump Irreversible
The pKa is high (9.3) …fast
onset
The pKa is low (4) ….delayed
onset
CYP2C19 independent CYP2C19 dependent
pCABs are useful
than PPIs as an initial
empirical test before
instrumental
diagnostic tests to
exclude acid-reflux
disease
Vonoprazan approved in Japan (2015)  Erosive
Esophagitis.
pCABs Vs PPI.pptx

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pCABs Vs PPI.pptx

  • 1.
  • 2. Gastrin Histamine Ac. Ch H K+ Cl- HCo3 Proton Pump Gastric Lumen H2 blockers (1976) X X Proton Pump inhibitors P-CABs Vonoprazan in 2015  X Ionic binding Covalent Parietal Cell
  • 3. pCABs PPI Active drug Pro-drug, rapid 1st pass metabolism Stable in acid Unstable in acid Fast onset of action Needs 4-5 days to reach maximal effect Resting and active pumps No food effect Needs active proton pump, must before meals Reversible binding to proton pump Irreversible The pKa is high (9.3) …fast onset The pKa is low (4) ….delayed onset CYP2C19 independent CYP2C19 dependent
  • 4. pCABs are useful than PPIs as an initial empirical test before instrumental diagnostic tests to exclude acid-reflux disease Vonoprazan approved in Japan (2015)  Erosive Esophagitis.