Pharmacology Flashcards
What is the process of HCl secretion?
CO2 and water are converted to carbonic acid by carbonic anhydrase
HCO3 and H+ are also produced
HCO3 is pumped out fo the cell into the blood in exchange for Cl, which is pumped into the lumen
H+ is pumped into he lumen in exchange for K+ by the proton pump (H/K/ATPase)
H+ and Cl make HCl
Via which receptors do secretagogues cause secretion?
M3 muscarinic
G/CCK2
H2
What is the process that causes HCl secretion via M3 receptors?
ACh binds to receptor
Cause increased cAMP
Increases number of proton pumps
Increases acid secretion
What is the process that causes HCl secretion via G/CCK2 receptors?
Gastrin binds to receptor
Causes increase in intracellular calcium
Increases number of proton pumps
Increases acid secretion
What is the process that causes HCl secretion via H2 receptors?
Histamine from enterochromaffin cells binds to receptor
Increases cAMP
Increases number of proton pumps
Increases acid secretion
What is the mechanism of PPIs?
Irreversible inhibit proton pumps so H+ cannot be pumped into lumen, decreasing acid secretion
Where do PPIs not work, and what should be done to counter this?
In tubulovesicle proton pumps
Take 20 mins before eating because that is the time taken for proton pumps to move to the canalicular membrane
What are examples of PPIs?
Omeprazole
Lansoprazole
What are the side effects of PPIs?
Increased risk of infection, e.g. C. diff
Osteoporosis
What is the mechanism of H2 receptor antagonists?
Blocks H2 receptor so histamine cannot act on parietal cell to decrease acid production
How do H2 receptor antagonists compare to PPIs in terms of effectiveness, and why?
Less effective
H2 blocked but ACh and gastrin can still cause acid secretion
When are H2 receptor antagonists used?
If PPIs contraindicated, or not receptive to PPIs
What are examples of H2 receptor antagonists?
Ranitidine
Cimetidine
Famotidine
Nizatidine
What are the side effects of H2 receptors antagonists?
Masks symptoms of gastric malignancy
What is the mechanism of antacids?
Buffer HCl and make pH in the stomach more neutral
What is the mechanism of alginates?
Increase the viscosity of gastric juice and react with acid to produce a foam later that protects the oesophagus
What is the indication for antacid alginate combination?
OTC for short term symptomatic relief
What are examples of compound alginates?
Peptac
Gaviscon
Mucogel (antacid only)
What is the function of prostaglandins and somatostatin?
They reduce the effect of secretagogues and inhibit gastric acid secretion
What is the mechanism of NSAIDs?
Inhibit COX1
This causes decreased prostaglandins production
Less prostaglandins means more acid secretion