GI: Drugs that influence acid secretion Flashcards
What four classes of drugs influence gastric acid secretion?
Muscarinic receptor antagonists
Proton pump inhibitors
NSAIDS
H2 histamine receptor antagonists
Which of these drugs act competitively?
Muscarinic antagonists
and H2 antagonists
Which of these drugs act irrevesibly?
NSAIDS
Proton pump inhibitors
Which of these drugs act by covalent modification?
Proton pump inhibitors
What is the purpose of locally produced prostoglandins ?
Reduce acid secretion
Increase mucus bicarbonate
Increase mucosal blood flow
What is a peptic ulcer?
Any ulcer in an area where the mucosa is exposed to hydrochloric acid and pepsin
How can NSAIDs trigger or exacerbate a peptic ulcer?
Reduce prostaglandin formation because they inhibit COX
Name a drug that can reduce gastric damage due to long term NSAID treatment?
Misoprostol
Inhibits gastrin production
Maintains secretion of mucus and bicarbonate
What three drugs can be used to reduce gastric acid secretion?
Proton pump inhibitors
H2 antagonists
Muscarinic receptor antagonists
Name a proton pump inhibitor?
Omeprazole
How do proton pump inhibitors work?
Inhibit the ACTOVE pump .
At the cannaliculi they are activated to sulfenamide and thus covalent modification of proton pumps occurs
Decribe how omeprazole is a prodrug
Undergoes a conformational change at lower pH’s and becomes more active
When should omeprazole be administered?
When proton pumps are active
Why are proton pump inhibitors long acting despite short half life?
They inhibit the pump irreverssibly
What diseases are proton pump inhibitors used to treat?
Peptic ulcers
GORD
Zollinger Ellison syndrome
Name two histamine H2 receptor antagonists?
ranitidine
cimetidine
How does ranitide work?
Competiviely and revesibly blocks the H2 receptors and this blocs the histamine mediated component of acid secretion
Name two mucosal strengtheners?
Sucralfate
Bismuth chealate
How does sucralfate work?
Compex of aluminium hydroxide which binds to the ulcer base forming a complex gel with mucus - mucosal barrier against acid and pepsin is formed
Increases mucosal blood flow, mucus, bicarbonate and prostaglandin production
When is bismuth chealte particularly used?
With H pylori infection in combo with antibiotics and H2 antagonists
When does sucralfate work?
In acidic conditions- releases aluminium to acquire a strong negative charge
What are antacids?
Neutralise gastric acid for symptomatic relief eg gaviscon etc
Name two antacids?
Magnesium hydroxide
Aluminium hyroxide
Which antacid can cause diarrhoea?
Magnesium