GI Pharmacology - Resit Flashcards
H2 histamine receptor antagonist mechanism
- competitive antagonists of H2 receptors, which are activated by histamine
- when activated, it increased activity of the proton pump by increased cAMP via PKA
- by blocking this, there is reduced acid production
- reduce secretion evoked by gastrin and ACh
NSAIDs mechanism
- COX is formed from arachidonic acid
- reduce prostaglandin formation, via COX 1 inhibition
PPIs mechanism
- inhibit membrane inserted H+/K+ dependent ATPase
- pumps in the tubulovesicles are not inhibited
NSAIDs side effects
- gastric ulceration
- bleeding
what drug can be used to prevent gastric damage, due to long term NSAID use? what does it do?
PGE1 analogue (e.g misoprostol)
- inhibits basal and food stimulated gastric acid formation
- maintains/increases secretion of mucus and bicarbonate
what 3 things promote peptic ulcer healing?
- reduced acid secretion
- increased mucosal resistance
- eradicating H.pylori
why must PPIs make it to the canaliculus of the stomach?
so they can be activated here, due to the acidic pH (they are prodrugs)
why must PPIs make it to the canaliculus of the stomach?
so they can be activated here, due to the acidic pH
example of a PPI?
omeprazole
what gastric acid production are H2 histamine receptor antagonist effective against?
basal and stimulated
examples of H2 histamine receptor antagonist
ranitidine and cimetidine
sucralfate (mucosal strengtheners) mechanism
- activated in an acidic environment
- releases aluminium to acquire a strong negative charge
- blinds to ulcer base, forming a complex gel with mucus
- barrier against acid and pepsin
what does sucralfate do?
increases
- mucosal blood flow
- mucus
- bicarbonate
- prostaglandin
bismuth chealate (mucosal strengthener) is used for?
- H.pylori, as it promotes eradication
what are laxatives?
agents that are used to treat constipation
what are purgatives?
agents that cause purging (cleansing) of the bowels, by promoting evacuation
when should laxatives/purgatives NOT be used?
when there is a physical obstruction to the bowel
3 uses of laxatives/purgatives?
- when straining is damaging to health or defecation is painful
- clearing the bowel before a procedure
- to treat drug induced constipation or constipated bedridden/elderly patients
what are bulk laxatives? examples?
indigestible polysaccharide polymers e.g methylcellulose, ispagula husk