GI Pharmacology Flashcards
What gastric ph is desired prior to anaesthetic
3.5
Examples of H2 receptor antagonists
How do they work
Cimetidine, ranitidine
Reversible competative inhibitor at H2 receptor which usually stimulates acid secretion
Mimic the imidazole ring end of histamine to bond. Inhibits both basal level and stimulated release of acid.
Where are h2 receptors present
Effect of antagonists at these locations
Uterus, heart, blood vessels, los
Very little
Side effects of cimetidine
Gynaecomastia and impotence (antiandrogen effects)
Cyp450 inhibition
Reduces hepatic blood flow
Inhibition of suppressor T cells worsening autoimmune conditions
Bradyarrhythmias
Time to peak effect of cimetidine
80mins
Time to peak effect of ranitidine
Pharmacokinetics of oral administration
100mins
T1/2 2.5hrs
Substantial first pass metabolism
Metabolised in liver and causes some inhibition of cyp450
How do proton pump inhibitors work?
Effect acid secreting pumps of gastric parietal cells
Structure and pharmacokinetics of ppi
Imidazole and benzene ring together
Weak base with a high PKA
Administered in buffered capsules and slowly released
Absorbed whilst non ionised then activated by protination on luminal side (prodrug)
Accumulates and binds strongly to hkatpase pumps preventing h passage
What is the active form of omeprazole
Sulphenamide
What is the half life of omeprazole
Why does it last longer
3 minutes in plasma
Accumulates around receptors and binds strongly
How is omeprazole metabolised
Hepatically
Adverse effects of omeprazole
Hypergastrinaemia
Cyp450 inhibition
Effect of prostaglandins on stomach acid secretion
Example
Eg misoprostol
Reduce stomach acid secretion and stimulate mucus production thus useful in nsaid induced ulceration
Examples of antacids used in gastric acidic control
Mechanism
Aluminium hydroxide, sodium citrate
Simple chemical reaction of acid +base to salt + water
Side effects of antacid use
Co2 production with beltching and gastric distension
Very alkaline thus aspiration of the antacid could also cause damage
Alkalosis
salt and water retention (as a lot has to be given for significant effect)