Chemical basis of drug action Flashcards
What is a buffer made up of?
Mixture of strong acid + weak base or weak acid + strong base
Buffer
Resist changes to pH on addition of further acid or base
What is a prodrug + give an example
Drug needs to be activated to become the active drug species
e.g. Omeprazole
Proton pump inhibitor
Inhibit proton pump in parietal cells
Binds irreversibly to the pump
Amphoteric H2 - receptor antagonist
Famotidine
Examples of H2 - receptor antagonist
Cimetidine
Ranitidine
Famotidine
Nizatidine
What is the acidity/basicity of H2RAs
Cimetidine, Ranitidine + Nizatidine = weakly basic
Journey of omeprazole
Stomach -=> duodenum => Blood => Parietal cells
Stability of omeprazole in acid
Unstable - it undergoes reaction to form prodrug and then binds irreversibly to proton pump
What produces urease enzyme
Helicobacter pylori
Function of urease enzyme
Protects bacterium from acid by producing NH3 which neutralises stomach acid
Similarities 13C + 12C
Naturally occuring
non-radioactive isotopes of carbon
Agonist at H2-receptor
Histamine
What is imidazole ring responsible for in H2RA
ADR
What is furan / thiazole ring responsible for in H2RA
- increases selectivity + potency of antagonism at H2 receptors
- reduces interaction with cytochrome
What does histamine stimulate
- Acid secretion by parietal cells
- interacts with H2 receptors
When does the greatest secretion occur
Within 1 hour of eating
Acid secretion is _______ the volume of the meal
twice
What type of polymer is simeticone
Silicone polymer
Use of simeticone
Alters (lowers) surface tension of small bubbles + fuse them to form larger bubbles so gas in stomach can be easily lost
Relieves trapped wind