PUD+ GERD Dr. J Flashcards
True or false: PPIs are prodrugs
True
What type of environment do PPIs need to be in to be activated?
Acidic
What 3 components make up a PPI?
- Benzimidazole
- Methylsulfinyl
- Pyridine
When Omeprazole is activated by a proton catalyzed process, what does it generate?
A sulphenamide
The sulphenamide interacts _____ with the sulphydryl groups of cysteine residues
Covalently
To prevent premature degradation of proton pump inhibitors by acid in the gastric lumen, oral dosage forms are supplied in what kind of formulations?
Enteric coated
How are PPIs absorbed and how does it reach its site of action?
Systemically; through the blood
What CYP enzymes extensively metabolize PPIs?
- 2C19
- 3A4
Protonix is is freely ____ in water
Soluble
The stability of protonix in aqueous solution is dependent on what?
pH
The delayed release and enteric coated tablets dissolve only at what pH for PPIs?
Alkaline
What inhibits acid production by reversible competing with histamine for binding to H2 receptors on the basolateral membrane of parietal cells?
H2RAs
True or false: H2RAs are less potent than PPIs
True
The H2RAs predominantly inhibit what?
Basal acid secretion
Because of what H2RAs inhibit, what are they efficacious for?
Suppressing nocturnal secretion