Pharmacology Flashcards
Is prednisolone commonly ulcerogenic?
Not at normal doses. Unless concurrent gastric hypoxia, hypoperfusion, severe spinal disease, or concurrent use of NSAIDs
When are gastrointestinal protectants indicated?
In case of gastrointestinal ulceration or erosion
After initiating GI protectant therapy - when is improvement expected to be noted?
After 2-5 days if inciting cause is removed
Drug class - cimetidine, ranitidine, and famotidine
Histamine-2 Receptor antagonists (H2 receptor antagonists)
How do H-2 receptor antagonists function?
Block histamine receptor on gastric parietal cell - decrease gastric acid secretion
When is peak effect noted with H-2 receptor antagonists?
Almost immediately after beginning medication (does not need to build up efficacy)
Which is the most potent H2 receptor antagonist?
Famotidine
When should you give cimetidine in relation to food?
On an empty stomach - before feeding
Which H-2 receptor antagonists utilize P-450 enzymes?
Cimetidine, ranitidine
Which H-2 receptor antagonist utilizes P-450 enzymes and may cause toxic buildup of theophylline, lidocaine, and metronidazole (among others) when administered concurrently?
Cimetidine
Which H-2 receptor antagonist causes reduced hepatic blood flow?
Cimetidine
How are famotidine and nizatidine excreted from body?
Almost unchanged in urine
Which H-2 receptor antagonist may cause vomiting and lethargy if administered IV?
Ranitidine
Which H-2 receptor antagonist may cause interference with serum gastrin concentration?
Famotidine - causes transient increase in serum gastrin
Drug class - Omeprazole, pantoprazole, esomeprazole
Proton pump inhibitors (PPIs)
How do proton pump inhibitors function?
Inhibit hydrogen-potassium ATP on parietal cell - stop secretion of hydrogen into gastric lumen
Which PPI has longest duration of effect?
Dexlansoprazole
How long does it take for PPIs to reach maximum effect?
2-5 days
Where is omeprazole absorbed?
In duodenum
When should omeprazole be given in relation to food?
On empty stomach - one hour before meal
How are PPIs metabolized?
First pass hepatic metabolism
Which PPIs affect P-450 enzymes?
Omeprazole and esomeprazole
What are potential risks of alteration of gastric pH?
Altered metabolism of some drugs which rely on pH for absorption, potential for admission of some bacteria which would otherwise be destroyed by gastric pH
How does sucralfate function?
Locally acting - binds to epithelial cells, especially at erosions and ulcers and protects from pepsin and bile acids
What is sucralfate composed of?
Sucrose and aluminum hydroxide
When should sucralfate be administered in relation to antacids?
Prior to antacids
Drug class - misoprostol
Prostaglandin E1 analog
How does misoprostol function?
Antisecretory effect on parietal cells - inhibition of acid secretion, also stimulates secretion of mucus and bicarbonate to increase gastric mucosal blood flow
Where is misoprostol metabolized?
First pass metabolism in liver -to active form
Which gastroprotectants are prodrugs?
Misoprostol, omeprazole