Anti-ulcer drugs Flashcards
1
Q
role of gastric acid
A
- digestion of proteins
- activates proenzymes
- absorption of calcium, iron, B12
- suppresses bacterial growth
2
Q
stimulation of parietal cells
A
- ACh
- gastrin
- histamine
3
Q
Ach function
A
- major neural stimulatory of parietal cells
- increases gastrin release
- inhibits somatostatin
4
Q
gastrin function
A
- major endocrine regulator
- release triggered by a protein meal and gastric distention
- increases histamine release
5
Q
histamine function
A
- major autocrine/paracrine stimulator
6
Q
inhibitors of parietal cells
A
- somatostatin and prostaglandins
7
Q
somatostatin function
A
- inhibitor of acid secretion by inhibiting gastrin and histamine release
8
Q
prostaglandin function
A
- inhibit acid secretion by decreasing cAMP
- stimulation secretion of mucin and bicarbonate
- inhibited by NSAIDs
9
Q
PPI MOA
A
- irreversibly block active H/K ATPase pumps in parietal cells
- if the pumps are inactive the drug will not work
10
Q
PPI pharmacokinetics
A
- highly protein bound
- metabolized in the liver by P450, specifically CYP2C19 and CYP3A4
- should be taken 20-30 minutes before breakfast
11
Q
PPI adverse effects
A
- diarrhea
- increased gastrin level: hyperplasia of ECL cells, rebound hypersecretion of acid once PPI discontinued
- risk factor for C. difficile colitis
- risk factor for hip fracture and hypomagnesmia
12
Q
PPI drug interactions
A
- PPIs may inhibit CYP2C19 which decreases clopidogrels antiplatelet effect
- dexlansoprazole is only PPI FDA approved for concominant use with clopidogrel
- most are pregnancy B except omeprazole which is class C
13
Q
common H2RB
A
- ranitidine (Zantac)
- famotidine (Pepcid)
14
Q
HR2B MOA
A
- inhibit acid production by reversibly competing with histamine for binding to H2 receptors
- give at night
15
Q
H2RB pharmacokinetics
A
- absorbed rapidly, peak concentration in 1-2 hours
- small % protein bound