Anti-Ulcer Drugs

Question 1

What are the five different families for anti-ulcer agents?

Answer 1

H2 receptor antagonists, proton pump inhibitors, surface acting agents, PGE1 analogs, and Bismuth Compounds

Question 2

what are the three drugs in the H2 receptor family?

Answer 2

Climetidine, Famotidine, and Nizatidine

Question 3

what are the 6 drugs in the Proton pump inhibitor family?

Answer 3

lansoprazole, dexlansoprazole, omeprazole, esomeprazole, pantoprazole, and Rabeprazole

Question 4

what is the one drug in the surface acting agents family?

Answer 4

sucralfate

Question 5

what is the one drug in the PGE1 analogs family?

Answer 5

Misoprostol

Question 6

what is the one drug in the Bismuth compounds family?

Answer 6

Bismuth subsalicylate

Question 7

what 3 receptors stimulate the parietal cells to produce acid?

Answer 7

muscarinic, CCK, and H2

Question 8

what inhibits the parietal cells from producing acid?

Answer 8

prostaglandins

Question 9

what is the mechanism of action of histamine type 2 blockers (H2 blockers)?

Answer 9

they reversibly inhibit H2 receptors on the baso-lateral membrane of parietal cells

Question 10

when is the onset of effects seen for H2 blockers?

Answer 10

.5-2 hours

Question 11

when might an ulcer heal when on H2 blockers?

Answer 11

4-8+ weeks

Question 12

what are the common side effects associated with H2 blockers?

Answer 12

GI related or some CNS-related symptoms

Question 13

what is the rare adverse effect associated with H2 blockers- which one specifically?

Answer 13

cimetidine decreases testosterone binding to androgen receptor (there is a weak anti-androgen effect); could also cause blood dyscrasias

Question 14

what does the weak anti-androgen effect cause in people taking cimetidine?

Answer 14

gynecomastia in men or galactorrhea in women

Question 15

which drug in the histamine type 2 blockers family is associated with drug-interactions?

Answer 15

Cimetidine is the prototypical inhibitor of several CYP450 isoenzymes

Question 16

which H2 blocker is most commonly used in pregnancy when absolutely needed?

Answer 16

Famotidine

Question 17

What are the relative contraindications of H2 blockers?

Answer 17

pregnancy

Question 18

what is the mechanism of action of PPIs?

Answer 18

they covalently bind to sulfhydryl groups of H+/K+- ATPase at parietal cell secretory sites, thereby inhibiting gastric acid secretion by irreversibly inhibiting functioning “-ase” pumps

Question 19

when is the onset of effects seen with PPIs?

Answer 19

full symptoms effects seen in a few-several days; longer than H2 blockers

Question 20

when do ulcer possibly heal with PPI treatment?

Answer 20

4-8+ weeks

Question 21

What are the common adverse effects of PPIs?

Answer 21

primarily GI related; some CNS related

Question 22

what is the rare adverse effect associated with PPIs?

Answer 22

CDAD (clostridiodes difficile-associated diarrhea)

Question 23

if you have a patient on a PPI and they develop profuse watery diarrhea that is lasting days, they are getting dehydrated, running a fever, and feeling terrible what should you do?

Answer 23

get a stool culture for c. diff- if it is positive STOP the PPI medication

Question 24

What is the drug in the PPI family that is associated with drug-drug interactions?

Answer 24

omeprazole is the prototypical PPI for CYP450 inhibition

Question 25

what are the relative contraindications associated with PPIs?

Answer 25

pregnancy

Question 26

what PPI is commonly used for pregnant patients when absolutely needed?

Answer 26

lansoprazole

Question 27

what is sucralfate?

Answer 27

a sulfated polysaccharide | -an octasulfate of sucrose with Al(OH)3 added

Question 28

what is the mechanism of action of surface acting agents?

Answer 28

they undergo cross-linking from interaction with stomach acid, to create a viscous, sticky polymer which adheres to epithelial cells around ulcer's crater; prevents acid access to ulcer sites

Question 29

what are the adverse affects associated with surface acting agents?

Answer 29

constipation (Al(OH)3)

Question 30

what are the relative contraindications of surface acting agents?

Answer 30

if a patient has severe renal failure (aluminum-containing antacids should be avoided)

Question 31

are there drug interactions associated with surface acting agents?

Answer 31

possibly- so take 2 hours after other medications (but this is a 4 times a day drug, so that's difficult sometimes)

Question 32

In the stomach PGI and PGEs bind to what?

Answer 32

to the superficial epithelial cell (to make HCO3- and mucus) and to the parietal cell to inhibit acid production

Question 33

what is the mechanism of action of misoprostol?

Answer 33

it provides protective (agonistic) prostaglandin actions to gastric mucosa and reduces (inhibitory) gastric acid release from parietal cell; provides cytoproduction by increasing mucosal defenses

Question 34

When is the use of misoprostol indicated?

Answer 34

prevention (primary prophylaxis) of NSAID-induced gastric ulceration in patients at high risk of ulcerations and complications

Question 35

what are the off-label uses of misoprostol?

Answer 35

pregnancy termination, cervical ripening, post-partum hemorrhaging

Question 36

what are the contraindications of misoprostol?

Answer 36

pregnancy and IBD

Question 37

what is the mechanism of action of bismuth subsalicylate?

Answer 37

it was originally developed as an anti-diarrheal agent; it is also known for its antimicrobial actions (so it is used in combination therapy for H. pylori)

Question 38

what are the adverse effects associated with bismuth subsalicylate?

Answer 38

constipation and black/dark (regularly-formed) stools

Question 39

what are the drug interactions associated with bismuth subsalicylate?

Answer 39

there are lots, so take 2 hours after other medications

Question 40

what are the relative contraindications associated with bismuth subsalicylate?

Answer 40

severe renal failure; (antiplatelets and anticoagulants)

Question 41

what are the absolute contraindications associated with bismuth subsalicylate?

Answer 41

GI bleeding or salicylate hypersensitivity