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GI II > Anti-Ulcer Drugs > Flashcards

Anti-Ulcer Drugs Flashcards

1
Q

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

A

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

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2
Q

what are the three drugs in the H2 receptor family?

A

Climetidine, Famotidine, and Nizatidine

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3
Q

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

A

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

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4
Q

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

A

sucralfate

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5
Q

what is the one drug in the PGE1 analogs family?

A

Misoprostol

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6
Q

what is the one drug in the Bismuth compounds family?

A

Bismuth subsalicylate

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7
Q

what 3 receptors stimulate the parietal cells to produce acid?

A

muscarinic, CCK, and H2

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8
Q

what inhibits the parietal cells from producing acid?

A

prostaglandins

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9
Q

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

A

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

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10
Q

when is the onset of effects seen for H2 blockers?

A

.5-2 hours

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11
Q

when might an ulcer heal when on H2 blockers?

A

4-8+ weeks

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12
Q

what are the common side effects associated with H2 blockers?

A

GI related or some CNS-related symptoms

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13
Q

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

A

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

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14
Q

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

A

gynecomastia in men or galactorrhea in women

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15
Q

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

A

Cimetidine is the prototypical inhibitor of several CYP450 isoenzymes

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16
Q

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

A

Famotidine

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17
Q

What are the relative contraindications of H2 blockers?

A

pregnancy

18
Q

what is the mechanism of action of PPIs?

A

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

19
Q

when is the onset of effects seen with PPIs?

A

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

20
Q

when do ulcer possibly heal with PPI treatment?

A

4-8+ weeks

21
Q

What are the common adverse effects of PPIs?

A

primarily GI related; some CNS related

22
Q

what is the rare adverse effect associated with PPIs?

A

CDAD (clostridiodes difficile-associated diarrhea)

23
Q

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?

A

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

24
Q

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

A

omeprazole is the prototypical PPI for CYP450 inhibition

25
Q

what are the relative contraindications associated with PPIs?

A

pregnancy

26
Q

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

A

lansoprazole

27
Q

what is sucralfate?

A

a sulfated polysaccharide

-an octasulfate of sucrose with Al(OH)3 added

28
Q

what is the mechanism of action of surface acting agents?

A

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

29
Q

what are the adverse affects associated with surface acting agents?

A

constipation (Al(OH)3)

30
Q

what are the relative contraindications of surface acting agents?

A

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

31
Q

are there drug interactions associated with surface acting agents?

A

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

32
Q

In the stomach PGI and PGEs bind to what?

A

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

33
Q

what is the mechanism of action of misoprostol?

A

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

34
Q

When is the use of misoprostol indicated?

A

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

35
Q

what are the off-label uses of misoprostol?

A

pregnancy termination, cervical ripening, post-partum hemorrhaging

36
Q

what are the contraindications of misoprostol?

A

pregnancy and IBD

37
Q

what is the mechanism of action of bismuth subsalicylate?

A

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)

38
Q

what are the adverse effects associated with bismuth subsalicylate?

A

constipation and black/dark (regularly-formed) stools

39
Q

what are the drug interactions associated with bismuth subsalicylate?

A

there are lots, so take 2 hours after other medications

40
Q

what are the relative contraindications associated with bismuth subsalicylate?

A

severe renal failure; (antiplatelets and anticoagulants)

41
Q

what are the absolute contraindications associated with bismuth subsalicylate?

A

GI bleeding or salicylate hypersensitivity

GI II (20 decks)

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