Anti-Ulcer Flashcards by Madelaine Hess

name the five classes of anti-ulcer agents

H2 receptor antagonists
PPIs
surface acting agents
PGE1 Analogs
bismuth Compounds

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-tidine

H2 receptor antagonists

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-prazole

PPIs

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what are the four H2 receptor antagonists?

cimetidine
famotidine
nizatidine
ranitidine

note: some products made with antacids included (calcium, magnesium)

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name the six PPIs and note isomers

lansoprazole
delansoprazole
omeprazole
esomeprazole
pantoprazole
rabeprazole

1+2, 3+4

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name the one surface acting agent

sucralfate

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name the one PGE1 analog

misoprostol

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name the one bismuth compound

bismuth subsalicylate

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all H2 receptor antagonists are po/iv, except…

nizatidine (po)

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name the drug class–

MOA: reversibly inhibits its receptor on the basolateral membrane of parietal cell

onset: 30 mins. - 2 hours
ulcer healing: 4-8+ weeks

inhibits 20-50% of acid production

H2 receptor antagonists / -tidine

note: onset is longer than antacids but shorter than PPIs

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name the adverse effects of H2 receptor antagonists

rare adverse effect on another card

primarily GI related
few CNS related

relatively mild, transient, infrequent

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which H2 receptor antagonist has a rare adverse effect with long-term, high dosing?

describe the adverse effect

cimetidine

decreases testosterone binding to androgen receptor

gynecomastia in men
galactorrhea in women

blood dyscrasias

neutropenia
thrombocytopenia

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what are the prototypical inhibitors of several CYP450 enzymes?

cimetidine (H2 antagonist)
omeprazole (PPI)

STAR

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H2 receptor antagonists are relatively contraindicated during pregnancy. if necessary, which is safest?

ranitidine (most data)

otherwise, famotidine

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PPIs are primarily administered po, with the exception of…

esomeprazole and pantoprazole (po/iv)

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name the drug class –

MOA: inhibit gastric acid secretion by irreversibly inhibiting functioning -ase pumps

onset: full symptom effects seen in a few to several days
inhibit: 50-90% of acid
ulcer healing: 4-8+ weeks

PPIs

note: covalently bind to sulfhydryl groups of H/K-ATPase at parietal cells secretory sites

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which drug class has CDAD as a risk?

PPIs – c. diff-associated diarrhea
standard GI and CNS related adverse effects as well

associations: increased risk AKI, osteoporosis/bone fractures and MI

STAR

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PPIs are relatively contraindicated during pregnancy. which is safest if necessary?

lansoprazole (common) or pantoprazole

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name the drug class –

MOA: cross-linking from interactions w/ stomach acid, creating a viscous, sticky polymer which adheres to epithelial cells around ulcer’s crater

…and…

stimulates local PG and mucous production, and EDGF

sucralfate

prevents acid access to ulcer sites

…and…

cytoprotection; does not affect pH

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is it safe to use sucralfate for longer than one year?

which drug is indicated for duodenal ulcer?

sucralfate

also used for:

aphthous ulcer
mucositis/stomatitis
more…

what is the adverse effect of sucralfate?

constipation

what is the relative contraindication of sucralfate?

severe renal failure (d/t aluminum)

when should sucralfate be taken?

2 hours after other medications to avoid potential DDIs

dosed at QID for active ulcers so dose other medications accordingly, if possible

name the drug class -- MOA: provides protective prostaglandin to gastric mucosa and reduces gastric acid release from parietal cell ...and... provides cytoprotection by increasing mucosal defenses

misoprostol / cytotec (w/ NSAID, diclofenac) PGE1 analog; stimulates bicarb, mucous production, and mucosal blood flow standard doses reduce basal and nocturnal acid output (less than H2 antagonists and PPIs)

what is the primary indication for misoprostol?

prevention (primary prophylaxis) of NSAID-induced gastric ulceration in pts at high risk of ulcerations d/t complications

what are the off-label uses of misoprostol?

1. w/ or w/o mifepristone -- pregnancy termination 2. cervical ripening 3. post-partum hemorrhaging (high dose)

name the contraindications of misoprostol

1. pregnancy | 2. IBD (avoid, if possible)

name the adverse effects of misoprostol

GI related (primarily) and CNS related

name the drug class -- MOA: antimicrobial actions prevent microbial attachment to mucosa, possible inactivation of enterotoxins, and disruption of bacterial cell wall

bismuth compounds

what are the OTC indications of bismuth compunds?

reflux, indigestion, diarrhea

what are the Rx indications for bismuth compunds?

used in combination with antibiotics and acid suppressant for H. pylori

what are the adverse effects of bismuth compounds?

1. constipation 2. black/dark (regularly formed) stools **STAR**

when should a patient take bismuth compounds?

two hours after other medications d/t DDIs

what are the relative contraindications of bismuth compounds?

1. antiplatelets and anticoagulants | 2. severe renal failure

what are the absolute contraindications of bismuth compounds?

1. GI bleeding | 2. salicylate hypersensitivity

describe the general treatment process for H. pylori

combination therapy!! TRIPLE THERAPY - at least 2 antibiotics and an acid reducer (PPI* or H2-blocker) - BID for 14 days - the antibiotics: clarithromycin + amoxicillin OR metronidazole **STAR**

which products must be avoided four weeks prior to performing gastric urease or urea breath-test d/t potential cause of false-negative results?

1. bismuth preparations 2. some antimicrobials 3. some PPIs b/c they suppress H. pylori

describe quadruple therapy for H. pylori

for 10-14 days 1. PPI (BID) 2. metronidzaole (QID) 3. tetracycline (QID) 4. bismuth subsalicylate (QID)

which antibiotic is a safe replacement in the treatment of H. pylori when a patient has a penicillin allergy?

metronidazole

what are prevpac and omeclamox-pak?

BID packs for H. pylori prevpac -- ACL amoxicillin (1,000 mg) clarithromycin (500 mg) lansoprazole (30 mg) omeclamox -- ACO amoxicillin (1,000 mg) clarithromycin (500 mg) omeprazole (20 mg)

what is helidac?

QID pack for H. pylori -- BMT bismuth subsalicylate (525 mg) metronidzaole (250 mg) tetracycline (500 mg) *add PPI b/c not in pack* **STAR**

what is pylera?

QID pack for H. pylori -- BMT bismuth subsalicylate (140 mg) metronidazole (125 mg) tetracycline (125 mg) *add PPI / omperazole* **STAR**

failure of eradication with metronidazole-containing triple therapy should be followed with...

non-metronidzaole containing quadruple therapy clarithromycin and amoxicillin OR clarithromycin and tetracycline **STAR**

H. pylori w/ PCN allergy...

sub in metronidazole consider bismuth quadruple therapy **STAR**

H. pylori w/ metronidazole resistance...

sub in tetracycline consider quadruple therapy w/ clarithromycin and amoxicillin **STAR**

H. pylori w/ clarithromycin resistance...

sub in amoxicillin or tetracycline consider bismuth quadruple therapy **STAR**

describe the treatments for a pregnant patient w/o H. pylori

moderate - ranitidine severe - lansoprazole **STAR**

describe the treatment course for NSAID-at risk

1. if NSAID not required -- acetaminophen and D/C NSAID | 2. if NSAID required -- COX-2 NSAID and/or PPI or misoprostol