GI Pharm Flashcards by elliot sultanik

H2 Receptor Antagonists (4)

1) Cimetidine
2) Ranitidine
3) Famotidine
4) Nizatidine

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When are H2 receptor antagonist effects most pronounced?

At night due to nocturnal acid secretion (which depends largely on histamine)

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Nizatidine: Class? Pharmacokinetics?

1) H2 receptor Antagonist
2) Great bioavailbility dt reduced first pass hepatic metabolism

Serum half life is 1-4 hours

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H+K+ ATPase

Proton pump

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How often should H2 receptor antagonist be used for GERD?

<3x per week

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If doctor decides to use H2 receptor antagonist for peptic ulcer, when should they be given?

At night

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H2 receptor antagonist contraindicated?

Preganant women; crosses the placenta and gets into breast milk

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Two H2 receptor antagonists that effect hepatic metabolism of many drugs?

Cimetidine and Ranitidine

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Proton Pump Inhibitors (6)

1) Omeprazole
2) Esomprazole
3) Lansoprazole
4) dexlansoprazole
5) Pantoprazole
6) Rabeprazole

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PPIs: how do they work?

1) Prodrugs!– require acid environment; activated drug binds with H, K atapase and irreversibly inactivates the enzyme

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Most potent H2 receptor antagonist?

Famotidine

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How should PPI be used?

On empty stomach before meals

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Triple therapy of Hpylori associated ulcers?

1) PPI
2) Amoxicillin
3) Clarithromycin or metronidazole bid

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PPI adverse reactions in hospitalized patients?

C. difficile

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Sucralfate: Use? MOA? Drug drug interactions?

1) Ulcers
2) **Promotes mucosal defense; **Requires acidic activation
3) so do not give with PPI or H2);

Thought to selectively bind necrotic ulcer tissue and acts as barrier to acid, pepsin and bile

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Drug that promotes mucosal defense? Which drugs should it not be given with?

1) Sucralfate
2) PPI or H2 antagonist

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Colloidal Bismuth Compounds: MOA? Use?

1) Bind to ulcer, coat it and protect it
2) Ulcers (direct antimicrobial activity against H pylori)

(High rates of ulcer healing when combined with tetracyclines and metronidazole)

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Misoprostol: MOA? Use? Contraindication?

1) Prostoglandin analog; both mucosal and acid inhibitory properties; reduces histamine stimulated cAMP production
2) NSAID induced ulcers
3) will ABORT in pregnant woman

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3 functions of metoclopramide? Use? MOA? Side effects?

1a) Inc. esophageal clearance
b) Raises LES pressure
c) Inc. gastric emptying
2) used for gastric motor problems
3) DA receptor antagonist
4) Extrapyramidal

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DM II patient on medication for “gastric motility” develops a tremor– drug? MOA?

Metoclopramide

Dopamine antagonist

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Lubiprostone: use? MOA? side effects?

1) Inc. motility; soften stools (constipation)
2) FA derivative from prostoglandin– producing chloride rich secretions
3) Can’t use in children

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Prostoglandin derivative that cannot be used in children?

Lubiprostone

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Laxative used before colonoscopy

Polyethylene Glycol

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Diphenoxylate and loperamide: MOA?

Inhibits ACh release

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Two drugs that inhibit ACh release

Diphenoxylate and Loperamide

ACh inhibitor that has potential for addiction?

Diphenoxylate

Pain associated with IBS: drug class? Two drugs?

1) Tricyclic antidepressants 2) Amitriptyline and desipramine

Amitriptyline: Use? What is it?

1) IBS 2) Tricyclic antidepressant

Desipramine: Use? What is it?

1) IBS 2) Tricyclic antidepressant

Alosetron: Use? MOA?

1) Severe IBS with diarrhea 2) Seretonin antagonist

5-HT3 antagonist in GI tract

Alosetron

Mesalamine (5-ASA): use? MOA?

1) UC 2) Bowel specific aminosalicylate

First line treatment of mild to moderate UC?

Mesalamine (5-ASA)

Steroid that is released in distal ileum and colon?

Budesonide

Steroid with high first pass metabolism?

Budesonide

Antimetabolite used primarly for Crohn's?

Methotrexate

Natalizumab: MOA? Side effect? use?

1) Anti integrin antibody 2) Progressive multifocal leukoencephalopathy (caused by JC virus) 3) Moderate to severe Crohn's in patients who have failed other treatments

Anti seretonin drugs suffix?

"setron"

4 Anti 5-HT3 drugs?

1) Ondansetron 2) Granisetron 3) Dolasetron 4) Palonosetron

What drugs are used to enhance efficacy of antiemetic drugs? 2

1) Dexamethasone 2) aprepitant

2 neurokinen receptor antagonists? Use?

1) Fosaprepitant 2) Aprepitant Antiemetics

Antihistamine with fewest anticholinergic effects?

Meclizine

3 antihistamines used for motion sickness?

1) Diphenhydramine 2) Dimenhydrinate 3) Meclizine

Protease Inhibitors (3)

Tealprevir Boceprevir Simeprevir **All end in "previr"; Previr think protease**

Telaprevir

protease inhibitor

Simeprevir

Protease inhibitor

Boceprevir

Protease Inhibitor (previr think protease inhibitor)

Ribavirin

Nucleoside analog for HCV

Used to treat HCV? MOA?

1) Ribavirin 2) Nucleoside analog

Sofosbuvir

Nucleo**T**ide analog

NucleoTide analog

Sofosbuvir

Entecavir

HBV; nucleoside analog

Lamivudine

HBV; nucleoside analog

Telbivudine

HBV; nucleoside analog

Tenofovir

HBV; nucleoside analog

Adefovir

HBV; nucleoside analog

Treatment of HBV? 2 classes?

Interferons and Nucleoside analogs

How do nucleoside analogs inhibit HBV DNA synthesis?

Inhibit HBV **DNA** polymerase

Goal of HCV?

Sustained viral response

Goal of HBV?

Seroconversion from HBeAg

Treatment of HCV types 2 and 3?

Interferons and ribavirin

MOA of Ribavirin?

Inhibits GTP synthesis and capping of viral mRNA

New drug to treat HCV 2 and 3? MOA?

1) Sofosbuvir 2) NucleoTide analog that inhibits RNA polymerase

3 protease inhibitors for HCV 1 and 4? MOA?

Teleprevir Boceprevir Simeprevir Inhibit Viral protein processing

Metoclopramide: Use? MOA? Toxicities?

1) Inc. gastric emptying; inc esoph clearance; raises LESP in DM patients 2) Antagonism of D2 receptors 3) CNS; extrapyramidal; psych

Drug that increases gastric emptying by antagonizes D2 receptors?

Metoclopramide

Lubiprostone: Use? MOA? Toxicity?

1) Softens stool (chronic constipation) 2) FA deriv of **prosto**glandin E1 (prost) that activates chloride channels 3) Do not use in children

Drug for chronic diarrhea that activates chloride channels in GI epithelium?

Lubiprostone (do not give to children)

Psyllium?

Bulk forming laxative

methylcellulose?

Bulk forming laxative

Docusate?

stool softener

Polyethylene glycol?

Osmotic laxative

MgOH2; sorbitol; lactulose

Osmotic laxatives

Two drugs used for rapid bowel evacuation?

Magnesium citrate and sodium phosphate

Bisacodyl?

Stimulant laxative (Coyl of doody)

Diphenoxylate? MOA? Side effects

1) antidiarrheal 2) opioid agonist: inhibit ACh release 3) CNS and dependence

Want to start patient on antidiarrheal. Pt. says he has an addictive personality. Drug?

1) Loperamide because unlike diphenoxylate, it does not cross the BBB and has no potential for addiction

Antidiarrheals that act on ACh release from presynaptic vessels?

1) Diphenoxylate 2) Loperamide

How do we treat pain in IBS?

Low doses of TCA (amitriptyline or desipramine)

TCAs used to pain in IBS?

1) Amitriptyline 2) Desipramine

5HT3 antagonist for IBS?

Alosetron

5 HT3 antagonist

Salazines: use?

First line for ulcerative colitis (and used in Crohn's disease that affects colon or distal ileum)

Controlled release corticosteroid that acts on distal ileum and colon? Other?

1) Budesonide 2) High first pass metabolism

Budesonide: What is it? Other?

1) Controlled release corticosteroid that acts on terminal ileum and colon 2) High first pass metabolism

3 antimetabolites?

1) Azathioprine 2) 6MP 3) Methotrexate

Antimetabolite with uncertain effect on ulcerative colitis?

Methotrexate

Most significant side effects of anti TNF?

Opportunistic infection due to suppression of helper T cell (type 1 inflammatory response)

Antiintegrin? toxicity?

1) Natalizumab (Natali can't seem to hold onto anything; no integrin) 2) Progressive multifocal leukoencephalopathy

"setrons"

1) 5 HT3 antagonist 2) Antiemetics

What drugs increase therapy of 5HT3 antagonists

Corticosteroids and NK1 receptor antagonist (aprepitant)

Aprepitant and Fosaprepitant (Prepitants)

1) Neurokinin 1 antagonists 2) Used in combination with 5 HT3 antagonist and corticosteroids

Neurokinin 1 antagonists (2)

1) Aprepitant 2) Fosaprepitant **prepitants**

H1 antihistamine use?

Motion Sickness

H1 antihistamines (3) why one over the other? use?

1) Motion sickness 2) Diphenhydramine (benadryl); dimenhydrinate; meclizine 3) Meclizine has less anticholinergic properties and less sedating

H1 antihistamine with fewer anticholinergic properties and less sedation properties?

Meclizine

GI Pharm Flashcards

(96 cards)