GI Pharm Flashcards

1
Q

H2 Receptor Antagonists (4)

A

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

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2
Q

When are H2 receptor antagonist effects most pronounced?

A

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

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3
Q

Nizatidine: Class? Pharmacokinetics?

A

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

Serum half life is 1-4 hours

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4
Q

H+K+ ATPase

A

Proton pump

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5
Q

How often should H2 receptor antagonist be used for GERD?

A

<3x per week

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6
Q

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

A

At night

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7
Q

H2 receptor antagonist contraindicated?

A

Preganant women; crosses the placenta and gets into breast milk

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8
Q

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

A

Cimetidine and Ranitidine

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9
Q

Proton Pump Inhibitors (6)

A

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

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10
Q

PPIs: how do they work?

A

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

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11
Q

Most potent H2 receptor antagonist?

A

Famotidine

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12
Q

How should PPI be used?

A

On empty stomach before meals

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13
Q

Triple therapy of Hpylori associated ulcers?

A

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

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14
Q

PPI adverse reactions in hospitalized patients?

A

C. difficile

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15
Q

Sucralfate: Use? MOA? Drug drug interactions?

A

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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16
Q

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

A

1) Sucralfate
2) PPI or H2 antagonist

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17
Q

Colloidal Bismuth Compounds: MOA? Use?

A

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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18
Q

Misoprostol: MOA? Use? Contraindication?

A

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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19
Q

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

A

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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20
Q

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

A

Metoclopramide

Dopamine antagonist

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21
Q

Lubiprostone: use? MOA? side effects?

A

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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22
Q

Prostoglandin derivative that cannot be used in children?

A

Lubiprostone

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23
Q

Laxative used before colonoscopy

A

Polyethylene Glycol

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24
Q

Diphenoxylate and loperamide: MOA?

A

Inhibits ACh release

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25
Q

Two drugs that inhibit ACh release

A

Diphenoxylate and Loperamide

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26
Q

ACh inhibitor that has potential for addiction?

A

Diphenoxylate

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27
Q

Pain associated with IBS: drug class? Two drugs?

A

1) Tricyclic antidepressants
2) Amitriptyline and desipramine

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28
Q

Amitriptyline: Use? What is it?

A

1) IBS
2) Tricyclic antidepressant

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29
Q

Desipramine: Use? What is it?

A

1) IBS
2) Tricyclic antidepressant

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30
Q

Alosetron: Use? MOA?

A

1) Severe IBS with diarrhea
2) Seretonin antagonist

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31
Q

5-HT3 antagonist in GI tract

A

Alosetron

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32
Q

Mesalamine (5-ASA): use? MOA?

A

1) UC
2) Bowel specific aminosalicylate

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33
Q

First line treatment of mild to moderate UC?

A

Mesalamine (5-ASA)

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34
Q

Steroid that is released in distal ileum and colon?

A

Budesonide

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35
Q

Steroid with high first pass metabolism?

A

Budesonide

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36
Q

Antimetabolite used primarly for Crohn’s?

A

Methotrexate

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37
Q

Natalizumab: MOA? Side effect? use?

A

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

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38
Q

Anti seretonin drugs suffix?

A

“setron”

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39
Q

4 Anti 5-HT3 drugs?

A

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

40
Q

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

A

1) Dexamethasone
2) aprepitant

41
Q

2 neurokinen receptor antagonists? Use?

A

1) Fosaprepitant
2) Aprepitant

Antiemetics

42
Q

Antihistamine with fewest anticholinergic effects?

A

Meclizine

43
Q

3 antihistamines used for motion sickness?

A

1) Diphenhydramine
2) Dimenhydrinate
3) Meclizine

44
Q

Protease Inhibitors (3)

A

Tealprevir

Boceprevir

Simeprevir

All end in “previr”; Previr think protease

45
Q

Telaprevir

A

protease inhibitor

46
Q

Simeprevir

A

Protease inhibitor

47
Q

Boceprevir

A

Protease Inhibitor (previr think protease inhibitor)

48
Q

Ribavirin

A

Nucleoside analog for HCV

49
Q

Used to treat HCV? MOA?

A

1) Ribavirin
2) Nucleoside analog

50
Q

Sofosbuvir

A

NucleoTide analog

51
Q

NucleoTide analog

A

Sofosbuvir

52
Q

Entecavir

A

HBV; nucleoside analog

53
Q

Lamivudine

A

HBV; nucleoside analog

54
Q

Telbivudine

A

HBV; nucleoside analog

55
Q

Tenofovir

A

HBV; nucleoside analog

56
Q

Adefovir

A

HBV; nucleoside analog

57
Q

Treatment of HBV? 2 classes?

A

Interferons and Nucleoside analogs

58
Q

How do nucleoside analogs inhibit HBV DNA synthesis?

A

Inhibit HBV DNA polymerase

59
Q

Goal of HCV?

A

Sustained viral response

60
Q

Goal of HBV?

A

Seroconversion from HBeAg

61
Q

Treatment of HCV types 2 and 3?

A

Interferons and ribavirin

62
Q

MOA of Ribavirin?

A

Inhibits GTP synthesis and capping of viral mRNA

63
Q

New drug to treat HCV 2 and 3? MOA?

A

1) Sofosbuvir
2) NucleoTide analog that inhibits RNA polymerase

64
Q

3 protease inhibitors for HCV 1 and 4? MOA?

A

Teleprevir

Boceprevir

Simeprevir

Inhibit Viral protein processing

65
Q

Metoclopramide: Use? MOA? Toxicities?

A

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

66
Q

Drug that increases gastric emptying by antagonizes D2 receptors?

A

Metoclopramide

67
Q

Lubiprostone: Use? MOA? Toxicity?

A

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

68
Q

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

A

Lubiprostone (do not give to children)

69
Q

Psyllium?

A

Bulk forming laxative

70
Q

methylcellulose?

A

Bulk forming laxative

71
Q

Docusate?

A

stool softener

72
Q

Polyethylene glycol?

A

Osmotic laxative

73
Q

MgOH2; sorbitol; lactulose

A

Osmotic laxatives

74
Q

Two drugs used for rapid bowel evacuation?

A

Magnesium citrate and sodium phosphate

75
Q

Bisacodyl?

A

Stimulant laxative (Coyl of doody)

76
Q

Diphenoxylate? MOA? Side effects

A

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

77
Q

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

A

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

78
Q

Antidiarrheals that act on ACh release from presynaptic vessels?

A

1) Diphenoxylate
2) Loperamide

79
Q

How do we treat pain in IBS?

A

Low doses of TCA (amitriptyline or desipramine)

80
Q

TCAs used to pain in IBS?

A

1) Amitriptyline
2) Desipramine

81
Q

5HT3 antagonist for IBS?

A

Alosetron

82
Q

Alosetron

A

5 HT3 antagonist

83
Q

Salazines: use?

A

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

84
Q

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

A

1) Budesonide
2) High first pass metabolism

85
Q

Budesonide: What is it? Other?

A

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

86
Q

3 antimetabolites?

A

1) Azathioprine
2) 6MP
3) Methotrexate

87
Q

Antimetabolite with uncertain effect on ulcerative colitis?

A

Methotrexate

88
Q

Most significant side effects of anti TNF?

A

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

89
Q

Antiintegrin? toxicity?

A

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

90
Q

“setrons”

A

1) 5 HT3 antagonist
2) Antiemetics

91
Q

What drugs increase therapy of 5HT3 antagonists

A

Corticosteroids and NK1 receptor antagonist (aprepitant)

92
Q

Aprepitant and Fosaprepitant (Prepitants)

A

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

93
Q

Neurokinin 1 antagonists (2)

A

1) Aprepitant
2) Fosaprepitant

prepitants

94
Q

H1 antihistamine use?

A

Motion Sickness

95
Q

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

A

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

96
Q

H1 antihistamine with fewer anticholinergic properties and less sedation properties?

A

Meclizine