Pharmacology - GI Drugs I & II - Patsy Iannolo Flashcards

1
Q

Class: Calcium carbonate (Rolaids, Tums)

A

Antacid

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2
Q

Class: Sodium bicarbonate

A

Antacid

Rarely used due to causing systemic alkalosis

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3
Q

Class: Magnesium hydroxide, magnesium carbonate (Maalox, Mylanta)

A

Antacid

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4
Q

Class: Aluminum hydroxide (Alternagel)

A

Antacid

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5
Q

Use: Calcium carbonate (Rolaids, Tums)

A

Ulcer tx, GERD

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6
Q

Use: Sodium bicarbonate

A

Ulcer tx, GERD

Rarely used due to causing systemic alkalosis

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7
Q

Use: Magnesium hydroxide, magnesium carbonate (Maalox, Mylanta)

A

Ulcer tx, GERD

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8
Q

Use: Aluminum hydroxide (Alternagel)

A

Ulcer tx, GERD

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9
Q

Side Effects: Calcium carbonate (Rolaids, Tums)

A

Milk-alkali syndrome, nephrocalcinosis,
“rebound” acidity,
digitalis antagonism,
constipation

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10
Q

Side Effects: Sodium bicarbonate

A

Systemic alkalosis;
Enhanced effects of amphetamine, quinidine, and cinchophen

Rarely used due to causing systemic alkalosis

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11
Q

Side effects: Magnesium hydroxide, magnesium carbonate (Maalox, Mylanta)

A

Diarrhea;
Hypokalemia,
hypermagnesemia,
iron deficiency

Magnesium toxicity mostly in presence of renal disease; liquid-based, so act fast

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12
Q

Side effects: Aluminum hydroxide (Alternagel)

A

Phosphate depletion and sequelae (weakness, anemia, tetany, apnea);
Constipation

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13
Q

What antacid is safe for use in patients with renal failure?

A

Aluminum hydroxide

also eliminates phosphate

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14
Q

What antacid should not be used in patients that have renal failure?

A

Magnesium hydroxide, magnesium carbonate (Maalox, Mylanta)

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15
Q

Class: Cimetidine

A

Histamine (H2) receptor blocker

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16
Q

Class: Famotidine

A

Histamine (H2) receptor blocker

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17
Q

Class: Ranitidine

A

Histamine (H2) receptor blocker

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18
Q

Class: Nizatidine

A

Histamine (H2) receptor blocker

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19
Q

MOA: Histamine (H2) receptor blockers - Cimiidine, Ranitidine, Famotidine, Nizatidine

A

Inhibits 50-80% of 24 hour acid production

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20
Q

Use: Histamine (H2) receptor blockers - Cimiidine, Ranitidine, Famotidine, Nizatidine

A

Ulcer treatment (satisfy all 4 requirements); prophylactically for stress ulcers; GERD

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21
Q

Side Effects: Ulcer treatment (satisfy all 4 requirements); prophylactically for stress ulcers; GERD

A

Rebound acidity if stopped;

Uncommon; headache, lethargy, confusion, depression, and hallucination

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22
Q

Class: Omeprazole

A

H/K/ATPase inhibitor

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23
Q

Class: Lansoprazole

A

H/K/ATPase inhibitor

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24
Q

Class: Rabeprazole

A

H/K/ATPase inhibitor

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25
Q

Class: Pantoprazole

A

H/K/ATPase inhibitor

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26
Q

Class: Esomeprazole

A

H/K/ATPase inhibitor

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27
Q

MOA: H/K/ATPase inhibitors:

Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole, Esomeprazole

A

Inhibit >90% of 24 hour acid secretion (better than H2 antagonists);
requires acid environment to activate, selectively diffuse to acidic environments (don’t take with antacids)

**noncompetitive inhibitors

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28
Q

Uses: Omeprazole and Lansorazole

A

Ulcer treatment,
treatment for H. pylori;
GERD

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29
Q

Uses: Rabeprazole, Pantoprazole, Esomeprazole

A

Ulcer treatment; GERD

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30
Q

Side Effects: H/K/ATPase inhibitors:

Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole, Esomeprazole

A

Headache, gynecomastia, gastric hyperplasia in humans and carcinoid tumors in rats long term (do not use long-term)

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31
Q

What is Dexlansoprazole?

A

A rapid-formulation of slow release Lansoprazole

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32
Q

What is the only H/K ATPase inhibitor available for IV administration?

A

Pantoprazole

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33
Q

T/F: H/K ATPase inhibitors will heal H2 antagonist refractory ulcers.

A

True

Also, better pain relief and faster healing rates than with H2 antagonists.

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34
Q

What H/K ATPase inhibitor has no P450 interaction?

A

Pantoprazole

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35
Q

What is the only drug that is FDA approved for the prevention of NSAID-induced gastric ulcers?

A

Misoprostol

H2 antagonists and sucralfate are ineffective if NSAID
therapy is being continued.

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36
Q

Class: Misoprostol

A

Prostaglandin E analog

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37
Q

MOA: Misoprostol

A

Decrease acid production, increase mucous and bicarbonate secretion

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38
Q

Use: Misoprostol

A

Ulcer treatment when prostaglandin production decreased (RA patients taking lots of NSAIDs)

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39
Q

What antacid should not be used in pregnancy?

A

Misoprostol

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40
Q

Side effects: Misoprostol

A

Transient diarrhea

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41
Q

What is the therapy for H. Pylori infection?

A

Quadruple therapy:
A PPI twice a day
Tetracycline HCl 500 mg 4 times a day
Bismuth subsalicylate or subcitrate 4 times a day Metronidazole 500 mg 3 times a day

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42
Q

Class: Atropine sulfate

A

Anticholinergics

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43
Q

Class: Probantheline;

Metantheline bromide

A

Anticholinergics

44
Q

MOA: Anticholinergics -
Atropine sulfate;
Probantheline;
Metantheline bromide

A

Reduce acid secretion;

reduce spasm

45
Q

Use: Atropine sulfate

A

Ulcer treatment

46
Q

Side effects: Anticholinergics -
Atropine sulfate;
Probantheline;
Metantheline bromide

A

Anticholinergic effects

47
Q

What are the contraindications for Probantheline;

Metantheline bromide

A

Known pyloric obstruction, hiatal hernia, or peptic esophagitis (not used much)

48
Q

What are the contraindications for Atropine sulfate?

A

Aspirin;
Belladonna;
known pyloric obstruction, hiatal hernia, or peptic esophagitis (not used much)

49
Q

Use: Probantheline;

Metantheline bromide

A

Ulcer treatment (taken 15-30 minutes before meals, and before bed)

50
Q

Class: Sucralfate (Carafate)

A

Mechanical protector

51
Q

Class: Bismuth salts

A

Mechanical protector

52
Q

MOA: Sucralfate

A

Coat the ulcer crater, increase mucosal resistance (requires acid environment)

53
Q

MOA: Bismuth salts

A

Coat the ulcer crater, increase mucosal resistance

54
Q

Side effects: Sucralfate

A

Aluminum toxicity possible in renal failure

55
Q

Use: Sucralfate, Bismuth salts

A

Ulcer treatment, treatment for H. pylori

56
Q

Side effects: Bismuth salts

A

Aluminum toxicity possible in renal failure; turns bowel movements (and sometimes tongues) black

57
Q

Class: Ondansetron

A

Serotonin (5HT3) receptor antagonists

58
Q

Class: Granesitron

A

Serotonin (5HT3) receptor antagonists

59
Q

Class: Dolasetron

A

Serotonin (5HT3) receptor antagonists

60
Q

Class: Promethazine

A

Phenothiazines (neuroleptic class)

61
Q

Class: Prochlorperazine

A

Phenothiazines (neuroleptic class)

62
Q

MOA: Prochlorperazine

A

Probable CNS interaction with dopaminergic receptor-antagonist (leading to reduction of stimulation in the CRTZ in the medulla)

63
Q

Use:
Prochlorperazine;
Promethazine

A

Anti-emetic

64
Q

MOA: Promethazine

A

Antihistamine (H1 receptor);

anticholinergic

65
Q

Side effects: Prochlorperazine

A

Largely extra-pyramidal (torticollis!)

66
Q

Side effects: Promethazine

A

Somnolence (esp in elderly)

67
Q

MOA:
Ondansetron;
Granesitron;
Dolasetron

A

Blocks serotonin at 5HT3 receptor (in central CRTZ)

68
Q

Use:

Ondansetron;

A

Anti-emetic

69
Q

Use:
Granesitron;
Dolasetron

A

Post-op anti-emetic

70
Q

Class: Metochlopramide

A

Promotility agent (dopamine antagonist)

71
Q

MOA: Metochlopramide

A

Increase motor tone in lower esophageal sphincter (prevent reflux) and stomch (esp. antrum: improves gastric emptying); peripheral (stomach) and CNS (vomiting, via CRTZ) dopamine antagonist

72
Q

Use: Metochlopramide

A

GERD, anti-emetic, gastroparesis

73
Q

Side effects: Metochlopramide

A

Hand tremor if used 4X/day (optimum use); possible extra-pyramidal symptoms, but not so severe

74
Q

Class: Domperidone

A

Promotility agent

75
Q

MOA: Domperidone

A

Improves gastric tone

76
Q

Use: Domperidone

A

Gastroparesis

77
Q

An important complication of Cisparide is:

A

possibility of sudden cardiac death

78
Q

Class: Cisparide

A

Promotility agent (dopamine agonist)

79
Q

MOA: Cisparide

A

Increase motor tone in lower esophageal sphincter and stomach

80
Q

Use: Cisparide

A

GERD, gastroparesis

81
Q

Class: Lubiprostone

A

82
Q

Class: Linaclotide

A

83
Q

Class: Naloxegol

A

Mu receptor antagonist

84
Q

MOA: Lubiprostone

A

acts on chloride channel

85
Q

MOA: Linaclotide

A

cGMP

86
Q

Use: Lubiprostone

A

Anti-constipation

87
Q

MOA: Naloxegol

A

88
Q

Use: Naloxegol

A

Anti-constipation;

effective in opioid addicted population

89
Q

Class: Sulfasalazine

A

Anti-inflammatory

90
Q

Class: Olsalazine

A

Anti-inflammatory

91
Q

Class: Mesalamine

A

Anti-inflammatory

92
Q

Class: Prednisone

A

Corticosteroid

93
Q

Class: Azathioprine

A

Immunosuppressive

94
Q

Class: Cyclosporine

A

Immunosuppressive

95
Q

Class: Infliximab

A

MAb Immunisuppressive

96
Q

MOA: Sulfasalazine

A

Work from lumen to reduce inflammation

97
Q

MOA: Olsalazine

A

Work from lumen to reduce inflammation; 5-ASA dimer

Broken down into bowel by bacteria into 2 moleules of 5-ASA

98
Q

MOA: Mesalamine

A

Work from lumen to reduce inflammation

Delayed release 5-ASA, for terminal ileum, colon

99
Q

MOA: Azathioprine

A

Purine antimetabolite; interferes with DNA synthesis

100
Q

MOA: Cyclosporine

A

Suppresses T helper and T suppressor lymphocytes

101
Q

MOA: Infliximab

A

Binds and neutralized TNFa

102
Q

Use:
Sulfasalazine;
Olsalazine;
Mesalamine

A

Acute IBD (UC)

103
Q

Use: Prednisone

A

Acute and chronic IBD

Can be given systemically or as enemas

104
Q

Use:
Azathioprine;
Cyclosporine;
Infliximab

A

Chronic IBD

105
Q

Side Effects: Sulfasalazine

A

Toxicity coming from systemic absorption of sulfapyridine

106
Q

T/F: Olsalazine has less toxicity that Sulfasalazine

A

True