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Old Gastrointestinal Cards > GI Pharmacology-B > Flashcards

GI Pharmacology-B Flashcards

1
Q

Which Anti-androgenic Agent causes a disulfuram type reaction

A

Nilutamide

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2
Q

Abiraterone: Drug Class

A

Anti-androgenic Agent

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3
Q

Abiraterone: Mechanism of action

A

Selectively and irreversibly inhibits CYP17, an enzyme required for androgen biosynthesis, thus inhibiting the formation of testosterone precursors

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4
Q

Abiraterone: Uses

A

FDA approved for Tx of metastatic, castration-resistant prostate cancer in patients previously treated with docetaxel (now approved as first line Tx)

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5
Q

Enzalutamide: Drug Class

A

Anti-androgenic Agent

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6
Q

Enzalutamide: Mechanism of action

A

It is a pure androgen receptor signaling inhibitor. It has no agonistic properties, It inhibits androgen receptor nuclear translocation, DNA binding, and coactivator mobilization leading to cellular apoptosis

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7
Q

Enzalutamide: Uses

A

FDA approved for Tx of metastatic, castration-resistant prostate cancer in patients previously treated with docetaxel

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8
Q

Enzalutamide: Side Effects

A

Peripheral edema, fatigue, headache, hot flashes, diarrhea, neutropenia

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9
Q

Abiraterone: Side Effects

A

Edema, hypertriglyceridemia, hypokalemia, hypophosphatemia, diarrhea

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10
Q

Which Anti-androgenic Agent must be given with prednisone because it inhibits the production of cortisol

A

Abiraterone

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11
Q

Fulvestrant: Drug Class

A

Estrogen Receptor Antagonist

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12
Q

Fulvestrant: Mechanism of action

A

Steroid compound that competitively binds estrogen receptors. Produces nuclear complex that decreases DNA synthesis and inhibits estrogen effects. No ER agonist activity (pure antagonist). Down-regulates ER and inhibits tumor growth

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13
Q

Fulvestrant: Uses

A

2nd line therapy in postmenopausal women after disease progression on SERM or AI therapy

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14
Q

Fulvestrant: Side Effects

A

Hot flashes, nausea, angioedema, weakness, local site reaction

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15
Q

Degarelix: Drug Class

A

Gonadotropin Releasing Hormone Antagonist

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16
Q

Degarelix: Mechanism of action

A

LHRH antagonist. Major advantage is immediate down regulation of testosterone; no tumor flare

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17
Q

Degarelix: Uses

A

Equivalent to leuprolide in decreasing testosterone levels for up to one year and FDA approved for treatment of advanced prostate cancer

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18
Q

Degarelix: Side Effects

A

Hot flashes, injection site reactions

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19
Q

Cholestyramine: Drug Class

A

Bile acid resin

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20
Q

Bile acid resins: Mechanism of action

A

Bind negatively charged bile acids which bind consumed cholesterol and everything is excreted

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21
Q

Bile acid resins: Side Effects

A

Non-compliance (It tastes bad), Increases HMGCoA activity and triglyceride synthesis (May lead to a transient increase in TG/VLDL), steatorrhea, abdominal bloating

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22
Q

Colestipol: Drug Class

A

Bile acid resin

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23
Q

Name the two Bile acid resins

A

Cholestyramine and Colestipol

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24
Q

Ezetimibe: Drug Class

A

Transport inhibitor

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25
Q

Ezetimibe: Mechanism of action

A

Blocks absorption of cholesterol in the small intestine

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26
Q

Ezetimibe is contraindicated in what patients

A

Patients with moderate to severe hepatic insufficiency

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27
Q

Simvastatin + Ezetimibe: Combination drug with what trade name

A

Vytorin

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28
Q

What advantage does combination therapy like Simvastatin + Ezetimibe (Vytorin) have

A

It reduces the potential side effects of statins by allowing for lower dose of the statin drug to be used to obtain specific reduction in cholesterol

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29
Q

Fluvastatin: Drug Class

A

HMG Co A Reductase inhibitor

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30
Q

HMG Co A Reductase inhibitors: Mechanism of action

A

Inhihibits HMGCoA reductase which catalyzes the conversion of Acetyl CoA to Malvonic acid (a key step in the synthesis of cholesterol). This causes low cholesterol in the liver which responds by increasing hepatic LDL receptors removing LDL from the blood).

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31
Q

Lovastatin: Drug Class

A

HMG Co A Reductase inhibitor

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32
Q

Pravastatin: Drug Class

A

HMG Co A Reductase inhibitor

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33
Q

HMG Co A Reductase inhibitors: Mechanism of action

A

Can cause rhabdomyolysis (rare but may be life threatening), transaminase hepatitis (check liver enzymes)

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34
Q

Simvastatin: Drug Class

A

HMG Co A Reductase inhibitor

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35
Q

HMG Co A Reductase inhibitors are contraindicated in what patients

A

Contraindicated in patients with renal failure and patients taking cyclosporine, macrolide antibiotics, various antifungal agents, and cytochrome P-450 inhibitors

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36
Q

Atorvastatin: Drug Class

A

HMG Co A Reductase inhibitor

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37
Q

Rosuvastatin: Drug Class

A

HMG Co A Reductase inhibitor

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38
Q

Name the six statins in order from least to most potent

A

(For Love People Say Anything Really) Fluvastatin < Lovastatin < Pravastatin < Simvastatin < Atorvastatin < Rosuvastatin

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39
Q

Clofibrate: Drug Class

A

Fibric Acid

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40
Q

Name the two Fibric Acids

A

Clofibrate and Gemfibrozil

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41
Q

Fibric Acids: Side Effects

A

Dyspepsia, gallstones, myopathy (particularly in combination with statins)

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42
Q

Gemfibrozil: Drug Class

A

Fibric Acid

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43
Q

Fibric Acids: Mechanism of action

A

Inhibits fatty acid synthesis, causes lipoprotein lipase-enhanced hydrolysis, stimulates synthesis of apoA-1

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44
Q

Niacin: Drug Class

A

Nicotinic Acid

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45
Q

Niacin: Mechanism of action

A

Inhibits VLDL secretion and increases clearance of VLDL via lipoprotein lipase pathway

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46
Q

Niacin: Side Effects

A

Intense flushing, and associated pruritis (one aspirin can relieve symptom), nausea, abdominal pain, hyperuricemia, hyperglycemia (acanthosis nigricans associated with insulin resistance), hepatotoxicity (increased transaminase, & ALT, flu-like fatigue)

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47
Q

What is the most effective agent for increasing HDL

A

Niacin

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48
Q

Niacin is contraindicated in what patients

A

Contraindicated in patients with peptic ulcer disease

49
Q

Cimetidine (Tagamet): Function and drug class

A

Control of Gastric Acid, H2 blocker

50
Q

Name the four H2 blockers

A

Cimetidine, Ranitidine, Famotidine, Nizatidine

51
Q

Which H2 blocker inhibits CYP450 and thus can cause drug-drug interactions

A

Cimetidine

52
Q

Ranitidine (Zantac): Function and drug class

A

Control of Gastric Acid, H2 blocker

53
Q

Cimetidine (Tagamet) may increase the secretion of what hormone

A

Prolactin

54
Q

Famotidine (Pepcid): Function and drug class

A

Control of Gastric Acid, H2 blocker

55
Q

Nizatidine (Axid): Function and drug class

A

Control of Gastric Acid, H2 blocker

56
Q

H2 blockers are useful in treating what

A

Gastric and duodenal ulcers, and zollinger-Ellison Syndrome (non-beta islet cell, gastrin-secreting tumor of the pancreas that stimulates the acid-secreting cells of the stomach to maximal activity)

57
Q

Omeprazole (Prilosec): Function and drug class

A

Control of Gastric Acid, Proton Pump Inhibitor

58
Q

Proton Pump Inhibitors: Mechanism of action

A

Inhibit the K+/H+ ATPase on parietal cells

59
Q

Proton Pump Inhibitors are superior to H2 blockers in healing of what

A

NSAID-induced gastric ulcers

60
Q

Lansoprazole (Prevacid): Function and drug class

A

Control of Gastric Acid, Proton Pump Inhibitor

61
Q

Name the five proton pump inhibitors

A

Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole, Esomeprazole

62
Q

Long term use of proton pump inhibitors is associated with

A

Hip fractures and possibly hypomagnesemia

63
Q

Rabeprazole (Aciphex): Function and drug class

A

Control of Gastric Acid, Proton Pump Inhibitor

64
Q

Pantoprazole (Protonix): Function and drug class

A

Control of Gastric Acid, Proton Pump Inhibitor

65
Q

Esomeprazole (Nexium): Function and drug class

A

Control of Gastric Acid, Proton Pump Inhibitor

66
Q

The transient rebound in stomach acid secretion after withdrawing a proton pump inhibitor is a result of increased gastrin levels and can last up to how long

A

Up to 4 weeks

67
Q

Atropine: Function and drug class

A

Control of Gastric Acid, Antimuscarinic

68
Q

By what mechanism do antimuscarinics affect acid secretion by parietal cells

A

They block stimulation of muscarinic receptors on parietal cells. Stimulation of these receptors would normally result in increased intracellular Ca++ and activation of the H+/K+ ATPase that pumps proteins into the lumen

69
Q

Which two antimuscarinics are used to reduce gastric acid secretion

A

Atropine and Glycopyrrolate

70
Q

Glycopyrrolate: Function and drug class

A

Control of Gastric Acid, Antimuscarinic

71
Q

Misoprostol: Function and drug class

A

Control of Gastric Acid, Cytoprotective

72
Q

Misoprostol is an analogue of what

A

PGE-1

73
Q

Misoprostol: Mechanism of action

A

It stimulates PG receptor leading to increased mucous & bicarbonate secretion, and decreases cAMP which decreases HCL secretion

74
Q

Misoprostol is only used to treat what

A

A NSAID-induced ulcer

75
Q

When is Misoprostol contraindicated

A

During pregnancy (its an abortifacient)

76
Q

Sucralfate: Function and drug class

A

Control of Gastric Acid, Cytoprotective

77
Q

Sucralfate: Mechanism of action

A

It polymerizes into a sticky gel under acidic conditions which has affinity for exposed protein in crater of an ulcer and inhibits back diffusion of H+ and reduces pepsin activity

78
Q

Metronidazole & Tetracycline: Function and drug class

A

Ulcer repair, Antibiotic

79
Q

Metronidazole & Tetracycline is administered with what

A

Bismuth subsalicylate (pepto bismol)

80
Q

What are the two antibiotic regimens for H. Pylori infection

A

Metronidazole + Tetracycline and Clarithromycin

81
Q

Clarithromycin: Function and drug class

A

Ulcer repair, Antibiotic

82
Q

Clarithromycin is administered with what

A

Omeprazole

83
Q

How long are Metronidazole + Tetracycline or Clarithromycin administered for treatment of H. Pylori

A

14 days

84
Q

Metoclopramide: Function and drug class

A

Prokinetic Agent, Increase Acetylcholine

85
Q

Metoclopramide: Mechanism of action

A

It is a cholinomimetic and a D2 receptor blocker. It promotes the release of acetylcholine from myenteric neurons

86
Q

Metoclopramide is used to treat what

A

GERD and diabetic gastroparisis

87
Q

Cisapride: Function and drug class

A

Prokinetic Agent, Increase Acetylcholine

88
Q

Cisapride

A

It promotes the release of acetylcholine from myenteric neurons and acts as a 5-HT4 receptor agonist. Has similar prokinetic effects as metoclopramide

89
Q

How does Cisapride differ from Metoclopramide

A

It is not a D2 blocker and so does not have antiemetic properties. It also has greater effect on the colon

90
Q

Name the two prokinetic agents

A

Metoclopramide and Cisapride

91
Q

Diphenoxylate (Lomotil): Function and drug class

A

Antidiarrheal, Opioid

92
Q

What is Diphenoxylate administered with to discourage deliberate abuse

A

Sub-therapeutic dose of atropine

93
Q

Loperamide (Imodium): Function and drug class

A

Antidiarrheal, Opioid

94
Q

Name the two antidiarrheal agents

A

Diphenoxylate and Loperamide

95
Q

Bismuth subsalicylate (Pepto): Function and drug class

A

Antidiarrheal, Salicylate

96
Q

Bismuth subsalicylate (Pepto) can cause what syndrome

A

Reyes Syndrome

97
Q

Thymoglobulin: What drug class [and is it used for induction or maintainance therapy]

A

Anti-lymphocyte globulin (Rabbit derived) [used as an induction agent]

98
Q

Thymoglobulin: Mechanism of Action

A

Complement-mediated cell lysis of circulating T-cells

99
Q

Cytokine release syndrome, serum sickness, leukopenia, and thrombocytopenia are the side effects of what drug

A

Thymoglobulin

100
Q

Basiliximab: What drug class [and is it used for induction or maintainance therapy]

A

Monoclonal Antibody (against IL-2 receptor) [used as an induction agent]

101
Q

Basiliximab: Mechanism of Action

A

It binds to the alpha unit of the IL-2 receptor inhibiting binding of IL-2 thereby preventing activation of lymphocytes

102
Q

Abdominal pain, dizziness, and insomnia are the side effects of what drug

A

Basiliximab

103
Q

Methylprednisolone: What drug class [and is it used for induction or maintainance therapy]

A

Corticosteroid [used as an induction agent]

104
Q

Methylprednisolone: Mechanism of Action

A

Blocks cytokine gene expression resulting in a decreased immune response

105
Q

Hypertension, fluid retention, hyperglycemia, impaired wound healing, mood disturbances, and vivid dreams are the side effects of what drug

A

Methylprednisolone

106
Q

Tacrolimus: What drug class [and is it used for induction or maintainance therapy]

A

Calcineurin Inhibitor [used as a maintainance agent]

107
Q

Tacrolimus: Mechanism of Action

A

Inhibits IL-2 synthesis by blocking calcineurin

108
Q

Alopecia, hyperglycemia, hyperkalemia, nephrotoxicity, neurologic toxicity are the side effects of what drug

A

Tacrolimus

109
Q

Mycophenolate: What drug class and is it used for induction or maintainance therapy

A

Antimetabolite [used as a maintainance agent]

110
Q

Mycophenolate: Mechanism of Action

A

Inhibits proliferation of T and B cells by preventing RNA and DNA synthesis

111
Q

GI intolerance, bone marrow suppression are the side effects of what drug

A

Mycophenolate

112
Q

Sirolimus: What drug class and is it used for induction or maintainance therapy

A

mTOR Inhibitor [used as a maintainance agent]

113
Q

Sirolimus: Mechanism of Action

A

Binds to FKBP-12 forming a complex that inhibits the activation of T cells and B cells by inhibiting their response to interleukin-2 (IL-2)

114
Q

Anemia, hepatic artery thrombosis, hyperlipidemia, impaired wound healing, proteinuria are the side effects of what drug

A

Sirolimus

115
Q

Prednisone: What drug class and is it used for induction or maintainance therapy

A

Corticosteroid [used as a maintainance agent]

116
Q

Prednisone: Mechanism of Action

A

Blocks cytokine gene expression resulting in a decreased immune response

117
Q

Chronic adrenal insufficiency, GERD, Hyperglycemia, hypertension, and osteoporosis are the side effects of what drug

A

Prednisone

118
Q

The effectiveness of which Immunosuppression drug(s) is decreased by CYP450 3A4 inducers

A

Tacrolimus and Sirolimus

119
Q

The effectiveness of which Immunosuppression drug(s) is decreased by aluminum & magnesium containing antacids and by cyclosporine

A

Mycophenolate

Old Gastrointestinal Cards (4 decks)

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