GI Pharmacology-B Flashcards
(119 cards)
1
Q
Which Anti-androgenic Agent causes a disulfuram type reaction
A
Nilutamide
2
Q
Abiraterone: Drug Class
A
Anti-androgenic Agent
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
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)
5
Q
Enzalutamide: Drug Class
A
Anti-androgenic Agent
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
7
Q
Enzalutamide: Uses
A
FDA approved for Tx of metastatic, castration-resistant prostate cancer in patients previously treated with docetaxel
8
Q
Enzalutamide: Side Effects
A
Peripheral edema, fatigue, headache, hot flashes, diarrhea, neutropenia
9
Q
Abiraterone: Side Effects
A
Edema, hypertriglyceridemia, hypokalemia, hypophosphatemia, diarrhea
10
Q
Which Anti-androgenic Agent must be given with prednisone because it inhibits the production of cortisol
A
Abiraterone
11
Q
Fulvestrant: Drug Class
A
Estrogen Receptor Antagonist
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
13
Q
Fulvestrant: Uses
A
2nd line therapy in postmenopausal women after disease progression on SERM or AI therapy
14
Q
Fulvestrant: Side Effects
A
Hot flashes, nausea, angioedema, weakness, local site reaction
15
Q
Degarelix: Drug Class
A
Gonadotropin Releasing Hormone Antagonist
16
Q
Degarelix: Mechanism of action
A
LHRH antagonist. Major advantage is immediate down regulation of testosterone; no tumor flare
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
18
Q
Degarelix: Side Effects
A
Hot flashes, injection site reactions
19
Q
Cholestyramine: Drug Class
A
Bile acid resin
20
Q
Bile acid resins: Mechanism of action
A
Bind negatively charged bile acids which bind consumed cholesterol and everything is excreted
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
22
Q
Colestipol: Drug Class
A
Bile acid resin
23
Q
Name the two Bile acid resins
A
Cholestyramine and Colestipol
24
Q
Ezetimibe: Drug Class
A
Transport inhibitor
25
Ezetimibe: Mechanism of action
Blocks absorption of cholesterol in the small intestine
26
Ezetimibe is contraindicated in what patients
Patients with moderate to severe hepatic insufficiency
27
Simvastatin + Ezetimibe: Combination drug with what trade name
Vytorin
28
What advantage does combination therapy like Simvastatin + Ezetimibe (Vytorin) have
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
29
Fluvastatin: Drug Class
HMG Co A Reductase inhibitor
30
HMG Co A Reductase inhibitors: Mechanism of action
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).
31
Lovastatin: Drug Class
HMG Co A Reductase inhibitor
32
Pravastatin: Drug Class
HMG Co A Reductase inhibitor
33
HMG Co A Reductase inhibitors: Mechanism of action
Can cause rhabdomyolysis (rare but may be life threatening), transaminase hepatitis (check liver enzymes)
34
Simvastatin: Drug Class
HMG Co A Reductase inhibitor
35
HMG Co A Reductase inhibitors are contraindicated in what patients
Contraindicated in patients with renal failure and patients taking cyclosporine, macrolide antibiotics, various antifungal agents, and cytochrome P-450 inhibitors
36
Atorvastatin: Drug Class
HMG Co A Reductase inhibitor
37
Rosuvastatin: Drug Class
HMG Co A Reductase inhibitor
38
Name the six statins in order from least to most potent
(For Love People Say Anything Really) Fluvastatin < Lovastatin < Pravastatin < Simvastatin < Atorvastatin < Rosuvastatin
39
Clofibrate: Drug Class
Fibric Acid
40
Name the two Fibric Acids
Clofibrate and Gemfibrozil
41
Fibric Acids: Side Effects
Dyspepsia, gallstones, myopathy (particularly in combination with statins)
42
Gemfibrozil: Drug Class
Fibric Acid
43
Fibric Acids: Mechanism of action
Inhibits fatty acid synthesis, causes lipoprotein lipase-enhanced hydrolysis, stimulates synthesis of apoA-1
44
Niacin: Drug Class
Nicotinic Acid
45
Niacin: Mechanism of action
Inhibits VLDL secretion and increases clearance of VLDL via lipoprotein lipase pathway
46
Niacin: Side Effects
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)
47
What is the most effective agent for increasing HDL
Niacin
48
Niacin is contraindicated in what patients
Contraindicated in patients with peptic ulcer disease
49
Cimetidine (Tagamet): Function and drug class
Control of Gastric Acid, H2 blocker
50
Name the four H2 blockers
Cimetidine, Ranitidine, Famotidine, Nizatidine
51
Which H2 blocker inhibits CYP450 and thus can cause drug-drug interactions
Cimetidine
52
Ranitidine (Zantac): Function and drug class
Control of Gastric Acid, H2 blocker
53
Cimetidine (Tagamet) may increase the secretion of what hormone
Prolactin
54
Famotidine (Pepcid): Function and drug class
Control of Gastric Acid, H2 blocker
55
Nizatidine (Axid): Function and drug class
Control of Gastric Acid, H2 blocker
56
H2 blockers are useful in treating what
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
Omeprazole (Prilosec): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
58
Proton Pump Inhibitors: Mechanism of action
Inhibit the K+/H+ ATPase on parietal cells
59
Proton Pump Inhibitors are superior to H2 blockers in healing of what
NSAID-induced gastric ulcers
60
Lansoprazole (Prevacid): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
61
Name the five proton pump inhibitors
Omeprazole, Lansoprazole, Rabeprazole, Pantoprazole, Esomeprazole
62
Long term use of proton pump inhibitors is associated with
Hip fractures and possibly hypomagnesemia
63
Rabeprazole (Aciphex): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
64
Pantoprazole (Protonix): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
65
Esomeprazole (Nexium): Function and drug class
Control of Gastric Acid, Proton Pump Inhibitor
66
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
Up to 4 weeks
67
Atropine: Function and drug class
Control of Gastric Acid, Antimuscarinic
68
By what mechanism do antimuscarinics affect acid secretion by parietal cells
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
Which two antimuscarinics are used to reduce gastric acid secretion
Atropine and Glycopyrrolate
70
Glycopyrrolate: Function and drug class
Control of Gastric Acid, Antimuscarinic
71
Misoprostol: Function and drug class
Control of Gastric Acid, Cytoprotective
72
Misoprostol is an analogue of what
PGE-1
73
Misoprostol: Mechanism of action
It stimulates PG receptor leading to increased mucous & bicarbonate secretion, and decreases cAMP which decreases HCL secretion
74
Misoprostol is only used to treat what
A NSAID-induced ulcer
75
When is Misoprostol contraindicated
During pregnancy (its an abortifacient)
76
Sucralfate: Function and drug class
Control of Gastric Acid, Cytoprotective
77
Sucralfate: Mechanism of action
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
Metronidazole & Tetracycline: Function and drug class
Ulcer repair, Antibiotic
79
Metronidazole & Tetracycline is administered with what
Bismuth subsalicylate (pepto bismol)
80
What are the two antibiotic regimens for H. Pylori infection
Metronidazole + Tetracycline and Clarithromycin
81
Clarithromycin: Function and drug class
Ulcer repair, Antibiotic
82
Clarithromycin is administered with what
Omeprazole
83
How long are Metronidazole + Tetracycline or Clarithromycin administered for treatment of H. Pylori
14 days
84
Metoclopramide: Function and drug class
Prokinetic Agent, Increase Acetylcholine
85
Metoclopramide: Mechanism of action
It is a cholinomimetic and a D2 receptor blocker. It promotes the release of acetylcholine from myenteric neurons
86
Metoclopramide is used to treat what
GERD and diabetic gastroparisis
87
Cisapride: Function and drug class
Prokinetic Agent, Increase Acetylcholine
88
Cisapride
It promotes the release of acetylcholine from myenteric neurons and acts as a 5-HT4 receptor agonist. Has similar prokinetic effects as metoclopramide
89
How does Cisapride differ from Metoclopramide
It is not a D2 blocker and so does not have antiemetic properties. It also has greater effect on the colon
90
Name the two prokinetic agents
Metoclopramide and Cisapride
91
Diphenoxylate (Lomotil): Function and drug class
Antidiarrheal, Opioid
92
What is Diphenoxylate administered with to discourage deliberate abuse
Sub-therapeutic dose of atropine
93
Loperamide (Imodium): Function and drug class
Antidiarrheal, Opioid
94
Name the two antidiarrheal agents
Diphenoxylate and Loperamide
95
Bismuth subsalicylate (Pepto): Function and drug class
Antidiarrheal, Salicylate
96
Bismuth subsalicylate (Pepto) can cause what syndrome
Reyes Syndrome
97
Thymoglobulin: What drug class [and is it used for induction or maintainance therapy]
Anti-lymphocyte globulin (Rabbit derived) [used as an induction agent]
98
Thymoglobulin: Mechanism of Action
Complement-mediated cell lysis of circulating T-cells
99
Cytokine release syndrome, serum sickness, leukopenia, and thrombocytopenia are the side effects of what drug
Thymoglobulin
100
Basiliximab: What drug class [and is it used for induction or maintainance therapy]
Monoclonal Antibody (against IL-2 receptor) [used as an induction agent]
101
Basiliximab: Mechanism of Action
It binds to the alpha unit of the IL-2 receptor inhibiting binding of IL-2 thereby preventing activation of lymphocytes
102
Abdominal pain, dizziness, and insomnia are the side effects of what drug
Basiliximab
103
Methylprednisolone: What drug class [and is it used for induction or maintainance therapy]
Corticosteroid [used as an induction agent]
104
Methylprednisolone: Mechanism of Action
Blocks cytokine gene expression resulting in a decreased immune response
105
Hypertension, fluid retention, hyperglycemia, impaired wound healing, mood disturbances, and vivid dreams are the side effects of what drug
Methylprednisolone
106
Tacrolimus: What drug class [and is it used for induction or maintainance therapy]
Calcineurin Inhibitor [used as a maintainance agent]
107
Tacrolimus: Mechanism of Action
Inhibits IL-2 synthesis by blocking calcineurin
108
Alopecia, hyperglycemia, hyperkalemia, nephrotoxicity, neurologic toxicity are the side effects of what drug
Tacrolimus
109
Mycophenolate: What drug class and is it used for induction or maintainance therapy
Antimetabolite [used as a maintainance agent]
110
Mycophenolate: Mechanism of Action
Inhibits proliferation of T and B cells by preventing RNA and DNA synthesis
111
GI intolerance, bone marrow suppression are the side effects of what drug
Mycophenolate
112
Sirolimus: What drug class and is it used for induction or maintainance therapy
mTOR Inhibitor [used as a maintainance agent]
113
Sirolimus: Mechanism of Action
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
Anemia, hepatic artery thrombosis, hyperlipidemia, impaired wound healing, proteinuria are the side effects of what drug
Sirolimus
115
Prednisone: What drug class and is it used for induction or maintainance therapy
Corticosteroid [used as a maintainance agent]
116
Prednisone: Mechanism of Action
Blocks cytokine gene expression resulting in a decreased immune response
117
Chronic adrenal insufficiency, GERD, Hyperglycemia, hypertension, and osteoporosis are the side effects of what drug
Prednisone
118
The effectiveness of which Immunosuppression drug(s) is decreased by CYP450 3A4 inducers
Tacrolimus and Sirolimus
119
The effectiveness of which Immunosuppression drug(s) is decreased by aluminum & magnesium containing antacids and by cyclosporine
Mycophenolate
