EXAM #2: REVIEW Flashcards Preview

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Flashcards in EXAM #2: REVIEW Deck (165):
1

What drug is used to prevent the adverse effects of high dose methotrexate?

Leucovorin

2

What are the unique adverse effects associated with Methotrexate?

Nephrotoxicity
Interstitial pneumonitis

3

What enzyme does 5-FU inhibit?

Thymidylate Synthase

4

What are the unique adverse effects associated with 5-FU?

Oral and GI ulcers

5

What is Capecitabine?

Oral 5-FU

6

What is disease is Cytarabine primarily used as a chemotheraputic agent for?

AML

7

What enzyme does Cytarabine require to be activated?

Deoxycytidine Kinase

8

What enzyme inactivates Cytatabine?

Cytidine Deaminase

9

What is the unique syndrome seen with Cytarabine? What are the symptoms?

Cerebellar Syndrome
- Ataxia
- Dysarthria
- Nystagmus

10

What enzyme activates Gemcitabine into its active form?

Deoxycytidine Kinase

11

What enzyme does Gemcitabine specifically inhibit?

Ribonucleotide Reductase

12

What enzyme do 6-Mercaptopurine and 6-Thioguanine require for activation?

HGPRT

13

What enzyme inactivates 6-Mercaptopurine?

Thiopurine Methyltransferase (TPMT)

14

What diseases are 6-MU and 6-TG commonly used to treat?

AML and ALL

15

What disease is Fludarabine used to treat?

CLL

16

What enzyme activates Fludarabine?

Deoxycytidine Kinase

17

What enzymes does Fludarabine specifically inhibit?

Ribonucleotide Reductase
DNA polymerase

*****Also inhibits mRNA translation*****

18

What disease is Cladrabine used to treat?

Hairy Cell Leukemia

19

What enzyme does Cladrabine specifically inhibit?

Ribonucleotide Reductase

20

What is the mechanism of action of Cyclophosphamine?

Nitrogen mustard DNA alkylating agent

21

What is the metabolite of Cyclophosphamine that is particularly harmful? What does it cause?

Acrolein-->Hemmorhagic cystitis

22

What drug is used to prevent Hemorrhagic cystitis in Cyclophosphamine administration?

MENSA

23

What is the mechanism of action of Carmustine? What is it used to treat?

Nitrosurea alkylating agent that is highly lipophilic --> Brain cancer

24

What two enzymes reduce the efficacy of the DNA alkylating agents?

Glutathione
MGMT

25

List the three Platinum compounds. What is their mechanism of action?

Cisplastin
Carbiplatin
Oxiplatin

These drugs are all non-classical DNA alkylating agents

26

What are the unique adverse effects associated with Cisplatin?

Nephrotoxicity
Peripheral Neuropathy
Anaphylaxis

27

How is the neprotoxicity associated with Cisplastin prevented?

Co-administration with IV saline

28

What adverse effect is seen with Carbiplatin?

Anaphylaxis only

29

What is the mechanism of action of Procarbazine? What is it used to treat?

Non-classical alkylating agent used to treat Hodgkins' Disease

30

What is the mechanism of action of Dacarbazine? What is it used to treat?

Non-classical alkylating agent used to treat Melamona and Sarcoma

31

What is the mechanism of action of Temozolamide? What is it used to treat?

Non-classical alkylating agent used to treat Glioblastoma and Melanoma

32

List the Anti-microtubule drugs. What phase of the cell cycle do these agents perturb?

Vinblastine
Vincristine
Paclitaxel
Docetaxel

M-phase

33

Which of the anti-microtubule drugs inhibit microtubule polymerization?

Vinblastine and Vincristine

34

Which of the anti-microtubule drugs inhibit microtubule depolymerization?

Paclitaxel
Docetaxel

35

What is the unique adverse effect seen with Vincristine?

Neurotoxicity

36

What is the unique adverse effect seen with Paclitaxel?

Peripheral Neuropathy
Anaphylaxis
Myelosuppression

37

What drugs are used to prevent the anaphylaxis seen with Paclitaxel?

Diphenhydramine
Dexamethasone

38

What drug is given to counteract the myelosuppression seen with Paclitaxel?

Filgrastim, a G-CSF drug

39

List the Topoisomerase I inhibitors.

Topotecan
Irinotecan

40

List the Topoisomerase II inhibitor.

Etoposide

41

What is the mechanism of action of Doxorubicin?

This is an antibiotic that:
- Topoisomerase II inhibitor
- Intercalates DNA
- Inhibits DNA polymerase

42

What is the unique adverse effect seen with Doxorubicin?

Irreversible cardiomyopathy

43

How is the cardiomyopathy seen with Doxorubicin prevented?

Dexrazoxane

44

What is the mechanism of action of Bleomycin?

Small peptide that cause single and double strand DNA breaks in G2

45

What unique adverse effect is seen with Bleomycin?

Pulmonary toxicity

46

What is the mechanism of action of Tamoxifen?

Estrogen receptor antagonist

*****Treats estrogen receptor positive breast cancer

47

What is the mechanism of action of Anastrazole?

Inhibits aromatase to prevent conversion of Testosterone to estrogen in post-menopausal women with estrogen receptor positive breast cancer

48

What is the mechanism of action of Leuprolide and Goserelin?

These are GnRH AGONISTS used to treat prostate cancer

49

What is the mechanism of action of Degarelix?

GnRH ANTAGONIST used to treat prostate cancer

50

What is the mechanism of action of Trastuzumab?

HER-2 receptor antagonist

51

What is the unique side effect seen with Trastuzumab?

Cardiotoxicity

52

What is the mechanism of action of Cetuximab?

EGFR antagonist used to treat COLON CANCER

53

Activating mutation of what proto-oncogene limits the efficacy of Cetuximab?

Ras

54

What is the mechanism of action of Bevacizumab?

VEGF inhibitor

55

What is the mechanism of action of Lapinotab?

EGFR and HER-2blocker (downstream target) used for REFRACTORY BREAST CANCER

56

What is the mechanism of action of Erlotinib?

EGFR receptor blocker used for NON SMALL CELL LUNG CANCER

57

What is the unique side effect associated with Asparaginase?

Anaphylaxis

58

What is the mechanism of action of Bortezomib?

Proteasome inhibitor that increases p53

59

What is the unique adverse effect associated with Bortezomib?

Peripheral neuropathy

60

What is the mechanism of action of Temsirolimus?

mTOR1 inhibitor

61

What are the unique adverse effects seen with Temsirolimus?

Hyperglycemia
Triglyceridemia

62

Which antineoplastic agents are nephrotoxic?

Cisplastin
Methotrexate

63

Which antineoplastic agents are neurotoxic?

Vincristine
Cytarabine
Cisplastin
Bortezomib
Paclitaxel

64

Which antineoplastic agents are cardiotoxic?

Doxorubicin
Trastuzumab

65

Which antineoplastic agents cause bladder toxicity?

Cyclophosmphamide

66

Which antineoplastic agents cause hypersensitivity reactions/ anaphylaxis?

Asparaginase
Paclitaxel

67

List the ADP receptor antagonists/ P2Y12 antagonists.

Clopidegril
Prasugrel
Ticagrelor
Cangrelor

68

Which ADP receptor antagonists are irreversible?

Clopidegril
Prasugel

69

Which ADP receptor antagonists are reversible?

Ticagrelor
Cangrelor

70

Which ADP receptor antagonists have been shown to be more efficacious? What is their drawback?

Prasugrel
Ticagrelor

****Despite being more efficacious, also associated with more bleeding****

71

What CYP enzyme metabolizes Clopidegril?

CY2C19

72

What is the clinical significance of CYP2C19?

- Highly polymorphic
- Inhibited by omeprazole i.e. omeprazole increases the efficacy of Clopidegril

73

List the GPIIb/IIIa antagonists. Which of these are a Fab antibody, peptide, and non-peptide small molecule?

Abciximab - Fab antibody
Integrelin
Eptifabitide- peptide
Tirofiban- non-peptide small molecule
Lamifiban

74

What are the adverse effects seen with GPIIb/IIIa administration?

Thrombocytopenia
Bleeding

75

What is the mechanism of action of Voraxapar?

PARR antagonist

76

What is the adverse effect associated with Voraxapar?

Intracranial bleeding

****Note that this drug is contraindicated in patients with a history of intracranial bleeding

77

What is dual anti-platelet therapy? Triple?

Dual= ASA and clopidegril
Triple= + Warfarin

78

List the indirect thrombin/ Factor X inhibitors. What is the difference between these three drugs?

Heparin
Enoxaparin - LMWH
Fondapainaux - Pentasaccharide

79

What are the adverse effects associated with Heparin?

Bleeding
Osteoporosis
HIT

80

What drug reverses Heparin?

Protamine

81

List the direct thrombin inhibitors.

Lepirudin
Bivalrudin
Argatraban
Dabigatran (oral)

82

Which of the direct thrombin inhibitors is divalent? What does this mean?

"rudins" --> block the active site and E1 site on Thrombin

83

Which of the direct thrombin inhibitors is monovalent? What does this mean?

"an's" -->block only the active site

84

List the direct Factor Xa inhibitors.

Rivaroxaban
Apixaban

85

What enzyme metabolizes Warfarin?

CYP2C9

86

List the fibrinolytic drugs.

Streptokinase
Alteplase
Reteplase
Tenectaplase

(t-PA)

87

What are the unique adverse effects seen with Streptokinase administration?

Tolerance
Hypersensitivity reaction

88

What drugs can reverse fibrinolytic therapy?

Aminocaproic acid
Tranexamic acid

89

Draw the general pathway of cholesterol metabolism.

N/A

90

What drug blocks NPC1L1?

Ezetimibe

91

What is the function of Apo C-II?

Activation of LPL

92

What is the transporter that get cholesterol from the periphery into HDL?

ABAC1

93

What disorder is characterized by decreased LPL expression or function?

Primary Chylomicronemia

94

What is the manifestation of Primary Chylomicronemia?

Increased chylomicrons and VLDL

95

Which drugs are best at treating Primary Chylomicronemia?

Fibrates and Niacin

96

What disease is characterized by decreased Apo E function of expression?

Dysbetalipoproteinemia

97

What is the manifestation of Dysbetalipoproteinemia?

Increased IDL and chylomicron remnants

98

What is the best therapy for Dysbetalipoproteinemia?

Fibrates and Niacin

99

What disease is characterized by decreased apo C-II function or expression?

Familial Hypertriglyceridemia

100

What is the manifestation of Familial Hypertriglyceridemia ?

Increased Chylomicrons and VLDL

101

What is the best therapy for Familial Hypertriglyceridemia ?

Fibrates and Niacin

102

What disease is characterized by decreased LDLR function or expression?

Familial Hypercholesterolemia

103

What is the manifestation of Familial Hypercholesterolemia?

Increased LDL

104

What is the best therapy for Familial Hypercholesterolemia?

Statins
Ezetimibe
Bile acid binding resins
Niacin

105

What is the effect of decreased Apo-B 100 function of expression?

Increased LDL

106

What is the best treatment for an ApoB-100 defect?

Statins
Ezetimibe
Bile acid binding resins
Niacin

107

List the Fibrates.

Gemfibrozil
Fenofibrate

108

What is the mechanism of action of the Fibrates?

PPAR activation

109

List the bile acid binding resins.

Cholestyramine
Cholesevelam
Colestipol

110

What is the mechanism of action of Niacin?

Inhibition of adipocyte hormone sensitive lipase

111

List the statins.

Atorvastatin
Rouvastatin
Lovastatin
Pitastatin
Simvastatin
Flouvastatin

112

What are the indications for Quinidine?

Refractory:
- A-fib/flutter
- Life threatening ventricular arrhythmia

113

What are the indications for Procainamide?

1) Re-entry SVT
2) A-fib
3) A-flutter with WPW
4) Life threatening ventricular arrhythmia

114

What are the indications for Lidocaine?

- Post MI arrhythmia
- Digitalis induced arrhythmia

115

What are the indications for Propafenone?

1) PSVT
2) Atrial arrhythmia
3) Ventricular arrhythmia in patients WITHOUT heart disease

116

What are the indications for Amiodarone?

1) Acute conversion of VT or VF
2) A-fib
3) AVNRT
4) WPW

117

What are the indications for Verapamil?

1) SVT
2) A-fib with RVR
3) Angina
4) HTN

118

What are the contraindications to Verapamil?

- Conduction block
- WPW + a-fib
- Ventricular Tachycardia

119

What are the adverse effects seen with Adenosine administration?

1) Bradycardia/ heart block
2) Flushing
3) Dyspnea
4) Hypotension (A2 mediated vasodilation)

120

What are the indications for Acetazolamide?

1) Glaucoma
2) Acute Mountain Sickness
3) Urinary Alkalization
4) Edema

121

What are the adverse effects of Acetazolamide?

- Hyperchloremic metabolic acidosis
- Renal stones
- Renal K+ loss

122

What are the contraindications for Acetazolamide?

Cirrhosis

123

What are the indications for osmotic diuretics?

1) Prophylaxis for acute renal failure
2) Cerebral edema
3) Dialysis disequilibrium
4) Acute glaucoma

124

What are the adverse effects of osmotic diuretics?

- Pulmonary edema
- Hypo/hypernatremia

125

List the loop diuretics.

Furosemide
Bumetanide
Ethacrynic acid

126

What are the indications for loop diuretics?

1) Pulmonary edema
2) CHF
3) Acute renal failure
4) Hyperglycemia

127

What are the adverse effects of the loop diuretics?

- Hypokalemia, natremia, calcemia, magnesia
- Ototoxicity
- Hyperuricemia

128

List the Thiazide diuretics?

Chlorathalidone
Hydrochlorothiazide
Metalazone
Indapamide

129

What is unique about the Thiazide diuretics in terms of ion secretion/ absorption?

Stimulation of PTH causes Ca++ REABSORPTION

130

What are the indications for Thiazide diuretics?

HTN
CHF
Hypercalciuria/ renal stones
Nephrogenic DM Insipidus

131

List the K+ sparing diuretics.

Amiloride
Triamtrene

132

What is the MOA of K+ diuretics?

Block epithelial Na+ channels on principal cells; thus, K+ is NOT secreted

133

What are the indications for the K+ diuretics?

- Hypokalemic alkalosis
- Combination therapy to prevent hypokalemia

134

List the Aldosterone antagonists.

Spironolactone
Eplerenone

135

What are the indications for Aldosterone antagonists?

1) Edema
2) CHF
3) HTN
4) Primary or secondary hyperaldosteronism

136

What are the adverse effects of the aldosterone antagonists?

- Hyperkalemia
- Metabolic acidosis in cirrhosis
- Hormonal effects (gynecomastia, impotence...etc.)

137

What are the contraindications for ACE inhibitors?

1) Pregnancy
2) Bilateral renal artery stenosis
3) Angioedema

138

Under what circumstances will ACE inhibitors have an increase in favorable effects?

- Low K+ or hypokalemia
- Pre-DM
- Albuminuria

139

Under what circumstances will ACE inhibitors have an unfavorable effects?

- High K+ or hyperkalemia
- Volume depletion

140

What are the adverse effects of ACE inhibitors?

C= cough
A= angioedema
P= potassium (increased)
T= taste change
O= hypOtension
P= pregnancy--> fetopathic
R= rash
i
l

141

List the ACE inhibitors.

Lisinpril
Captopril
Fosinopril

142

What are the contraindications for ARB therapy?

Pregnancy
Bilateral renal artery stenosis

143

List the ARBs.

Losartan
Valsartan
Candesartan

144

What is the role of DHP Ca++ blockers in HTN?

1) First line or add on therapy for uncomplicated
2) Add on therapy for DM and CAD

145

When should DHP Ca++ blockers be avoided?

LV dysfunction

146

List the DHP Ca++ blockers used in anti-HTN therapy.

Nifedipine
Amlodipine
Felodipine

147

Under what circumstances can DHP Ca++ therapy have increased favorable effects?

1) Reynaud Syndrome
2) Elderly patient with isolated systolic HTN
3) Cyclosporine induced HTN

148

Under what circumstances can DHP Ca++ therapy unfavorable effects?

- Peripheral edema
- Tachycardia

149

What is the role of NDPH Ca++ blockers in HTN?

1) First line or add on for uncomplicated HTN
2) Add on for DM
3) Alternative to Beta-blockers in CAD

****These drugs will DECREASE myocardial oxygen consumption*****

150

When should NDHP Ca++ blockers be avoided?

- AV block
- LV dysfunction

151

Under what circumstances can NDHP Ca++ therapy have increased favorable effects?

1) Reynaud Syndrome
2) Migraine
3) Arrhythmia
4) Tachycardia

152

Under what circumstances can NDHP Ca++ therapy unfavorable effects?

- Peripheral edema
- Bradycardia
- AV block

153

When are Thiazide diuretics first-line therapy in HTN?

1) LV dysfunction
2) S/p CVA

154

When should Thiazide diuretics be avoided?

1) Allergy to Sulfa
2) Gout
3) Hyponatremia
4) Hypokalemia
5) Pre-DM/ elevated fasting glucose

155

What comorbid conditions should Thiazide diuretics be used in, if a patient has HTN?

- Osteoporosis b/c of increased Ca++ reabsorption
- Hyperkalemia b/c of K+ excretion

156

When are Beta blockers first line therapy for patients with HTN?

CAD and LV dysfunction

157

Are aldosterone antagonists first line therapy or add on therapy?

Add on therapy

158

What situations should aldosterone antagonists be used as add on therapy?

Resistant HTN
CAD
LV Dysfunction

159

In addition to their normal use, when is aldosterone antagonist therapy beneficial?

Hypokalemia
CKD

160

What is the role of alpha-1 antagonists in HTN therapy?

- Used in conjunction w/ diuretics
- Lower cholesterol and trigylcerides

161

List the central alpha 2 agonists.

Clonidine
A-methyldopa

162

What adverse effects are seen with alpha-methyldopa?

1) Hepatotoxicity
2) Positive direct coombs test

163

What is the mechanism of action of Hydralazine?

- Arterial vasodilation by blocking IP3 induced Ca++ release
- Opens K+ channels to hyperpolarize vascular smooth muscle

164

What is the role of Hydralazine in HTN therapy?

- Add on for resistant HTN esp. in CKD
- SAFE in pregnancy

165

What enzyme activates organic nitrates?

Mitochondiral aldehyde reductase

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