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Pharmacology > EXAM #2: REVIEW > Flashcards

EXAM #2: REVIEW Flashcards

1
Q

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

A

Leucovorin

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2
Q

What are the unique adverse effects associated with Methotrexate?

A

Nephrotoxicity

Interstitial pneumonitis

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3
Q

What enzyme does 5-FU inhibit?

A

Thymidylate Synthase

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4
Q

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

A

Oral and GI ulcers

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5
Q

What is Capecitabine?

A

Oral 5-FU

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6
Q

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

A

AML

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7
Q

What enzyme does Cytarabine require to be activated?

A

Deoxycytidine Kinase

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8
Q

What enzyme inactivates Cytatabine?

A

Cytidine Deaminase

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9
Q

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

A

Cerebellar Syndrome

  • Ataxia
  • Dysarthria
  • Nystagmus
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10
Q

What enzyme activates Gemcitabine into its active form?

A

Deoxycytidine Kinase

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11
Q

What enzyme does Gemcitabine specifically inhibit?

A

Ribonucleotide Reductase

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12
Q

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

A

HGPRT

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13
Q

What enzyme inactivates 6-Mercaptopurine?

A

Thiopurine Methyltransferase (TPMT)

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14
Q

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

A

AML and ALL

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15
Q

What disease is Fludarabine used to treat?

A

CLL

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16
Q

What enzyme activates Fludarabine?

A

Deoxycytidine Kinase

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17
Q

What enzymes does Fludarabine specifically inhibit?

A

Ribonucleotide Reductase
DNA polymerase

Also inhibits mRNA translation

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18
Q

What disease is Cladrabine used to treat?

A

Hairy Cell Leukemia

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19
Q

What enzyme does Cladrabine specifically inhibit?

A

Ribonucleotide Reductase

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20
Q

What is the mechanism of action of Cyclophosphamine?

A

Nitrogen mustard DNA alkylating agent

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21
Q

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

A

Acrolein–>Hemmorhagic cystitis

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22
Q

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

A

MENSA

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23
Q

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

A

Nitrosurea alkylating agent that is highly lipophilic –> Brain cancer

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24
Q

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

A

Glutathione

MGMT

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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

Pharmacology (64 decks)

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