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Med Chem Cardio > Test 3: Antithrombotic/Antianginal > Flashcards

Test 3: Antithrombotic/Antianginal Flashcards

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1
Q

Which of the following drugs are Anticoagulants?

A. Warfarin

B. UFH (unfractionated heparin)

C. Aspirin

D. Alteplase

E. Rivaroxaban

F. Dabigatran

A

A, B, E, F

C is an antiplatlet medication

D is a fibrinolytic

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2
Q

Antiplatelet medications are medications that inhibit which of the follwing?

A. PGY12 receptors

B. Factor Xa

C. Factor IIa

D. TxA2 synthesis

E. GPIIb/IIIa

F. PDE3

A

A,D,E,F

Any medication that affects PGY12 receptors, TxA2, GPIIb/IIIa and PDE3 will affect the activation of platelets and are thus known as antiplatelet medications.

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3
Q

Warfarin is knonw as a derivative of ______

A. Pyrimidne

B. Coumarin

C. Vitamin K

D. Cyclopentanetriazolopyrimidne

A

B

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4
Q

In Warfarin’s structure what does the star signify? (Select all that apply)

A. Chiral Carbon that can have R and S isomer

B. Chiral Carbon that can have a potent R isomer and a less potent S isomer.

C. Non-Chiral carbon that can have a potent S isomer and less potent R isomer

D. Chiral Carbon that can have a potent S isomer and a less potent R isomer.

A

A, D

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5
Q

Which group gives warfarin it’s acidic functionality?

A. Red- Ketone

B. Blue- Phenyl

C. Green- Enol

D. Purple- Ester linkage

A

C

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6
Q

In order to make Warfarin more soluble it is being made into a _____ by adding a(n) ______

A. Salt, Acid HCl

B. Salt, Base KOH

C. Salt, Acid H2SO4

D. Salt, Base NaOH

A

D

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7
Q

In what form does Vitamin K exist in the body?

A. Oxidized form (Quinone)

B. Epoxide form

C. Reduced form (Hydorquinone)

D. VKORC

A

C

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8
Q

The enzyme ______ is needed to convert the epoxide form of vitamin k to the ______ form.

A. Vitamin K 2,3-Quinone Reductase, Oxidized

B. Vitamin K 2,3-Epoxide Reductase, Reduced

C. Vitamin K 2,3 Epoxide Reductase, Oxidized

D. Vitamin K 2,3 Quinone Reductase, Reduced

A

C

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9
Q

The enzyme _______ is needed to convert the Oxidized form of vitamin K to the Reduced form.

A. Vitamin 2,3 Epoxide Reductase

B. Vitamin 2,3 Quinone Reductase

C. Vitamin K Dependent Carboxylase

D. Warfarin

A

B

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10
Q

What drug is blocking the actions of these two enzymes?

A. Warfarin

B. Heparin

C. Dabigatran

D. Enoxaparin

A

A

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11
Q

Warfarin will block the synthesis of which factors? (select all)

A. VIII

B. VII

C. II

D. IIa

E. IX

F. X

A

B, C, E, F

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12
Q

What is gene that codes for Vitamin K 2,3 Epoxide Reductase?

A. MAO

B. VKORC1

C. mtALDH

D. BCPR

A

B

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13
Q

What is the antidote given in Warfarin Overdoses?

A Protamine Sulfate

B. NAC

C. Vitamin K

D. Rifampin

A

C

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14
Q

What is the Major metabolite of Warfarin?

A. CYP1A2

B. CYP3A4

C. CYP 3A5

D. CYP2C9

E. CYP2C19

A

D

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15
Q

The drug ____ will increase warfarin serum concentration by acting as an _____ of the enzyme ______

A. Rifampin, inhibitor, CYP2C9

B. Rifampin, inducer, CYP2C9

C. Amiodarone, Inhibitor, CYP2C9

D. Amiodarone, Inducer, CYP2C9

A

C

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16
Q

The drug _____ will decrease serum concentrations of warfarin by acting as an _____ of the enzyme _____

A. Rifampin, Inducer, CYP2C9

B. Rifampin, Inhibitor, CYP2C9

C. Amiodarone, Inhibitor, CYP2C9

D. Amiodarone, Inducer, CYP2C9

A

A

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17
Q

What is the t1/2 of Warfarin?

A. 1.5 hours

B. 4 hours

C. 20-60 hours

D. 17 hours

A

C

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18
Q

What is the enzyme responsible for creating the Major metabolites you see here?

A. CYP2C9

B. CYP2C19

C, Reductase

D. CYP3A4

A

A

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19
Q

What enzyme is responsible for the Minor metabolite shown in this path?

A. CYP2C19

B. Reductase

C. CYP2C9

D. Esterase

A

B

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20
Q

What are the names of the two Major inactive metabolites created in this pathway?

A. 6-Hydroxywarfarin, 7-Hydroxywarfarin

B. 6-Dihydroxywarfarin, 7-Dihydroxywarfarin

C. 6-Methoxywarfarin, 7-Methoxywarfarin

A

A

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21
Q

What is created in the minor metabolite of wafrarin?

A. Tertiary Alcohol

B. Secondary Alcohol

C. Primary Alcohol

D. Quarternary Alcohol

A

B

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22
Q

Heparin is a derivative of:

A. Pyrimidine

B. Glycosaminoglycan

C. Nucleotides

D. Adenosine

A

B

Because heparin contains many carbohydrates

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23
Q

Due to the many carboxylate and sulfate groups in heparin it has: (Select All)

A High positive charge density

B. Potential for Covalent bonding

C. Potential for Ionic bonding

D. High negative charge density

A

C, D

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24
Q

Heparin can form ____bonds to the ____ and ____ amino acid side chains of _____

A. Covalent, Arginine, Lysine, thrombin

B. Ionic, Arginine, Cystine, Antithrombin

C. Covalent, Arginine, Lysine, Antithrombin

D. Ionic, Arginine, Lysine, Antithrombin

E. Ionic, Arginine , Lysine, Thrombin

A

D

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25
Q

Why is heparin not given orally?

A

It is very unstable in acidic environments and can be broken down easily by enzymes since it is a large polysaccharide

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26
Q

Which of the following statements is true about Heparin (UFH)? (select all)

A. Acts as a direct inactivator to factors Xa and IIa

B. Acts as an indirect inactivator to factors Xa and IIa

C. Acts as an Allosteric agonist to Antithrombin

D. Has a half-life of 20-60 hours

E. Has a half-life of 1.5 hours

F. Acts as a catalyst in the binding of antithrombin to factors Xa and IIa

A

B,C,E,

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27
Q

What is the antidote given with overdoses of Heparin?

A. Protamine Sulfate

B. Vitamin K

C. Rifampin

D. NAC

A

A

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28
Q

When comparing Heparin (UFH) to Enoxaparin, Enoxaparin has: (Select All)

A. Less binding affinity for IIa than UFH

B. More binding affinity for Xa than IIa

C. Binds only to IIa

D. t1/2 elimination of 4 hours

E. Better absorption of 90% and lower toxicity

F. Uniform structure

A

A, B, D, E, F

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29
Q

When comparing Enoxaparin to Fondaparinux, Fondaparinux: (select all)

A. A synthetic consistant dosage form

B. Specific only to factor IIa

C. Has a half-life of 17 hours and better pharmacokinetics

D. Has a 5-carbohydrate sequence and specific molecular weight

E. Has a shorter half-life than enoxaparin

A

A, C, D

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30
Q

Which of these is the correct selectivity order for Factor Xa?

A. Fondaparinux > LMWHs > UFH

B. UFH > LMWH > Fondaparinux

C. LMWH > Fondaparinux > UFH

D. Fondaparinux > UFH > LMWH

A

A

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31
Q

What is the name of the circled structure in Rivaroxaban?

A. Morpholine

B. Pyrimadine

C, Furan

D. Oxazolidinone

A

D

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32
Q

In comparison to Warfarin, Rivaroxiban:

A. Has a shorter Elimination half-life

B. A coumarin core

C. Metabolized by CYP3A4/5

D. Does not need to be monitored like Warfarin does.

E. Does not need INR checked

A

A, C, D, E

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33
Q

What kind of metabolism can Rivaroxaban undergo?

A. Amid hydrolysis

B. Hydrolysis at the Oxazolidinone core

C. Reduction at the morpholine group on the left.

D. A & B

A

D

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34
Q

Which of the following are Direct Factor Xa inhibitors?

A.Enoxaparin

B. Apixaban

C. UFH

D. Warfarin

E. Edoxaban

F. Rivaroxaban

A

B,E,F

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35
Q

All of the following are Direct Thrombin inhibitors EXCEPT:

A. Dabigatran Etexilate

B. Lepirudin

C. Apixaban

D. Desirudin

E. Bivalirudin

F. Argatroban

A

C

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36
Q

Which of these direct thrombin inhibitors is a prodrug?

A. Bivalirudin

B. Desirudin

C. Dabigatran Etexilate

D. Lepirudin

E. Argatroban

A

C

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37
Q

Which portions of Dabigatran can undergo Ester hydrolysis? (select all)

A. Green

B. Red

C. Purple

D. Orange

A

B, D

38
Q

What kind of enzyme is needed to convert dabigatran into it’s active metabolite?

A. Redutase

B. Esterase

C. MAO

D. GLUT

A

B

39
Q

What does the circled portion of Dabigatran resemble?

A. Quarternary amine (Needed for activity)

B. Tertiary amine (Needed for activity)

C. Guanidine (Needed for activity)

D. Amide (Needed for activity)

A

C

40
Q

What kind of metabolism can this circled group undergo?

A. Sulfation

B. Glucuronidation (Inactive metabolite)

C. Glucuronidation (Active metabolite)

D. Carboxylation

A

C

41
Q

Lepirudin and Desirudin are derivatives of:

A. Recombinant Hirudin

B. Guanadine

C. Cyclopentyltriazolpyrimiadines

D. Adenosine

A

A

42
Q

Which of the following is true? (Select all)

A. Lepirudin is given Orally

B. Lepirudin is given IV

C. Dsirudin is given SC

D. Bivalrudin is given Orally

E. Bivalrudin is given IV

A

B, C, E

43
Q

What functional group in Argatroban is circled? What amino acid does it come from?

A. Tertiary amine, Arginine

B. Urea, Asparagine

C. Guanadine, Asparagine

D. Guanadine, Arginine

A

D

44
Q

Which of these Direct IIa inhibitors is taken orally?

A. Dabigatran Etexilate

B. Lepirudin

C. Bivalirudin

D. Desirudin

E. Argatroban

A

A

45
Q

Which of the following statements is true about Argatroban?

A. Synthetic molecule

B. Metabolized by CYP3A4

C. Metabolized by CYP2C9

D. S-Isomer more potent than R isomer

E. Given Parenterally

A

A, B, D, E

46
Q

Which of the follwing classes of drugs are antiplatlet agents?

A. COX-1 Inhibitors

B. PDE3 inhibitors

C. Factor Xa inhibitors

D. Direct thrombin inhibitors

E. P2Y12 receptor antagoinits

F. Glycoprotine IIB/IIIa receptor antagonists

A

A, B, E, F

47
Q

What is the major cyclooxygenase (COX-1) product needed for platelets to aggregate?

A. TxA2

B. ADP

C. Fibrinogen

D. ADH

A

A

48
Q

Aspirin will form a(n)______ bond with the ______ amino acid on the COX1 enzyme in order to prevent ______ from being formed.

A. Ionic, Serine, TxA2

B. Covalent, Serine, TxA2

C. Ionic, Lysine, TxA2

D. Covalent, Lysine, TxA2

A

B

49
Q

T/F TxA2 stimulates platelet aggregation

A

T

50
Q

What major COX-1 product does Aspirin reduce?

A. ADP

B. ADH

C. TxA2

D. Thrombin

A

C

51
Q

Which of the following statements is true regarding Aspirin? (Select All)

A. Rapid oral absorption

B. Lasts for the life of the platelet (7-10 days)

C. Reversible Antagonist

D. Hydrolyzed to salicylate for elimination

E. Causes gastric bleeding

F. Low oral bioavailability

A

A, B, D, E

52
Q

Which of the following drugs is a PDE-3 inhibitor?

A. Rivaroxaban

B. Apixaban

C. Enoxaparin

D. Dipyridamole

A

D

53
Q

What kind of hepatic metabolism can the circled groups undergo in Dipyridamole?

A. Hydroxylation

B. Glucuronidation

C. Reduction

D. Hydrolysis

A

B

54
Q

Which of the following statments is true regarding Dipyridamole? (select all)

A. Increases Intracellular cAMP by inducing PDE3

B. Decreases Intracelular cAMP by inhibiting PDE3

C. Can undergo glucuronidation

D. It is a PgP inhibitor

E. Increases Intracellular cAMP by inhibiting PDE3

A

C,D,E

55
Q

Which of the following drugs are irreversible P2Y12 antagonists?

A. Ticagrelor

B. Clopidogrel

C. Cangrelor

D. Ticlopidine

E. Prasugrel

A

B,D,E

56
Q

Which of the following drugs are Antiplatelet medications?

A. Aspirin

B. Rivaroxaban

C. Enoxaparin

D. Clopidogrel

E. Abcixmab

F. Dipyridamole

A

A, D, E, F

57
Q

Which of the following P2Y12 inhibitors are Prodrugs?

A. Cangrelor

B. Prasugrel

C. Ticagrelor

D. Ticlopidine

E. Clopidogrel

A

B, D, E

58
Q

What is the name of the structure circled in Ticlopidine?

A. Pyrimidine

B. Thienopyridine

C. Thiophene

D. Furan

A

B

59
Q

Which of the following statements is true about Ticlopidine?

A. It is an irreversible antagonist

B. It is a reversible antagonist

C. It is a thienopyridine derivative

D. It is a prodrug

E. It is active when administered

A

A, C, D

60
Q
A
61
Q

In comparison to Ticlopidine Clopidogrel is:

A. More Potent and less toxic

B. Can undergo hydrolyis by esterases

C, Is primarily metabolized by CYP2C19

D. All of the above

A

D

62
Q

What is true about the FGs circled in the drug clopidogrel? (select all)

A. Ester circled in red can undergo ester hydrolysis to form the active metabolite

B. Ester circled in red can undergo ester hydrolysis to form an inactive metabolite

C. Thiophene group circled in blue can undergo CYP2C19 metabolism to form an inactive metabolite

D Thiophene group circled in blue can undergo CYP2C19 metabolism to form an active metabolite

A

B, D

63
Q

What is the primary enzyme is responsible for the major active thiol metabolite formed by clopidogrel?

A. CYP2C9

B. CYP2C19

C. CYP3A4

D. CYP3A5

A

B

64
Q

The amino acid _____ of the P2Y12 receptor forms a _____ disulfide bond with the Active Thiol Metabolite of clopidogrel.

A. Arginine, Covalent

B. Asparginine, Ionic

C. Cysteine, Ionic

D. Cysteine, Disulfide

A

D

65
Q

The _____ enzymes are responsible for forming the _____ form of the clopidogrel metabolite.

A. CYP2C19, Inactive

B. CYP2C9, Active

C. Esterase, Inactive

D. Esterase, Active

A

C

66
Q

Based on the image shown you can infer that: (Select All)

A. Giving a CYP2C19 inhibitor will decrease the amount of active drug in the body

B. GIving a CYP2C19 inducer will increase the amount of active drug in the body.

C. Giving an esterase inhibitor will increase the amount of inactive drug in the body

D. Giving a CYP2C19 inhibitor will make clopidogrel more active

A

A,B,D

67
Q

Which of the following drugs are CYP2C19 inhibitors and can decrease the effectiveness of clopidogrel?

A. Azole antifungals (ketoconazole)

B. SSRI (fluvoxamine)

C. PPI (Esomeprazole)

D. All of the above

A

D

68
Q

The ____ enzymes are responsible for converting the _____ group to the _____ group in the inactive metabolite of Prasugrel

A. Esterase, Ester, Thiolactone

B. CYP2C19, Ester, Lactam

C. CYP2C19, Carboxylic, Thiolactone

D. Esterase, Carboxylic, Thiolactone

A

A

69
Q

What is the name of the inactive metabolite circled here?

A. Thiol intermediate

B. 2-oxo intermediate

C. Sterified intermediate

D. Reduced intermediate

A

B

70
Q

Based on the structure and the natural substrate for P2Y12 receptors what is cangrelor an analog of?

A. Cysteine

B. Guanidine

C. Adenosine

D. Thymine

A

C

it resembles ADP (adenosine diphosphate) which is the natural substrate for P2Y12 receptors.

71
Q

What is true about the drug cangrelor? (Select All)

A. This is a Prodrug

B. Irreversibly binds to P2Y12 receptors

C. Reversibly binds to P2Y12 receptors

D. Not a Prodrug

E. Competitive antagonist to the P2Y12 receptor

A

C, D, E

72
Q

Based on the structure of Ticagrelor which of the statements is true?

A. Not a Prodrug

B. Red and blue structures resemble an adenosine derivative

C. Red and blue structures resemble a cyclopentyltriazolopyrimidine derivative

D. Non-competitively binds to P2Y12 receptors

E. Binds to a different site on the P2Y12 receptor

A

A,C,D,E

73
Q

In comparison to other P2Y12 inhibitors, Ticagrelor:

A. Competitively binds to the P2Y12 receptor

B. Binds to a different site than thienopyridine derivatives (Clopidogrel, Ticlopidine, Prasugrel)

C. Is a prodrug

D. Binds irreversibly to P2Y12 receptors

A

B

74
Q

Which of the following drugs are GPIIb/IIIa antagonists?

A. Abciximab (ReoPro)

B. Ticagrelor (Brilinta)

C. Eptifibatide (Integrelin)

D. Enoxaparin (Lovenox)

E. Tirofiban (Aggrastat)

A

A,C,E

75
Q

Abciximab is derived from __A__

Eptifibatide is derived from __B__

Tirofiban is derived from __C__

A. A=Monoclonal antibodies, B=Non-peptide, C=Cyclic peptide

B. A=Monoclonal antibodies, B=Cyclic peptide, C, Non peptide

C. A= Cyclic Peptide, B= Non peptide, C= Monoclonal antibodies

A

B

76
Q

Which of the following drugs are Fibrinolytics?

A Streptokinase

B. Urokinase

C. Alteplase

D. Enoxaparin

E. Reteplase

A

A,B,C,E

77
Q

Streptokinase is derived from:

A. Viral DNA

B. Beta-hemolytic streptococci

C. Fungi

D. Kidney cells

A

B

78
Q

What does Streptokinase and Urokinase have in common?

A. Both are derived from streptococci

B. Both are Fibrin-specific

C. Both are Fibrin-nonspecific

D. Both are not assosciated with allergic reactions

A

C

79
Q

What are the differences between Streptokinase and Urokinase? (Select All)

A. Streptokinase is derived from beta-hemolytic streptococci

B. Urokinase is derived from fetal-kidney cells

C. Streptokinase can cause allergic reactions.

D. Urokinase does not have antigenicity

E. All of the above

A

E

80
Q

Which of these fibrinolytics are fibrin-specific? (Select All)

A. Alteplase

B. Streptokinase

C. Urokinase

D. Reteplase

E. Tenecteplase

A

A, D, E

81
Q

What is Alteplase, Reteplase and Tenecteplase derived from?

A. Nucleotides

B. Recombinant modified tPA

C. Bacteria

D. Viral DNA

A

B

82
Q

When managing acute anginal attacks ____ nigroglycerin is preferred

A. Sublingual

B. Oral

C. Ointment

D. Patch

A

A

83
Q

What is the duration of SL NTG?

A. 3-6 hours

B. 30-60 minutes

C. 3-5 minutes

D. 2-8 hours

A

B

84
Q

What is the duration of Oral NTG?

A. 30-60 min

B. 2-8 hours

C. 3-6 hours

D. 3-5 minutes

A

C

85
Q

Based on the structure of nigroglycerin, it closely resembles:

A. Fatty Acids

B. Triglycerides

C. Urea

D. Glycerol

A

D.

This is the structure of glycerol

86
Q

Based on the reaction seen here what is the major enzyme needed to release a free NO2 from Nitroglycerin?

A. Esterase

B. Carboxylase

C. mtALDH

D. NAT

A

C

87
Q

Based on the structure of these two nitrates it can be safely assumed that: (Select All)

A. Red is Isosorbide mononitrate

B. Red is Isosorbide dinitrate

C. Blue is Isosorbide mononitrate

D. Blue is Isosorbide dinitrate

A

B,C

88
Q

What class of drugs should not be given with Nitrates?

A. PDE5 inhibitors

B. Long Acting NTG

C. Beta Blockers

D. ACE-I

A

A

If given with this you will have increased levels of cGMP and further vasodilation.

89
Q

What kind of metabolism can be seen in these two groups?

A. O-Hydroxylation

B. O-Alkylation

C. N-Dealkylation

D. Reduction

A

B

90
Q

The following groups can undergo:

A. N-Dealkylation

B. Amide hydrolysis

C. Hydroxylation

D. Reduction

A

A

91
Q

The amide group in Ranolazine can undergo:

A. Reduction

B. Ester (amide) Hydrolysis

C. N-Demethylation

D. Oxidation

A

B

There are other groups on the drug that can undergo Acyl glucuronidation.

92
Q
A

Med Chem Cardio (4 decks)

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