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Pharmacology & Drugs > Cardio-Thromboembolitic > Flashcards

Cardio-Thromboembolitic Flashcards

1
Q

What is the mechanism of action of thrombolytic drugs

A

Aka fibrinolytic drugs
-Activates the endogenous fibrinolytic system, resulting in the converting of plasminogen to plasmin and the breaking up of clots

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2
Q

What are the agents used in prosthetic heart valves

A

Diphyridamole with warfarin

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3
Q

What class of drug is dabigatran

A

Oral Direct thrombin inhibitor

*Oral Anticoagulants

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4
Q

What is the mechanism of action of the ADP receptor antiplatelet drugs

A

1-Blockers of ADP receptors results in continues AC activation
2- AC results in cAMP levels to remain high
3- High cAMP results in lack of platelet aggregation

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5
Q

What can be given to patients with heparin-induced thrombocytopenia (HIT) to reverse the effects of the heparin

A

Protamine sulfate

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6
Q

What are the pharmokenetics of Clopidogrel

A

-High variability as metabolized by CYP2C19 (some nonfunctional alleles in Asians,African Americans)

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7
Q

Which direct thrombin inhibitor can cause anaphylactic reactions

A

Lepirudin

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8
Q

What is the state of usage of the inhibitors of phosphodiesterase inhibitors as antiplatelet drugs

A

Used in conjunction with other agents

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9
Q

What is the mechanism of action for warfarin

A

Inhibits the reactivation of vitamin K by inhibiting the Vitamin K epoxide reductase (inhibits carboxylation of glutamate residues cia gamma-glutamyl carboxylase)

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10
Q

What class of drug is rivaroxaban

A

Oral Factor Xa inhibitor

*Oral Anticoagulants

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11
Q

What are the factors and proteins involved in the use of Warfarin

A

Factor 2, 7, 9, 10

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12
Q

What is the mechanism of action for Tirofiban

A

Targets the RGD sequence on the GP2b/3a sequence on platelets, which prevents aggregation

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13
Q

What class of drug is lepirudin

A

Direct thrombin inhibitors

*Parenteral Anticoagulants

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14
Q

What is the mechanism of action of abciximab

A

Targets the RGD sequence on the GP2b/3a sequence on platelets, which prevents aggregation

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15
Q

What class of drug is reteplase

A

Tissue type plasminogen activator

*Thrombolytic (fibrinolytic) drug

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16
Q

What class of drug is urokinase

A

Urokinase type plasminogen activator

*Thrombolytic (fibrinolytic) drug

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17
Q

What are the pharmacokinetics of warfarin

A
  • Oral administration
  • 100% bioavailability
  • Delayed onset of action (12 hours), but long half life (36 hours)
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18
Q

What are the kind of thrombus forming in the low pressure veins and heart

A

Red thrombus

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19
Q

Which of the ADP receptor antiplatelet drugs are impacted by P450

A

-Clopidogrel

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20
Q

What class of drug is Warfarin

A

Oral Coumarin anticoagulants

*Oral Anticoagulants

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21
Q

What class of drug is edoxaban

A

Oral Factor Xa inhibitor

*Oral Anticoagulants

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22
Q

What class of drug is ticlopidine

A

ADP receptor blocker

*Antiplatelet

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23
Q

What is the disadvantage of using dabigatran

A

80% of renal excretion, so needs to be avoided in renal failure

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24
Q

What are the drawbacks of warfarin

A
  • High variability
  • Bleeding compilations
  • requires INR monitoring
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25
Q

What class of drug is cilostazol

A

Inhibitors of phosphodiesterase

*Antiplatelet

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26
Q

What are the advantages of dabigatran

A
  • No interactions with P450 drugs

- Approved antidote

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27
Q

What is the characteristics of binding for bivalirudin

A

Reversible inhibitor of thrombin

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28
Q

How do red thrombus form

A

-Forms in low pressure veins and the heart, resulting in platelet binding and aggregation, followed by fibrin tails with RBC presence

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29
Q

What are the advantages of warfarin

A
  • Oral administration
  • Long duration of action
  • Drug clearance is independent of renal function
  • Reversal of action is developed
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30
Q

What is the mechanism of action for argatroban

A

Directly binds at the thrombin active site

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31
Q

When is cilostazol primarily used

A

Treatment of intermittent claudication (impairment of walking due to pain, numbness, discomfort or standing)

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32
Q

What is the mechanism of action for high molecular weight heparin

A

Binds to both thrombin and antithrombin 3 (inactivates thrombin)
Binds to both factor Xa and antithrombin 3 (inactivates factor Xa)

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33
Q

What class of drug is clopidogrel

A

ADP receptor blocker

*Antiplatelet

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34
Q

What is the mechanism of action for lepirudin

A

Bivalent binding-directly binds to thrombin at the substrate recognition spot, as well as the active site

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35
Q

What class of drug is apixaban

A

Oral Factor Xa inhibitor

*Oral Anticoagulants

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36
Q

What is the mechanism of action for streptokinase

A

Binds to plasminogen and forms a complex, which converts it plasmin without being cleaved

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37
Q

What are the adverse effects of heparin

A
  • Bleeding

- Heparin induced thrombocytopenia (HIT), which includes thrombosis

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38
Q

What is the mechanism of action of tPA

A

Cleaves plasminogen into plasmin, but requires fibrin

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39
Q

What is is the drug used to break a clot and what is the time frame it should be used

A

tPA, generally needs to be used within 3 hours of emboli stroke

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40
Q

What is the mechanism of pathogenesis of heparin-induced thrombocytopenia (HIT)

A

-Complex formation of heparin, IgG, platelet with PF4 (platelet factor 4) leading to thrombocytopenia, along with formation of thrombi

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41
Q

What class of drug is enoxaparin

A

Low molecular weight heparin, an indirect thrombin and factor Xa inhibitor

*Parenteral Anticoagulants

42
Q

Which drugs tend to increased the prothrombin time

A
  • Azoles
  • Aspirin
  • cephalosporins
  • Hyperthyroidism
43
Q

What is the main general function of thrombolytics

A

Destroying blood clots after they have formed to re-establish blood flow

44
Q

What is the cause of the white thrombus

A

Forming in high pressure arteries as a result of the platelet forming on the damaged endothelium with little fibrin

45
Q

What is the clinical use for the direct oral anticoagulants

A
  • Prevention, treatment of thromboembolism

- Prevention of stroke in patients in atrial fibrillation

46
Q

What is the mechanism of action of dabigatran

A

Direct thrombin inhibitor

47
Q

What class of drug is alteplase

A

Tissue type plasminogen activator

*Thrombolytic (fibrinolytic) drug

48
Q

Which patients population is less resistant to warfarin

A

Asian Americans

*Low dose haplotype VKORC1 (vitamin K epoxide reductase complex)

49
Q

Which patient population is more resistant to warfarin

A

African Americans

*High does haplotype VKORC1 (Vitamin K epoxide reductase complex 1)

50
Q

Clinically, how is fondaparinux different from heparin

A
  • Does not inhibit thrombin formation
  • Rarely induces HIT
  • Not reversed by protamine sulfate
51
Q

What are the agents used in prevention cerebrovascular ischemia

A

Diphyridamole with aspirin

52
Q

What are the clinical indications for direct thrombin inhibitors

A

HIT

Coronary angioplasty

53
Q

What are the pathological conditions associated with white thrombus

A

Local ischemia due to arterial occlusion, especially in the coronary arteries leading to MI and unstable angina

54
Q

What class of drug is dalteparin

A

Low molecular weight heparin, an indirect thrombin and factor Xa inhibitors

*Parenteral Anticoagulants

55
Q

What is the main general function of anticoagulants

A

Regulation in the synthesis of clots, primarily prevention in the venous system or heart (red thrombus)

56
Q

What class of drug is abciximab

A

Platelet glycoprotein receptor

*Antiplatelet

57
Q

What are the tests used to monitor patients on heparin

A
  • Activated partial thromboplastin time (aPTT)

- Anti-Xa assay

58
Q

What is the general mechanisms of action for indirect thrombin and factor Xa inhibitors

A

-Bind plasma serine protease inhibitor antithrombin 3

59
Q

What is the mechanism of action for aspirin

A

Inhibition of cyclooxygenase and decreased TxA2 production

60
Q

What class of drug is tenecteplase

A

Tissue type plasminogen activator

*Thrombolytic (fibrinolytic) drug

61
Q

What class of drug is tirofiban

A

Platelet glycoprotein receptor

*Antiplatelet

62
Q

What is the antidote in the case of dabigatran overdose

A

-Idarucizumab (directly binds to drug)

63
Q

What are the adverse effects of the direct thrombin inhibitors

A

Bleeding, there is no antidote so should be used with caution

64
Q

What is the mechanism of action of bivalirudin

A

Bivalent binding-directly binds to thrombin at the substrate recognition spot, as well as the active site

65
Q

What class of drug is bivalirudin

A

Direct thrombin inhibitors

*Parenteral Anticoagulants

66
Q

What class of drug is fondaparinux

A

Synthetic pentasaccharide, and indirect thrombin and factor Xa inhibitor

*Parenteral Anticoagulants

67
Q

What are the kind of thrombus the form in the high pressure arteries

A

White, platelet rich thrombus

68
Q

What class of drug is diphyridamole

A

Inhibitors of phosphodiesterase

*Antiplatelet

69
Q

What is the mechanism of action for fondaparinux

A

Inhibits factor Xa and antithrombin 3

*no affects on thrombin

70
Q

What class of drug is prasugrel

A

ADP receptor blocker

*Antiplatelet

71
Q

What are the adverse effects of aspirin

A
  • Peptic ulcer

- GI bleeding

72
Q

What is the mechanism of action of Eptifibatide

A

Targets the RGD sequence on the GP2b/3a sequence on platelets, which prevents aggregation

73
Q

What class of drug is streptokinase

A

Streptokinase preparations

*Thrombolytic (fibrinolytic) drug

74
Q

What are the clinical uses for warfarin

A
  • Used to prevent thrombosis or thromboembolism
  • Atrial fibrillation
  • Prosthetic heart valves
75
Q

What is the main general function of antiplatelet drugs

A

Inhibits platelet function, primarily in the formation of white thrombi (arteries)

76
Q

What class of drug is Aspirin

A

Inhibitor of thromboxane A2 synthesis

*Antiplatelet

77
Q

Which enzyme is responsible for the dose variation in Caucasian patients

A

CYP2C9

78
Q

What class of drug is eptifibatide

A

Platelet glycoprotein receptor

*Antiplatelet

79
Q

What class of drug is ticagrelor

A

ADP receptor blocker

*Antiplatelet

80
Q

How does fondaparinux act as a antithrombin 3 catalyst

A

Binds directly to antithrombin 3, which causes as a conformational change that increases the binding to factor Xa and its inactivation

81
Q

The activated partial thromboplastin time (aPTT) looks at which pathway and factors

A
  • Intrinsic and common pathway

- Evaluates serine proteases 2,9,10,11,12 (are affected by heparin)

82
Q

What are the adverse affects of warfarin

A
  • Teratogenic effects (bleeding and abnormal bone formation in fetus)
  • Skin necrosis, infarction of breasts, intestine and extremities
  • Osteoporosis
  • Bleeding
83
Q

What are the clinical uses for fondaparinux

A
  • Prevention of DVT
  • Treatment of acute DVT
  • Treatment of a PE
84
Q

What is the mechanism of action for edoxaban

A

Direct factor Xa inhibitor

85
Q

What class of drug is tinzaparin

A

Low molecular weight heparin, an indirect thrombin and factor Xa inhibitors

*Parenteral Anticoagulants

86
Q

What is the mechanism of action for low molecular weight heparin

A

Inhibits factor Xa with antithrombin 3

*No affect on thrombin

87
Q

What are the advantages of direct oral anticoagulants

A
  • Orally administered
  • doesnt need to be monitored
  • rapid onset
88
Q

What class of drug is heparin sodium

A

Parenteral unfractionated heparin, an indirect thrombin and factor Xa inhibitors

*Anticoagulants

89
Q

What is the clinical use for aspirin

A

-Primary and secondary Prevention of heart attack and vascular events (white thrombosis)

90
Q

What is the characteristic of the binding of lepirudin

A

Irreversible binding to thrombin

91
Q

What is the mechanism of apixaban

A

Direct factor Xa inhibitor

92
Q

What can heparin be used to treat

A
  • Protects against emboli stroke (red, fibrin rich), Pulmonary emboli
  • Patients with DVTs, arrhythmias, other conditions with increased with red thrombi
  • Prevention of emboli with surgery or hospitalized patients
93
Q

What is the mechanism of action of rivaroxaban

A

Direct factor Xa inhibitor

94
Q

What is the S-warfarin metabolized by

A

CYP2C9

95
Q

What is the mechanism of action of the phosphodiesterase inhibitor antiplatelet drugs

A

1-Inhibits phosphodiesterase
2-cAMP levels remain high
3- cAMP levels prevent the platelet aggregation

96
Q

What are the pathological conditions associated in red thrombus

A

Pain, swelling, embolism with potential for stroke

97
Q

Which drugs tend to decrease prothrombin time

A
  • Diuretics
  • Vitamin K
  • Hypothyroidism
  • Barbituates
98
Q

What are the disadvantages of direct oral anticoagulants

A

Excreted by kidneys, need to be monitored and dose adjustments

99
Q

What is R-warfarin metabolized by

A

CYP3A4

100
Q

What class of drug is argatroban

A

Direct thrombin inhibitors

*Parenteral Anticoagulants

Pharmacology & Drugs (43 decks)

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