B.44 Anticoagulant and Antiplatelet TX Flashcards

1
Q

B.44 Anticoagulant and Antiplatelet TX

Unfractionated Heparin (UFH)

A

anti-coagulant

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2
Q

B.44 Anticoagulant and Antiplatelet TX

List all the anti-coagulants

A
  1. Warfarin - A vitamin K antagonist that requires regular monitoring of INR levels and is used for various thromboembolic disorders.
  2. Direct Oral Anticoagulants (DOACs):
  • Dabigatran - Direct thrombin inhibitor.
  • Rivaroxaban - Factor Xa inhibitor.
  • Apixaban - Factor Xa inhibitor.
  • Edoxaban - Factor Xa inhibitor.
  1. Heaprin
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3
Q

B.44 Anticoagulant and Antiplatelet TX

List all the Anti-platelets

A
  1. Aspirin - Inhibits cyclooxygenase (COX-1) and decreases thromboxane A2 production.
  2. Clopidogrel - A thienopyridine that irreversibly blocks the P2Y12 ADP receptor.
  3. Prasugrel - A thienopyridine that irreversibly inhibits the P2Y12 ADP receptor, more potent than clopidogrel.
  4. Ticagrelor - A reversible inhibitor of the P2Y12 ADP receptor.
  5. Dipyridamole - An antiplatelet drug that inhibits the uptake of adenosine and increases platelet cyclic AMP levels.
  6. Gp IIb/IIIa antagonists - These include:
  • Abciximab
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4
Q

B.44 Anticoagulant and Antiplatelet TX

Unfractionated Heparin (UFH) MOA

A

Unfractionated heparin acts by binding to antithrombin III, which inhibits thrombin and factor Xa, leading to anticoagulation.

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5
Q

B.44 Anticoagulant and Antiplatelet TX

How is unfractionated heparin administered?

A

A: Unfractionated heparin is administered parenterally, either through subcutaneous (SC) injection or continuous intravenous (IV) infusion.

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6
Q

B.44 Anticoagulant and Antiplatelet TX

What is a major clinical use of unfractionated heparin?

A

A: Unfractionated heparin is used for the prevention and treatment of venous thromboembolism (VTE) and in acute coronary syndrome (ACS).

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7
Q

B.44 Anticoagulant and Antiplatelet TX

UFH clinical use

A

immediate anticoagulation for PE, ACS, MI, DVT

can be used during pregnacy, does not cross placenta

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8
Q

B.44 Anticoagulant and Antiplatelet TX

how to monitor UFH

A

aPTT

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9
Q

B.44 Anticoagulant and Antiplatelet TX

SE UFH

A

Bleeding
Thrombocytopenia (HIT)
Osteoporosis
drug-drug interaction

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10
Q

B.44 Anticoagulant and Antiplatelet TX

Antidote UFH

A

protamine sulfate

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11
Q

B.44 Anticoagulant and Antiplatelet TX

What is the range of plasma half-life for unfractionated heparin?

A

A: The plasma half-life of unfractionated heparin typically ranges from 30 to 60 minutes, depending on the dose and clearance mechanisms.

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12
Q

B.44 Anticoagulant and Antiplatelet TX

What monitoring is required for patients on unfractionated heparin?

A

A: Patients on unfractionated heparin require monitoring of activated partial thromboplastin time (aPTT) to ensure appropriate anticoagulation levels.

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13
Q

B.44 Anticoagulant and Antiplatelet TX

What is one of the key disadvantages of using unfractionated heparin?

A

A: The anticoagulant response to unfractionated heparin can be unpredictable due to variable patient responses and binding to plasma proteins.

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14
Q

B.44 Anticoagulant and Antiplatelet TX

Why is unfractionated heparin often replaced by low-molecular-weight heparins (LMWH)?

A

A: LMWH has more predictable pharmacokinetics, longer half-life, lower risk of heparin-induced thrombocytopenia, and does not require routine monitoring.

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15
Q

B.44 Anticoagulant and Antiplatelet TX

In what situation is the use of unfractionated heparin preferred over LMWH?

A

A: Unfractionated heparin is preferred in patients requiring rapid reversal of anticoagulation, such as in cases of major bleeding or urgent surgical procedures.

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16
Q

B.44 Anticoagulant and Antiplatelet TX

What is one of the significant complications of long-term unfractionated heparin use?

A

A: Long-term use of unfractionated heparin can lead to osteoporosis and vertebral fractures due to decreased bone density.

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17
Q

B.44 Anticoagulant and Antiplatelet TX

Low molecular weight heparin/Enoxaprin

A

Anti-coagulant

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18
Q

B.44 Anticoagulant and Antiplatelet TX

MOA LMWH

A

predominately acts on factor Xa

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19
Q

B.44 Anticoagulant and Antiplatelet TX

Clinical Use LMWH/Enoxaparin

A

immediate anticoagulation for PE, ACS, MI, DVT

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20
Q

B.44 Anticoagulant and Antiplatelet TX

LMWH/Enoxaparin administration

A

Subcutaneously, does not need lab monitoring

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21
Q

B.44 Anticoagulant and Antiplatelet TX

LMWH/Enoxaparin bioavaliability

A

better than UFH 2-4x longer half life

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22
Q

B.44 Anticoagulant and Antiplatelet TX

LMWH/Enoxaparin CI

A

renal insufficiency

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23
Q

B.44 Anticoagulant and Antiplatelet TX

LMWH/Enoxaparin antidote

A

partially inhibited by protamine sulfate . but not easily done

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24
Q

B.44 Anticoagulant and Antiplatelet TX

What is the mechanism of action for enoxaparin (LMWH)?

A

A: Enoxaparin potentiates the inhibitory effect of antithrombin on factor Xa more than on thrombin, leading to anticoagulation.

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25
Q

B.44 Anticoagulant and Antiplatelet TX

How is enoxaparin administered?

A

A: Enoxaparin is administered subcutaneously (SC) for prophylaxis and treatment of venous thromboembolism and can also be given intravenously if rapid effect is required.

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26
Q

B.44 Anticoagulant and Antiplatelet TX

What are the pharmacokinetic advantages of enoxaparin compared to unfractionated heparin?

A

A: Enoxaparin has more predictable pharmacokinetics, longer half-life, and higher bioavailability (~90%) after subcutaneous injection, making it easier to use without routine monitoring.

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27
Q

B.44 Anticoagulant and Antiplatelet TX

What is the typical dosing regimen for enoxaparin in the treatment of venous thromboembolism?

A

A: The usual dosing is 1 mg/kg every 12 hours or 1.5 mg/kg once daily, depending on the clinical situation and patient’s weight.

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28
Q

B.44 Anticoagulant and Antiplatelet TX

What is one of the major benefits of using LMWH like enoxaparin over unfractionated heparin?

A

A: Enoxaparin has a lower risk of inducing heparin-induced thrombocytopenia (HIT) and fewer drug-related complications, making it safer for long-term use.

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29
Q

B.44 Anticoagulant and Antiplatelet TX

Which patients may require caution or dosage adjustments when using enoxaparin?

A

A: Patients with renal impairment may require dosage adjustments, as LMWH is primarily cleared by the kidneys.

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30
Q

B.44 Anticoagulant and Antiplatelet TX

What are common indications for enoxaparin use?

A

A: Indications include prevention of deep vein thrombosis (DVT) in surgical or hospitalized patients, treatment of DVT and pulmonary embolism (PE), and management of acute coronary syndromes.

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31
Q

B.44 Anticoagulant and Antiplatelet TX

What is the risk of bleeding with enoxaparin compared to unfractionated heparin?

A

A: While bleeding risk exists with both, enoxaparin’s predictable response and lower incidence of thrombocytopenia make it associated with a relatively lower risk of bleeding complications.

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32
Q

B.44 Anticoagulant and Antiplatelet TX

What should patients be monitored for while on enoxaparin therapy?

A

A: Although routine monitoring is not necessary, patients should be monitored for signs of bleeding, renal function, and possibly anti-factor Xa levels in high-risk situations.

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33
Q

B.44 Anticoagulant and Antiplatelet TX

How does the efficacy of enoxaparin compare to that of unfractionated heparin?

A

A: Enoxaparin has been shown to be as effective as unfractionated heparin for the treatment and prevention of thromboembolic events, with the added benefits of convenience and safety.

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34
Q

B.44 Anticoagulant and Antiplatelet TX

What is Fondaparinux

A

It is a anti-coagulant, synthetic heparin

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35
Q

B.44 Anticoagulant and Antiplatelet TX

Fondaparinux MOA

A

Acts on on Factor Xa

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36
Q

B.44 Anticoagulant and Antiplatelet TX

What is fondaparinux?

A

A: Fondaparinux is a synthetic anticoagulant that is a selective inhibitor of factor Xa and a synthetic analogue of the antithrombin-binding pentasaccharide sequenc

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37
Q

B.44 Anticoagulant and Antiplatelet TX

How is fondaparinux administered?

A

A: Fondaparinux is administered subcutaneously (SC), typically once daily.

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38
Q

B.44 Anticoagulant and Antiplatelet TX

What is the mechanism of action of fondaparinux?

A

A: Fondaparinux binds to antithrombin, leading to the inhibition of factor Xa, but does not significantly inhibit thrombin.

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39
Q

B.44 Anticoagulant and Antiplatelet TX

What are the primary indications for fondaparinux use?

A

A: Fondaparinux is used for thromboprophylaxis in patients undergoing surgery, and for the treatment of acute deep vein thrombosis (DVT) and pulmonary embolism (PE).

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40
Q

B.44 Anticoagulant and Antiplatelet TX

What is the bioavailability of fondaparinux?

A

A: Fondaparinux has a bioavailability of approximately 100% after subcutaneous injection.

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41
Q

B.44 Anticoagulant and Antiplatelet TX

How is fondaparinux cleared from the body?

A

A: Fondaparinux is cleared primarily via the kidneys in an unchanged form, making renal function an important consideration in dosing.

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42
Q

B.44 Anticoagulant and Antiplatelet TX

What is the typical dosing for fondaparinux in the treatment of DVT or PE?

A

A: The initial dose is typically 7.5 mg once daily, with adjustments made for body weight: 5 mg for patients weighing <50 kg and 10 mg for those >100 kg.

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43
Q

B.44 Anticoagulant and Antiplatelet TX

What are the major side effects of fondaparinux?

A

A: The primary side effect of fondaparinux is bleeding. It does not cause heparin-induced thrombocytopenia (HIT) because it does not bind to PF4.

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44
Q

B.44 Anticoagulant and Antiplatelet TX

Why is fondaparinux considered beneficial for patients with a history of HIT?

A

A: Fondaparinux does not cross-react with HIT antibodies, making it a safer alternative for anticoagulation in patients who have developed HIT.

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45
Q

B.44 Anticoagulant and Antiplatelet TX

What significant limitation is associated with fondaparinux regarding reversal of anticoagulation?

A

A: Fondaparinux has no specific antidote, and protamine sulfate does not reverse its anticoagulant effects, complicating management in case of major bleeding.

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46
Q

B.44 Anticoagulant and Antiplatelet TX

What is Dabigatran

A

Anti-coagulant

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47
Q

B.44 Anticoagulant and Antiplatelet TX

MOA Dabigatran

A

Direct thrombin (IIa) inhibitor

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48
Q

B.44 Anticoagulant and Antiplatelet TX

Administration Dabigatran

A

PO

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49
Q

B.44 Anticoagulant and Antiplatelet TX

Dabigatran antidote

A

Idarucizumab

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50
Q

B.44 Anticoagulant and Antiplatelet TX

What is dabigatran?

A

A: Dabigatran is a direct oral anticoagulant (DOAC) that inhibits thrombin, thereby preventing the formation of blood clots.

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51
Q

B.44 Anticoagulant and Antiplatelet TX

How does dabigatran work?

A

A: Dabigatran directly binds to the active site of thrombin, inhibiting its ability to convert fibrinogen to fibrin, which is essential for clot formation.

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52
Q

B.44 Anticoagulant and Antiplatelet TX

What are the primary indications for dabigatran use?

A

A: Dabigatran is used for stroke prevention in patients with nonvalvular atrial fibrillation and for the treatment and prevention of venous thromboembolism (VTE).

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53
Q

B.44 Anticoagulant and Antiplatelet TX

What is the bioavailability of dabigatran?

A

A: Dabigatran has a low bioavailability of approximately 6% due to extensive first-pass metabolism; it is often given with food to enhance absorption.

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54
Q

B.44 Anticoagulant and Antiplatelet TX

What are the typical dosing regimens for dabigatran when used for stroke prevention?

A

A: The usual dose for stroke prevention in nonvalvular atrial fibrillation is 150 mg taken twice daily, with a reduced dose of 75 mg twice daily for patients with moderate renal impairment.

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55
Q

B.44 Anticoagulant and Antiplatelet TX

What are the major side effects of dabigatran?

A

A: The most common side effect of dabigatran is bleeding, particularly gastrointestinal bleeding. Dyspepsia is also reported in about 10% of patients.

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56
Q

B.44 Anticoagulant and Antiplatelet TX

How is dabigatran cleared from the body?

A

A: Dabigatran is primarily cleared by the kidneys; therefore, caution is advised in patients with renal impairment, and dosage adjustments may be necessary.

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57
Q

B.44 Anticoagulant and Antiplatelet TX

What is the reversal agent for dabigatran?

A

A: Idarucizumab is the specific reversal agent for dabigatran, and it binds dabigatran with high affinity to neutralize its anticoagulant effect.

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58
Q

B.44 Anticoagulant and Antiplatelet TX

When should dabigatran be stopped prior to surgical procedures?

A

A: Dabigatran should be stopped 1-2 days before procedures associated with a moderate to high risk of bleeding; the timing depends on renal function.

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59
Q

B.44 Anticoagulant and Antiplatelet TX

What monitoring is recommended for patients on dabigatran therapy?

A

A: Routine coagulation monitoring is generally not required; however, assessment of renal function and monitoring for signs of bleeding are important.

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60
Q

B.44 Anticoagulant and Antiplatelet TX

What is argatroban?

A

A: Argatroban is a direct thrombin inhibitor used as an anticoagulant, specifically for patients with heparin-induced thrombocytopenia (HIT).

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61
Q

B.44 Anticoagulant and Antiplatelet TX

How does argatroban work?

A

A: Argatroban binds to the active site of thrombin, inhibiting its ability to convert fibrinogen to fibrin, thus preventing clot formation.

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62
Q

B.44 Anticoagulant and Antiplatelet TX

In which patient population is argatroban primarily used?

A

A: Argatroban is primarily used in patients with HIT, especially those who require anticoagulation and cannot use heparin.

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63
Q

B.44 Anticoagulant and Antiplatelet TX

What is the route of administration for argatroban?

A

A: Argatroban is administered via continuous intravenous (IV) infusion.

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64
Q

B.44 Anticoagulant and Antiplatelet TX

What is the half-life of argatroban?

A

A: The plasma half-life of argatroban is approximately 45 minutes.

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65
Q

B.44 Anticoagulant and Antiplatelet TX

How is the anticoagulant effect of argatroban monitored?

A

A: The activated partial thromboplastin time (aPTT) is used to monitor argatroban’s anticoagulant effect, with the goal of achieving an aPTT that is 1.5 to 3 times the baseline value.

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66
Q

B.44 Anticoagulant and Antiplatelet TX

What adjustment is needed when transitioning from argatroban to warfarin?

A

A: Argatroban prolongs INR, complicating the transition to warfarin; monitoring factor X levels can help in this transition instead of relying solely on INR.

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67
Q

B.44 Anticoagulant and Antiplatelet TX

What are the major side effects associated with argatroban?

A

A: The most common side effect of argatroban is bleeding. Other potential complications may include elevated liver enzymes.

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68
Q

B.44 Anticoagulant and Antiplatelet TX

Is renal function a concern when using argatroban?

A

A: No, argatroban is metabolized in the liver and is not cleared by the kidneys, making it safer for patients with renal impairment.

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69
Q

B.44 Anticoagulant and Antiplatelet TX

What is the dosing regimen for argatroban in the management of HIT?

A

A: The typical starting dose of argatroban is 2 mcg/kg/min, which may be adjusted based on aPTT results and clinical responses.

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70
Q

B.44 Anticoagulant and Antiplatelet TX

What is bivalirudin?

A

A: Bivalirudin is a direct thrombin inhibitor that is used as an anticoagulant, especially in patients undergoing percutaneous coronary intervention (PCI).

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71
Q

B.44 Anticoagulant and Antiplatelet TX

How does bivalirudin work?

A

A: Bivalirudin binds to the active site of thrombin and also interacts with exosite 1, inhibiting thrombin’s ability to convert fibrinogen to fibrin and thus preventing blood clot formation.

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72
Q

B.44 Anticoagulant and Antiplatelet TX

What are the primary indications for using bivalirudin?

A

A: Bivalirudin is indicated for anticoagulation in patients undergoing PCI and for patients with heparin-induced thrombocytopenia (HIT).

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73
Q

B.44 Anticoagulant and Antiplatelet TX

What is the half-life of bivalirudin?

A

A: Bivalirudin has a relatively short half-life of approximately 25 minutes.

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74
Q

B.44 Anticoagulant and Antiplatelet TX

How is bivalirudin administered?

A

A: Bivalirudin is administered via intravenous (IV) infusion, often starting with a bolus dose followed by a continuous infusion.

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75
Q

B.44 Anticoagulant and Antiplatelet TX

What is the typical dosing regimen for bivalirudin during PCI?

A

A: For PCI, bivalirudin is typically given as a bolus of 0.75 mg/kg followed by a continuous infusion of 1.75 mg/kg/hour.

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76
Q

B.44 Anticoagulant and Antiplatelet TX

What are the major side effects of bivalirudin?

A

A: The major side effect of bivalirudin is bleeding. Other side effects may include thrombocytopenia and elevated liver enzymes.

77
Q

B.44 Anticoagulant and Antiplatelet TX

How is the anticoagulant effect of bivalirudin monitored?

A

A: The activated clotting time (ACT) is commonly used to monitor the anticoagulant effect of bivalirudin, particularly during PCI procedures.

78
Q

B.44 Anticoagulant and Antiplatelet TX

Is renal function a concern when using bivalirudin?

A

A: Yes, while bivalirudin is partially cleared via the kidneys, dosage adjustments may be necessary for patients with renal impairment.

79
Q

B.44 Anticoagulant and Antiplatelet TX

What is the advantage of using bivalirudin over heparin in certain patients?

A

A: Bivalirudin does not cause heparin-induced thrombocytopenia (HIT), making it a safer alternative for patients with this condition undergoing procedures.

80
Q

B.44 Anticoagulant and Antiplatelet TX

What is rivaroxaban?

A

A: Rivaroxaban is an oral anticoagulant that belongs to the class of direct Factor Xa inhibitors, used for preventing and treating thromboembolic disorders.

81
Q

B.44 Anticoagulant and Antiplatelet TX

What is the primary mechanism of action of rivaroxaban?

A

A: Rivaroxaban inhibits Factor Xa, which is crucial in the coagulation cascade, thereby preventing the conversion of prothrombin to thrombin and reducing clot formation.

82
Q

B.44 Anticoagulant and Antiplatelet TX

What are the primary indications for using rivaroxaban?

A

A: Rivaroxaban is indicated for the prevention of stroke in non-valvular atrial fibrillation, treatment and prevention of venous thromboembolism (VTE), and for secondary prevention of cardiovascular events in patients with coronary artery disease.

83
Q

B.44 Anticoagulant and Antiplatelet TX

What is the typical dosing regimen of rivaroxaban for non-valvular atrial fibrillation?

A

A: The standard dose for non-valvular atrial fibrillation is 20 mg once daily, with a reduced dose of 15 mg for patients with a creatinine clearance of 15–49 mL/min.

84
Q

B.44 Anticoagulant and Antiplatelet TX

How is rivaroxaban administered?

A

A: Rivaroxaban is administered orally, with certain doses required to be taken with food to enhance absorption.

85
Q

B.44 Anticoagulant and Antiplatelet TX

What are some common side effects associated with rivaroxaban?

A

A: Common side effects include bleeding (e.g., gastrointestinal and intracranial bleeding) and, less commonly, liver enzyme elevations

86
Q

B.44 Anticoagulant and Antiplatelet TX

What is the half-life of rivaroxaban?

A

A: The half-life of rivaroxaban ranges from 7 to 11 hours, which can vary based on renal function and other factors.

87
Q

B.44 Anticoagulant and Antiplatelet TX

What should be considered in patients with renal impairment when using rivaroxaban?

A

A: In patients with renal impairment, the dose of rivaroxaban may need to be adjusted, particularly for those with a creatinine clearance of less than 50 mL/min.

88
Q

B.44 Anticoagulant and Antiplatelet TX

How is rivaroxaban reversed in cases of bleeding?

A

A: The reversal of rivaroxaban can be achieved using andexanet alfa, a recombinant variant of Factor Xa that sequesters the drug.

89
Q

B.44 Anticoagulant and Antiplatelet TX

What monitoring is necessary for patients on rivaroxaban?

A

A: Rivaroxaban generally does not require routine monitoring, but assessments of adherence, bleeding risk, and renal function should be considered. Prothrombin time (PT) can provide qualitative information about its anticoagulant effect.

90
Q

B.44 Anticoagulant and Antiplatelet TX

What is apixaban?

A

A: Apixaban is an oral anticoagulant that belongs to the class of direct Factor Xa inhibitors, used for preventing and treating thromboembolic disorders.

91
Q

B.44 Anticoagulant and Antiplatelet TX

What is the primary mechanism of action of apixaban?

A

A: Apixaban inhibits Factor Xa, which plays a crucial role in the coagulation cascade, preventing the conversion of prothrombin to thrombin and thereby reducing thrombus formation.

92
Q

B.44 Anticoagulant and Antiplatelet TX

What are the primary indications for using apixaban?

A

A: Apixaban is indicated for the prevention of stroke in non-valvular atrial fibrillation, treatment and prevention of venous thromboembolism (VTE), and secondary prevention of thrombotic events in patients with coronary artery or peripheral artery disease.

93
Q

B.44 Anticoagulant and Antiplatelet TX

What is the typical dosing regimen of apixaban for non-valvular atrial fibrillation?

A

A: The standard dose for non-valvular atrial fibrillation is 5 mg taken twice daily, with a reduced dose of 2.5 mg twice daily for patients meeting at least two of the “ABC” criteria (age >80 years, weight <60 kg, and serum creatinine >1.5 mg/dL).

94
Q

B.44 Anticoagulant and Antiplatelet TX

How should apixaban be administered?

A

A: Apixaban is taken orally, and it can be administered with or without food.

95
Q

B.44 Anticoagulant and Antiplatelet TX

What are some common side effects associated with apixaban?

A

A: Common side effects include bleeding (such as gastrointestinal and intracranial bleeding) and, less commonly, elevated liver enzymes.

96
Q

B.44 Anticoagulant and Antiplatelet TX

What is the half-life of apixaban?

A

A: The half-life of apixaban is approximately 12 hours, which can vary based on individual factors, including renal function.

97
Q

B.44 Anticoagulant and Antiplatelet TX

How is apixaban adjusted in patients with renal impairment?

A

A: In patients with renal impairment, dosage reductions may be necessary for those with a creatinine clearance of 15–50 mL/min, especially for secondary prevention.

98
Q

B.44 Anticoagulant and Antiplatelet TX

How can the effects of apixaban be reversed in cases of bleeding?

A

A: The reversal of apixaban can be achieved using andexanet alfa, which serves as a decoy to sequester oral Factor Xa inhibitors.

99
Q

B.44 Anticoagulant and Antiplatelet TX

Is routine monitoring required for patients on apixaban?

A

A: Routine coagulation monitoring is not required for patients on apixaban, but it may be helpful in specific situations such as assessing adherence, detecting accumulation or overdose, or evaluating bleeding mechanisms.

100
Q

B.44 Anticoagulant and Antiplatelet TX

What is warfarin?

A

A: Warfarin is an oral anticoagulant medication that inhibits vitamin K-dependent clotting factors, used to prevent and treat thromboembolic disorders.

101
Q

B.44 Anticoagulant and Antiplatelet TX

What is the primary mechanism of action of warfarin?

A

A: Warfarin works by inhibiting the vitamin K epoxide reductase complex, which is essential for the synthesis of clotting factors II, VII, IX, and X, and proteins C and S.

102
Q

B.44 Anticoagulant and Antiplatelet TX

What are the primary indications for using warfarin?

A

A: Warfarin is used for the prevention and treatment of venous thromboembolism (VTE), pulmonary embolism (PE), myocardial infarction, and for stroke prevention in patients with atrial fibrillation.

103
Q

B.44 Anticoagulant and Antiplatelet TX

Why is the anticoagulant effect of warfarin delayed?

A

A: The anticoagulant effect of warfarin is delayed because it inhibits the synthesis of new clotting factors, which takes time, as existing factors in circulation must degrade before the effects become evident.

104
Q

B.44 Anticoagulant and Antiplatelet TX

What is the typical dosing regimen for warfarin?

A

A: Warfarin dosing is individualized based on monitoring of the International Normalized Ratio (INR), with typical starting doses ranging from 2 to 5 mg daily, adjusted according to INR results.

105
Q

B.44 Anticoagulant and Antiplatelet TX

What monitoring is necessary for patients taking warfarin?

A

A: Patients on warfarin require regular INR monitoring to ensure that the anticoagulation effect is within the therapeutic range, typically every 3 to 4 weeks for stable patients.

106
Q

B.44 Anticoagulant and Antiplatelet TX

What are some common side effects associated with warfarin?

A

A: Common side effects include bleeding (both minor and major), purple toe syndrome, skin necrosis, and, less commonly, liver enzyme elevation.

107
Q

B.44 Anticoagulant and Antiplatelet TX

What is the risk of bleeding complications with warfarin?

A

A: At least half of the bleeding complications occur when the INR exceeds the therapeutic range; major bleeding events, such as gastrointestinal or intracranial bleeding, can occur as well.

108
Q

B.44 Anticoagulant and Antiplatelet TX

How can warfarin’s anticoagulant effect be reversed?

A

A: Warfarin can be reversed with oral vitamin K for minor INR elevation or serious bleeding treated with intravenous vitamin K and prothrombin complex concentrates.

109
Q

B.44 Anticoagulant and Antiplatelet TX

In which patient populations is warfarin contraindicated?

A

A: Warfarin is contraindicated in pregnancy due to the risk of fetal abnormalities and in patients with active bleeding or conditions that increase the risk of bleeding, such as thrombocytopenia.

110
Q

B.44 Anticoagulant and Antiplatelet TX

What is aspirin?

A

A: Aspirin is a widely used antiplatelet medication and nonsteroidal anti-inflammatory drug (NSAID) that inhibits platelet aggregation and reduces inflammation.

111
Q

B.44 Anticoagulant and Antiplatelet TX

What is the primary mechanism of action of aspirin?

A

A: Aspirin produces its antithrombotic effect by irreversibly acetylating cyclooxygenase-1 (COX-1), leading to the inhibition of thromboxane A2 (TXA2) synthesis, which is critical for platelet activation and aggregation.

112
Q

B.44 Anticoagulant and Antiplatelet TX

What are the primary indications for using aspirin?

A

A: Aspirin is used for secondary prevention of cardiovascular events in patients with established coronary artery, cerebral artery, or peripheral artery disease.

113
Q

B.44 Anticoagulant and Antiplatelet TX

What is the recommended dose of aspirin for most indications?

A

A: The usual dose of aspirin is between 75–325 mg once daily. Lower doses of 75–100 mg daily are often preferred due to a favorable balance of efficacy and safety.

114
Q

B.44 Anticoagulant and Antiplatelet TX

What are the most common side effects of aspirin?

A

A: The most common side effects of aspirin are gastrointestinal and include dyspepsia, erosive gastritis, and peptic ulcers, which can lead to bleeding.

115
Q

B.44 Anticoagulant and Antiplatelet TX

Why is the use of aspirin for primary prevention controversial?

A

A: Recent studies suggest that the potential gastrointestinal and intracerebral hemorrhage risks associated with aspirin may outweigh its benefits in primary prevention for cardiovascular events.

116
Q

B.44 Anticoagulant and Antiplatelet TX

What is aspirin resistance?

A

A: Aspirin resistance is the failure of aspirin to adequately prevent thrombotic events in some patients, which may be due to various factors such as poor compliance, drug interactions, or genetic variability.

117
Q

B.44 Anticoagulant and Antiplatelet TX

What patients should not receive aspirin?

A

A: Aspirin should not be administered to patients with a known history of aspirin allergy characterized by bronchospasm, especially those with asthma, chronic urticaria, or nasal polyps.

118
Q

B.44 Anticoagulant and Antiplatelet TX

What precautions should be taken when using aspirin in combination therapies?

A

A: When aspirin is used with other antiplatelet drugs or anticoagulants, low-dose aspirin (75–100 mg daily) is recommended, and the risk of gastrointestinal bleeding may be reduced by administering proton pump inhibitors.

119
Q

B.44 Anticoagulant and Antiplatelet TX

Can aspirin be used in pregnancy?

A

A: Aspirin should be used with caution during pregnancy, especially in the third trimester, due to the potential risks of bleeding; however, low-dose aspirin may be beneficial in certain high-risk patients under medical supervision.

120
Q

B.44 Anticoagulant and Antiplatelet TX

What is clopidogrel?

A

A: Clopidogrel is an oral antiplatelet agent that inhibits platelet aggregation by irreversibly blocking the P2Y12 ADP receptor on platelets.

121
Q

B.44 Anticoagulant and Antiplatelet TX

What is the primary mechanism of action of clopidogrel?

A

A: Clopidogrel is a prodrug that requires metabolic activation by the hepatic cytochrome P450 enzyme system to produce its active form, which then blocks the P2Y12 receptor, preventing ADP-induced platelet activation.

122
Q

B.44 Anticoagulant and Antiplatelet TX

What are the main indications for clopidogrel?

A

A: Clopidogrel is indicated for the prevention of cardiovascular events in patients with recent myocardial infarction, recent ischemic stroke, or a history of peripheral artery disease. It is also used in combination with aspirin after coronary stenting.

123
Q

B.44 Anticoagulant and Antiplatelet TX

What is a common initial dose of clopidogrel?

A

A: The common initial dose of clopidogrel is 75 mg once daily; however, a loading dose of 300-600 mg may be given for rapid platelet inhibition, especially in urgent situations such as coronary intervention.

124
Q

B.44 Anticoagulant and Antiplatelet TX

What are some potential side effects of clopidogrel?

A

A: The most common side effects of clopidogrel include bleeding complications, such as minor bruising or major bleeding events. Other rare side effects include neutropenia and thrombotic thrombocytopenic purpura (TTP).

125
Q

B.44 Anticoagulant and Antiplatelet TX

Why is clopidogrel sometimes considered less effective than aspirin?

A

A: In some studies, clopidogrel has shown to be slightly less effective than aspirin alone for certain primary prevention scenarios, although it is more effective in the context of dual antiplatelet therapy, particularly after stenting.

126
Q

B.44 Anticoagulant and Antiplatelet TX

What is clopidogrel resistance?

A

A: Clopidogrel resistance refers to the variability in the drug’s effectiveness among individuals, often linked to genetic polymorphisms in the CYP2C19 enzyme that impair its metabolic activation.

127
Q

B.44 Anticoagulant and Antiplatelet TX

Can clopidogrel be used in combination with aspirin?

A

A: Yes, clopidogrel is often used in conjunction with aspirin to enhance antiplatelet effects, particularly in patients with acute coronary syndromes or after stent placement, but this combination increases the risk of bleeding.

128
Q

B.44 Anticoagulant and Antiplatelet TX

What considerations should be taken when prescribing clopidogrel?

A

A: Caution should be exercised in patients with a high risk of bleeding, and clopidogrel may need to be stopped 5-7 days prior to major surgery to minimize bleeding risks.

129
Q

B.44 Anticoagulant and Antiplatelet TX

What are the alternatives to clopidogrel if a patient cannot tolerate it?

A

A: Alternatives to clopidogrel include other P2Y12 inhibitors such as prasugrel and ticagrelor, which may be more effective in certain populations but come with different efficacy and safety profiles.

130
Q

B.44 Anticoagulant and Antiplatelet TX

What is prasugrel?

A

A: Prasugrel is an oral antiplatelet medication that inhibits platelet aggregation by irreversibly blocking the P2Y12 ADP receptor.

131
Q

B.44 Anticoagulant and Antiplatelet TX

How does prasugrel differ from clopidogrel in terms of action?

A

A: Unlike clopidogrel, prasugrel is more potent and has a more rapid onset of action because it has a more straightforward metabolic activation pathway and does not rely heavily on the CYP450 enzyme system.

132
Q

B.44 Anticoagulant and Antiplatelet TX

What are the primary indications for prasugrel?

A

A: Prasugrel is indicated for the prevention of thrombotic cardiovascular events in patients with acute coronary syndromes undergoing percutaneous coronary intervention (PCI).

133
Q

B.44 Anticoagulant and Antiplatelet TX

What is the typical dosing regimen for prasugrel?

A

A: After an initial loading dose of 60 mg, prasugrel is given at a daily maintenance dose of 10 mg; however, patients over 75 years old or weighing less than 60 kg should receive 5 mg daily.

134
Q

B.44 Anticoagulant and Antiplatelet TX

What are common side effects associated with prasugrel?

A

A: The most common side effects include bleeding complications, such as major or life-threatening bleeding, and other rare hematologic effects like thrombocytopenia.

135
Q

B.44 Anticoagulant and Antiplatelet TX

Why is prasugrel contraindicated in certain patients?

A

A: Prasugrel is contraindicated in patients with a history of prior stroke or transient ischemic attack due to an increased risk of bleeding.

136
Q

B.44 Anticoagulant and Antiplatelet TX

How does prasugrel’s efficacy compare to clopidogrel?

A

A: In clinical trials, prasugrel was associated with a lower incidence of cardiovascular death, myocardial infarction (MI), and stent thrombosis compared to clopidogrel, though it also led to higher rates of bleeding.

137
Q

B.44 Anticoagulant and Antiplatelet TX

When should prasugrel be stopped before surgery?

A

A: Prasugrel should typically be discontinued 5-7 days prior to major surgical procedures to reduce the risk of bleeding.

138
Q

B.44 Anticoagulant and Antiplatelet TX

What unique considerations should be taken for elderly patients on prasugrel?

A

A: Elderly patients (over 75 years old) are at a higher risk of bleeding; thus, a lower maintenance dose of 5 mg is recommended for safety.

139
Q

B.44 Anticoagulant and Antiplatelet TX

What other medications might be used in conjunction with prasugrel?

A

A: Prasugrel is often used in combination with aspirin to enhance antiplatelet effects after coronary interventions, particularly PCI.

140
Q

B.44 Anticoagulant and Antiplatelet TX

What is abciximab?

A

A: Abciximab is a glycoprotein IIb/IIIa antagonist used as an antiplatelet agent to prevent platelet aggregation during and after percutaneous coronary intervention (PCI).

141
Q

B.44 Anticoagulant and Antiplatelet TX

What is the mechanism of action of abciximab?

A

A: Abciximab inhibits the binding of fibrinogen and von Willebrand factor to glycoprotein IIb/IIIa receptors on activated platelets, thereby preventing platelet aggregation.

142
Q

B.44 Anticoagulant and Antiplatelet TX

What are the primary indications for abciximab?

A

A: Abciximab is indicated for use in patients undergoing PCI and is especially beneficial for those who have not been pretreated with other antiplatelet agents like aspirin or clopidogrel.

143
Q

B.44 Anticoagulant and Antiplatelet TX

How is abciximab administered?

A

A: Abciximab is given as an intravenous bolus (0.25 mg/kg) followed by an infusion (0.125 µg/kg/min) for up to 12 hours.

144
Q

B.44 Anticoagulant and Antiplatelet TX

What are the common side effects associated with abciximab?

A

A: Common side effects include bleeding complications and thrombocytopenia, which is immune-mediated and can be severe in some patients.

145
Q

B.44 Anticoagulant and Antiplatelet TX

What is the unique characteristic of abciximab compared to other Gp IIb/IIIa inhibitors?

A

A: Abciximab is a Fab fragment of a humanized monoclonal antibody, giving it a long plasma half-life and a prolonged effect on platelet aggregation inhibition.

146
Q

B.44 Anticoagulant and Antiplatelet TX

When is it necessary to monitor for platelet counts in patients receiving abciximab?

A

A: Platelet counts should be monitored, especially if thrombocytopenia is suspected, as this condition can occur approximately in 5% of patients treated with abciximab.

147
Q

B.44 Anticoagulant and Antiplatelet TX

What should be done if excessive bleeding or thrombocytopenia occurs with abciximab?

A

A: If serious bleeding occurs, abciximab should be discontinued immediately, and supportive measures should be taken, including potential platelet transfusions.

148
Q

B.44 Anticoagulant and Antiplatelet TX

In what clinical situations is abciximab particularly beneficial?

A

A: Abciximab is particularly beneficial in high-risk patients undergoing PCI who may require intensive antiplatelet therapy to decrease the risk of events like stent thrombosis.

149
Q

B.44 Anticoagulant and Antiplatelet TX

Does abciximab have any contraindications?

A

A: Yes, abciximab is contraindicated in patients with active bleeding, severe hypertension, and in those with a history of stroke within the last 30 days.

150
Q

B.44 Anticoagulant and Antiplatelet TX

What is dipyridamole?

A

A: Dipyridamole is an antiplatelet agent that inhibits platelet aggregation, often used in combination with aspirin for secondary prevention of thromboembolic events.

151
Q

B.44 Anticoagulant and Antiplatelet TX

What is the primary mechanism of action of dipyridamole?

A

A: Dipyridamole works by inhibiting phosphodiesterase, leading to increased levels of cyclic adenosine monophosphate (cAMP) in platelets, which inhibits platelet activation and aggregation.

152
Q

B.44 Anticoagulant and Antiplatelet TX

What formulations of dipyridamole are commonly used?

A

A: Dipyridamole is available in an oral form, and it is often used in an extended-release formulation combined with low-dose aspirin, known as Aggrenox.

153
Q

B.44 Anticoagulant and Antiplatelet TX

What are the indications for dipyridamole?

A

A: Dipyridamole is indicated for the secondary prevention of stroke in patients with a history of transient ischemic attacks (TIAs) or ischemic stroke when used in combination with aspirin.

154
Q

B.44 Anticoagulant and Antiplatelet TX

How effective is dipyridamole in combination with aspirin compared to aspirin alone?

A

A: Studies have shown that dipyridamole combined with aspirin can reduce the risk of recurrent stroke compared to aspirin alone.

155
Q

B.44 Anticoagulant and Antiplatelet TX

What are common side effects associated with dipyridamole?

A

A: Common side effects include headaches, gastrointestinal complaints, dizziness, facial flushing, and hypotension due to its vasodilatory effects.

156
Q

B.44 Anticoagulant and Antiplatelet TX

In what patient populations should dipyridamole be used with caution?

A

A: Dipyridamole should be used cautiously in patients with coronary artery disease due to its potential vasodilatory effects.

157
Q

B.44 Anticoagulant and Antiplatelet TX

Why is dipyridamole not recommended for patients with symptomatic coronary artery disease?

A

A: Due to limited data supporting its effectiveness in this population and the risk of vasodilatory side effects, alternative antiplatelet therapies, such as clopidogrel, are preferred.

158
Q

B.44 Anticoagulant and Antiplatelet TX

Can dipyridamole be used as a monotherapy for antiplatelet treatment?

A

A: Dipyridamole is generally not effective as a monotherapy for antiplatelet treatment; it is most effective when used in combination with aspirin.

159
Q

B.44 Anticoagulant and Antiplatelet TX

What is cilostazol?

A

A: Cilostazol is an antiplatelet medication primarily used to treat intermittent claudication in patients with peripheral artery disease (PAD).

160
Q

B.44 Anticoagulant and Antiplatelet TX

What is the mechanism of action of cilostazol?

A

A: Cilostazol inhibits phosphodiesterase type 3 (PDE3), leading to increased levels of cyclic adenosine monophosphate (cAMP) in platelets, which reduces platelet aggregation and promotes vasodilation.

161
Q

B.44 Anticoagulant and Antiplatelet TX

What is cilostazol primarily indicated for?

A

A: Cilostazol is indicated for the management of intermittent claudication, improving walking distance and quality of life in patients with PAD.

162
Q

B.44 Anticoagulant and Antiplatelet TX

What is the recommended dosing for cilostazol?

A

A: The typical dosing regimen for cilostazol is 100 mg taken twice daily.

163
Q

B.44 Anticoagulant and Antiplatelet TX

What are common side effects of cilostazol?

A

A: Common side effects include headache, diarrhea, dizziness, palpitations, and peripheral edema.

164
Q

B.44 Anticoagulant and Antiplatelet TX

Are there any contraindications for cilostazol?

A

A: Yes, cilostazol is contraindicated in patients with heart failure of any severity due to potential worsening of the condition.

165
Q

B.44 Anticoagulant and Antiplatelet TX

How does cilostazol compare to other antiplatelet agents?

A

A: Cilostazol is specifically effective for improving exercise tolerance in patients with PAD, but it may not be as widely used for other indications like myocardial infarction prevention.

166
Q

B.44 Anticoagulant and Antiplatelet TX

Can cilostazol be used in combination with other antiplatelet therapies?

A

A: Yes, cilostazol can be used with other agents like aspirin, but careful monitoring is necessary to avoid increased bleeding risk.

167
Q

B.44 Anticoagulant and Antiplatelet TX

What is an important consideration for cilostazol’s effectiveness?

A

A: Cilostazol may take several weeks to show significant improvement in symptoms, thus patience and adherence to the treatment regimen are essential.

168
Q

B.44 Anticoagulant and Antiplatelet TX

What lifestyle modifications can enhance the efficacy of cilostazol in treating PAD?

A

A: Patients should be advised to engage in a supervised exercise program and make lifestyle changes such as smoking cessation to maximize the benefits of cilostazol.

169
Q

B.44 Anticoagulant and Antiplatelet TX

What is ticagrelor?

A

A: Ticagrelor is an oral antiplatelet medication used to reduce the risk of thrombotic cardiovascular events in patients with acute coronary syndrome or those undergoing percutaneous coronary intervention.

170
Q

B.44 Anticoagulant and Antiplatelet TX

How does ticagrelor work?

A

A: Ticagrelor selectively inhibits the P2Y12 ADP receptor on platelets, leading to reversible inhibition of platelet activation and aggregation, which helps prevent clot formation.

171
Q

B.44 Anticoagulant and Antiplatelet TX

What is the onset of action for ticagrelor compared to clopidogrel?

A

A: Ticagrelor has a more rapid onset of action than clopidogrel, as it does not require metabolic activation.

172
Q

B.44 Anticoagulant and Antiplatelet TX

What is the typical dosing regimen for ticagrelor?

A

A: The usual dosing regimen for ticagrelor is an initial loading dose of 180 mg, followed by 90 mg twice daily.

173
Q

B.44 Anticoagulant and Antiplatelet TX

What are the major indications for ticagrelor?

A

A: Ticagrelor is indicated for the secondary prevention of atherothrombotic events in patients with acute coronary syndrome and can also be used following percutaneous coronary intervention.

174
Q

B.44 Anticoagulant and Antiplatelet TX

What are common side effects of ticagrelor?

A

A: Common side effects include bleeding, dyspnea (shortness of breath), and asymptomatic ventricular pauses.

175
Q

B.44 Anticoagulant and Antiplatelet TX

How is ticagrelor metabolized?

A

A: Ticagrelor is primarily metabolized in the liver via the CYP3A4 enzyme, which can be affected by other medications that inhibit or induce this enzyme.

176
Q

B.44 Anticoagulant and Antiplatelet TX

What should be noted about ticagrelor and surgery?

A

A: Ticagrelor should be discontinued at least 5 days prior to major surgery to reduce the risk of bleeding.

177
Q

B.44 Anticoagulant and Antiplatelet TX

What is unique about ticagrelor’s effect on platelet function?

A

A: Unlike clopidogrel, ticagrelor provides greater and more predictable inhibition of platelet aggregation, making it a preferred option in higher-risk patients.

178
Q

B.44 Anticoagulant and Antiplatelet TX

Is there an antidote for ticagrelor-related bleeding?

A

A: While platelet transfusions may not be effective due to ticagrelor’s mechanism, a reversal agent called bentracimab is under development to rapidly reverse ticagrelor’s effects in emergency situations.

179
Q

B.44 Anticoagulant and Antiplatelet TX

A

What is dual antiplatelet therapy (DAPT)?
A: DAPT is the use of two antiplatelet medications concurrently to reduce the risk of thrombotic events, typically combining aspirin with a second antiplatelet agent, such as clopidogrel or ticagrelor.

180
Q

B.44 Anticoagulant and Antiplatelet TX

Why is DAPT used?

A

A: DAPT is used to prevent cardiovascular events, particularly after procedures like coronary stenting or in patients with acute coronary syndrome (ACS).

181
Q

B.44 Anticoagulant and Antiplatelet TX

A

A: DAPT is used to prevent cardiovascular events, particularly after procedures like coronary stenting or in patients with acute coronary syndrome (ACS).

182
Q

B.44 Anticoagulant and Antiplatelet TX

What are the indications for DAPT?

A

A: Indications include post-percutaneous coronary intervention (PCI), acute myocardial infarction (AMI), and non-ST elevation myocardial infarction (NSTEMI).

183
Q

B.44 Anticoagulant and Antiplatelet TX

What is the main mechanism of action of aspirin in DAPT?

A

A: Aspirin irreversibly inhibits cyclooxygenase-1 (COX-1), leading to decreased thromboxane A2 production, which reduces platelet activation and aggregation.

184
Q

B.44 Anticoagulant and Antiplatelet TX

How does clopidogrel work in DAPT?

A

A: Clopidogrel irreversibly inhibits the P2Y12 ADP receptor on platelets, preventing their activation and aggregation in response to adenosine diphosphate (ADP).

185
Q

B.44 Anticoagulant and Antiplatelet TX

What is the recommended duration of DAPT after coronary stenting?

A

A: DAPT is usually recommended for at least 6-12 months after drug-eluting stent placement, while bare metal stents typically require at least 1 month of DAPT.

186
Q

B.44 Anticoagulant and Antiplatelet TX

What are the risks associated with DAPT?

A

A: The main risk is increased bleeding, including gastrointestinal bleeding and intracranial hemorrhage, particularly in older adults or those with a history of bleeding disorders.

187
Q

B.44 Anticoagulant and Antiplatelet TX

How does ticagrelor differ from clopidogrel in DAPT?

A

A: Ticagrelor is a reversible inhibitor of the P2Y12 receptor, has a faster onset of action, and does not require metabolic activation, making it more effective in some patients.

188
Q

B.44 Anticoagulant and Antiplatelet TX

What factors influence the decision to use DAPT?

A

A: Factors include the type of stent used, the patient’s risk of thrombotic versus bleeding events, and clinical guidelines based on the patient’s overall health and history of cardiovascular disease.