PharmDecks

Heart & Respiratory Disease Management

Introduction

  • Thrombosis is the formation of blood clots, which can be life-threatening when they form in arteries (arterial thrombosis) or veins (venous thrombosis).
  • Antithrombotic agents are a class of medications that prevent or reduce the formation of these potentially deadly blood clots.
  • These agents are broadly classified into anticoagulants and antiplatelets, each targeting different aspects of the clotting process.

Anticoagulants

  • Anticoagulants primarily work by inhibiting the coagulation cascade and the formation of fibrin, a protein that forms the meshwork of a blood clot.
  • They decrease the blood’s ability to clot, either by breaking down existing clots or by preventing new ones from forming.
  • Commonly used to treat and prevent conditions like strokes, pulmonary embolisms, and heart attacks in individuals with increased risk factors.

A. Types of Anticoagulants

  1. Intravenous and Injectable Anticoagulants

    • Heparin and its derivatives:
      • Unfractionated heparin (UFH): Activates antithrombin, requiring constant monitoring due to bleeding risk.
      • Low-molecular-weight heparin (LMWH): More predictable effects and does not require the same level of monitoring as UFH.
      • Fondaparinux: A synthetic medication similar to heparin, mainly used for clot prevention.
    • Direct Thrombin Inhibitors: Prevent thrombin from promoting clotting, used post-surgery to prevent clot formation (e.g., argatroban, desirudin, bivalirudin).
  2. Oral Anticoagulants

    • Warfarin (Vitamin K antagonist): Blocks Vitamin K utilisation, essential in clotting. Requires lab testing due to bleeding risk.
    • Direct Oral Anticoagulants (DOACs): Target specific clotting factors, e.g., Dabigatran (direct thrombin inhibitor) and Factor Xa inhibitors (e.g., apixaban, rivaroxaban), often without needing regular lab testing.

B. Advantages and Disadvantages of Anticoagulants

  • Advantages:
    • Effective for preventing life-threatening conditions due to clots.
    • Variety of forms allows treatment tailored to individual needs.
  • Disadvantages:
    • Bleeding is the most common side effect.
    • Warfarin has a high bleeding risk and requires careful dosing.
    • Heparin may cause heparin-induced thrombocytopenia (HIT), a dangerous condition.

Antiplatelets

  • Antiplatelets inhibit clot formation by preventing platelet activation and aggregation.
  • They are primarily used to treat and prevent heart attacks and strokes caused by clots.

A. Types of Antiplatelet and Mechanisms

  • Aspirin: Irreversibly inhibits the cyclooxygenase enzyme, preventing platelet aggregation.
  • ADP Receptor Inhibitors: (e.g., clopidogrel) Prevent ADP-induced platelet aggregation.
  • Glycoprotein IIb/IIIa Inhibitors: Block receptors that promote platelet aggregation, often used in acute coronary syndrome.
  • Dipyridamole & Cilostazol: Increase intra-platelet cyclic AMP, inhibiting aggregation and inducing vasodilation.

B. Advantages and Disadvantages of Antiplatelets

  • Advantages:
    • Effective in preventing heart attacks and strokes.
    • Help relieve symptoms like chest pain and shortness of breath.
  • Disadvantages:
    • Excessive bleeding and drug interactions are common risks.
    • Potential side effects include asthma, heavy bleeding, and stomach upset.

Key Differences Between Anticoagulants and Antiplatelets

  • Target: Anticoagulants target the coagulation cascade, while antiplatelet target platelets.
  • Mechanism: Anticoagulants inhibit fibrin formation, and antiplatelet inhibit platelet aggregation.
  • Monitoring: Some anticoagulants require regular blood tests, but antiplatelet generally do not.

References

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