(4.5) ANTI-PLATELET PHARMACOLOGY
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Questions and Answers

What role does phosphodiesterase play in platelet activation?

  • It promotes the formation of fibrin.
  • It activates cyclic AMP.
  • It breaks down cyclic AMP into other products. (correct)
  • It inhibits platelet plug disintegration.
  • How does increasing cyclic AMP levels affect platelets?

  • It inhibits platelet activation. (correct)
  • It activates fibrinogen conversion.
  • It promotes platelet aggregation.
  • It increases clot production.
  • What is the function of TPA in the context of clot formation?

  • To stimulate platelet aggregation.
  • To promote the formation of fibrinogen.
  • To initiate the disintegration of clots. (correct)
  • To prevent the breakdown of fibrin.
  • Which factors contribute to the finalization of clot formation?

    <p>Fibrin and fibrinogen.</p> Signup and view all the answers

    Which statement accurately describes glycoproteins in platelet physiology?

    <p>They are identified by distinct numbering.</p> Signup and view all the answers

    What would be the clinical implication of inhibiting phosphodiesterase?

    <p>Increased cyclic AMP levels leading to reduced clot production.</p> Signup and view all the answers

    What is the primary mechanism by which antiplatelet therapies may act?

    <p>By inhibiting phosphodiesterase activity.</p> Signup and view all the answers

    What is the main reason for chewing enteric-coated baby aspirin during a heart attack?

    <p>To break the enteric coating for faster absorption</p> Signup and view all the answers

    What type of bond does clopidogrel create with its receptor during activation?

    <p>Disulfide bond</p> Signup and view all the answers

    Which factor is essential for the activation of clopidogrel into its active form?

    <p>CYP2C19 enzyme</p> Signup and view all the answers

    Which scenario makes clopidogrel an unsuitable choice for a patient?

    <p>Being a poor metabolizer of CYP2C19</p> Signup and view all the answers

    In what clinical situations would clopidogrel be administered?

    <p>Post myocardial infarction and after stent placement</p> Signup and view all the answers

    What mechanism allows aspirin to bind irreversibly to COX-1?

    <p>Acetylation of a serine residue</p> Signup and view all the answers

    Why is the irreversible action of aspirin particularly significant for platelets?

    <p>Platelets cannot synthesize new COX-1</p> Signup and view all the answers

    How does the action of reversible inhibitors like ibuprofen differ from aspirin?

    <p>Reversible inhibitors dissociate easily from receptors</p> Signup and view all the answers

    What is the average lifespan of a platelet that has been inhibited by aspirin?

    <p>28 days</p> Signup and view all the answers

    In patients with ischemic events, why is aspirin often recommended as part of their treatment?

    <p>It prevents further clot formation</p> Signup and view all the answers

    When a stent is inserted, why is aspirin commonly administered?

    <p>To prevent clot formation on the stent</p> Signup and view all the answers

    Which of the following best describes the nature of aspirin as an antiplatelet therapy?

    <p>It is an irreversible inhibitor of COX-1</p> Signup and view all the answers

    What is a common side effect of taking NSAIDs, specifically related to cardiovascular health?

    <p>Increased risk of myocardial infarction upon discontinuation</p> Signup and view all the answers

    Which antiplatelet drug class does aspirin belong to?

    <p>Irreversible inhibitors</p> Signup and view all the answers

    What role does acetylation play in the mechanism of action of aspirin?

    <p>It leads to irreversible inhibition of COX-1</p> Signup and view all the answers

    Which antiplatelet agent irreversibly inhibits P2Y12 receptors on platelets?

    <p>Clopidogrel</p> Signup and view all the answers

    What mechanism does aspirin use to exert its antiplatelet effects?

    <p>Acetylation of cyclooxygenase-1</p> Signup and view all the answers

    Which antiplatelet drug is known to inhibit the final common pathway of platelet aggregation?

    <p>Eptifibatide</p> Signup and view all the answers

    What is a common adverse effect of antiplatelet medications?

    <p>Risk of gastrointestinal bleeding</p> Signup and view all the answers

    In which clinical situation is the use of Vorapaxar particularly indicated?

    <p>Long-term prevention of thrombotic cardiovascular events</p> Signup and view all the answers

    Which mechanism is primarily targeted by PAR-1 antagonists in antiplatelet therapy?

    <p>Inhibition of protease-activated receptor signaling</p> Signup and view all the answers

    What is a key adverse effect commonly associated with the use of antiplatelet medications?

    <p>Gastrointestinal bleeding</p> Signup and view all the answers

    In the context of thrombosis pathophysiology, the role of thromboxane A2 (TxA2) is best described as:

    <p>Stimulating platelet activation and aggregation</p> Signup and view all the answers

    Which antiplatelet drug is known for its irreversible inhibition of cyclooxygenase (COX-1)?

    <p>Aspirin</p> Signup and view all the answers

    Which of the following antiplatelet medications specifically targets the ADP receptor?

    <p>Clopidogrel</p> Signup and view all the answers

    Platelet plug formation primarily requires which of the following factors to stabilize the plug?

    <p>Fibrinogen</p> Signup and view all the answers

    What is a primary clinical application of antiplatelet therapy?

    <p>To prevent arterial thrombosis and myocardial infarction</p> Signup and view all the answers

    Which of the following antiplatelet agents acts by irreversibly binding to the ADP receptor?

    <p>Clopidogrel</p> Signup and view all the answers

    What is one of the main adverse effects associated with the use of GPIIb/IIIa inhibitors?

    <p>Bleeding</p> Signup and view all the answers

    Which mechanism describes how aspirin functions as an antiplatelet drug?

    <p>Irreversible acetylation of COX-1</p> Signup and view all the answers

    What does the administration of phosphodiesterase inhibitors like Cilostazol primarily help achieve?

    <p>Inhibit platelet activation via cAMP</p> Signup and view all the answers

    Which condition is NOT an indication for the use of Ticagrelor?

    <p>Treatment of acute asthma exacerbation</p> Signup and view all the answers

    What important enzyme does Clopidogrel require for its activation?

    <p>CYP2C19</p> Signup and view all the answers

    Which kind of drug is Abciximab classified as and what is its primary function?

    <p>Antibody; inhibits GPIIb/IIIa receptors</p> Signup and view all the answers

    In patients classified as CYP2C19 poor metabolizers, what is a potential risk with Clopidogrel?

    <p>Ineffective activation leading to increased thrombotic events</p> Signup and view all the answers

    What is a common indication for GPIIb/IIIa inhibitors like Eptifibatide?

    <p>Prevention of thrombotic events during PCI</p> Signup and view all the answers

    What is the expected clinical effect of using phosphodiesterase inhibitors in platelet management?

    <p>Inhibition of platelet aggregation</p> Signup and view all the answers

    Study Notes

    Anti-Platelet Pharmacology

    • Goal: Prevent heart attacks and strokes by inhibiting platelet activation.
    • Electron micrograph shows inactivated vs. activated platelets.
    • Key markers (from the presentation) are essential for understanding drug effects on platelet levels.
    • Focus is on one drug per drug class.

    Platelet Activation

    • Cholesterol deposits in artery walls, exposing collagen.
    • Collagen triggers platelet activation cascade.
    • Three main steps in platelet plug formation:
      • Adhesion (platelets stick to collagen).
      • Granule release (messengers attract other platelets).
      • Aggregation (platelets clump together).
    • Healthy endothelium prevents collagen exposure.
    • Nitric oxide and prostacyclin regulate platelet activation by increasing cyclic AMP, reducing calcium availability.

    Aspirin

    • Inhibits cyclooxygenase (COX-1) irreversibly.
    • Prevents thromboxane A2 production.
    • Prevents platelet aggregation.
    • Adverse effect: GI bleeding.

    Other Antiplatelet Drugs

    • P2Y12 inhibitors (e.g., clopidogrel):
      • Inhibit ADP-induced platelet aggregation.
      • Clopidogrel requires metabolism by CYP2C19.
    • GP2B3A inhibitors (e.g., abciximab, tirofiban):
      • Block fibrinogen binding.
      • Used primarily during procedures (e.g., angioplasty).
    • Adverse effects vary by drug.
    • Important to consider individual patient factors such as metabolic rate of CYP2C19, and whether they have known bleeding issues

    Phosphodiesterase inhibitors

    • Inhibit cyclic AMP breakdown, increasing cyclic AMP levels which inhibits platelet activation.
    • Psilocybin/PDE3 inhibitors work on similar mechanism.
    • Usage varies based on individual patient factors and condition.

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    Description

    This quiz focuses on the pharmacology of anti-platelet drugs, specifically their role in preventing heart attacks and strokes. It covers platelets' activation process, including crucial steps such as adhesion, granule release, and aggregation. Key drugs like Aspirin and their mechanisms will also be highlighted.

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