Ch 23 pp. 424-426
81 Questions
4 Views

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition
Chat to lesson

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

Which statement about tenecteplase is accurate?

  • It has increased fibrin specificity compared to t-PA (correct)
  • It is less resistant to plasminogen activator inhibitor 1 than t-PA
  • It has a shorter half-life than t-PA
  • It is administered as a double bolus
  • What distinguishes reteplase from streptokinase and t-PA?

  • It is administered as a single weight-based bolus
  • It has longer half-life and increased fibrin specificity (correct)
  • It is less effective in treating thrombosis
  • It has a shorter half-life than streptokinase
  • What is the role of protamine in anticoagulation?

  • It reverses the effects of heparin (correct)
  • It increases the effects of heparin
  • It is an agonist of heparin
  • It forms a stable complex with fibrin
  • How does tenecteplase compare to t-PA in terms of bleeding risk?

    <p>Similar (and possibly decreased) risk of bleeding</p> Signup and view all the answers

    What allows tenecteplase to be administered as a single weight-based bolus?

    <p>Its longer half-life</p> Signup and view all the answers

    How is reteplase administered?

    <p>As a double bolus</p> Signup and view all the answers

    Which adverse effect is associated with ticlopidine?

    <p>Aplastic anemia</p> Signup and view all the answers

    What is the primary clinical use of clopidogrel?

    <p>Secondary prevention of atherosclerotic events</p> Signup and view all the answers

    Which platelet inhibitor is a reversible inhibitor of the P2Y12 ADP receptor?

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

    What is the mechanism of action of GPIIb-IIIa antagonists?

    <p>Prevent binding of fibrinogen and other adhesion ligands</p> Signup and view all the answers

    What is the primary use of prasugrel?

    <p>Acute coronary syndromes with percutaneous coronary intervention</p> Signup and view all the answers

    Which adverse effect is associated with eptifibatide?

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

    Which medication is a competitive inhibitor of protease-activated receptor 1 (PAR-1)?

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

    Which medication is an indirect inhibitor of factor Xa with negligible anti-thrombin activity?

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

    Which medication has many contraindications and inhibits hepatic epoxide reductase?

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

    Which type of heparin is used for open-heart surgery and disseminated intravascular coagulation?

    <p>Unfractionated heparin</p> Signup and view all the answers

    Which medication is a selective Factor Xa Inhibitor used for prophylaxis and treatment of deep vein thrombosis and pulmonary embolism?

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

    Which medication has a higher incidence of heparin-induced thrombocytopenia?

    <p>Unfractionated heparin</p> Signup and view all the answers

    Which agent is ineffective against fondaparinux?

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

    Which agent inhibits serine proteases plasmin, t-PA, and thrombin, but may increase the risk of postoperative acute renal failure and fatal anaphylactic reactions?

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

    Which agents are lysine analogues that inhibit plasminogen and plasmin, used to reduce perioperative bleeding during coronary artery bypass grafting without increasing the risk of postoperative acute renal failure?

    <p>Aminocaproic acid and tranexamic acid</p> Signup and view all the answers

    What do antiplatelet agents primarily interfere with?

    <p>Platelet adhesion, release reaction, and aggregation</p> Signup and view all the answers

    What do anticoagulants primarily target?

    <p>Plasma coagulation factors</p> Signup and view all the answers

    What do thrombolytic agents mediate?

    <p>Clot dissolution by promoting the conversion of plasminogen to plasmin</p> Signup and view all the answers

    Which of the following is a shared adverse effect of Apixaban and Rivaroxaban?

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

    How often is Apixaban administered?

    <p>Twice daily</p> Signup and view all the answers

    Which thrombolytic agent is used for ST elevation myocardial infarction and deep vein thrombosis?

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

    What is the primary use of recombinant activated protein C (r-APC)?

    <p>Severe sepsis with organ dysfunction and high risk of death</p> Signup and view all the answers

    Which thrombolytic agent is a genetically engineered variant of t-PA with increased specificity for fibrin?

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

    What is the primary indication for dabigatran?

    <p>Prevention of thromboembolism in non-valvular atrial fibrillation</p> Signup and view all the answers

    What distinguishes tenecteplase from t-PA?

    <p>Increased fibrin specificity and resistance to plasminogen activator inhibitor 1</p> Signup and view all the answers

    What is a distinguishing feature of reteplase compared to streptokinase and t-PA?

    <p>Longer half-life and increased specificity for fibrin</p> Signup and view all the answers

    What is the primary role of protamine in anticoagulation?

    <p>To reverse the effects of heparin in life-threatening hemorrhage</p> Signup and view all the answers

    How is reteplase administered?

    <p>As a 'double bolus' (two boluses, 30 minutes apart)</p> Signup and view all the answers

    Which of the following is a potential adverse effect of direct thrombin inhibitors?

    <p>Cerebral ischemia</p> Signup and view all the answers

    What is the primary use of Argatroban?

    <p>Coronary artery thrombosis</p> Signup and view all the answers

    Which thrombolytic agent is used for acute cerebrovascular thrombosis?

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

    What distinguishes tenecteplase and reteplase from streptokinase and t-PA?

    <p>Higher specificity for fibrin</p> Signup and view all the answers

    Which medication is used for prophylaxis against deep vein thrombosis and anticoagulation in patients undergoing coronary angiography and angioplasty?

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

    What is the primary use of recombinant activated protein C (r-APC)?

    <p>Severe sepsis with organ dysfunction</p> Signup and view all the answers

    Which medication is associated with anaphylactoid reactions and stroke as potential adverse effects?

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

    What is the primary indication for dabigatran?

    <p>Non-valvular atrial fibrillation</p> Signup and view all the answers

    How is apixaban administered?

    <p>Twice daily</p> Signup and view all the answers

    What is a potential adverse effect of rivaroxaban?

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

    What distinguishes recombinant tissue plasminogen activator (t-PA) from tenecteplase and reteplase?

    <p>Increased risk of intracranial hemorrhage</p> Signup and view all the answers

    Which agent is used for prevention of thromboembolism in non-valvular atrial fibrillation?

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

    Which factor Xa inhibitor has negligible anti-thrombin (anti-IIa) activity?

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

    What is the primary clinical use of Vorapaxar?

    <p>Prevention of myocardial infarction, stroke, and cardiovascular death</p> Signup and view all the answers

    Which medication is an indirect inhibitor of factor Xa with specific indications for prophylaxis and treatment of deep vein thrombosis and pulmonary embolism?

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

    Which anticoagulant is used for various conditions, including open-heart surgery and disseminated intravascular coagulation?

    <p>Unfractionated heparin</p> Signup and view all the answers

    Which anticoagulant has selective inactivation mechanisms that differ from low-molecular-weight heparins?

    <p>Unfractionated heparin</p> Signup and view all the answers

    Which anticoagulant is a competitive inhibitor of protease-activated receptor 1 (PAR-1)?

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

    Which anticoagulant has specific contraindications and should be avoided in certain conditions?

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

    Which anticoagulant inhibits hepatic epoxide reductase and has many contraindications?

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

    Which anticoagulant is used for specific indications and has its own adverse effects, including drug–drug interactions that must be carefully considered?

    <p>Low-molecular-weight heparins</p> Signup and view all the answers

    Which anticoagulant has a higher incidence of heparin-induced thrombocytopenia compared to low-molecular-weight heparins?

    <p>Unfractionated heparin</p> Signup and view all the answers

    Which anticoagulant is a selective Factor Xa Inhibitor used for prophylaxis and treatment of deep vein thrombosis and pulmonary embolism?

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

    Which anticoagulant must be carefully considered for drug–drug interactions, especially with albumin-bound drugs and those that induce and/or compete for P450 metabolism?

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

    What is the primary role of aprotinin in hemostasis?

    <p>Inhibiting plasminogen and plasmin</p> Signup and view all the answers

    What is the primary mechanism of action of aminocaproic acid and tranexamic acid?

    <p>Inhibiting plasminogen and plasmin</p> Signup and view all the answers

    What distinguishes hemostasis from pathologic thrombosis?

    <p>Response to vascular injury</p> Signup and view all the answers

    What is the primary target of antiplatelet agents?

    <p>Platelet adhesion</p> Signup and view all the answers

    What is the primary target of anticoagulants?

    <p>Coagulation factors</p> Signup and view all the answers

    What is the primary mechanism of action of thrombolytic agents?

    <p>Mediating clot dissolution</p> Signup and view all the answers

    What is a potential limitation of virtually every antithrombotic and thrombolytic agent?

    <p>Mechanism-based toxicity of bleeding</p> Signup and view all the answers

    What is the potential benefit of pharmacogenomic techniques in the field of hemostasis and thrombosis?

    <p>Identifying genetic risk of thrombosis</p> Signup and view all the answers

    What remains an opportunity for the development of therapies in hemostasis and thrombosis?

    <p>Targeting unexploited components of hemostasis</p> Signup and view all the answers

    What will be critical for optimizing the indications, dose, and duration of treatment for new drugs and drug combinations in this field?

    <p>Clinical trials</p> Signup and view all the answers

    What is the potential role of aspirin and warfarin in the field of hemostasis and thrombosis?

    <p>Orally bioavailable and inexpensive</p> Signup and view all the answers

    What is a likely challenge for new agents under development in the field of hemostasis and thrombosis?

    <p>Mechanism-based toxicity of bleeding</p> Signup and view all the answers

    Which adverse effect is associated with ticlopidine?

    <p>Aplastic anemia</p> Signup and view all the answers

    What is the primary use of clopidogrel?

    <p>Secondary prevention of atherosclerotic events</p> Signup and view all the answers

    What is the mechanism of action of GPIIb-IIIa antagonists?

    <p>Prevent binding of fibrinogen and other adhesion ligands</p> Signup and view all the answers

    What is the primary use of prasugrel?

    <p>Acute coronary syndromes with percutaneous coronary intervention</p> Signup and view all the answers

    Which adverse effect is associated with eptifibatide?

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

    What is the primary use of ticagrelor?

    <p>Acute coronary syndromes and percutaneous coronary intervention</p> Signup and view all the answers

    Which adverse effect is associated with abciximab?

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

    What is the primary use of dipyridamole?

    <p>Prophylaxis against thromboembolic disorders</p> Signup and view all the answers

    What is the primary use of ticlopidine?

    <p>Prophylaxis against thromboembolic disorders</p> Signup and view all the answers

    What is the primary use of ticlopidine?

    <p>Prophylaxis against thromboembolic disorders</p> Signup and view all the answers

    What is the primary use of ticlopidine?

    <p>Prophylaxis against thromboembolic disorders</p> Signup and view all the answers

    Study Notes

    Anticoagulant and Thrombolytic Agents: Key Points

    • Apixaban and Rivaroxaban are used for different indications including prevention of thromboembolism and treatment of deep vein thrombosis and pulmonary embolism.
    • Both drugs have shared adverse effects such as hematoma, hemorrhage, and severe hypersensitivity reactions.
    • Apixaban is administered twice daily, while rivaroxaban is administered once daily.
    • Direct thrombin inhibitors include lepirudin, desirudin, and bivalirudin, and are used for prophylaxis against deep vein thrombosis and anticoagulation in patients undergoing coronary angiography and angioplasty.
    • These inhibitors have adverse effects like hemorrhage, cerebral ischemia, and peripheral nerve paralysis.
    • Argatroban is used for coronary artery thrombosis and prophylaxis in percutaneous coronary intervention, and can cause gastrointestinal, intracranial, and genitourinary tract hemorrhage.
    • Dabigatran is used for prevention of thromboembolism in non-valvular atrial fibrillation and treatment of deep vein thrombosis and pulmonary embolism.
    • Recombinant activated protein C (r-APC) is used for severe sepsis with organ dysfunction and high risk of death, but is associated with hemorrhage and contraindications such as intracranial mass and recent intracranial surgery.
    • Streptokinase is used for ST elevation myocardial infarction and deep vein thrombosis, but can cause major bleeding and intracranial hemorrhage.
    • Recombinant tissue plasminogen activator (t-PA) (Alteplase) is used for acute myocardial infarction, acute cerebrovascular thrombosis, and pulmonary embolism, and can cause intracranial hemorrhage and sepsis.
    • Tenecteplase and reteplase are genetically engineered variants of t-PA with increased specificity for fibrin and cause adverse effects such as gastrointestinal and intracranial hemorrhage.
    • These thrombolytic agents have potential contraindications and adverse effects, including anaphylactoid reactions and stroke.

    Pharmacology of Hemostasis and Thrombosis

    • Protamine is effective against large unfractionated heparin molecules and can partially reverse the anticoagulant effects of low-molecular-weight heparins, but it is inactive against fondaparinux.
    • Aprotinin inhibits serine proteases plasmin, t-PA, and thrombin, promoting clot stabilization, but may increase the risk of postoperative acute renal failure and fatal anaphylactic reactions.
    • Aminocaproic acid and tranexamic acid are lysine analogues that inhibit plasminogen and plasmin, used to reduce perioperative bleeding during coronary artery bypass grafting without increasing the risk of postoperative acute renal failure.
    • Hemostasis regulates blood fluidity and forms stable fibrin-based clots in response to vascular injury, while pathologic thrombosis results from endothelial injury, abnormal blood flow, and hypercoagulability.
    • Antiplatelet agents interfere with platelet adhesion, release reaction, and aggregation, providing prophylaxis against thrombosis in susceptible individuals.
    • Anticoagulants primarily target plasma coagulation factors and disrupt the coagulation cascade by inhibiting crucial intermediates.
    • Thrombolytic agents mediate clot dissolution by promoting the conversion of plasminogen to plasmin.
    • Effective, orally bioavailable, and inexpensive therapeutic agents like aspirin and warfarin are already available for many clinical indications in this field.
    • Virtually every antithrombotic and thrombolytic agent is associated with the mechanism-based toxicity of bleeding, which is likely to plague new agents under development.
    • Pharmacogenomic techniques may identify individuals with an increased genetic risk of thrombosis who may benefit from long-term antithrombotic treatment.
    • Opportunities remain for the development of safer and more effective antiplatelet, anticoagulant, and thrombolytic therapies, including new agents targeting unexploited components of hemostasis.
    • Carefully designed clinical trials will be critical to optimize the indications, dose, and duration of treatment for new drugs and drug combinations.

    Platelet Inhibitors: Mechanisms and Clinical Considerations

    • Phosphodiesterase inhibitors like dipyridamole inhibit platelet cAMP degradation, used for prophylaxis against thromboembolic disorders and as an alternative in thallium myocardial perfusion imaging.
    • Dipyridamole adverse effects include exacerbation of angina, liver failure, stroke, and rare bronchospasm.
    • Ticlopidine, clopidogrel, prasugrel, and ticagrelor are ADP receptor pathway inhibitors with varying clinical uses and adverse effects.
    • Ticlopidine adverse effects include aplastic anemia, neutropenia, and thrombotic thrombocytopenic purpura.
    • Clopidogrel is used for secondary prevention of atherosclerotic events and acute coronary syndromes, with less myelotoxicity than ticlopidine.
    • Prasugrel is used for acute coronary syndromes with percutaneous coronary intervention and has a more efficient platelet inhibition but increased bleeding risk compared to clopidogrel.
    • Ticagrelor is a reversible inhibitor of the P2Y12 ADP receptor, used for acute coronary syndromes and percutaneous coronary intervention.
    • GPIIb-IIIa antagonists like eptifibatide, abciximab, and tirofiban prevent binding of fibrinogen and other adhesion ligands.
    • Eptifibatide is used for acute coronary syndromes and percutaneous coronary intervention, with major bleeding and thrombocytopenia as adverse effects.
    • Abciximab is used as an adjunct to percutaneous coronary intervention to prevent acute cardiac ischemic complications, with thrombocytopenia and stroke as adverse effects.
    • Tirofiban is used for acute coronary syndromes and has similar therapeutic considerations as eptifibatide, but is a nonpeptide tyrosine analogue.
    • GPIIb-IIIa antagonists have specific contraindications and considerations, such as avoiding co-administration with a second antagonist and minimizing use in certain medical conditions.

    Studying That Suits You

    Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

    Quiz Team

    Description

    Test your knowledge of anticoagulant and thrombolytic agents with this quiz. Explore indications, administration, adverse effects, and contraindications of drugs such as Apixaban, Rivaroxaban, Direct Thrombin Inhibitors, Argatroban, Dabigatran, Recombinant Activated Protein C, Streptokinase, and Recombinant Tissue Plasminogen Activator.

    More Like This

    Anticoagulants and Thrombolytics Quiz
    38 questions
    Pharmacology Chapter 40 Quiz
    18 questions
    Use Quizgecko on...
    Browser
    Browser