Pharmacology of the Blood
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Questions and Answers

What should be administered to counteract excessive anticoagulation and bleeding due to an overdose?

  • Vitamin K
  • Coumadin
  • Warfarin
  • Protamine sulfate (correct)
  • Which drug is commonly used as a rodenticide due to its ability to produce fatal internal bleeding?

  • Heparin
  • Rivaroxaban
  • Dabigatran
  • Warfarin (correct)
  • What factor does warfarin inhibit that is crucial for blood coagulation?

  • Vitamin K-dependent clotting factors (correct)
  • Fibrinogen
  • Thrombin
  • Factor XIII
  • Which of the following is a characteristic of warfarin and coumarin derivatives?

    <p>High protein binding</p> Signup and view all the answers

    Which new drug is highlighted as a promising thrombin inhibitor?

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

    What is a notable disadvantage of new anticoagulants like dabigatran?

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

    What advantage do direct factor Xa inhibitors have over thrombin inhibitors?

    <p>Less bleeding adverse events</p> Signup and view all the answers

    What potential interaction should be considered when using heparin?

    <p>Use with anticoagulant drugs that interfere with coagulation</p> Signup and view all the answers

    What is the primary role of the active metabolite of clopidogrel?

    <p>To provide antiplatelet effects</p> Signup and view all the answers

    Which of the following conditions is clopidogrel used to treat in veterinary medicine?

    <p>Feline arterial thromboembolism</p> Signup and view all the answers

    What initiates the process of fibrinolysis in a platelet clot?

    <p>Activation of plasminogen by endothelial cells</p> Signup and view all the answers

    What is a significant concern regarding the use of fibrinolytic agents in animals?

    <p>There is a lack of evidence supporting their efficacy</p> Signup and view all the answers

    Which of the following best describes the action of plasminogen-activating agents?

    <p>They enhance the conversion of plasminogen to plasmin</p> Signup and view all the answers

    Excessive fibrinolysis can lead to which of the following conditions?

    <p>Excessive bleeding disorders</p> Signup and view all the answers

    Which of the following drugs is an antifibrinolytic agent used for hyperfibrinolytic conditions?

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

    Which condition has not been associated with successful treatment using fibrinolytic agents in animals?

    <p>Healthy rabbits</p> Signup and view all the answers

    What are the two forms of heparin mentioned?

    <p>Unfractionated heparin and low-molecular weight heparins</p> Signup and view all the answers

    Which factor is predominantly inhibited by heparin?

    <p>Thrombin (factor IIa)</p> Signup and view all the answers

    What is a primary indication for the use of heparin?

    <p>Preventing and treating thromboembolism</p> Signup and view all the answers

    What is a significant risk associated with the use of unfractionated heparin (UFH)?

    <p>Excessive bleeding due to increased anticoagulant activity</p> Signup and view all the answers

    Why is heparin usually administered subcutaneously (SC) or intravenously (IV)?

    <p>To avoid hematoma formation associated with intramuscular (IM) injection</p> Signup and view all the answers

    What major difference exists between the action of unfractionated heparin (UFH) and low-molecular weight heparins (LMWH)?

    <p>UFH binds to and inactivates thrombin, while LMWH only inhibits factor Xa</p> Signup and view all the answers

    What condition has been noted as a concern with heparin use in humans but generally not in animals?

    <p>Heparin-induced thrombocytopenia</p> Signup and view all the answers

    What is the role of anti-thrombin (AT) when heparin is administered?

    <p>To enhance the inhibitory effect on coagulation factors</p> Signup and view all the answers

    What is the primary use of desmopressin acetate (DDAVP) in the context of coagulation disorders?

    <p>To elevate levels of von Willebrand factor (vWF)</p> Signup and view all the answers

    Why is the response to low-dose aspirin in dogs considered inconsistent?

    <p>As many as 30% of dogs do not respond to it</p> Signup and view all the answers

    What is a critical limitation of administering desmopressin acetate repeatedly?

    <p>It reduces the effect of subsequent doses due to depletion of storage pools</p> Signup and view all the answers

    What role do platelets play in thrombus formation?

    <p>They form the initial plug and promote coagulation</p> Signup and view all the answers

    Which of the following is true regarding clopidogrel's mechanism of action?

    <p>It prevents ADP from promoting cyclic AMP-dependent aggregation</p> Signup and view all the answers

    What is the typical duration of elevation of von Willebrand factor (vWF) after administering DDAVP?

    <p>2-3 hours</p> Signup and view all the answers

    What is a major challenge associated with using heparin for dogs with immune-mediated hemolytic anemia?

    <p>Heparin is ineffective in these patients</p> Signup and view all the answers

    Which statement about aspirin and clopidogrel combination therapy is accurate?

    <p>They are both effective in preventing thrombi associated with specific cardiac conditions</p> Signup and view all the answers

    Study Notes

    Pharmacology of the Blood

    • The presentation covers hemostasis, anticoagulants, thrombin inhibitors, factor Xa inhibitors, agents for treating coagulopathies, antiplatelet drugs (aspirin and clopidogrel), fibrinolytic drugs, and antifibrinolytic drugs.

    Hemostasis

    • Hemostasis and the clotting cascade are revised
    • The clotting cascade involves vascular and platelet phases.
    • The clotting cascade includes inactive clotting factors that are activated.
    • Factors activated in the pathway include VIIa, Xa, Va and IIa (thrombin).
    • Heparin potentiates antithrombin inhibition.
    • Warfarin decreases factor VII, IX and X.

    Anticoagulants

    • Heparin, calcium, and sodium, are used to prevent and treat hypercoagulability.
    • It has direct and rapid effects by inactivating coagulation factors.
    • This can be used for thromboembolism, venous thrombosis, disseminated, and pulmonary.
    • Heparin is usually given via IV or SC. IM is not ideal because of causing potential hematomas.

    Heparin

    • Conventional form is unfractionated heparin (UFH)
    • Recent use has low-molecular-weight heparins (LMWH): tinzaparin, enoxaparin, and dalteparin.
    • Heparin binds with antithrombin, enhancing its inhibitory effects on thrombin and factors Xa and IXa.
    • UFH inactivates both factor Xa and thrombin increasing anticoagulation.
    • LMWH inactivates Xa since it's not big enough to bind thrombin.
    • Adverse effects include heparin induced thrombocytopenia which can lead to bleeding problems.
    • Excessive anticoagulation can be reversed by protamine sulfate.
    • Should be used cautiously with other drugs that interact with coagulation.

    Warfarin and Coumarin Derivatives

    • Warfarin sodium (Coumadin) is the most common.
    • It's a vitamin K antagonist.
    • These drugs inhibit the hepatic synthesis of vitamin K-dependent clotting factors (II, VII, IX, and X).
    • Warfarin and similar drugs are used as rodenticides because they cause fatal internal bleeding.

    Thrombin Inhibitors

    • Thrombin plays a significant role in producing anticoagulant effects.
    • Thrombin is the final step in the cascade.
    • Dabigatran etexilate (Pradaxa) is a prominent thrombin inhibitor.
    • Thrombin inhibitors are targeted because of the crucial role of thrombin in the final coagulation step.
    • Thrombin is an activator of platelets

    Factor Xa Inhibitors

    • Direct factor Xa inhibitors include rivaroxaban (Xarelto), apixaban (Eliquis), and edoxaban (Savaysa).
    • The inhibition of Xa apparently produces less bleeding adverse effects than thrombin inhibition.

    Agents for Treating Specific Coagulopathies

    • Desmopressin acetate (DDAVP) is a synthetic analogue of vasopressin
    • Used to treat central diabetes insipidus and to elevate von Willebrand factor (vWF) levels for short term elevations to help in surgical procedures/treat symptoms of vWD or to stop/reduce bleeding.
    • DDAVP action includes releasing stored vWF from endothelial cells and macrophages.

    Antiplatelet Drugs (Aspirin + Clopidogrel)

    • Platelets play a critical role in initiating and propagating thrombus formation.
    • Platelets release substances that promote coagulation and form the initial platelet plug.
    • Aspirin and Clopidogrel decrease platelet function to prevent thrombotic disease in animals.

    Acetylsalicylic Acid (Aspirin)

    • Aspirin is an NSAID that inhibits COX enzymes, especially COX-1, even in low doses.
    • Oral aspirin inhibits platelet COX-1 activity.
    • Variability in clinical response exists in different species (dogs/cats), influenced by inconsistencies in experimental data.

    Clopidogrel

    • Clopidogrel is a prodrug that is metabolized into an active metabolite.
    • The active metabolite inhibits ADP receptors.
    • This drug has a role in preventing thrombotic issues in various clinical presentations, including heart issues, thromboembolic disorders, heartworm disease, immune-mediated hemolytic anemia, and cats prone to certain thromboembolisms.

    Fibrinolysis

    • Plasminogen, when activated to plasmin, degrades fibrin clots and surrounding substances.
    • Fibrinolysis is when fibrin clots are broken down.

    Fibrinolytic Agents (Thrombolytics)

    • These agents accelerate fibrinolysis.
    • These agents are used in emergency situations like strokes, myocardial infarction, and thromboembolism in humans.
    • These agents are less successful for use in animals
    • The main use in veterinary medicine is in thromboembolic issues (especially canine & feline)

    Antifibrinolytic Agents

    • Antifibrinolytic agents inhibit fibrinolysis
    • Aminocaproic acid and tranexamic acid stop plasminogen activation, and therefore, inhibit fibrinolysis.

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    Description

    This quiz explores key concepts in the pharmacology of blood, focusing on hemostasis, anticoagulants, and different classes of drugs used to manage coagulopathies. Participants will test their knowledge on the clotting cascade, anticoagulant mechanisms, and specific agents such as heparin and warfarin.

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