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  • BDS/MBBS Thrombolytics and Antiplatelet Drugs

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    Dr.U.P.Rathnakar.MD.DIH.PGDHM
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    Fibrinolytics such as streptokinase, urokinase, and alteplase work to break down blood clots by activating plasminogen to plasmin. They target either directly or indirectly to break down fibrin clots. Streptokinase is administered as a bolus dose while alteplase is given as a bolus followed by infusion to treat conditions such as myocardial infarction, pulmonary embolism, and deep vein thrombosis. Antifibrinolytics like tranexamic acid and aminocaproic acid work to inhibit fibrinolysis and reduce bleeding. They are used to reduce bleeding during surgery or trauma. Choice of fibrinolytic depends on factors like half-life, fibrin specificity,

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    BDS/MBBS Thrombolytics and Antiplatelet drugs

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    Fibrinolytics such as streptokinase, urokinase, and alteplase work to break down blood clots by activating plasminogen to plasmin. They target either directly or indirectly to break down fibrin clots. Streptokinase is administered as a bolus dose while alteplase is given as a bolus followed by infusion to treat conditions such as myocardial infarction, pulmonary embolism, and deep vein thrombosis. Antifibrinolytics like tranexamic acid and aminocaproic acid work to inhibit fibrinolysis and reduce bleeding. They are used to reduce bleeding during surgery or trauma. Choice of fibrinolytic depends on factors like half-life, fibrin specificity,

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    139 views33 pages

    BDS/MBBS Thrombolytics and Antiplatelet Drugs

    Uploaded by

    Dr.U.P.Rathnakar.MD.DIH.PGDHM
    Fibrinolytics such as streptokinase, urokinase, and alteplase work to break down blood clots by activating plasminogen to plasmin. They target either directly or indirectly to break down fibrin clots. Streptokinase is administered as a bolus dose while alteplase is given as a bolus followed by infusion to treat conditions such as myocardial infarction, pulmonary embolism, and deep vein thrombosis. Antifibrinolytics like tranexamic acid and aminocaproic acid work to inhibit fibrinolysis and reduce bleeding. They are used to reduce bleeding during surgery or trauma. Choice of fibrinolytic depends on factors like half-life, fibrin specificity,

    Copyright:

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    Flag for inappropriate content
    of 33

    Fibrinolytics, antifibrinolytics and

    antiplatelet drugs
    Dr.Rathnakar U.P

    BDS
    www.scribd.com
    Blood coagulation
    Two contrasting
    properties of Blood

    Remains fluid in circulation


    Solidifies when vessels are injured
    Blood Clotting [Hemostasis]

    [Pathophysiology]

    Vascular Phase
     Platelet Phase
     Coagulation Phase
     Fibrinolytic Phase
    Therapeutic targets
    Coagulation
    1.
    Anticoagulant
    Parenteral Heparin Inactivation of clotting DVT
    factors

    Oral Warfarin Decrease synthesis of DVT


    clotting factors
    2.
    Antiplatelet Aspirin Decrease platelet Prevent arterial
    aggregation thrombosis
    3.
    Thrombolytic Streptokinase Fibrinolysis Breakdown of
    4 thrombi
    Antiplatelets
    Damaged vessel
    Collagen wall Platelet
    release activation
    As
    pir
    in

    TXA2 Release ADP release Thrombin

    GPIIb
    /IIIa P2Y1
    Anta 2 anta
    RECEPTOR
    S
    PD
    E-I Platelet
    adhesion
    Platelet inhibitors
    Platelet cox-1 inhibitor Aspirin

    P2y12[Adenosine] Ticlopidine, Clopidogrel ,


    receptor blockade Prasugrel, Elinogrel, Ticagrelor

    GPIIb/IIIa antagonist Abciximab, Eptifibatide, Tirofiban

    Phosphodiesterase Dipyridamole, Pentoxifylline,


    inhibitor Cilostazol

    Thrombaxane A2 synthesis GR3219


    inhibitor
    Natural patelet PGI2 [Epoprosteno]l, nitric oxide
    aggregation inhibitor
    Aspirin-imp/points
    Aspirin in low doses inhibits cox-1 of platelets
    in liver
    Platelets have no nuclei-hence no regeneration

    Inhibition irreversible [Other NSAIDs


    reversible]
    Higher doses inhibit PGI2 in vessel wall
    Low dose-can produce peptic ulceration and
    bleeding
    Aspirin resistance-Failure to respond.-Genetic,
    Platelet inhibitors
    Platelet cox-1 inhibitor Aspirin

    P2y12[Adenosine] Ticlopidine, Clopidogrel ,


    receptor blockade Prasugrel, Elinogrel, Ticagrelor

    GPIIb/IIIa antagonist Abciximab, Eptifibatide, Tirofiban

    Phosphodiesterase Dipyridamole, Pentoxifylline,


    inhibitor Cilostazol

    Thrombaxane A2 synthesis GR3219


    inhibitor
    Natural patelet PGI2 [Epoprosteno]l, nitric oxide
    aggregation inhibitor
    [P2Y12 receptor antagonist]

    250mg twice
    daily
    orally
    Clopidogrel
    [P2Y12 receptor antagonist]
    Closely related to ticlopidine
    75mg once daily, orally

    • Less than
    Platelet inhibitors
    Platelet cox-1 inhibitor Aspirin

    P2y12[Adenosine] Ticlopidine, Clopidogrel ,


    receptor blockade Prasugrel, Elinogrel, Ticagrelor

    GPIIb/IIIa antagonist Abciximab, Eptifibatide, Tirofiban

    Phosphodiesterase Dipyridamole, Pentoxifylline,


    inhibitor Cilostazol

    Thrombaxane A2 synthesis GR3219


    inhibitor
    Natural patelet PGI2 [Epoprosteno]l, nitric oxide
    aggregation inhibitor
    Glycoprotein IIb/ IIIa
    receptor antagonist
     ABCIXIMAB:
    A Monoclonal antibody
    MOA: Inhibition of this receptor blocks binding of
    fibrin to platelets and platelet aggregation

    USE: Used with Aspirin+Heparin during coronary


    artery interventions.
    i.v.infusion

    ADE: Bleeding, Thrombocytopinia, constipation


    Indications[Uses] for antiplatelet drugs
    Acute ischemic stroke
    Acute MI Acute ischemic event
    Before
    During Procedure Percutaneous Coronary
    After Interventions

    Previous MI
    Previous stroke High risk of vascular events
    PVD
    LL Arterial graft
    CABG Revascularization procedures
    Carotid endarterectomies
    AF

    Usually with anticogulants Prosthetic valves


    Summary: Antiplatelets
    Fibrinolytics[Thrombolytics]
    INTRINSIC
    EXTRINSIC Factor
    Streptokinase XIIA Fibrin
    Urokinase Activators Kallikrein [Insoluble]
    rt-PA t-PA

    PLASMINOGE PLASMIN
    N

    EACA α2Antiplasmin Fibrin


    Tranexaemic acid α2Macroglobulin [Soluble]
    Inhibitors
    Aprotinin
    INTRINSIC
    EXTRINSIC
    22 Fibrinolytic system
    Fibrinolytics

    Streptokinase and Urokinase

    Prourokinase
    Alteplase
    Reteplase
    Tenecteplase
    Anisstreplace
    [Anisoylated purified
    streptokinase activator
    complex]
    Streptokinase
    Urokinase
    Charecteristic Streptokinase Urokinase Alteplase

    t1/2[Minutes] 15-25 15-20 4-8

    Fibrin specificity Minimal Moderate Maximum

    Plasminogen Indirect Direct Direct


    Binding

    Antigenicity Yes No NO

    Dose 1.5 MU 3-4 MU 100mg

    3Lac.i.v-10mts 15mg bolus


    Administration 1.5MU i.v. 3Lac/h-12h 50mg-30mts
    [MI] 35mg-60mts
    1
    6

    •DVT
    •Pulmonary embolism
    Contra
    Indications:
    Fibrinolytics
    Uses of Antifibrinolytics
    ADEs Antifibrinolytics
    Summary: Fibrinolytics

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