1) Anticoagulants like heparin and warfarin are used to treat conditions involving blood clots such as DVT, pulmonary embolism, and heart attacks.
2) Heparin works directly in the blood to prevent clotting while warfarin (a coumarin) works indirectly by interfering with vitamin K and clotting factor production in the liver.
3) Potential adverse effects of anticoagulants include bleeding, osteoporosis, thrombocytopenia, and embryonic defects if used during early pregnancy. Protamine sulfate and vitamin K antagonize the effects of heparin and warfarin respectively.
1) Anticoagulants like heparin and warfarin are used to treat conditions involving blood clots such as DVT, pulmonary embolism, and heart attacks.
2) Heparin works directly in the blood to prevent clotting while warfarin (a coumarin) works indirectly by interfering with vitamin K and clotting factor production in the liver.
3) Potential adverse effects of anticoagulants include bleeding, osteoporosis, thrombocytopenia, and embryonic defects if used during early pregnancy. Protamine sulfate and vitamin K antagonize the effects of heparin and warfarin respectively.
1) Anticoagulants like heparin and warfarin are used to treat conditions involving blood clots such as DVT, pulmonary embolism, and heart attacks.
2) Heparin works directly in the blood to prevent clotting while warfarin (a coumarin) works indirectly by interfering with vitamin K and clotting factor production in the liver.
3) Potential adverse effects of anticoagulants include bleeding, osteoporosis, thrombocytopenia, and embryonic defects if used during early pregnancy. Protamine sulfate and vitamin K antagonize the effects of heparin and warfarin respectively.
1) Anticoagulants like heparin and warfarin are used to treat conditions involving blood clots such as DVT, pulmonary embolism, and heart attacks.
2) Heparin works directly in the blood to prevent clotting while warfarin (a coumarin) works indirectly by interfering with vitamin K and clotting factor production in the liver.
3) Potential adverse effects of anticoagulants include bleeding, osteoporosis, thrombocytopenia, and embryonic defects if used during early pregnancy. Protamine sulfate and vitamin K antagonize the effects of heparin and warfarin respectively.
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Coagulants and
Anti Coagulants Venus Eisha L. Barte
1 Clinical uses of Anticoagulant • DVT • Pulmonary embolism • Coronary occlusion with acute MI • Reduces arterial embolism in patients with atrial fibrillation, mitral stenosis, or prosthetic heart valve • Cerebrovascular accidents • Systemic Coagulopathy • Cardiovascular operations
2 Coagulation cascade Stage 1
Intrinsic Vascular Injury Extrinsic
-Collagen Tissue factor III exposure exposure -Contact activation involving VIIa VII kininogen and prekallikrein
XII XIIa X X1 X1a Membrane Ca VIII
IX Xa Ca IXa Heparin 3 Coagulation cascade Stage 2
Prothrombin Thrombin IIa
XIII Membrane Ca V Ca
Heparin XIIIa Heparin
Coagulation cascade Stage 3
Fibrinogen Fibrin Cross linked
monomer Ca fibrin
Calcium is needed in every aspect of transformation
4 Mechanism of Action • A. Direct Acting (Systemic) - Parenteral – Heparin Na – Blocks Stages: • 1 = Formation of Factor Xa is inhibited • 2 = Interferes with the conversion of prothrombin to thrombin • 3 = Antagonizes the action of thrombin to fibrinogen so there is no fibrin formation • B. Indirect Acting (Oral) 5 • B. Indirect Acting (Oral) – Coumarin (more common) and Indandiones (Less common) – Interfere with the uptake of vitamin K responsible for the manufacture of factor 9 10 7 2 by the hepatic cells, so there is no synthesis of several factors such as: • Factor II – Prothrombin Hypoprothrombinemia • Factor VII – Convertin • Factor IX – Plasma thromboplastin, Christmas factor • Factor X – Stuart-Prower factor
PTU (Propythiouracil also inhibits) 6
Drug Trade Name Onset Duration Routes
Direct Acting Heparin Quick Short Oral, IV
infusion, deep SC Indirect Acting Slow Long - Coumarin - Bishydroxicoumarin Dicumarol 36-48 h 24-108 h PO - Ethylbiscon Tromexan 18-30 h 36-60 h PO macetate - Warfarin Coumadin 35-48 h 84 – 108 h PO Panwarfarin PO, SC, IV Indandione - Diphenadione Dipaxin 48-60 h 96-168 h PO - Phenandione Hedulin 36-48 h 72-96 h PO Danilone
7 Drug Trade Name Onset Duration Route
Fibrinolytic Agents -Plasmin IV -Arvin -Streptokinase -Urokinase
Most popular
In vitro -Na Citrate -Na oxalate
8 Adverse Drug reaction • Heparin – Bleeding (most common) from mucous membranes and open wounds – intracranial hemorrhage – With long term use (> 3months) – Osteoporosis fracture – Thrombocytopenia • Induces platelet aggregation • Production of heparin dependent anti-platelet antibody – Venous or arterial thrombosis (stroke, gangrene) – Transplant and reversible alopecia 9 Adverse Drug Reaction • Warfarin (Indirect) – Hypoprothrombinemia (associated with Vitamin K deficiency) – ecchymosis and hemorrhage – Alopecia, urticaria, dermatitis – Abdominal cramps, nausea, LBM – First 10 weeks of pregnancy (Teratogenic) – causes Embryopathy nasal hypoplasia and stippled epiphyses) 10 Anticoagulant Antagonists DRUG Trade Name Dose and Route Preparation Direct Acting: 1mg for each 1% sterile Protamine SO4 100u of Heparin solution (vial by VERY slow form) IV Indirect Acting Vit K prep: 1. Menadiol Synakyvite 5-10mg PO Tablets, sodium 5-15 mg IV solutions diphosphate 2. Menadione Hykinone 2-10mg PO Tabs, caps, oily 1-2 mg IV solution 3. Menadione Monokay 5-10mg oral, IV Tabs, solution sodium bisulfate 4. Phytonadione Mephyton 5mg PO Tabs, solution 25-250mg IV 11 Drugs that increase effect of Coumarins • (Coumarins are INDIRECT / PO coagulants) – Antibiotics affecting intestinal flora (TCN) – Clofibrate – Causes displacement – Chloral hydrate Reduces Vitamin K Absorption – Disulfiram – Inhibits biotransformation – Dextrothyroxine – Methylphenidate – Propylthiouracil – Phenylbutazone – Salicylates – Inhibits platelet aggregation
12 Drugs that decrease effect of Coumarins • Barbiturates – through enzyme induction • Ethchlorvynol All are PO • Glutethimide • Griseofulvin
13 Drugs that enhance PO anticoagulant activity (Causes more bleeding)
• Decrease vitamin K absorption
– Anitbiotics (TCN – broad spectrum) – Mineral oil • Displacement from plasma proteins – Salicylates (NSAID’s) – Phenylbutazone – Chloral hydrate (Sedative hypnotics) – Clofibrate (Anti cholesterol) 14 Drugs that enhance PO anticoagulant activity (Causes more bleeding) • Inhibition of biotransformation – Allopurinol (Anti gout) – Disulfiram (For alcoholics) – Metronidazole (Ameobiasis) – Chloramphenicol (Broad spectrum antibiotic) – for Typhoid fever • Inhibition of platelet aggregation(Antiplatelet) – Aspirin (NSAID’s) – Epoprosterol (synthetic prostacyclin) – Ticlopidine – Clopidogrel (Plavix) – Dipyridamole 15 Drugs that enhance PO anticoagulant activity (Causes more bleeding)
• Decreases clotting factors
– Quinidine (Myocardial anti depressant) anti arrhythmia
16 Drugs that reduce PO anticoagulant activity (But they no anticoagulant activity) • Enzyme induction – Barbiturates – Glutethimide – Griseofulvin • Increase clotting factor production – Vitamin K – PO contraceptive
17 Procoagulants I. Replacement of deficient clotting factors A. Anti hemophilic factor – Factor VIII: Hemophilia A – Supplied as fresh frozen plasma, cryoprecipitates or lyophilized concentrate – Pooled plasma from blood donors B. Factor IX Complex (Dried Human Plasma Fraction containing Factors II, VII, IX & X) – for hemophilia B 18 Procoagulants II. Increased endogenous clotting factors in the plasma – Desmopressin – Stimulates the release of endogenous pools of factor VIII and vWF
III. Inhibition of Natural Fibrinolytic pathway
– competitive inhibitor of plasmin binding to fibrin A. Aminocaproic acid B. Tranexanic acid (Hemostan) 19 Coagulants • Local (Stops capillary bleeding) – Sterile wax – Oxidized cellulose – Absorbable gelatin – Fibrin foam – Thrombin – Microfibrillar collagen Hemostat • Systemic – Vitamin K prep (secondary to Warfarin use) – Tolonium Cl – Protamine SO4 – Hexadimetrine bromide 20 Procoagulants • 3 inhibition of natural fibrinolytic pathway competitive inhibitor of plasmin binding to fibrin – Aminocaproic acid – Tranexamic acid (Hemostan)
21 Side notes • Herbal tannins are coagulants • If profuse bleeding, give IV if no response to PO therapy • Aloe vera juice is also good for bleeding
