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Dr Jayashree Sidigonde
ANTICOAGULANTS
Coagulation is the process by which blood changes from a liquid to a
gel-like clot in order to stop bleeding after injury. It is an important
part of hemostasis, the body’s mechanism for preventing blood loss.
Steps in Coagulation
1.Vasoconstriction – Blood vessels constrict to reduce blood flow.
2.Platelet Plug Formation – Platelets stick to the injured area and
form a temporary plug.
3.Coagulation Cascade – Clotting factors in the blood activate one
another in a sequence, ultimately producing fibrin.
4.Clot Formation – Fibrin forms a mesh that stabilizes the platelet
plug and creates a firm clot.
Introduction
•Anticoagulants are drugs that prevent or reduce blood
coagulation.
•They are used in prevention and treatment of
thromboembolic disorders.
•Common indications include deep vein thrombosis (DVT),
pulmonary embolism, myocardial infarction, and atrial
fibrillation.
Classification of Anticoagulants
1. Parenteral Anticoagulants
• Unfractionated Heparin (UFH)
• Low Molecular Weight Heparin (LMWH)
• Fondaparinux
• Direct thrombin inhibitors (e.g.,
Bivalirudin)
2. Oral Anticoagulants
• Vitamin K antagonists
◦Warfarin
• Direct Oral Anticoagulants (DOACs)
◦Dabigatran
◦Rivaroxaban
◦Apixaban
◦Edoxaban
eparin – Introduction
Heparin is a naturally occurring anticoagulant.
Obtained from animal tissues such as porcine intestinal mucosa.
dministered mainly through intravenous (IV) or subcutaneous (SC) route
roduces rapid anticoagulant action.
Mechanism of Action of Heparin
•Heparin activates antithrombin
III.
•Antithrombin III inhibits:
◦Thrombin (Factor IIa)
◦Factor Xa
•Prevents conversion of
fibrinogen into fibrin.
•Thus inhibits clot formation.
Pharmacokinetics of Heparin
•Not effective orally due to large molecular size.
•Administered IV or SC.
•Rapid onset of action.
•Short half-life (1–2 hours).
•Metabolized mainly in the liver.
•Does not cross placenta, therefore safer in pregnancy.
Therapeutic Uses of Heparin
•Deep vein thrombosis (DVT)
•Pulmonary embolism
•Acute coronary syndrome
•Myocardial infarction
•During cardiac surgery
•Hemodialysis
•Disseminated intravascular coagulation (DIC)
Adverse Effects of Heparin
•Bleeding (most common)
•Heparin-induced thrombocytopenia (HIT)
•Osteoporosis with prolonged use
•Hypersensitivity reactions
•Alopecia
Contraindications of Heparin
•Active bleeding disorders
•Severe hypertension
•Peptic ulcer disease
•Hemophilia
•Recent surgery involving brain or eye
Monitoring and Antidote
Monitoring
•Activated Partial Thromboplastin Time
(aPTT)
Antidote
•Protamine sulfate neutralizes heparin.
Low Molecular Weight Heparin (LMWH)
Examples
•Enoxaparin
•Dalteparin
Advantages
•Longer duration of action
•More predictable anticoagulant response
•Lower risk of HIT
•Less monitoring required
Classification of Oral Anticoagulants
1. Vitamin K Antagonists
•Warfarin
•Acenocoumarol
2. Direct Oral Anticoagulants (DOACs)
Direct Thrombin Inhibitor
•Dabigatran
Factor Xa Inhibitors
•Rivaroxaban
•Apixaban
•Edoxaban
Mechanism of Action of
Warfarin
•Warfarin blocks recycling of vitamin K.
•Prevents activation of vitamin K
dependent clotting factors.
•Anticoagulant effect appears after
depletion of existing clotting factors.
Pharmacokinetics
•Well absorbed orally.
•Highly protein bound.
•Metabolized in liver by CYP450 enzymes.
•Long half-life.
•Delayed onset of action.
Therapeutic Uses
•Deep vein thrombosis (DVT)
•Pulmonary embolism
•Atrial fibrillation
•Prosthetic heart valves
•Prevention of stroke
Adverse Effects
•Bleeding
•Skin necrosis
•Purple toe syndrome
•Teratogenicity
•Numerous drug interactions
Antidote of Warfarin
•Vitamin K (Phytonadione)
•Fresh frozen plasma in severe bleeding
•Prothrombin complex concentrate
Warfarin induced skin necrosis
Purple toe syndrome
Direct Oral Anticoagulants (DOACs)
Dabigatran
•Direct thrombin inhibitor
Rivaroxaban & Apixaban
•Direct Factor Xa inhibitors
Advantages
•Rapid onset of action
•Predictable response
•Less monitoring required
Advantages of DOACs
•Fewer food interactions
•Lower risk of intracranial hemorrhage
•Fixed dosing
•Convenient administration
Contraindications
•Active bleeding
•Severe liver disease
•Pregnancy (especially warfarin)
•Recent major surgery
•Uncontrolled hypertension
| Feature | Warfarin | DOACs |
| Monitoring | Required | Usually not required |
| Onset | Slow | Rapid |
| Food interactions | Many | Few |
| Half-life | Long | Short |
| Pregnancy | Contraindicated | Mostly avoided |
Anticoagulants prevent and treat thromboembolic disorders by inhibiting blood clot formation.
hey are used in conditions such as DVT, pulmonary embolism, atrial fibrillation, and myocardial infarctio
Major classes include heparins, warfarin, and direct oral anticoagulants (DOACs).
hey reduce morbidity and mortality associated with thrombosis.
Bleeding is the major adverse effect; therefore, careful monitoring is important.
Newer anticoagulants offer better safety, predictable action, and improved patient compliance.
Rational drug selection and appropriate dosing are essential for safe and effective therapy.
Summary
Comprehensive Overview of Anticoagulants: Mechanisms, Uses, and Safety