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Platelet Inhibitors Platelet inhibitors, also known as antiplatelet drugs , prevent blood platelets from clumping together (aggregating) and forming clots. Clinical Use Commonly used to prevent thrombosis (clot formation) in arteries. Helps reduce risk of: o Heart attack o Stroke o Peripheral artery disease Types of Platelet Inhibitors
1. Aspirin Mechanism: Irreversibly inhibits COX-1 , reducing thromboxane A2 production. Uses: o Secondary prevention of myocardial infarction o Secondary prevention of stroke o In patients with coronary artery **disease
o Acute myocardial infarction (heart attack) o Ischemic stroke o Pulmonary embolism Administration & Clinical Use Route: Given intravenously (IV) Timing: Most effective when used within the first few hours (< 6 hours) after: o Acute myocardial infarction (MI) o Cerebrovascular accident (CVA / ischemic stroke) Effect: Reduces mortality when administered promptly Generic Name Brand Name(s) Alteplase (tPA) Activase Reteplase (r- PA) Retavase Streptokinase Kabikinase Side Effects Serious side effect: o Bleeding (major risk with all thrombolytics) Types of Thrombolytic Drugs
1. Tissue Plasminogen Activator (tPA) Mechanism: Directly activates plasminogen to plasmin. Examples: o Alteplase: Recombinant form of human tPA. o Tenecteplase & Reteplase: Modified versions of tPA with: Longer half-lives Different administration protocols 2. Streptokinase Mechanism: o A bacterial protein that forms a complex with plasminogen → activates it to plasmin. Note: o Has broader activity but is less specific than tPA. 3. Urokinase Mechanism: Naturally occurring enzyme that directly converts plasminogen to plasmin. Use: Less frequently used compared to tPA. Therapeutic Uses of Thrombolytic Agents 1. Acute Myocardial Infarction (Heart Attack) Used to dissolve clots in coronary arteries. Restores blood flow to the heart muscle. Reduces the extent of heart damage. 2. Acute Ischemic Stroke Breaks down clots in cerebral arteries to restore blood flow to the brain. Must be administered within a narrow time window : o Typically 3–4.5 hours from symptom onset. Provides maximum efficacy when given promptly. 3. Pulmonary Embolism In severe, life-threatening cases , thrombolytics can: o Rapidly dissolve the clot obstructing the pulmonary artery. 4. Deep Vein Thrombosis (DVT) May be used in severe cases of DVT: o Especially when there is a risk of limb loss o Or other serious complications 5. Peripheral Arterial Thrombosis Used to dissolve clots in the arteries of the limbs. Prevents tissue damage and potential amputation. Side Effects and Risks of Thrombolytic Therapy Primary Risk: Bleeding — due to breakdown of clots and reduced ability of blood to clot. Possible Complications: Intracranial Hemorrhage o Bleeding within the brain; can be life- threatening. Gastrointestinal Bleeding o Occurs in the stomach or intestines. Hematuria o Presence of blood in the urine. Bleeding at Injection Sites o Especially common when intravenous lines are placed.
o Do not take any other medication without physician approval. o Avoid OTC medications , especially antacids and cold remedies. o Do not abruptly stop taking digitalis after prolonged use → must be tapered gradually under physician supervision.