Generic Name : Alteplase.

Trade Name    : Cathflo Activase.

Drug Class      : Thrombolytics, Tissue plasminogen activator (TPN).

Forms Of The Drug

  1. Powder for injection: 2mg, 50mg, 100mg.

Mechanism Of Action

Its mechanism of action involves promoting the conversion of plasminogen to plasmin, an enzyme responsible for breaking down fibrin, the main component of blood clots. Here’s how alteplase works:

  1. Conversion of Plasminogen: Alteplase acts as a recombinant form of tissue plasminogen activator, mimicking the body’s natural enzyme that initiates the breakdown of blood clots. It binds to fibrin within blood clots and catalyzes the conversion of plasminogen to plasmin.
  2. Activation of Plasmin: Plasmin is an enzyme that targets and breaks down fibrin strands, which form the structure of blood clots. By activating plasminogen, alteplase accelerates the formation of plasmin, leading to the dissolution of the blood clot into smaller fragments.
  3. Thrombolysis: The breakdown of fibrin by plasmin results in the dissolution of the blood clot, restoring blood flow in affected vessels. This process is known as thrombolysis and is crucial in conditions where blood clots obstruct blood flow, such as acute myocardial infarction (heart attack), acute ischemic stroke, or pulmonary embolism.

Indications

  1. Acute Ischemic Stroke.
  2. Acute Myocardial Infarction (Heart Attack).
  3. Pulmonary Embolism (PE).
  4. Acute Peripheral Arterial Occlusion.

Contraindications

  1. Active Bleeding or High Risk of Bleeding.
  2. Recent Intracranial Hemorrhage.
  3. Suspected Aortic Dissection.
  4. Recent Major Surgery or Trauma.
  5. Known Hypersensitivity.
  6. Severe Uncontrolled Hypertension.
  7. Pregnancy and Breastfeeding.

Side Effects

  1. Stroke (1.6%).
  2. Accelerated idioventricular rhythm.
  3. Pulmonary edema.
  4. Arterial embolism.
  5. Bruising.
  6. Bleeding.
  7. DVT.
  8. Hypotension.
  9. Intracranial hemorrhage.
  10. GI/GU hemorrhage.
  11. Pulmonary embolism.
  12. Fever/chills.
  13. Nausea/vomiting.
  14. Sensitivity reaction.
  15. Sepsis.
  16. Shock.
  17. Hypersensitivity.
  18. Cerebral edema.
  19. Cerebral herniation.
  20. Seizure.
  21. Ischemic stroke.
  22. Thromboembolism.

Drug Interactions

Other drugs that can interact with it.

  1. Anticoagulants and Antiplatelet Drugs: Concurrent use of other anticoagulants (such as warfarin, heparin) or antiplatelet drugs (like aspirin, clopidogrel).
  2. NSAIDs such as ibuprofen, naproxen.
  3. Other Medications Affecting Coagulation.

Precautions

  1. Pregnancy: Category C.
  2. Lactation: Due to the potential risk of bleeding and the lack of sufficient evidence on the effects of alteplase on nursing infants, healthcare providers generally recommend avoiding the use of alteplase during breastfeeding unless the benefits to the mother significantly outweigh the potential risks to the infant.

Leave a Reply

Your email address will not be published. Required fields are marked *