Alteplase

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Alteplase
Clinical data
Trade namesActivase, Actilyse
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • US: C (Risk not ruled out)
ATC code
Legal status
Legal status
Identifiers
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC2569H3928N746O781S40
Molar mass59042.3 g/mol g·mol−1
  (verify)

Alteplase (trade names Activase, Actilyse) is a thrombolytic drug, used to treat acute myocardial infarctions (heart attacks) and other severe conditions caused by blood clotting by breaking up the blood clots that cause them.

It is a tissue plasminogen activator. It is approved by the U.S. Food and Drug Administration (FDA) for the treatment of myocardial infarction with ST-elevation (STEMI), acute ischemic stroke (AIS), acute massive pulmonary embolism, and occluded central venous access devices (CVAD).[1][2][3]

It is on the World Health Organization's List of Essential Medicines, which lists the safest and most effective medicines needed in a health system.[4]

Medical uses[edit]

The primary uses of alteplase, as approved by the FDA, include acute ischemic stroke, acute myocardial infarction, and acute massive pulmonary embolism.[5]

In regards to acute myocardial infarction, a randomized controlled trial published in January 2019, specifically looking at patients with acute STEMI, showed there was no reduction in microvascular obstruction when adjunctive low-dose intracoronary alteplase was administered during the primary PCI. [6]

Mechanism of action[edit]

Alteplase is a serine protease that assists fibrin in the conversion of plasminogen to plasmin. When in the systemic circulation, alteplase binds to fibrin in a thrombus and initiates fibrinolysis. [5]

References[edit]

  1. ^ "Thrombolytic Therapy: Background, Thrombolytic Agents, Thrombolytic Therapy for Acute Myocardial Infarction". 2017-05-02. Cite journal requires |journal= (help)
  2. ^ Drugs.com: Monograph for Activase.
  3. ^ Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. 2017. Actilyse-Pulver und Lösungsmittel zur Herstellung einer Injektions- oder Infusionslösung. ISBN 3-85200-196-X.
  4. ^ "World Health Organization model list of essential medicines: 21st list 2019". 2019. hdl:10665/325771. Cite journal requires |journal= (help)
  5. ^ a b Activase [package insert]. South San Francisco, CA: Genentech, Inc.; 2018.
  6. ^ McCartney, Peter (January 2019). "Effect of Low-Dose Intracoronary Alteplase During Primary Percutaneous Coronary Intervention on Microvascular Obstruction in Patients with Acute Myocardial Infarction". JAMA. 321: 56–68.