Alteplase

Alteplase (t-PA) is a thrombolytic medication, used to treat acute ST elevation myocardial infarction (a type of heart attacks), pulmonary embolism associated with low blood pressure, acute ischemic stroke, and blocked central venous access devices (CVAD).[2] It is given by injection into a vein or artery.[2]

Alteplase
Clinical data
Trade namesActivase, Actilyse, others
Other namest-PA, rt-PA
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • US: C (Risk not ruled out) [1]
    ATC code
    Legal status
    Legal status
    Identifiers
    CAS Number
    DrugBank
    ChemSpider
    • none
    UNII
    KEGG
    Chemical and physical data
    FormulaC2569H3928N746O781S40
    Molar mass59042.52 g·mol−1
      (verify)

    Common side effects are bleeding including intracranial bleeding and GI bleeding.[2] Other side effects may rarely include allergic reactions.[2] It is not recommended in those allergic to gentamicin.[3] Safety of use in pregnancy is unclear.[1] Alteplase is a manufactured form of tissue plasminogen activator.[2] It works by converting plasminogen to plasmin in a blood clot.[2]

    Alteplase was approved for medical use in the United States in 1987.[2][4] It is on the World Health Organization's List of Essential Medicines.[5]

    Medical uses

    The main uses of alteplase are acute ischemic stroke, acute myocardial infarction, and acute massive pulmonary embolism.[6]

    In regards to acute myocardial infarction, a randomized controlled trial of people with acute STEMI, showed there was no reduction in microvascular obstruction when adjunctive low-dose intracoronary alteplase was administered during the primary PCI.[7]

    Mechanism of action

    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.[6]

    Society and culture

    It is on the World Health Organization's List of Essential Medicines,[5] having been added in 2019.[8]

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    References

    1. "Alteplase Use During Pregnancy". Drugs.com. Retrieved 12 November 2019.
    2. "Alteplase Monograph for Professionals". Drugs.com. Retrieved 11 November 2019.
    3. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 216. ISBN 9780857113382.
    4. "Activase: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 4 January 2020.
    5. World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
    6. "Activase- alteplase kit". DailyMed. 5 December 2018. Retrieved 4 January 2020.
    7. 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. doi:10.1001/jama.2018.19802. PMC 6583564. PMID 30620371.
    8. World Health Organization (2019). Executive summary: the selection and use of essential medicines 2019: report of the 22nd WHO Expert Committee on the selection and use of essential medicines. Geneva: World Health Organization. hdl:10665/325773. WHO/MVP/EMP/IAU/2019.05. License: CC BY-NC-SA 3.0 IGO.
    • "Alteplase". Drug Information Portal. U.S. National Library of Medicine.
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