Alteplase

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Alteplase
Clinical data
Trade namesActivase, Actilyse, others
Other namest-PA, rt-PA
AHFS/Drugs.comMonograph
License data
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)

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]

Medical uses

The main uses of alteplase are acute ischemic stroke, acute myocardial infarction, and acute massive pulmonary embolism.[3]

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.[4]

Indications and Contraindications

The use of alteplase is similar to those of other thrombolytics, but can vary depending on the pathology.[5][6]

Acute Ischemic Stroke

After a patient is diagnosed with an acute ischemic stroke, they may be eligible for treatment with alteplase.[7] A person may be eligible for treatment with alteplase if:

  • they are being treated within 4.5 hours of symptom onset
  • do not have other causes of stroke symptoms
  • benefits of treatment are determined to outweigh the risks

Contraindications

A patient would not eligible for alteplase if testing shows they are not suffering from an acute ischemic stroke or if the risks of treatment are likely to outweigh the benefits. Some considerations include:[7]

  • Computed tomography shows irreversible brain damage
  • Mild, nondisabling stroke symptoms
  • Blood pressure greater than 185/110 mm Hg
  • Blood glucose less than than 50 mg/dL
  • Recent history of severe head trauma
  • Infective endocarditis
  • Aortic arch dissection
  • Bleeding disorder
  • Other risk factors for severe bleeding such as recent surgeries, GI bleeding, GI cancer, and others

People suffering from an acute ischemic stroke may also be treated with other therapies including mechanical thrombectomy.[7]

Myocardial Infarction

Pulmonary Embolism

Side Effects

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.[8] 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]

History and Culture

Alteplase was approved for medical use in the United States in 1987.[2][9] It is on the World Health Organization's List of Essential Medicines.[10]

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.[3]

Society and culture

It is on the World Health Organization's List of Essential Medicines,[10] having been added in 2019.[11]

References

  1. ^ a b "Alteplase Use During Pregnancy". Drugs.com. Retrieved 12 November 2019.
  2. ^ a b c d e f g "Alteplase Monograph for Professionals". Drugs.com. Retrieved 11 November 2019.
  3. ^ a b "Activase- alteplase kit". DailyMed. 5 December 2018. Retrieved 4 January 2020.
  4. ^ 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 (1): 56–68. doi:10.1001/jama.2018.19802. PMC 6583564. PMID 30620371.
  5. ^ WRITING COMMITTEE MEMBERS*; O’Gara, Patrick T.; Kushner, Frederick G.; Ascheim, Deborah D.; Casey, Donald E.; Chung, Mina K.; de Lemos, James A.; Ettinger, Steven M.; Fang, James C.; Fesmire, Francis M.; Franklin, Barry A. (29 January 2013). "2013 ACCF/AHA Guideline for the Management of ST-Elevation Myocardial Infarction: A Report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines". Circulation. 127 (4). doi:10.1161/CIR.0b013e3182742cf6. ISSN 0009-7322.
  6. ^ Powers, William J.; Rabinstein, Alejandro A.; Ackerson, Teri; Adeoye, Opeolu M.; Bambakidis, Nicholas C.; Becker, Kyra; Biller, José; Brown, Michael; Demaerschalk, Bart M.; Hoh, Brian; Jauch, Edward C. (December 2019). "Guidelines for the Early Management of Patients With Acute Ischemic Stroke: 2019 Update to the 2018 Guidelines for the Early Management of Acute Ischemic Stroke: A Guideline for Healthcare Professionals From the American Heart Association/American Stroke Association". Stroke. 50 (12). doi:10.1161/STR.0000000000000211. ISSN 0039-2499.
  7. ^ a b c Powers, William J.; Rabinstein, Alejandro A.; Ackerson, Teri; Adeoye, Opeolu M.; Bambakidis, Nicholas C.; Becker, Kyra; Biller, José; Brown, Michael; Demaerschalk, Bart M.; Hoh, Brian; Jauch, Edward C. (12 2019). "Guidelines for the Early Management of Patients With Acute Ischemic Stroke: 2019 Update to the 2018 Guidelines for the Early Management of Acute Ischemic Stroke: A Guideline for Healthcare Professionals From the American Heart Association/American Stroke Association". Stroke. 50 (12): e344–e418. doi:10.1161/STR.0000000000000211. ISSN 1524-4628. PMID 31662037. {{cite journal}}: Check date values in: |date= (help)
  8. ^ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 216. ISBN 9780857113382.
  9. ^ "Activase: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 4 January 2020.
  10. ^ a b 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.
  11. ^ 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.

External links

  • "Alteplase". Drug Information Portal. U.S. National Library of Medicine.
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