Alteplase
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Trade names | Activase, Actilyse, others |
Other names | t-PA, rt-PA |
AHFS/Drugs.com | Monograph |
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Chemical and physical data | |
Formula | C2569H3928N746O781S40 |
Molar mass | 59042.52 g·mol−1 |
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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:[7]
- 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 outweigh the likely benefits.[7] 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
- History of or current intracranial hemorrhage
- Infective endocarditis
- Aortic arch dissection
- Bleeding disorder (coagulopathy)
- 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
Currently, the preferred treatment for ST elevation myocardial infarction (STEMI) is percutaneous coronary intervention (PCI).[5] If a person suffering from a STEMI is treated in a non-PCI capable hospital and cannot be transferred to receive PCI in under 120 minutes, they may be eligible for treatment with alteplase in combination with other drugs.[5]
Contraindications
Contraindications for use of alteplase in STEMI are similar to those of acute ischemic stroke.[5] A person suffering from a STEMI may be eligible to receive alteplase if the risks of treatment outweigh the likely benefits.[5] Some considerations include:[5]
- Ischemic stroke within 3 months but not including acute ischemic stroke within 4.5 hours
- History of or current intracranial hemorrhage
- Aortic arch dissection
- Any active bleeding excluding menses
- Recent history of severe head trauma
- Recent surgery (timeline and risk variable depending on surgery type)
- Known intracranial pathology
Pulmonary Embolism
Adverse Effects
Because
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
- ^ a b "Alteplase Use During Pregnancy". Drugs.com. Retrieved 12 November 2019.
- ^ a b c d e f g "Alteplase Monograph for Professionals". Drugs.com. Retrieved 11 November 2019.
- ^ a b "Activase- alteplase kit". DailyMed. 5 December 2018. Retrieved 4 January 2020.
- ^ 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.
- ^ a b c d e f 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.
- ^ 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.
- ^ a b c d e 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.
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(help) - ^ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 216. ISBN 9780857113382.
- ^ "Activase: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 4 January 2020.
- ^ 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.
- ^ 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.