Alteplase 2mg powder for solution for injection vials
Requires a prescription from a doctor or prescriber
Alteplase is a recombinant tissue plasminogen activator (rt-PA) used as a thrombolytic agent.[L43125] It cleaves plasminogen to form plasmin, an enzyme involved in the degradation of fibrin clots.
Official documents, adverse reaction reporting, and safety monitoring
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Safety monitoring data
Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Alteplase
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
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Suspected adverse reactions reported for Alteplase
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1 branded products available
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Actilyse Cathflo 2mg powder for solution for injection vials
WHO defined daily dose (DDD)
100 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via NHS dm+d BNF mapping files. Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Clinical guidelines and formulary information
British National Formulary
Alteplase
Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(6)
Alteplase for treating acute ischaemic stroke (TA264)
Tenecteplase for treating acute ischaemic stroke (TA990)
Guidance on the use of drugs for early thrombolysis in the treatment of acute myocardial infarction (TA52)
Therapeutic hypothermia for acute ischaemic stroke (HTG511)
Stroke and transient ischaemic attack in over 16s: diagnosis and initial management (NG128)
Mechanical thrombectomy devices for acute ischaemic stroke (MIB153)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
Pharmacy stock checkers
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Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
156 found
Half-life
5 minutes
Mechanism
Alteplase is a recombinant tissue plasminogen activator (rt-PA) that converts pl…
Food interactions
1 warning
Human targets
4 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
3.3 ng/ml
Half-life
5 minutes
Protein binding
Volume of distribution
3.9 to 4.3 L
[L43125]…
Metabolism
[A252270]…
Elimination
80%
[A252270]
Clearance
570 mL/min
[L43125]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
[L43125]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 706 interactions
[L43125]
Symptomatic and supportive measures are recommended. The carcinogenic potential of alteplase or its effect on fertility have not been evaluated. In vivo studies evaluating tumorigenicity and in vitro studies evaluating mutagenicity were negative.
[L43125]
It has been estimated that the acute oral and dermal toxicity of alteplase is above 5,000 mg/kg.
[L43175]
In patients with acute myocardial infarction, alteplase reduces fibrinogen levels 3 to 6 hours after treatment. In patients with acute ischemic stroke, patients treated with alteplase have a significantly higher resolution of hyperdense artery sign, a marker of clot formation in the proximal middle cerebral artery, compared to those treated with placebo.[A252330] The use of alteplase increases the risk of bleeding and thromboembolic events. Rare cases of cholesterol embolism have also been reported.[L43125]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[A252270]
Acute myocardial infarction patients (n=12) given 10 mg of alteplase in a 2-minute infusion reached a peak plasma concentration of 3310 ng/ml. This was followed by 50 mg of alteplase in 1 h and 30 mg in 1.5 h, resulting in steady-state plasma levels of 2210 ng/ml and 930 ng/ml, respectively.
[A252285]
[L43125]
[L43125]
The average volume of distribution of the central compartment goes from 3.9 to 4.3 L, and the volume of distribution at steady state goes from 7.2 to 12 L.
[A252270]
[A252270]
In vivo studies suggest that alteplase follows zero-order kinetics, meaning that its metabolism is saturable at higher plasma concentrations.
[A252270]
[A252270]
[L43125]
Proteins and enzymes this drug interacts with in the body
PMID:6447255
Cleavage of fibronectin and laminin leads to cell detachment and apoptosis.
Also cleaves fibrin, thrombospondin and von Willebrand factor. Its role in tissue remodeling and tumor invasion may be modulated by CSPG4. Binds to cells
Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However, subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets via an ITGB3-dependent pathway.
Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the immune response via both innate and T-cell mediated pathways
Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However, subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets via an ITGB3-dependent pathway.
Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the antibacterial immune response via both innate and T-cell mediated pathways
PMID:15853774
Is a primary inhibitor of tissue-type plasminogen activator (PLAT) and urokinase-type plasminogen activator (PLAU). As PLAT inhibitor, it is required for fibrinolysis down-regulation and is responsible for the controlled degradation of blood clots .
PMID:17912461 PMID:8481516 PMID:9207454 PMID:21925150
As PLAU inhibitor, it is involved in the regulation of cell adhesion and spreading .
PMID:9175705
Acts as a regulator of cell migration, independently of its role as protease inhibitor .
PMID:15001579 PMID:9168821
It is required for stimulation of keratinocyte migration during cutaneous injury repair .
PMID:18386027
It is involved in cellular and replicative senescence .
PMID:16862142
Plays a role in alveolar type 2 cells senescence in the lung (By similarity).
Is involved in the regulation of cementogenic differentiation of periodontal ligament stem cells, and regulates odontoblast differentiation and dentin formation during odontogenesis PMID:25808697 PMID:27046084
Involved compounds
ATC B01AD02
ATC S01XA13
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Alteplase
Additional database identifiers
Drugs Product Database (DPD)
7297
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9071
GenAtlas
PLG
GeneCards
PLG
GenBank Gene Database
X05199
GenBank Protein Database
387026
Guide to Pharmacology
2394
UniProt Accession
PLMN_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3661
GenAtlas
FGA
GeneCards
FGA
GenBank Gene Database
AF361104
GenBank Protein Database
13591824
UniProt Accession
FIBA_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3694
GenAtlas
FGG
GeneCards
FGG
GenBank Gene Database
M10014
GenBank Protein Database
182439
UniProt Accession
FIBG_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:8583
GenAtlas
SERPINE1
GeneCards
SERPINE1
GenBank Gene Database
X04429
GenBank Protein Database
35272
UniProt Accession
PAI1_HUMAN
International reference pricing
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications: