Alteplase
- Atc Codes:B01AD02#S01XA13
- CAS Codes:105857-23-6
- PHARMGKB ID:105857-23-6
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Actilyse; Belgium: Actilyse; Czech Republic: Actilyse; Denmark: Actilyse; Estonia: Actilyse; Finland: Actilyse; France: Actilyse; Germany: Actilyse, Lysatec; Greece: Actilyse; Hungary: Actilyse; Ireland: Actilyse; Italy: Actilyse; Latvia: Actilyse; Lithuania: Actilyse; Luxembourg: Actilyse; Malta: Actilyse; Netherlands: Actilyse; Poland: Actilyse; Portugal: Actilyse; Romania: Actilyse; Slovakia: Actilyse; Slovenia: Actilyse; Spain: Actilyse; Sweden: Actilyse; UK: Actilyse.
North America
Canada: Activase, Cathflo; USA: Activase.
Latin America
Argentina: Actilyse; Brazil: Actilyse; Mexico: Actilyse.
Asia
Japan: Activacin, Grtpa.
Drug combinations
Chemistry
Alteplase: C~2569~H~3894~N~746~O~781~S~40~. Mw: 59007.61. A serine protease with a primary sequence composed of 527 aa. The sequence is identical to the naturally occurring protease produced by endothelial cells of vessel walls. Plasminogen activator (human tissue-type protein moiety). CAS-105857-23-6 (1989).
Pharmacologic Category
Thrombolytic Agents; Enzymes. (ATC-Code: B01AD02; S01XA13).
Mechanism of action
Local fibrinolysis by binding to intrathrombotic fibrin, converting entrapped plasminogen to plasmin.
Therapeutic use
Management of acute myocardial infarction (for the lysis of thrombi in coronary arteries). Acute ischemic stroke. Acute pulmonary embolism.
Pregnancy and lactiation implications
Use with caution if administered during pregnancy or lactation.
Unlabeled use
Acute peripheral arterial occlusive disease.
Contraindications
Hypersensitivity to alteplase or any component of the formulation. Active internal bleeding. History of cerebrovascular accident. Recent intracranial or intraspinal surgery or trauma. Intracranial neoplasm. Arteriovenous malformation or aneurysm. Bleeding diathesis. Severe uncontrolled hypertension. Intracranial hemorrhage or suspicion of subarachnoid hemorrhage. Prolonged external cardiac massage. Aortic dissection. Serious head trauma or previous stroke. Seizure. Active internal bleeding. Gastrointestinal or urinary tract hemorrhage. Aggressive treatment to lower blood pressure. Glucose level <50 mg/dL or >400 mg/dL. Arterial or lumbar puncture. Post-myocardial infarction pericarditis. Pregnancy. Breast-feeding.
Warnings and precautions
Coronary thrombolysis may result in reperfusion arrhythmias. Doses >150 mg are associated with increased risk of intracranial hemorrhage. Treatment of acute ischemic stroke more than 3 hours after symptom onset is not recommended. Risk of bleeding. Use with caution in patients receiving oral anticoagulants, in patients with advanced age (e.g. >75 years) or in pregnancy (due to increased risk of bleeding). Concurrent heparin anticoagulation may contribute to bleeding.