Actilyse Alteplase Powder and Solvent for Solution for Injection

1. Indications and Usage
Acute Ischemic Stroke: Treatment of acute ischemic stroke within 3 hours (or up to 4.5 hours per certain guidelines) of symptom onset.
Acute Myocardial Infarction: Treatment of acute myocardial infarction for facilitating coronary artery recanalization (typically within 12 hours of symptom onset).
Acute Pulmonary Embolism: Treatment of acute, massive pulmonary embolism with hemodynamic instability.
2. Dosage and Administration
Route of Administration: For Intravenous (IV) Administration ONLY.
Recommended Dosage:
Acute Ischemic Stroke: 0.9 mg/kg (maximum 90 mg). 10% of the total dose is administered as an IV bolus, followed by the remaining 90% infused over 60 minutes.
Acute Myocardial Infarction: 100 mg total (weight-based accelerated regimen) or fixed 100 mg dose administered over 90 minutes to 3 hours.
Acute Pulmonary Embolism: 100 mg administered as a continuous IV infusion over 2 hours.
Critical Administration Instructions:
Reconstitution: Reconstitute the lyophilized powder with the provided Sterile Water for Injection to specific concentrations (e.g., 1 mg/mL or 2 mg/mL). Gently swirl; do not shake.
Dilution: Further dilute with 0.9% Sodium Chloride Injection if necessary. Do not use glucose-containing solutions for reconstitution.
Equipment: Use a separate IV line for administration. Do not mix with other drugs or solutions.
3. Mechanism of Action
Protease Activation: Alteplase is a serine protease that selectively converts endogenous plasminogen into plasmin.
Fibrinolysis: The generated plasmin degrades fibrin clots, leading to the dissolution of thrombi. It exhibits relative fibrin specificity, meaning it preferentially activates fibrin-bound plasminogen over circulating plasminogen, thereby minimizing systemic fibrinogen depletion.
4. Safety and Warnings
Bleeding Risk: The most serious adverse reaction is bleeding (e.g., intracranial hemorrhage, gastrointestinal bleeding, retroperitoneal bleeding). Strict adherence to exclusion criteria regarding blood pressure, coagulation status, and recent trauma or surgery is mandatory.
Hypersensitivity: Anaphylactic or anaphylactoid reactions may occur.
Reperfusion Injury: Reperfusion of ischemic areas may precipitate arrhythmias (e.g., accelerated idioventricular rhythm) or cerebral edema.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Bleeding events (including intracranial hemorrhage), nausea, vomiting, and fever.
Clinical Research Highlights: Pivotal trials (e.g., NINDS, GUSTO) have established alteplase as a cornerstone of reperfusion therapy, demonstrating significant improvements in neurological recovery and survival when administered within the therapeutic time window.
6. Drug Interactions
Anticoagulants and Antiplatelets: Concomitant use with heparin, warfarin, or platelet aggregation inhibitors significantly increases the risk of hemorrhage.
Other Thrombolytics: Concomitant or sequential use with other thrombolytic agents is contraindicated.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Alteplase (recombinant t-PA). Excipients: Arginine, sucrose, polysorbate 80, hydrochloric acid/sodium hydroxide (for pH adjustment).
Appearance: White to off-white lyophilized cake or powder. The provided solvent is Sterile Water for Injection.
Packaging: Single-use vial (10 mg, 20 mg, 50 mg, or 100 mg).
Storage: Store in the original carton at 2°C to 8°C. Do not freeze.