Alteplase (t-PA) is a thrombolytic medication, used to treat acute ST-elevation myocardial infarction, pulmonary embolism associated with low blood pressure, acute ischemic stroke, and blocked central venous catheter.
It is the standard agent used in early reperfusion therapy.
A thrombolytic drug, used to dissolve clots to restore tissue perfusion.
Alteplase binds to fibrin in a blood clot and activates the clot-bound plasminogen.
Ot cleaves plasminogen at the site of its Arg561-Val562 peptide bond to form plasmin.
Plasmin is a fibrinolytic enzyme that cleaves the cross-links between polymerized fibrin molecules, causing the blood clot to break down and dissolve in a process called fibrinolysis.
Administered by injection into a vein or artery.
It is the same as human plasminogen activator.
It is synthesized via recombinant DNA technology from vascular endothelial cells.
Activase is the trade name.
Pregnancy category US: C (Risk not ruled out)
It potentially can reverse blood flow with obstructed by coagulated blood.
Uses: acute ischemic stroke, acute myocardial infarction, massive pulmonary embolism, clogged catheters.
It is delivered intravenously into the body and administered directly into the catheter to treat blocked catheters.
In adults with acute ischemic stroke, thrombolytic therapy with alteplase is given in early management, within 4.5 hours of symptom onset.
It is contraindicated if there is a risk of major bleeding or if there may be another cause of stroke symptoms.
CHOICE study demonstrated the use of Alteplase following thrombectomy is more effective than Alteplase alone in Acute ischemic stroke.
The preferred treatment for ST-elevation myocardial infarction (STEMI) is percutaneous coronary intervention (PCI), however, alteplase is recommended for use for STEMI if the patient is at a non-PCI capable hospital and cannot be transferred to receive PCI in under 120 minutes.
Alteplase should not be used in cases of acute coronary syndrome other than STEMI.
It is the most commonly used medication to treat pulmonary embolism.
It has a short infusion time of 2 hours and a half-life of 4–6 minutes.
It is approved for the treatment by systemic thrombolysis or catheter-directed thrombolysis for pulmonary embolism.
In Acute pulmonary embolism systemic thrombolysis with alteplase can quickly restore right ventricular function, heart rate, and blood pressure.
Standard doses of alteplase given by systemic thrombolysis may lead to massive bleeding, such as intracranial hemorrhage.
Bleeding is particularly common in older patients.
Low-dose alteplase is safer than and as effective as the standard amount for thrombolysis,
Catheter-directed thrombolysis may be more efficient than systemic thrombolysis.
Alteplase used to treat PE if patients have a high risk for complications: hypotensive with a systolic blood pressure less than 90 mmHg, they are in cardiac arrest presumed to be caused by a pulmonary embolism or
their clinical exam shows signs of deterioration or worsening of symptoms.
It can be used in small doses to clear blood clots that obstruct a catheter, as
obstruction is commonly observed with a central venous catheters.
Adverse effects of alteplase for clearing blood clots are rare phenomena.
Use not appropriate with acute ischemic stroke or if the risks of treatment outweighs the likely benefits.
Use contraindicated in those with bleeding disorders, current intracranial hemorhage and subarachnoid hemorrhage. and in those with an abnormally low platelet count.
Active internal bleeding and high hypertension are additional contraindications for alteplase.
Safety in the pediatric population has not been determined.
Additional contraindications for alteplase when used specifically for acute ischemic stroke include current intracranial hemorhage and subarachnoid hemorrhage.
A common adverse effect is bleeding, which can be life threatening.
Angioedema can be life-threatening rare association.
Alteplase is a pregnancy category C drug.
Plasminogen activator inhibitor 1 stops alteplase activity by binding and forming an inactive complex.
The plasminogen activator inhibitor 1 alteplase complex is removed from the bloodstream by the liver.
Plasmin induced fibrinolysis is very short-lived due to plasmin inhibitors, which inactivate and regulate plasmin activity.
Use is effective to treat ischemic stroke.
Among patients with acute ischemic stroke treated with intravenous alteplase the use of NOACs within the preceding seven days, compared with no use of anticoagulants, was not associated with significantly increased risk of intracranial hemorrhage.
Among patient with ischemic stroke treated within 4 1/2 hours after the symptom onset reteplase was more likely result in an excellent functional outcome than Alteplase (RAISE investigators).
In patients with acute ischemic stroke eligible for intravenous thrombolysis within 4.5 hours after stroke onset tenecteplase was not inferior to alteplase with respect to excellent functional outcome at 90 days and had a similar safety profile (Meng X).