Altiplase (Tissue Plasminogen Activator)

Indications
 Intravenous
Acute myocardial infarction
Adult: A total dose of 100 mg should be given as soon as possible after the onset of symptoms; total dose should be ≤1.5 mg/kg in patients weighing <65 kg. For admin within 6 hr of MI: 15 mg as bolus, then 0.75 mg/kg (up to a max of 50 mg) to be infused over 30 minutes, followed by the remainder dose to be infused over subsequent 60 minutes. For admin >6 hr after MI: 10 mg as bolus, then 50 mg to be infused over 60 minutes, followed by remainder dose to be infused over subsequent 2 hr.
Intravenous
Acute massive pulmonary embolism
Adult: Total dose: 100 mg but not >1.5 mg/kg for patients weighing <65 kg. First 10 mg as bolus, followed by infusion of the remainder dose over 2 hr.
Intravenous
Acute ischaemic stroke
Adult: To be given within 3 hr of the onset of symptoms: Infuse 0.9 mg/kg (up to a max total dose of 90 mg) over 60 minutes with 10% of the dose given as a bolus over the first minute.
Injection
Clearance of central venous lines
Adult: Using solution at a concentration of 1 mg/mL. Usual dose: 2 mg, may repeat after 2 hr if needed. Not to exceed a total dose of 4 mg. Patients weighing <30 kg: Dose is 110% of the internal lumen volume of the catheter (not >2 mg), may repeat after 2 hr if needed.

Reconstitution: Reconstitute by adding 50 ml of sterile water for inj without preservatives to a vial containing 50 mg of drug using a large-bore (e.g. 18-gauge) needle and directing the stream of diluent into the lyophilized plug of powder; diluents other than sterile water for inj without preservatives should not be used for reconstitution. Final concentration: 1 mg/ml.
Incompatibility: Y-site incompatibility: Dopamine, nitroglycerin, heparin and dobutamine. Admixture incompatibility: Dopamine, dobutamine, heparin.
Contraindications
 Recent surgery or trauma, susceptibility to internal bleeding, history of cerebrovascular accident, uncontrolled hypertension, esophageal varices, heavy vaginal bleeding, coagulation defects, aneurysm and poor glycaemic control.
Warnings / Precautions
 Children, elderly. Pregnancy. Monitor intracranial haemorrhage and BP in acute stroke. Renal impairment.
Adverse Reactions
 Vomiting, bleeding from puncture sites, gingival tissues and urinary tract.
Potentially Fatal: Haemorrhage esp with previous trauma or unsuspected underlying cause of bleeding, intracerebral bleeding.
Drug Interactions
 Heparin reduces risk of coronary reocclusion. Prostacyclin and nitrates increase plasma alteplase clearance.
Potentially Fatal: Increased risk of GI bleeding with NSAIDs. Increased risk of hemorrhage with warfarin.
See Below for More alteplase Drug Interactions
Lab Interactions
 May interfere with estimation of plasma fibrinogen and other coagulation tests.
Mechanism of Actions
 Alteplase initiates local fibrinolysis and dissolution of clots by binding to fibrin in a thrombus and the fibrin-bound plasminogen is converted to plasmin.
Excretion: Cleared rapidly from the plasma mainly by hepatic metabolism. Half-life: 4-5 minutes (initial); about 40 minutes (terminal).
Storage Conditions
 Injection: For Activase®: Lyophilised product: May store at room temperature (<30°C) or under refrigeration. Reconstituted solution: Use within 8 hr. Intravenous: For Activase®: Lyophilised product: May store at room temperature (<30°C) or under refrigeration. Reconstituted solution: Use within 8 hr.
ATC Classification
 S01XA13 - alteplase ; Belongs to the class of other ophthalmologicals.
B01AD02 - alteplase ; Belongs to the class of enzymes. Used in the treatment of thrombosis.
Storage
 Injection: For Activase®: Lyophilised product: May store at room temperature (<30°C) or under refrigeration. Reconstituted solution: Use within 8 hr. Intravenous: For Activase®: Lyophilised product: May store at room temperature (<30°C) or under refrigeration. Reconstituted solution: Use within 8 hr.
Available As
  • Altiplase (Tissue Plasminogen Activator) 20 mg
  • Altiplase (Tissue Plasminogen Activator) 50 mg

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