Alteplase information from DrugsUpdate
P - Caution when used during pregnancy
LI - Lab *
Tissue plasminogen activator (abbreviated tPA or PLAT) is a protein involved in the breakdown of blood clots. Specifically, it is a serine protease (EC 3.4.21.68) found on endothelial cells, the cells that line the blood vessels. As an enzyme, it catalyzes the conversion of plasminogen to plasmin, the major enzyme responsible for clot breakdown. Because it works on the clotting system, tPA is used in clinical medicine to treat only embolic or thrombolytic stroke. Use is contraindicated in hemorrhagic stroke and head trauma.
tPA may be manufactured using recombinant biotechnology techniques. tPA created this way may be referred to as recombinant tissue plasimogen activator or rtPA.
Pharmacodynamics
Pharmacokinetics
Absorption
C max is 3 to 4 mg/L.
Distribution
Vd is 2.8 to 4.6 L and doubles at steady state.
Elimination
Initial t ½ is less than 5 min. Plasma Cl is 380 to 570 mL/min; total body Cl is 34.3 to 38.4 L/h. More than 80% is cleared from plasma within 10 minutes.
Alteplase Indications / Alteplase Uses
Information Not Available
Alteplase Adverse Reactions / Alteplase Side Effects
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.
Precautions
Monitor
Bleeding
Most frequent and serious adverse reaction. Monitor patient for signs of internal and superficial bleeding throughout therapy, paying particular attention to recent puncture and cutdown sites. If bleeding develops (epistaxis, hematuria, hematemesis, bloody or black, tarry stools) notify health care provider immediately. Should uncontrollable bleeding occur, discontinue alteplase therapy and concurrent heparin. Be prepared to administer protamine to reverse heparin effects.
Special Precautions
Children, elderly. Pregnancy. Monitor intracranial haemorrhage and BP in acute stroke. Renal impairment.
Other 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.
Other Interactions
Information Not Available
Dosage
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 hours 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 hours 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 hours.
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 hours.
Intravenous
Acute ischaemic strokes
Adult: To be given within 3 hours 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 hours 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 hours 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 injection 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.
Food(before/after)
Information Not Available
List of Contraindications
Alteplase and Pregnancy
Caution when used during pregnancy
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Alteplase and Lactation
Information Not Available
Alteplase and Children
Safety and efficacy not established ( Activase ); safety and efficacy in children younger than 2 yr of age or who weigh less than 10 kg have not been established ( Cathflo Activase ).
Alteplase and Geriatic
Take special precautions
Alteplase and Other 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.
Storage
Injection
For Activase®: Lyophilised product: May store at room temperature (<30°C) or under refrigeration. Reconstituted solution: Use within eight hours.
Intravenous
For Activase®: Lyophilised product: May store at room temperature (<30°C) or under refrigeration. Reconstituted solution: Use within eight hours.
Lab interference
Injection
For Activase®: Lyophilised product: May store at room temperature (<30°C) or under refrigeration. Reconstituted solution: Use within eight hours.
Intravenous
For Activase®: Lyophilised product: May store at room temperature (<30°C) or under refrigeration. Reconstituted solution: Use within eight hours.
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