Tenecteplase

What is Tenecteplase?

• Tenecteplase (TNKase and Metalyse) is a tissue plasminogen activator (tPA) produced by recombinant DNA technology using an established mammalian cell line (Chinese Hamster Ovary cells).
• Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA (cDNA) for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296—299 in the protease domain.

What are the uses of this medicine?

• Tenecteplase (TNKase and Metalyse) is indicated for use in the reduction of mortality associated with acute myocardial infarction (AMI).
• Treatment should be initiated as soon as possible after the onset of AMI symptoms.

How does this medicine work?

• Tenecteplase is a modified form of human tissue plasminogen activator (tPA) that binds to fibrin and converts plasminogen to plasmin. In the presence of fibrin, in vitro studies demonstrate that Tenecteplase conversion of plasminogen to plasmin is increased relative to its conversion in the absence of fibrin.
• This fibrin specificity decreases systemic activation of plasminogen and the resulting degradation of circulating fibrinogen as compared to a molecule lacking this property.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Active internal bleeding
• History of cerebrovascular accident
• Intracranial or intraspinal surgery or trauma within 2 months
• Intracranial neoplasm, arteriovenous malformation, or aneurysm
• Known bleeding diathesis
• Severe uncontrolled hypertension

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• Anticoagulants (such as heparin and vitamin K antagonists)
• drugs that alter platelet function (such as acetylsalicylic acid, dipyridamole, and GP IIb/IIIa inhibitors)

Is this medicine FDA approved?

• Yes, it was FDA approved.

How should this medicine be used?

Recommended dosage: The recommended total dose should not exceed 50 mg and is based upon patient weight as fallows:

• <60kg: 30mg
• ≥60 to <70 kg: 35mg
• ≥70 to <80 kg: 40mg
• ≥80 to <90 kg: 45mg
• ≥90 kg: 50mg

Administration:

• TNKase is a sterile, white to off-white, lyophilized powder for single intravenous (IV) bolus administration after reconstitution with Sterile Water for Injection.
• TNKase® (Tenecteplase) is for intravenous administration only.
• A single bolus dose should be administered over 5 seconds based on patient weight.
• The product should be visually inspected prior to administration for particulate matter and discoloration.
• TNKase may be administered as reconstituted at 5 mg/mL.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a sterile, white to off-white, lyophilized powder for single intravenous (IV) bolus administration after reconstitution with Sterile Water for Injection.

This medicine is available in fallowing brand namesː

• TNKase and Metalyse

What side effects can this medication cause?

The most common side effects of this medicine may include:

• bleeding

Less common, but serious side effects may include:

• Hypersensitivity
• cardiogenic shock, arrhythmias, atrioventricular block, pulmonary edema, heart failure, cardiac arrest, recurrent myocardial ischemia, myocardial reinfarction, myocardial rupture, cardiac tamponade, pericarditis, pericardial effusion, mitral regurgitation, thrombosis, embolism, and electromechanical dissociation.
• Nausea and/or vomiting, hypotension, and fever have also been reported.

What special precautions should I follow?

• The most common complication encountered during TNKase therapy is bleeding. If serious bleeding (not controlled by local pressure) occur, any concomitant heparin or antiplatelet agents should be discontinued immediately and treated appropriately.
• The use of thrombolytics can increase the risk of thrombo-embolic events in patients with high likelihood of left heart thrombus, such as patients with mitral stenosis or atrial fibrillation.
• Cholesterol embolism has been reported rarely in patients treated with all types of thrombolytic agents; the true incidence is unknown.
• Coronary thrombolysis may result in arrhythmias associated with reperfusion. It is recommended that anti‑arrhythmic therapy for bradycardia and/or ventricular irritability be available when TNKase is administered.
• Standard management of myocardial infarction should be implemented concomitantly with TNKase treatment.
• Hypersensitivity, including urticarial / ]]anaphylactic]] reactions, have been reported after administration of TNKase (e.g., anaphylaxis, angioedema, laryngeal edema, rash, and urticaria). Monitor patients treated with TNKase during and for several hours after infusion. If symptoms of hypersensitivity occur, appropriate therapy should be initiated.
• During TNKase therapy, results of coagulation tests and/or measures of fibrinolytic activity may be unreliable unless specific precautions are taken.
• It is not known if TNKase is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when TNKase is administered to a nursing woman.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies in pregnant women.
• TNKase should be given to pregnant women only if the potential benefits justify the potential risk to the fetus.

Can this medicine be used in children?

• The safety and effectiveness of TNKase in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• TENECTEPLASE

Inactive ingredients:

• ARGININE
• PHOSPHORIC ACID
• POLYSORBATE 20

Who manufactures and distributes this medicine?

Manufactured by:

• Genentech, Inc.
• A Member of the Roche Group
• South San Francisco, CA

What should I know about storage and disposal of this medication?

• Store lyophilized TNKase at controlled room temperature not to exceed 30°C (86°F) or under refrigeration 2–8°C (36–46°F).
• Do not use beyond the expiration date stamped on the vial.

• Dailymed label info on Tenecteplase
• FDA Tenecteplase

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