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Tenecteplase

Class: Thrombolytic Agents
- Tissue-type Plasminogen Activator (Recombinant)
Brands: TNKase

Medically reviewed by Drugs.com on Oct 13, 2020. Written by ASHP.

Introduction

Thrombolytic agent; biosynthetic (recombinant DNA origin) form of human tissue-type plasminogen activator (t-PA).

Uses for Tenecteplase

Acute MI

Used for reperfusion therapy in patients with acute MI, in conjunction with appropriate anticoagulant (e.g., heparin) and antiplatelet (e.g., aspirin and clopidogrel) therapies.

Current standard of care in patients with ST-segment-elevation MI (STEMI) is timely reperfusion (with primary PCI or thrombolytic therapy). The American College of Cardiology Foundation/American Heart Association (ACCF/AHA) guideline states that reperfusion therapy should be administered to all eligible patients with STEMI and onset of ischemic symptoms within the previous 12 hours. Select appropriate reperfusion method based on a risk-benefit analysis, considering the time from onset of MI symptoms, patient's clinical and hemodynamic status, comorbidities (e.g., severe heart failure), bleeding risk, contraindications, and availability (and timeliness) of PCI.

Primary PCI is preferred when it can be performed in a timely manner. Thrombolytic therapy is recommended when it is anticipated that PCI cannot be performed within 120 minutes of first medical contact.

Benefits of thrombolytic therapy in patients with STEMI are well established; 30-day and 1-year mortality rates similar after tenecteplase 30–50 mg or an accelerated infusion of alteplase.

Clinical benefit diminishes as the time period from symptom onset to initiation of therapy increases. Administer as soon as possible after onset of acute MI symptoms. ACCF and AHA recommend administration within 30 minutes of hospital arrival.

Pulmonary Embolism

Has been used for the treatment of acute PE.

The American College of Chest Physicians (ACCP) generally recommends against the use of systemic thrombolytic therapy in most patients with acute PE; however, in patients with acute PE associated with hypotension (e.g., systolic BP <90 mm Hg), thrombolytic therapy may provide some benefit in terms of mortality reduction and is suggested as a possible treatment in patients without a high risk of bleeding.

Tenecteplase Dosage and Administration

General

  • Initiate therapy as soon as possible after acute MI. (See Acute MI under Uses.)

Administration

IV Administration

For solution compatibility information, see Solution Compatibility under Stability.

Administer IV.

Reconstitution

Consult the manufacturer's labeling for instructions for using the B-D 10-mL Syringe with TwinPak Dual Cannula Device for reconstitution and administration.

Reconstitute with 10 mL of sterile water for injection without preservatives to provide a solution containing 5 mg/mL.

If foaming (usually slight) occurs, leave vial undisturbed for several minutes to allow dissipation of any large bubbles. Gently swirl until contents are completely dissolved; avoid shaking.

Rate of Administration

Administer over 5 seconds.

Dosage

Expressed in mg.

Biologic potency is determined using an in vitro clot lysis assay and is expressed in tenecteplase-specific units. Each mg is equivalent to 200 tenecteplase-specific units.

Dose based on patient weight.

Adults

Acute MI
IV

Patient Weight (kg)

Tenecteplase Dose (mg)

<60

30

≥60 to <70

35

≥70 to <80

40

≥80 to <90

45

≥90

50

Prescribing Limits

Adults

Acute MI
IV

Total dose should not exceed 50 mg.

Cautions for Tenecteplase

Contraindications

  • Active internal bleeding.

  • History of cerebrovascular accident.

  • Recent (within 2 months) intracranial or intraspinal surgery or trauma.

  • Intracranial neoplasm.

  • Intracranial vascular disease (i.e., arteriovenous malformation, aneurysm).

  • Known bleeding diathesis.

  • Severe uncontrolled hypertension.

Warnings/Precautions

Warnings

Effects on Hemostasis

Possible bleeding involving internal bleeding at intracranial or retroperitoneal sites or bleeding from the GI, GU, or respiratory tract. Superficial or surface bleeding at vascular puncture and access sites (e.g., venous cutdowns, arterial punctures) or sites of recent surgical intervention also may occur.

Weigh increased risks of therapy against anticipated benefits in patients with recent major surgery (e.g., CABG), obstetric delivery, organ biopsy, previous puncture of noncompressible vessels, cerebrovascular disease, hypertension (SBP ≥180 mm Hg and/or DBP ≥110 mm Hg), hemostatic defects (e.g., secondary to severe hepatic or renal disease), recent GI (active peptic ulcer) or GU bleeding, or recent trauma. Also, weigh risks against benefits of therapy in patients with diabetic hemorrhagic retinopathy or other hemorrhagic ophthalmic conditions. Weigh risks against benefits in patients receiving concurrent oral anticoagulant therapy (e.g., warfarin) or recent therapy with platelet glycoprotein (GP IIb/IIIa) inhibitors. Weigh risks against benefits in patients with any condition in which bleeding constitutes a substantial hazard or would be particularly difficult to manage because of its location.

Initiate therapy only after careful screening for contraindications.

Minimize risk of bleeding by carefully selecting patients and monitoring all potential bleeding sites (e.g., venous punctures). Avoid IM injections for the first few hours following therapy. Perform invasive venous procedures carefully and as infrequently as possible. Minimize arterial punctures. Avoid arterial and venous invasive procedures in areas that are inaccessible to manual compression (e.g., internal jugular or subclavian punctures). Use of an artery in an upper extremity is preferred if an arterial puncture is essential. Apply pressure to the puncture site for ≥30 minutes followed by a pressure dressing and frequent inspection of the puncture site for bleeding.

If serious bleeding occurs, immediately discontinue heparin and platelet-aggregation inhibitors. Can reverse heparin anticoagulation with protamine sulfate.

Cardiovascular Effects

Weigh risks against anticipated benefits of therapy in patients with a high likelihood of left heart thrombus (e.g., mitral stenosis with atrial fibrillation), acute pericarditis, subacute bacterial endocarditis, septic thrombophlebitis, or an occluded arteriovenous cannula at a seriously infected site.

Cholesterol Embolization

Possibly fatal cholesterol crystal embolization associated with invasive vascular procedures (e.g., cardiac catheterization, angiography, vascular surgery) and/or thrombolytic agents. Clinical features of cholesterol embolism include livedo reticularis, “purple toe” syndrome, acute renal failure, gangrenous digits, hypertension, pancreatitis, MI, cerebral infarction, spinal cord infarction, retinal artery occlusion, bowel infarction, and rhabdomyolysis.

Arrhythmias

Possible reperfusion-related arrhythmias (e.g., sinus bradycardia, accelerated idioventricular rhythm, ventricular premature depolarizations, ventricular tachycardia).

Manage with standard antiarrhythmic measures. Have appropriate antiarrhythmic therapy available during and after administration.

Sensitivity Reactions

Hypersensitivity Reactions

Allergic-type reactions (e.g., angioedema, laryngeal edema, rash, urticaria) or anaphylactoid reactions reported rarely.

Institute appropriate therapy if an anaphylactoid reaction occurs.

Readministration

Use with caution in patients with previous drug exposure. Repeat courses not systematically studied.

Specific Populations

Pregnancy

Category C.

Increased risk of therapy in pregnant women; weigh risks against benefits of therapy in pregnant women.

Lactation

Not known whether tenecteplase is distributed into milk. Caution if used in nursing women.

Pediatric Use

Safety and efficacy not established in children <18 years of age.

Geriatric Use

Intracranial hemorrhage, stroke, death, and major bleeding (i.e., bleeding requiring blood transfusions or leading to hemodynamic compromise) more frequent in patients ≥65 years of age than in younger adults. Weigh risks of drug against potential benefits.

Hepatic Impairment

Weigh risks of therapy against potential benefits in patients with severe hepatic impairment.

Common Adverse Effects

Bleeding.

Interactions for Tenecteplase

Specific Drugs

Drug

Interaction

Comments

Aspirin

Increased risk of hemorrhage

Dipyridamole

Increased risk of hemorrhage

Safety of concomitant therapy not established

GP IIb/IIIa-receptor inhibitors

Increased risk of hemorrhage

Safety of concomitant therapy not established

Weigh risks against benefits

Heparin

Increased risk of hemorrhage

Warfarin

Increased risk of hemorrhage

Weigh risks against benefits

Tenecteplase Pharmacokinetics

Distribution

Extent

Not known whether tenecteplase is distributed into human milk.

Elimination

Metabolism

Cleared by the liver.

Half-life

Initial half-life is 20–24 minutes. Terminal half-life is 90–130 minutes.

Stability

Storage

Parenteral

Powder for Injection

Controlled room temperature ≤30°C or under refrigeration at 2–8°C.

Reconstituted solutions contain no preservative. Preferably use solution immediately after preparation; may be used up to 8 hours after reconstitution if refrigerated. Discard any unused solution after 8 hours.

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility

Incompatible with dextrose.

If administered via an IV administration set that is used for infusing a dextrose-containing solution, flush line with 0.9% sodium chloride-containing solution prior to and following drug administration.

Do not use bacteriostatic water for injection as diluent.

Actions

  • Binds to fibrin and converts plasminogen to plasmin.

  • A relatively fibrin-selective plasminogen activator. Exhibits higher fibrin selectivity and greater resistance to plasminogen-activator inhibitors (e.g., PAI-1) than alteplase.

Advice to Patients

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses or recent surgery.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Tenecteplase

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

For IV use only

50 mg (with sterile water for injection)

TNKase

Genentech

AHFS DI Essentials™. © Copyright 2021, Selected Revisions October 23, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

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