(ten EK te plase)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
TNKase: 50 mg
Brand Names: U.S.
- Thrombolytic Agent
Promotes initiation of fibrinolysis by binding to fibrin and converting plasminogen to plasmin. Tenecteplase is essentially alteplase with the exception of 3 point mutations and is more fibrin specific, more resistant to plasminogen activator inhibitor -1 (PAI-1), with a longer duration of action compared to alteplase. Produced by recombinant DNA technology using a mammalian cell line (Chinese hamster ovary cells).
Vd is weight related and approximates plasma volume
Clearance: Plasma: 99 to 119 mL/minute
Biphasic: Initial: 20 to 24 minutes; Terminal: 90 to 130 minutes
Use: Labeled Indications
Management of ST-elevation myocardial infarction (STEMI) for the lysis of thrombi in the coronary vasculature to restore perfusion and reduce mortality.
Recommended criteria for treatment of STEMI (ACCF/AHA; O’Gara, 2013): Ischemic symptoms within 12 hours of treatment or evidence of ongoing ischemia 12-24 hours after symptom onset with a large area of myocardium at risk or hemodynamic instability.
STEMI ECG definition: New ST-segment elevation at the J point in at least 2 contiguous leads of ≥2 mm (0.2 mV) in men or ≥1.5 mm (0.15 mV) in women in leads V2-V3 and/or of ≥1 mm (0.1 mV) in other contiguous precordial leads or limb leads on ECG. New or presumably new left bundle branch block (LBBB) may interfere with ST-elevation analysis and should not be considered diagnostic in isolation.
At non-PCI-capable hospitals, the ACCF/AHA recommends thrombolytic therapy administration when the anticipated first medical contact (FMC)-to-device time at a PCI-capable hospital is >120 minutes due to unavoidable delays.
Off Label Uses
Pulmonary embolism associated cardiac arrest
Several case reports suggest that the use of tenecteplase may be beneficial in the treatment of patients in cardiac arrest due to suspected pulmonary embolism (PE) [Nobre 2015], [Perrot 2010]. A prospective multicenter observational clinical trial in patients with non-traumatic undifferentiated cardiac arrest failing to respond to advanced cardiac life support measures demonstrated improved rates of ROSC, increased short term survival and neurologically intact survival to hospital discharge when treated with tenecteplase [Bozeman 2006]. Subsequently, however, a double-blind, multicenter trial conducted in patients with witnessed out of hospital undifferentiated cardiac arrest (patients with suspected pulmonary embolism were administered open label tenecteplase) did not demonstrate improvement in any outcomes; number of confirmed pulmonary embolism cases were too small to determine benefit in this subpopulation [Böttiger 2008]. Additional randomized controlled trials are needed to further define the role of tenecteplase for cardiac arrest due to PE.
Based on the American Heart Association guidelines for cardiopulmonary resuscitation and emergency cardiovascular care, thrombolytics may be considered when PE is presumed or confirmed as the cause of cardiac arrest. Contraindications should be considered but can be overridden since this therapy is potentially lifesaving [Lavonas 2015].
Active internal bleeding; history of cerebrovascular accident; recent (ie, within 2 months) intracranial/intraspinal surgery or trauma; intracranial neoplasm; arteriovenous malformation or aneurysm; bleeding diathesis; severe uncontrolled hypertension
Additional contraindications (ACCF/AHA; O’Gara 2013): Ischemic stroke within 3 months; prior intracranial hemorrhage; active bleeding (excluding menses); suspected aortic dissection; significant closed head or facial trauma within 3 months
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to tenecteplase or any component of the formulation.
STEMI: IV: The recommended total dose should not exceed 50 mg and is based on weight. Administer as a single bolus over 5 seconds:
<60 kg: 30 mg
≥60 to <70 kg: 35 mg
≥70 to <80 kg: 40 mg
≥80 to <90 kg: 45 mg
≥90 kg: 50 mg
Note: Thrombolytic should be administered within 30 minutes of hospital arrival. Generally, there is only a small trend for benefit of therapy after a delay of 12 to 24 hours from symptom onset, but thrombolysis may be considered for selected patients with ongoing ischemic pain and extensive ST elevation; however, primary PCI is preferred in these patients. Administer concurrent aspirin, clopidogrel, and anticoagulant therapy (ie, unfractionated heparin, enoxaparin, or fondaparinux) with tenecteplase (O’Gara 2013).
Pulmonary embolism (PE) associated with cardiac arrest (off-label use): IV: Administer as a single bolus over 5 seconds (Böttiger 2008; Bozeman 2006):
<60 kg: 30 mg
≥60 to <70 kg: 35 mg
≥70 to <80 kg: 40 mg
≥80 to <90 kg: 45 mg
≥90 kg: 50 mg
Refer to adult dosing. Although dosage adjustments are not recommended, the elderly have a higher incidence of morbidity and mortality with the use of tenecteplase.
Dosing: Renal Impairment
No dosage adjustment necessary.
Hemodialysis: Dialyzable: Unknown, but unlikely (NCS/SCCM [Frontera 2016])
Dosing: Hepatic Impairment
Mild to moderate impairment: No dosage adjustment provided in manufacturer's labeling.
Severe impairment: No dosage adjustment provided in manufacturer's labeling; weigh the risk of bleeding against the benefits with tenecteplase especially in those with a coagulopathy.
Tenecteplase should be reconstituted using the supplied 10 mL syringe with TwinPak Dual Cannula Device and 10 mL sterile water for injection. Do not shake when reconstituting. Slight foaming is normal and will dissipate if left standing for several minutes. The reconstituted solution is 5 mg/mL. Any unused solution should be discarded. If reconstituted and not used immediately, store in refrigerator and use within 8 hours.
Tenecteplase is incompatible with dextrose solutions. Dextrose-containing lines must be flushed with a saline solution before and after administration. Administer as a single IV bolus over 5 seconds. Avoid IM injections and nonessential handling of patient.
Store under refrigeration of 2°C to 8°C (36°F to 46°F) or at room temperature; do not exceed 30°C (86°F). If reconstituted and not used immediately, store in refrigerator and use within 8 hours.
Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): May enhance the anticoagulant effect of Thrombolytic Agents. Monitor therapy
Anticoagulants: Thrombolytic Agents may enhance the anticoagulant effect of Anticoagulants. Management: See full drug monograph for guidelines for the use of alteplase for acute ischemic stroke during treatment with oral anticoagulants. Monitor therapy
Aprotinin: May diminish the therapeutic effect of Thrombolytic Agents. Consider therapy modification
Dabigatran Etexilate: Thrombolytic Agents may enhance the anticoagulant effect of Dabigatran Etexilate. Management: Carefully monitor for bleeding. Dabigatran Canadian labeling recommends avoiding use with thrombolytic agents. Consider avoiding alteplase treatment of acute ischemic stroke in patients receiving dabigatran (see full drug monograph for details). Monitor therapy
Desirudin: Thrombolytic Agents may enhance the anticoagulant effect of Desirudin. Management: Discontinue treatment with thrombolytic agents prior to desirudin initiation. If concomitant use cannot be avoided, monitor patients receiving these combinations closely for clinical and laboratory evidence of excessive anticoagulation. Consider therapy modification
Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Thrombolytic Agents. Bleeding may occur. Consider therapy modification
Limaprost: May enhance the adverse/toxic effect of Thrombolytic Agents. The risk for bleeding may be increased. Monitor therapy
Prostacyclin Analogues: Thrombolytic Agents may enhance the adverse/toxic effect of Prostacyclin Analogues. Specifically, the antiplatelet effects of prostacyclin analogues may lead to an increased risk of bleeding when combined with thrombolytic agents. Monitor therapy
Salicylates: May enhance the adverse/toxic effect of Thrombolytic Agents. An increased risk of bleeding may occur. Monitor therapy
Altered results of coagulation and fibrinolytic activity tests
Hematologic & oncologic: Hemorrhage (ASSENT-2 trial: minor: 22%; major: 5%), hematoma (local: minor: 12%; major: 2%)
1% to 10%:
Cardiovascular: Cerebrovascular accident (2%)
Gastrointestinal: Gastrointestinal hemorrhage (minor: 2%; major: 1%)
Genitourinary: Genitourinary tract hemorrhage (minor: 4%; major: <1%)
Hematologic & oncologic: Local hemorrhage (catheter puncture site: minor: 4%; major: <1%)
Respiratory: Pharyngeal bleeding (minor: 3%), epistaxis (minor: 2%)
Frequency not defined:
Cardiovascular: Atrioventricular block, cardiac arrhythmia, cardiac failure, cardiac tamponade, cardiogenic shock, embolism, hypotension, ischemic heart disease (recurrent), mitral valve insufficiency (regurgitation), myocardial reinfarction, myocardial rupture, pericardial effusion, pericarditis, pulmonary edema, thrombosis
Gastrointestinal: Nausea, vomiting
<1% (Limited to important or life-threatening): Anaphylaxis, angioedema, intracranial hemorrhage, laryngeal edema, respiratory tract hemorrhage, retroperitoneal hemorrhage, skin rash, thrombolytic drug-induced cholesterol embolism (clinical features may include acute renal failure, bowel infarction, cerebral infarction, gangrenous digits, hypertension, livedo reticularis, myocardial infarction, pancreatitis, “purple toe” syndrome, retinal artery occlusion, rhabdomyolysis, spinal cord infarction), urticaria
Concerns related to adverse effects:
• Arrhythmias: Coronary thrombolysis may result in reperfusion arrhythmias.
• Bleeding: Monitor all potential bleeding sites. If serious bleeding occurs, the infusion of tenecteplase and heparin should be stopped.
• Conditions that increase bleeding risk: For the following conditions the risk of bleeding is higher with use of tenecteplase and the use of tenecteplase should be weighed against the benefits of therapy: recent (within 10 days) major surgery (eg, CABG, obstetrical delivery, organ biopsy, previous puncture of noncompressible vessels), cerebrovascular disease, recent (within 10 days) gastrointestinal or genitourinary bleeding, recent trauma (within 10 days) including CPR, hypertension (systolic BP >180 mm Hg and/or diastolic BP >110 mm Hg), high likelihood of left heart thrombus (eg, mitral stenosis with atrial fibrillation), acute pericarditis, subacute bacterial endocarditis, hemostatic defects including ones caused by severe renal or hepatic dysfunction, severe hepatic dysfunction, pregnancy, diabetic hemorrhagic retinopathy or other hemorrhagic ophthalmic conditions, septic thrombophlebitis or occluded AV cannula at seriously infected site, and/or any other condition in which bleeding constitutes a significant hazard or would be particularly difficult to manage because of location.
• Appropriate use: Follow standard management for ST-elevation myocardial infarction (STEMI) while administering tenecteplase.
Concurrent drug therapy issues:
• Anticoagulants: Use with caution in patients receiving oral anticoagulants; increased risk of bleeding. Adjunctive use of parenteral anticoagulants (eg, enoxaparin, heparin, or fondaparinux) is recommended to improve vessel patency and prevent reocclusion and may also contribute to bleeding; monitor for bleeding (ACCF/AHA; O’Gara 2013).
• GP IIb/IIIa inhibitors: Use tenecteplase with caution in patients who had recent administration of GP IIb/IIIa inhibitors; bleeding risk increased.
• Elderly: Use with caution in patients with advanced age; increased risk of bleeding. The 30-day mortality in the ASSENT-2 trial was 2.5% for patients <65 years of age, 8.5% for patients 65-74 years, and 16.2% for patients ≥75 years. The intracranial hemorrhage rate was 0.4% for patients <65 years, 1.6% for patients 65 to 74 years, and 1.7% for patients ≥75 years. The risks and benefits of use should be weighed carefully in the elderly.
• Administration: Avoid intramuscular injections and nonessential handling of the patient for a few hours after administration. Venipunctures should be performed carefully and only when necessary. If arterial puncture is necessary, use an upper extremity vessel that can be manually compressed. Caution with readministration of tenecteplase.
CBC, aPTT, signs and symptoms of bleeding, ECG monitoring
Pregnancy Risk Factor
Adverse events have been observed in some animal reproduction studies. The risk of bleeding may be increased in pregnant women. Administer to pregnant women only if the potential benefits justify the risk to the fetus.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Have patient report immediately to prescriber signs of bleeding (vomiting blood or vomit that looks like coffee grounds; coughing up blood; blood in the urine; black, red, or tarry stools; bleeding from the gums, abnormal vaginal bleeding, bruises without a reason or that get bigger, or any bleeding that is very bad or that will not stop), signs of kidney problems (urinary retention, blood in urine, change in amount of urine passed, or weight gain), signs of pancreatitis (severe abdominal pain, severe back pain, severe nausea, or vomiting), signs of severe cerebrovascular disease (change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or change in eyesight), angina, severe headache, severe abdominal pain, skin discoloration, vision changes, muscle pain, dark urine, arrhythmia, or bradycardia (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
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- Drug class: thrombolytics
Other brands: TNKase