TNKASE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TNKASE (TNKASE).

How it works

Tenecteplase is a recombinant tissue plasminogen activator (tPA) that binds to fibrin and converts plasminogen to plasmin, leading to fibrinolysis. It has higher fibrin specificity and longer half-life than alteplase.

What the body does with it

Metabolism	Primarily cleared by hepatic metabolism via unknown pathways; not metabolized by CYP450 enzymes; renal clearance accounts for <5%.
Excretion	Primarily hepatic metabolism, with less than 5% renal excretion of unchanged drug. Biliary/fecal excretion is minimal.
Half-life	Terminal elimination half-life is 18–25 minutes in patients with acute myocardial infarction, reflecting predominantly hepatic clearance. The half-life increases with age and renal impairment, up to 40 minutes in elderly patients.
Protein binding	Approximately 50–60% bound to plasma proteins, primarily albumin and fibrinogen.
Volume of Distribution	Volume of distribution is 6.1–12.5 L (0.09–0.18 L/kg), indicating limited extravascular distribution, consistent with a large protein molecule that remains primarily in the intravascular space.
Bioavailability	Bioavailability: Intravenous administration only as bolus injection; oral bioavailability is negligible due to protein nature and gastrointestinal degradation.
Onset of Action	Intravenous bolus: clinical effect (thrombolysis) begins within 10–15 minutes of administration, with maximum fibrinolytic activity achieved within 30 minutes.
Duration of Action	Duration of thrombolytic effect is approximately 2–4 hours, based on plasma clearance. Residual fibrinolytic activity may persist for up to 24 hours due to fibrin-bound clot lysis.

Classification & Brands

Dosing & administration

0.5 mg/kg IV bolus over 5 seconds, maximum dose 50 mg, administered once.

Dosage form	VIAL
Renal impairment	No dose adjustment required for renal impairment. Contraindicated in severe renal impairment (CrCl <30 mL/min) due to increased bleeding risk.
Liver impairment	No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh class A or B). Use caution in severe hepatic impairment (Child-Pugh class C) due to coagulopathy.
Pediatric use	Not approved for use in pediatric patients; safety and efficacy not established.
Geriatric use	No specific dose adjustment; increased caution due to higher risk of bleeding. Same dosing as adults.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TNKASE (TNKASE).

Breastfeeding	It is unknown if tenecteplase is excreted in human milk. Due to high molecular weight, excretion is unlikely. M/P ratio not available. Caution recommended; consider risk of infant bleeding if exposure occurs.
Teratogenic Risk	TNKASE (tenecteplase) is a recombinant tissue plasminogen activator. Data in pregnant women are limited. In first trimester, animal studies show no evidence of teratogenicity, but human data are insufficient. Second and third trimester: risks include placental abruption, preterm labor, and maternal hemorrhage. Use only if potential benefit justifies risk to fetus.

Warnings & precautions

■ FDA Black Box Warning

Do not administer to patients with active internal bleeding, recent intracranial or intraspinal surgery, recent intracranial hemorrhage, intracranial neoplasm, arteriovenous malformation, aneurysm, bleeding diathesis, or severe uncontrolled hypertension.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Active internal bleeding","Recent intracranial or intraspinal surgery or trauma","Intracranial neoplasm","Arteriovenous malformation or aneurysm","Known bleeding diathesis","Severe uncontrolled hypertension (e.g., systolic >180 mmHg or diastolic >110 mmHg)"]

Clinical Precautions

Precautions

["Risk of bleeding (including intracranial hemorrhage)","Avoid in patients with recent major surgery or trauma","Monitor for hypotension and arrhythmias during infusion","Use caution in patients with history of stroke or transient ischemic attack"]

Clinical Tips & Counseling

Drug interactions

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TNKASE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TNKASE (TNKASE).

How it works

What the body does with it

Metabolism	Primarily cleared by hepatic metabolism via unknown pathways; not metabolized by CYP450 enzymes; renal clearance accounts for <5%.
Excretion	Primarily hepatic metabolism, with less than 5% renal excretion of unchanged drug. Biliary/fecal excretion is minimal.
Half-life	Terminal elimination half-life is 18–25 minutes in patients with acute myocardial infarction, reflecting predominantly hepatic clearance. The half-life increases with age and renal impairment, up to 40 minutes in elderly patients.
Protein binding	Approximately 50–60% bound to plasma proteins, primarily albumin and fibrinogen.
Volume of Distribution	Volume of distribution is 6.1–12.5 L (0.09–0.18 L/kg), indicating limited extravascular distribution, consistent with a large protein molecule that remains primarily in the intravascular space.
Bioavailability	Bioavailability: Intravenous administration only as bolus injection; oral bioavailability is negligible due to protein nature and gastrointestinal degradation.
Onset of Action	Intravenous bolus: clinical effect (thrombolysis) begins within 10–15 minutes of administration, with maximum fibrinolytic activity achieved within 30 minutes.
Duration of Action	Duration of thrombolytic effect is approximately 2–4 hours, based on plasma clearance. Residual fibrinolytic activity may persist for up to 24 hours due to fibrin-bound clot lysis.

Classification & Brands

Dosing & administration

0.5 mg/kg IV bolus over 5 seconds, maximum dose 50 mg, administered once.

Dosage form	VIAL
Renal impairment	No dose adjustment required for renal impairment. Contraindicated in severe renal impairment (CrCl <30 mL/min) due to increased bleeding risk.
Liver impairment	No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh class A or B). Use caution in severe hepatic impairment (Child-Pugh class C) due to coagulopathy.
Pediatric use	Not approved for use in pediatric patients; safety and efficacy not established.
Geriatric use	No specific dose adjustment; increased caution due to higher risk of bleeding. Same dosing as adults.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TNKASE (TNKASE).

Breastfeeding	It is unknown if tenecteplase is excreted in human milk. Due to high molecular weight, excretion is unlikely. M/P ratio not available. Caution recommended; consider risk of infant bleeding if exposure occurs.
Teratogenic Risk	TNKASE (tenecteplase) is a recombinant tissue plasminogen activator. Data in pregnant women are limited. In first trimester, animal studies show no evidence of teratogenicity, but human data are insufficient. Second and third trimester: risks include placental abruption, preterm labor, and maternal hemorrhage. Use only if potential benefit justifies risk to fetus.