RETAVASE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for RETAVASE (RETAVASE).

How it works

Reteplase is a recombinant non-glycosylated form of tissue plasminogen activator that binds to fibrin and converts plasminogen to plasmin, leading to fibrinolysis.

What the body does with it

Metabolism	Reteplase is primarily cleared by the liver and kidneys; specific metabolic pathways are not fully characterized.
Excretion	Primarily hepatic metabolism; no significant renal or biliary excretion of active drug. Elimination is via proteolytic degradation with subsequent renal excretion of inactive metabolites.
Half-life	Mean terminal elimination half-life: 3.0–4.5 hours (range 1.5–6.0 hours). Clinical context: The short half-life reduces bleeding risk compared to longer-acting thrombolytics; re-administration may be needed for sustained effect.
Protein binding	Approximately 50% bound to plasma proteins, primarily albumin.
Volume of Distribution	Approximately 0.5 L/kg (range 0.4–0.6 L/kg). Clinical meaning: Confined to plasma and extracellular fluid; limited tissue distribution.
Bioavailability	Intravenous: 100% (only route of administration); not available orally.
Onset of Action	Intravenous bolus: Onset of thrombolysis within 30 minutes; maximum effect by 90 minutes.
Duration of Action	Duration of fibrinolytic effect: 4–6 hours. Clinical note: Prolonged effect not expected; re-occlusion prevented by adjunctive anticoagulation.

Classification & Brands

Dosing & administration

10 IU (two 5 IU vials) administered as two separate IV bolus injections, each over 2 minutes, given 30 minutes apart.

Dosage form	VIAL
Renal impairment	No dose adjustment required for renal impairment; drug is minimally renally excreted.
Liver impairment	No dose adjustment recommended; pharmacokinetics not studied in hepatic impairment.
Pediatric use	Safety and effectiveness have not been established in pediatric patients.
Geriatric use	No specific dose adjustment; elderly patients may be at increased risk of bleeding, but no dose modification is recommended based on age alone.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for RETAVASE (RETAVASE).

Breastfeeding	No human data; M/P ratio unknown. Recombinant protein likely degraded in infant GI tract. Use caution due to risk of hemorrhage in lactating mother if systemic absorption occurs.
Teratogenic Risk	Pregnancy Category C. First trimester: No adequate human studies; animal studies show increased post-implantation loss. Second/third trimester: Fibrinolytic activity may cause placental abruption, hemorrhage, or preterm labor. Avoid use unless benefit outweighs risk.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Reteplase can cause fatal bleeding, including intracranial hemorrhage. Do not use in patients with active internal bleeding, recent intracranial or intraspinal surgery, intracranial neoplasm, arteriovenous malformation, aneurysm, bleeding diathesis, severe uncontrolled hypertension, or known intracranial hemorrhage.

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 (systolic >180 mmHg or diastolic >110 mmHg)","Current intracranial hemorrhage or subarachnoid hemorrhage"]

Clinical Precautions

Precautions

["Risk of serious bleeding, including intracranial hemorrhage","Monitor for bleeding during administration","Avoid use in patients with risk factors for bleeding (e.g., recent trauma, surgery, pregnancy, peptic ulcer disease)","Arrhythmias may occur with reperfusion","Hypersensitivity reactions including anaphylaxis"]

Clinical Tips & Counseling

Drug interactions

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RETAVASE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for RETAVASE (RETAVASE).

How it works

Reteplase is a recombinant non-glycosylated form of tissue plasminogen activator that binds to fibrin and converts plasminogen to plasmin, leading to fibrinolysis.

What the body does with it

Metabolism	Reteplase is primarily cleared by the liver and kidneys; specific metabolic pathways are not fully characterized.
Excretion	Primarily hepatic metabolism; no significant renal or biliary excretion of active drug. Elimination is via proteolytic degradation with subsequent renal excretion of inactive metabolites.
Half-life	Mean terminal elimination half-life: 3.0–4.5 hours (range 1.5–6.0 hours). Clinical context: The short half-life reduces bleeding risk compared to longer-acting thrombolytics; re-administration may be needed for sustained effect.
Protein binding	Approximately 50% bound to plasma proteins, primarily albumin.
Volume of Distribution	Approximately 0.5 L/kg (range 0.4–0.6 L/kg). Clinical meaning: Confined to plasma and extracellular fluid; limited tissue distribution.
Bioavailability	Intravenous: 100% (only route of administration); not available orally.
Onset of Action	Intravenous bolus: Onset of thrombolysis within 30 minutes; maximum effect by 90 minutes.
Duration of Action	Duration of fibrinolytic effect: 4–6 hours. Clinical note: Prolonged effect not expected; re-occlusion prevented by adjunctive anticoagulation.

Classification & Brands

Dosing & administration

10 IU (two 5 IU vials) administered as two separate IV bolus injections, each over 2 minutes, given 30 minutes apart.

Dosage form	VIAL
Renal impairment	No dose adjustment required for renal impairment; drug is minimally renally excreted.
Liver impairment	No dose adjustment recommended; pharmacokinetics not studied in hepatic impairment.
Pediatric use	Safety and effectiveness have not been established in pediatric patients.
Geriatric use	No specific dose adjustment; elderly patients may be at increased risk of bleeding, but no dose modification is recommended based on age alone.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for RETAVASE (RETAVASE).

Breastfeeding	No human data; M/P ratio unknown. Recombinant protein likely degraded in infant GI tract. Use caution due to risk of hemorrhage in lactating mother if systemic absorption occurs.
Teratogenic Risk	Pregnancy Category C. First trimester: No adequate human studies; animal studies show increased post-implantation loss. Second/third trimester: Fibrinolytic activity may cause placental abruption, hemorrhage, or preterm labor. Avoid use unless benefit outweighs risk.
Fetal Monitoring