BLACK BOX WARNING
- intracranial hemorrhage risk
reteplase
Brand: Retavase
⚠ BBW ISMP High Alert Prototype: alteplase
Drug Class: thrombolytic agent
Drug Family: thrombolytic
Subclass: recombinant plasminogen activator — deletion mutant
Organ Systems: cardiovascularhematology-oncology
Mechanism of Action
Deletion mutant of alteplase lacking the kringle 1 and finger domains; binds fibrin with lower affinity than alteplase but maintains plasminogen activation; slower hepatic clearance extends half-life, enabling a double-bolus dosing regimen for STEMI reperfusion.
plasminogen (fibrin-bound)fibrin clot
Indications
- acute STEMI
Contraindications
- active internal bleeding
- history of CVA
- intracranial or intraspinal surgery or trauma within 2 months
- intracranial neoplasm
- AV malformation or aneurysm
- severe uncontrolled hypertension
- suspected aortic dissection
- bleeding diathesis
- severe uncontrolled hypertension
Adverse Effects
Common
- bleeding at puncture sites
- ecchymosis
- epistaxis
Serious
- intracranial hemorrhage
- major systemic hemorrhage
- cholesterol embolism
Pharmacokinetics (ADME)
| Absorption | IV bolus administration only |
| Distribution | blood volume |
| Metabolism | hepatic clearance; deletion of fibronectin finger and EGF-like domains reduces hepatic receptor binding |
| Excretion | hepatic |
| Half-life | approximately 13-16 minutes |
| Onset | immediate |
| Peak | end of each bolus |
| Duration | double-bolus given 30 minutes apart; fibrinolysis maintained throughout |
| Protein Binding | low |
| Vd | approximately 6-12 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| anticoagulants and antiplatelet agents | additive bleeding and hemorrhagic risk | major |
| heparin | used with reteplase in STEMI protocol; monitor aPTT carefully | moderate |
Nursing Considerations
- Reteplase is given as two separate 10-unit IV boluses over 2 minutes each, separated by exactly 30 minutes; set a timer and document both doses with times in the medical record.
- Do not administer in the same IV line as heparin; flush line thoroughly with normal saline before and after each bolus; incompatible with dextrose solutions.
- Monitor for signs of reperfusion (resolution of chest pain, ECG normalization, reperfusion arrhythmias) and bleeding (access site, hemodynamic instability, neurological changes).
- Minimize arterial and venous punctures during and after administration; if non-compressible site bleeding occurs, apply prolonged pressure and notify the medical team.
Clinical Pearls
- Reteplase's double-bolus regimen (10 units + 10 units, 30 minutes apart) was developed as a simpler alternative to alteplase's weight-adjusted infusion, though tenecteplase's single bolus has largely replaced reteplase in many clinical settings.
- Lower fibrin specificity compared with alteplase results in greater systemic plasminogen depletion ('lytic state'), which may contribute to efficacy but also increases systemic bleeding risk.
Safety Profile
Pregnancy use-with-caution
Lactation insufficient-data
Renal Adjustment Not required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.