RETAVASE^® (reteplase) is a recombinant plasminogen activator which catalyzes the cleavage of endogenous plasminogen to generate plasmin. Plasmin degrades the fibrin matrix of the thrombus, exerting its thrombolytic action.

RETAVASE^® (reteplase) pharmacology & MOA

Pharmacology¹

RETAVASE has an effective half-life of 13–16 minutes and is cleared primarily by the liver and kidneys.

Mean Fibrinogen Levels¹

In a controlled trial, 36 of 56 patients treated for myocardial infarction had a decrease in fibrinogen levels to below 100 mg/dL by 2 hours following the administration of RETAVASE as 2 intravenous injections (10 + 10 unit) in which a dose of 10 units was followed 30 minutes later by a second dose of 10 units.

In this trial, the mean fibrinogen level returned to the baseline value by 48 hours.

Mechanism of action¹

RETAVASE is a recombinant plasminogen activator. It catalyzes the cleavage of endogenous plasminogen to generate plasmin, which in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.

RETAVASE vials

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How to order RETAVASE

Important Safety Information

RETAVASE^® (reteplase) for injection is contraindicated in patients with:

Active internal bleeding
Recent stroke
Recent intracranial or intraspinal surgery or serious head trauma
Intracranial neoplasm, arteriovenous malformation, or aneurysm
Known bleeding diathesis
Severe uncontrolled hypertension

RETAVASE can cause significant and sometimes fatal bleeding. In a trial of 2,965 patients administered RETAVASE, the overall rate of in-hospital, intracranial hemorrhage was 0.8%. Avoid intramuscular injections and other trauma as bleeding from recent puncture sites or other recent trauma may occur.

Hypersensitivity reactions have been reported and signs and symptoms included rash, pruritus, erythema, glossal (tongue) edema, hypotension and respiratory distress. If an anaphylactoid reaction occurs, withhold the second dose of RETAVASE and initiate appropriate therapy.

Cholesterol embolism has been reported in patients treated with thrombolytic agents. Cholesterol embolism may present with livedo reticularis, “purple toe” syndrome, acute renal failure, gangrenous digits, hypertension, pancreatitis, myocardial infarction, cerebral infarction, spinal cord infarction, retinal artery occlusion, bowel infarction, and rhabdomyolysis and can be fatal.

Heparin and RETAVASE are incompatible. Do not administer RETAVASE through an intravenous line containing heparin.

The most common adverse reaction (>5%) is bleeding.

Indication and Usage

RETAVASE is a tissue plasminogen activator (tPA) indicated for treatment of acute ST-elevation myocardial infarction (STEMI) to reduce the risk of death and heart failure.

Limitation of Use: The risk of stroke may outweigh the benefit produced by thrombolytic therapy in patients whose STEMI puts them at low risk for death or heart failure.

Please see Full Prescribing Information.

Reference: 1. RETAVASE^® (reteplase) Prescribing Information. 2017.