Eptase1.5 million unit

Eptase is a thrombolytic (fibrinolytic) enzyme used exclusively in emergency, hospital-based settings under continuous medical supervision. It is indicated for the following conditions:

Established/guideline-supported uses

• Acute ST-elevation myocardial infarction (STEMI): to reduce infarct size, preserve left ventricular function, and reduce mortality when administered early after symptom onset.
• Acute massive pulmonary embolism: with hemodynamic instability, to dissolve the obstructing thrombus.
• Deep vein thrombosis (DVT): extensive acute proximal DVT, in appropriately selected patients.
• Acute arterial thromboembolism/occlusion: of a native artery or bypass graft.
• Clearance of occluded arteriovenous (AV) cannulae: used for dialysis access, when the cannula is blocked by clotted blood and other methods have failed.

Notes on use

Eptase therapy is typically followed by anticoagulation (e.g., heparin) to prevent re-thrombosis. It requires strict patient selection based on bleeding risk and time since symptom onset, and is administered only by trained personnel in a hospital or emergency care setting with facilities for continuous monitoring and management of bleeding complications.

Each vial contains Streptokinase (a purified fibrinolytic protein derived from beta-hemolytic streptococci by fermentation) as a sterile lyophilized powder for reconstitution, typically available in strengths of 250,000 IU, 750,000 IU, and 1,500,000 IU per vial.

Eptase is a bacterial protein (a fibrinolytic/thrombolytic enzyme) obtained from certain strains of beta-hemolytic streptococci. Unlike direct-acting fibrinolytics, Eptase works indirectly by forming a complex with plasminogen, which then activates other plasminogen molecules into plasmin, the enzyme that breaks down (lyses) fibrin clots. It is supplied as a sterile powder for intravenous or intracoronary infusion after reconstitution, and is used only in hospital emergency settings for acute thrombotic and thromboembolic conditions.

Thrombolytic (fibrinolytic) agent

Streptokinase is not itself an enzyme; it first combines with circulating plasminogen in a 1:1 ratio to form an activator complex. This complex converts other plasminogen molecules into plasmin, a proteolytic enzyme that degrades fibrin, the structural protein of blood clots, resulting in clot dissolution (thrombolysis). Because Streptokinase activates plasminogen systemically, it produces a generalized lytic state affecting circulating fibrinogen, factor V, and factor VIII, which contributes to its bleeding risk. As a bacterial protein, Streptokinase is antigenic; the body develops neutralizing antibodies after exposure (including after streptococcal infections), which can reduce its effectiveness and increase the risk of allergic or anaphylactoid reactions on repeat administration.

Eptase has clinically significant interactions with the following agents:

• Anticoagulants (e.g., heparin, warfarin) and antiplatelet agents (e.g., aspirin, clopidogrel): concurrent use increases the risk of serious bleeding, including intracranial hemorrhage; when combined, careful monitoring is required.
• NSAIDs: may further increase bleeding risk when used with Eptase.
• Antifibrinolytic agents (e.g., tranexamic acid, aminocaproic acid, aprotinin): may reduce the thrombolytic effectiveness of Eptase and should generally be avoided during therapy unless used specifically to manage a bleeding complication.

See Contraindications and Precautions and Warnings for additional bleeding-risk considerations.

The most significant adverse effect of Eptase is bleeding, which can range from minor (bruising, oozing at puncture sites) to severe or life-threatening (gastrointestinal, genitourinary, retroperitoneal, or intracranial hemorrhage).

Other reported adverse effects

• Allergic/anaphylactoid reactions: rash, itching, flushing, fever, chills, breathing difficulty, and rarely anaphylaxis (related to antibody formation against this bacterial protein)
• Hypotension, particularly during rapid infusion
• Reperfusion arrhythmias after successful clot dissolution in myocardial infarction
• Nausea, vomiting
• Musculoskeletal or lower back pain
• Headache

Patients are monitored closely during and after infusion for these effects; serious bleeding requires immediate discontinuation and appropriate emergency management.

Eptase should be used during pregnancy only if the potential benefit clearly justifies the potential risk to the fetus, as it may cause placental separation or bleeding, and adequate, well-controlled studies in pregnant women are lacking. Its use is generally reserved for life-threatening thromboembolic emergencies in the mother where the treating physician judges the benefit outweighs the risk, and should only be given under specialist supervision.

It is not known whether Eptase is excreted in human breast milk. Because it is used only as a single short-course emergency infusion in acute care and is a large protein molecule expected to have limited oral bioavailability to the infant, breastfeeding women should consult their physician regarding a temporary interruption of breastfeeding following treatment.

Bleeding risk: The most serious risk associated with Eptase is bleeding, including intracranial hemorrhage, which can be fatal. Careful patient selection, avoidance of unnecessary invasive procedures during and shortly after therapy, and continuous monitoring are essential. See Contraindications for absolute exclusions.

Immunogenicity and reduced efficacy on retreatment: As a bacterial protein, Eptase stimulates antibody formation. Prior streptococcal infection or previous Eptase exposure (especially within the preceding 6 months to 2 years) can reduce its thrombolytic effectiveness and increase the risk of allergic or anaphylactoid reactions. An alternative thrombolytic agent is generally preferred if retreatment is needed within this window.

Hospital-only administration: Eptase must be administered only in a hospital or emergency care setting equipped for continuous cardiovascular monitoring and immediate management of bleeding or allergic reactions; it is not an outpatient or self-administered medication.

Relative caution: Increased bleeding risk should be carefully weighed in patients with recent major surgery, recent trauma, recent childbirth, severe hepatic or renal disease, subacute bacterial endocarditis, active peptic ulcer disease, or advanced age.

Overdose or excessive dosing of Eptase primarily manifests as increased risk of serious bleeding, including internal or intracranial hemorrhage. There is no specific antidote; management is supportive and may include stopping the infusion, administering antifibrinolytic agents (e.g., tranexamic acid or aminocaproic acid) and blood products as directed by a physician. Any suspected overdose or serious bleeding during or after Eptase therapy requires immediate medical attention; since this medicine is given only in a hospital setting, the treating medical team should be alerted immediately for emergency management.

Store the unopened vial in a refrigerator (2°C to 8°C), protected from light. Do not freeze. Once reconstituted, use the solution promptly as directed by the hospital pharmacy/healthcare provider and discard any unused portion. Keep out of reach of children. This medicine is handled and stored by hospital staff, not by patients at home.

Elderly: Older adults may have an increased risk of bleeding, including intracranial hemorrhage, with Eptase; treatment decisions should carefully weigh benefit versus bleeding risk, though no specific dose reduction is established.

Renal impairment: No specific dose adjustment is established; use with caution given the underlying condition and bleeding risk.

Hepatic impairment: Use with caution in patients with significant hepatic disease due to potential effects on clotting factor synthesis and increased bleeding risk.

Pregnancy and lactation: See Pregnancy and Lactation section.

Pediatric patients: See Pediatric Uses section.

The lyophilized powder is reconstituted by a healthcare professional using the diluent recommended by the manufacturer (typically 0.9% Sodium Chloride Injection or 5% Dextrose Injection), gently rolling or swirling the vial to dissolve the powder without vigorous shaking (to avoid excessive foaming), and further diluted as required for the intended infusion rate. Reconstituted solution should be used promptly per hospital pharmacy protocol and prepared only by trained personnel immediately before administration.

Thrombolytics / Fibrinolytic enzymes

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The safety and efficacy of Eptase have not been established in pediatric patients through adequate, well-controlled trials. It has occasionally been used off-label in children for selected life-threatening thrombotic events (e.g., catheter-related thrombosis) under the direct supervision of a pediatric hematology/cardiology specialist in a hospital setting, with dosing individualized to body weight, but this is not a standard, labeled indication. Eptase should not be used in children outside specialist hospital care.