Reteplase (Retavase) is a recombinant form of human tissue plasminogen activator. It is used to lyse clots in patients with acute ST-elevation myocardial infarction.

• Acute ST-elevation myocardial infarction:

  • It is used in acute ST-elevation myocardial infarction (STEMI) to reduce the risk of death and heart failure

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

Reteplase dose in Adults

Dosage in the treatment of acute ST-elevation myocardial infarction:

• 10 units given intravenously over 2 minutes, followed by a second dose 30 minutes later of 10 units intravenously over 2 minutes
• Thrombolytic should be given within 30 minutes of hospital arrival.
• Generally, there is only a small chance for benefit of therapy after a delay of 12 to 24 hours from symptom onset, but thrombolysis might be considered for selected patients with ongoing ischemic pain and extensive ST elevation
• However, primary PCI is preferred in these patients.
• Give concurrent aspirin, clopidogrel, and anticoagulant therapy (ie, unfractionated heparin, enoxaparin, or fondaparinux) with reteplase.

Reteplase dose in Childrens

Not recommended for use in Children.

Reteplase pregnancy Risk Factor: C

• In some studies on animal reproduction, adverse events could have been observed.
• Pregnant women are at greater risk of bleeding.

Reteplase use during breastfeeding:

• It is unknown if breast milk contains reteplase or not.

Reteplase dose in Renal Disease:

• There are no dosage adjustments given in the manufacturer's labeling.
• However, the risks of reteplase therapy are increased.

• Hemodialysis: Dialyzable: Unknown, but not likely

Reteplase dose in Liver disease:

• There are no dosage adjustments given in the manufacturer's labeling.
• However, the risks of reteplase therapy are increased.

Common Side Effects of Reteplase (Retavase) Include:

• Local:

  • Bleeding at the injection site

Less Common Side Effects of Reteplase (Retavase) Include:

• Gastrointestinal:

  • Gastrointestinal hemorrhage

• Hematologic & oncologic:

  • Hemorrhage
  • Anemia

Contraindication to Reteplase (Retavase) Include:

• Active internal bleeding
• Recent CVA
• Within 3 months, intracranial and intraspinal surgeries or serious head trauma are possible
• Intracranial conditions that increase bleeding risk (eg, aneurysm, arteriovenous malformations or neoplasm)
• bleeding diathesis
• Hypertension that is not controlled and severe
• Within 3 months, Ischemic stroke
• Any intracranial hemorhage that has occurred previously
• active bleeding (excluding menses)
• Suspected aortic dissection
• Significant closed head or facial trauma within three months, with radiographic evidence for bony fractures or brain injury

Warnings and precautions

• Arrhythmias:

  • Reperfusion arrhythmias can be caused by coronary thrombolysis (eg, ventricular pre-depolarizations, sinus bradycardia, and ventricular tachycardia).
  • Therapy should include antiarrhythmic therapy.

• Bleeding

  • It is possible for internal bleeding to occur (can be fatal) at any of the following locations: genitourinary intracranial, retroperitoneal or gastrointestinal.
  • All bleeding areas should be monitored.
  • If there is severe bleeding, the patient should be stopped from receiving reteplase or any other concurrent anticoagulants (eg heparin) and treated accordingly.

• Cholesterol embolization:

  • This has been observed in very few patients who have received thrombolytic drugs.
  • It can present as "purple toe", livedo reticularis or acute renal failure.

• Hypersensitivity reactions

  • These conditions include glossal edema, hypotension and respiratory distress.
  • Stop the second dose of Retplase if you experience an allergic reaction. Then, start appropriate therapy.

• Events that are thromboembolic:

  • Patients with high risk of left-heart thrombosis (e.g. patients with mitral or atrial fibrillation) may be more susceptible to bleeding.

• Conditions that increase bleeding risk

  • These conditions pose a high risk for bleeding when using thrombolytics. It is important to weigh the potential benefits of therapy against these risks.
    • History of hypertension that was severe and chronically uncontrolled
    • Significant hypertension upon presentation (systolic blood pressure >180 mm Hg, or diastolic blood pressure >110 mmHg).
    • History of ischemic strokes in the past >3 months
    • Alzheimer's
    • Traumatic or prolonged CPR (>10 mins)
    • Major surgery takes 3 weeks
    • Recent internal bleeding (within 2-4 weeks)
    • non-compressible vascular punctures
    • Active peptic ulcer
    • Oral anticoagulant therapy
    • Lumbar puncture in 10 days

• STEMI:

  • Use reteplase in a responsible manner:

Reteplase: Drug Interaction

Monitor:

• CBC
• aPTT (activated partial thromboplastin time)
• signs and symptoms of bleeding
• ECG monitoring

How to administer Reteplase (Retavase)?

• It is for IV use only
• Do not administer IM.
• Administer reconstituted dose over 2 minutes
• No other medication should be added to the injection solution.

Mechanism of action of Reteplase (Retavase):​​​​​​​

• Reteplase, a recombinant activator of plasminogen, catalyzes endogenous plasminogen cleavage to produce plasmin.
• Plasmin then degrades fibrin matrix in the thrombus and exerts its thrombolytic effect.

Onset of action:

• Thrombolysis: 30 - 90 minutes

Half-life elimination:

• 13 - 16 minutes

Excretion:

• Feces and urine Clearance: Plasma: 250 - 450 mL/minute

International Brands of Reteplase:

• Retavase
• Retavase Half-Kit
• Pai Tong Xin
• Rapilysin
• Rui Tong Li

Reteplase Brands in Pakistan:

Reteplase is not available in Pakistan.