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Pharmacology · Thrombolytics (fibrinolytics)

Reteplase !

A shortened recombinant tissue plasminogen activator with a longer half-life, given as two boluses in acute myocardial infarction.

Updated 2026-11-01

The figure shows full-length human plasminogen, the substrate that reteplase cuts into plasmin; the drug itself is not in the crystal.

Target in 3D: Plasminogen (the zymogen of plasmin), bound to fibrin. PDB structure 4DUR (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Reteplase is a recombinant tissue plasminogen activator from which several amino-acid sequences have been deleted. It keeps the protease domain, so it converts plasminogen into plasmin and dissolves the clot, but it is cleared more slowly than alteplase.

  1. The drug binds fibrin inside the clot
  2. It cuts fibrin-bound plasminogen into plasmin
  3. Plasmin breaks fibrin into degradation products
  4. The artery reopens; blood flow returns

Pharmacokinetics

Half-life
Longer than alteplase, which allows bolus dosing

Indications

Adverse effects

Common

  • Bleeding
  • Bruising at puncture sites

Contraindications

  • Previous intracranial haemorrhage, or a known cerebral vascular lesion or brain tumour
  • Active bleeding or a bleeding disorder
  • Suspected aortic dissection
  • Recent ischaemic stroke, significant head trauma or brain or spinal surgery
  • Severe uncontrolled hypertension

Key interactions

Heparin, anticoagulants and antiplatelets (aspirin, clopidogrel)
Add to the bleeding risk; serious haemorrhage is more frequent when heparin is given at the same time
Warfarin (raised INR)
Current warfarin use with a raised INR is a relative contraindication

What is monitored

  • Neurological status and blood pressure
  • Signs of bleeding; haemoglobin and coagulation tests
  • Reperfusion: ECG and symptoms in myocardial infarction

Administration and safety

  • Two intravenous boluses separated in time; record the time of each
  • Not to be confused with alteplase or tenecteplase: different doses and schedules

Nursing care

  • Check the time symptoms began and go through the contraindication checklist before the drug is mixed
  • Neurological checks and blood pressure often during and after the infusion; a sudden headache, vomiting or a drop in consciousness suggests intracranial bleeding
  • Look for bleeding at puncture sites, gums, urine and stool
  • Avoid new arterial punctures, intramuscular injections and unnecessary venepunctures

Pregnancy and breastfeeding

There are few data in pregnancy; it is used only when the maternal benefit outweighs the bleeding risk.

Test yourself

Think of the answer, then tap the question to see it.

How is reteplase different structurally from alteplase?

Several amino-acid sequences are deleted; the protease domain remains.

What is its main indication?

Acute ST-elevation myocardial infarction.

Why can it be given as boluses?

Its half-life is longer than that of alteplase.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Reteplase Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 36 (McGraw Hill, 2023); Farmacología básica y clínica (Katzung), 16.ª ed., cap. 34 (McGraw Hill, 2025); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.