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Thrombolytic

Alteplase

A recombinant tissue plasminogen activator given by vein to dissolve clots in acute ischemic stroke, heart attack and massive pulmonary embolism.

Also called rt-PA (abbreviation (recombinant tissue plasminogen activator)) or tPA (abbreviation).

Drug card

How it works
Turning plasminogen into plasmin, which breaks down the fibrin in clots
Used for
  • Acute ischemic stroke, within 3 hours of onset
  • Acute heart attack, to lower death and heart failure
  • Massive pulmonary embolism
Known for
Bleeding, including intracranial hemorrhage
Its name
-plase means a plasminogen activator (clot buster)

Study it as a flashcard, and it comes back before you forget it.

Mechanism of action

How does alteplase work?

A recombinant copy of human tissue plasminogen activator, a serine protease. It attaches to the fibrin of a thrombus and turns the plasminogen held there into plasmin, so clot breakdown stays mostly local; without fibrin it activates plasminogen only weakly. Its initial half-life is under 5 minutes, so it is given as an infusion, after a bolus in stroke and heart attack.

Like other thrombolytics: They turn plasminogen into plasmin, the enzyme that cuts fibrin apart, so a clot that has already formed dissolves and the blocked vessel can reopen. Alteplase and tenecteplase are recombinant forms of tissue plasminogen activator: they bind fibrin in the thrombus and act mainly on the plasminogen trapped there, so circulating fibrinogen is broken down less.

Uses

What is alteplase used for?

  • Acute ischemic stroke, within 3 hours of onset
  • Acute heart attack, to lower death and heart failure
  • Massive pulmonary embolism

Side effects

Side effects of alteplase

  • Bleeding, including intracranial hemorrhageKnown forSerious
  • Orolingual angioedemaSerious
  • Anaphylaxis, laryngeal edema, hivesSerious
  • Cholesterol embolismSerious
  • Re-embolism from deep vein clotsSerious
  • Arrhythmias and AV block after heart attackSerious
  • Low blood pressure
  • Nausea and vomiting
  • Seizures (after stroke treatment)Serious

Known for marks what an exam expects you to know it for.

Watch for

Cautions and what sets it apart

  • Stroke: exclude intracranial hemorrhage before treatment, and start within 3 hours of symptom onset.
  • Contraindicated with internal bleeding, recent brain or spinal surgery or serious head injury, a bleeding diathesis, or severe uncontrolled hypertension.
  • Avoid intramuscular injections and punctures of vessels that cannot be compressed; anticoagulants and antiplatelets add to bleeding.
  • Patients on ACE inhibitors are more prone to orolingual angioedema; watch for it during and for hours after the infusion.

Good to know: Cleared within minutes, so it runs as an infusion; tenecteplase, a modified tPA, is given as a single bolus.

Remember it

A way to remember it

Lytics lyse: they make plasmin, and plasmin snips the fibrin that holds a clot together.

Their main danger follows from that action: bleeding, especially at puncture sites and inside the skull. Tranexamic acid works the opposite way, by keeping plasmin off fibrin.

Written for biofideX

Its name

  • -plase means plasminogen activator (clot buster)

    Alteplase and tenecteplase are tissue plasminogen activators that dissolve clots. WHO lists them under -ase (enzymes) as -teplase; urokinase-type ones end in -uplase.

  • Every drug name stem

Its class

Thrombolytics

Other thrombolytics with a card:

Easily mixed up with antifibrinolytics and heparins.

Sources

Checked against

Written for biofideX in plain words, after checking these references:

For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.

Practice it

Blood clots and cholesterol

Alteplase is one of 19 drugs practiced together here: their classes, how they work, what they treat and what they're known for.

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