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Direct Thrombin Inhibitor

Dabigatran

An oral direct thrombin inhibitor, given as the prodrug dabigatran etexilate, to prevent stroke in atrial fibrillation and to treat DVT and PE.

Also called dabigatran etexilate (the prodrug form given by mouth).

Drug card

How it works
Binding thrombin directly, so fibrinogen is not turned into fibrin
Used for
  • Preventing stroke in nonvalvular atrial fibrillation
  • Treating DVT, and preventing it after hip replacement
  • Treating pulmonary embolism and preventing its return
Known for
  • Bleeding
  • Indigestion (dyspepsia)
Its name
-gatran means a direct thrombin inhibitor

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

Mechanism of action

How does dabigatran work?

Dabigatran etexilate is a prodrug that esterases convert to dabigatran, which binds thrombin competitively and blocks it whether free or clot-bound, along with the platelet aggregation thrombin induces. It is not handled by CYP450 enzymes; about 80% of its clearance is renal. Removing the capsule shell raises absorption by 75%.

Uses

What is dabigatran used for?

  • Preventing stroke in nonvalvular atrial fibrillation
  • Treating DVT, and preventing it after hip replacement
  • Treating pulmonary embolism and preventing its return

Side effects

Side effects of dabigatran

  • BleedingKnown forSerious
  • Indigestion (dyspepsia)Known for
  • Gastrointestinal bleedingSerious
  • Reflux, gastritis and esophagitis
  • Upper abdominal pain
  • Nausea
  • Diarrhea
  • Spinal or epidural hematoma after spinal proceduresSerious
  • Clots and stroke if stopped earlySerious
  • Rash, itching and hives
  • AnaphylaxisSerious

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

Watch for

Cautions and what sets it apart

  • Check kidney function before starting and during treatment; as it falls, dabigatran levels and bleeding risk rise.
  • Capsules are swallowed whole: breaking, chewing or opening them raises absorption by 75%.
  • Contraindicated with mechanical prosthetic heart valves.
  • Idarucizumab reverses it for emergency surgery or life-threatening bleeding; protamine and vitamin K do not work.

Good to know: A prodrug capsule that must stay whole; it relies heavily on the kidneys for clearance and has its own reversal agent, idarucizumab.

Remember it

A way to remember it

Dabigatran traps thrombin directly; idarucizumab sets it free.

It binds thrombin itself, free or clot-bound, with no antithrombin needed. Its own specific reversal agent, idarucizumab, undoes this for emergency surgery or life-threatening bleeding.

Written for biofideX

Its name

  • -gatran means direct thrombin inhibitor

    Dabigatran is taken as dabigatran etexilate. Argatroban, also a direct thrombin inhibitor, doesn't carry the stem.

  • Every drug name stem

Its class

Direct thrombin inhibitors

They bind thrombin (factor IIa) themselves and inactivate it, with no need for antithrombin. Free thrombin and thrombin already held in a clot are both blocked, so fibrinogen is not converted to fibrin and thrombin-driven platelet aggregation falls. Dabigatran, the oral member, binds thrombin competitively and reversibly.

Easily mixed up with direct factor Xa inhibitors 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

Dabigatran 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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