Core pharmacology

Class Group

Anticoagulants

Legacy Cicm Level

Level 2

Introduction

Competitive Direct Thrombin Inhibitor

Indications Uses

1. Non-valvular AF
2. VTE prophylaxis in orthopaedic
3. VTE treatment

Presentation

PO (Dabigitran etexilate- prodrug)

Monitor:
Direct assays of Thrombin activity:
- Thrombin time (TT)
- Ecarin clotting time (ECT)
- APTT 2.5x >control= increased risk of bleeding

Mechanism of action

MOA: Competitive direct thrombin inhibitor. Blocks pivotal part of common pathway

Gastric irritation (tartaric acid)

Adverse Effects Toxicity

Bleeding

Absorption

5% PO bioavailability

Protein binding

35% protein bound

Metabolism

Rapidly metabolized to active Dabigitran by hepatic and plasma esterases
Not metabolized further

Excretion

Renal excretion

Half-life

T1/2= 12-17 hours

Special Points

Reversal:
Idarucizumab

Cons:
1. Many drug interactions
2. Excretion dependent on renal function

Pros:
1. Predictable kinetics not affected by age, weight or gender
2. Oral
3. Monitoring generally not indicated
4. Reversal agent available
5. Lower bleeding risk than warfarin