Core pharmacology

Class Group

Anticoagulants

Legacy Cicm Level

Level 2

Introduction

Direct Xa inhibitor (free and bound)
Blocks amplification phase

Indications Uses

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

Presentation

PO

Monitor:
PT
Anti-Xa

Mechanism of action

MOA: Direct Xa inhibitor, blocking the final common pathway of clotting cascade

Adverse Effects Toxicity

Bleeding

Absorption

80-100% PO bioavailability

Protein binding

95% protein bound

Metabolism

Hepatic metabolism (3A4)
No active metabolites

Excretion

Renal and faeces

Half-life

T1/2= 5-13 hours

Special Points

Reversal:
Andexanet alfa or
4-factor PCC (Prothrombinex 3-factor PCC available in Australia)

Cons:
1. No specific reversal agent
2. Renal dose adjustment

Pros:
1. Predictable kinetics not affected by age, weight or gender
2. Oral
3. Monitoring generally not indicated
4. Renal dose adjustment not required for eGFR >30
5. Lower bleeding risk than warfarin