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

50% oral bioavailability

Protein binding

90% protein bound

Metabolism

Hepatic metabolism (3A4)
No active metabolites

Excretion

Renal and faeces (greater reliance on biliary elimination)

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
3. Dose adjustment based on age and weight

Pros:
1. Oral
2. Monitoring generally not indicated
3. Renal dose adjustment not required for eGFR >30
4. Lower bleeding risk than warfarin