Rivaroxaban

Chemical

Competitive IRREVERSIBLE inhibitor of Xa (free & blot bound)

Use

  1. Reduce embolic events in AF
  2. Prevent DVT post ortho
  3. Rx DVT/PE

Presentation

Tablets; 2.5 – 10mg

Dose

AF 20mg OD

DVT 15mg BD for 21d → 20mg OD

DVT prophylaxis 10mg OD

Route

PO

Onset / DoA

30 mins → max 2hrs → t ½ B 16hrs → offset of anticoagulation in 24hrs

MoA

  • Direct competitive REVERSIBLE inhibition Xa
  • ↓THROMBIN formation & effects of thrombin

PK

A

80 – 100% OBA

D

VD 50L

Very high PPB 95% ∴ not dialysable

M

Metabolised by liver enzymes

P450 3A4

No active metabolites

E

66% by kidneys

  • 50:50 inactive/active
  • Rest = faecal biliary route

Adverse Effects

  • Haemorrhage
  • Drug Interactions → CYP3A4 inhibitors (ketoconazole) → will ↑ [   ]
  • Other anticoag should be avoided

Monitoring

Anti-Xa-levels

→ Sold as no-monitoring required, but you need to monitor to assess PD in high risk patients (high age, low weight, low renal function)

→ NB: anti-Xa levels measure the drug [   ], not the anticoagulant activity

Reversal

Highly PPB → not dialysable

PROTHROMBIN-VF (II, IX, X, some V & VII)

?ANDEXXA = recombinant Xa coming out?

Haem consult

(effects wear off in 24hrs)