Bivalirudin

Chemical

Synthetic peptide

Use

  1. HITS
  2. Prevention of thrombosis

Presentation

250mg vial

Dose

(HITS/PCI)

0.75mg/kg IV bolus →1.75mg/kg/hr

Route

IV

Onset / DoA

5 mins onset →t ½ B 25 mins

MoA

DIRECT THROMBIN INHIBITOR

THROMBIN ACTIONS

  • Fibrinogen →fibrin
  • XIII →XIIIa
  • XI →Xia
  • VIII →VIIIa
  • V →Va
  • Platelet agonist +++
  • Intact endothelium THROMBOMODULIN →binds thrombin →activates PROTEIN C →anticoagulant

THROMBIN HAS 3 BINDING SITES

  • Active catalytic site
  • Fibrin binding site
  • Heparin binding site

Bivalirudin = BIVALENT THROMBIN INHIBITOR

∴ Binds catalytic & Fibrin Binding Site

  • Reversible Thrombin Inhibition →inhibits free & clot bound thrombin

PK

A

D

0.2L/kg

M

Proteolytic cleavage by plasma proteases

t ½ B 25 mins

E

Renally cleared

20% unchanged

Needs dose adjustment for severe renal impairment

Adverse Effects

  • Haemorrhage
  • Allergic reactions
  • Nausea
  • Hypotension
  • Pain
  • HA

Monitoring

PT, APTT, ACT all rise linearly


Most guidelines use APTT to monitor & titrate infusions

Reversal

  • Anticoagulant effect reverses rapidly on ceasing infusion
  • ACT to monitor
  • Give FFP & Four Factor Prothrombin concentrate ?Prothrombinex
  • Haem consult
  • Can be removed with haemodialysis