Pharmacopeia

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Field CLOPIDOGREL
Haematology · Haematology · Level 2
ABCIXIMAB
Haematology · Haematology · Level 3
TIROFIBAN
Haematology · Haematology · Level 3
Mechanism of action

Prodrug. Hepatic activation to active agent (Thiol derivative, by oxidation and hydrolysis) which is an ADP receptor antagonist
- Irreversible inhibition of P2Y12 receptor at platelet surface → Inhibits activation of GPIIb/IIIa → Inhibits platelet activation

Similar mechanism as tirofiban but monoclonal
antibody

Antagonises the GpIIb/IIIa
receptor, preventing the
binding of fibrinogen and
platelet crosslinking and
aggregation.

Absorption

- PO. BA 50%
- 600mg loading. 75mg maint.

— —
Protein binding

95% protein binding,

— —
Volume of distribution

Vd unknown

— —
Metabolism

- Hepatic CYP450 2C19 + Esterases to Inactive metab

Platelet function
typically returns to
normal 24-48 hours after
infusion ceases

Limited metabolism in humans.

Excretion

- Renal and faecal elimination

Platelet function
typically returns to
normal 24-48 hours after
infusion ceases

Excreted in urine and faeces, mostly
unchanged

Half-life

- T1/2b 7 hours parent drug (30mins metab) Dur: life of platelet

—

HL 1.9-2.2 hrs

Adverse Effects Toxicity

Bleeding
TTP
Agranulocytosis, Neutropenia
Significant drug interactions as requires activation by CYP450

Haemorrhage, thrombocytopenia, human antichimeric antibody development, allergic reaction

Haemorrhage
Difficulty reversing agent
Dose adjustment in renal impairment

Class Group

Antiplatelet

Antiplatelet

Antiplatelet

Introduction

ADP Receptor Antagonist - Thienopyridine

GP IIb/IIIA Inhibitor

GP IIb/IIIA Inhibitor

Legacy Cicm Level

Level 3

Level 3

Level 3

Main Action

Platelet inhibition

Platelet inhibition

Platelet inhibition