Pharmacopeia

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Field CLOPIDOGREL
Haematology · Haematology · Level 2
TICAGRELOR
Haematology · Haematology · Level 2
PRASUGREL
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

Allosteric, reversible antagonist at P2Y12-R (an ADP receptor), preventing activation of glycoprotein IIb/IIIa→ prevents platelet crosslinking

Irreversibly binds the P2Y12-R (an ADP receptor), preventing activation of glycoprotein IIb/IIIa→ prevents platelet crosslinking

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.

BA=40%

— — —
Protein binding

95% protein binding,

— — — —
Volume of distribution

Vd unknown

— — — —
Metabolism

- Hepatic CYP450 2C19 + Esterases to Inactive metab

Metabolized by CYP3A4

Prodrug- 1 step metabolism
Less susceptible to CYP polymorphism and CYP inhibition or induction than Clopidogrel

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

Antiplatelet

Antiplatelet

Introduction

ADP Receptor Antagonist - Thienopyridine

ADP Receptor Antagonist - Thienopyridine

ADP Receptor Antagonist - Thienopyridine

Prodrug

GP IIb/IIIA Inhibitor

GP IIb/IIIA Inhibitor

Legacy Cicm Level

Level 3

Level 3

Level 3

Level 3

Level 3

Main Action

Platelet inhibition

Platelet inhibition

Platelet inhibition

Platelet inhibition

Platelet inhibition