Pharmacopeia

Canonical comparison

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Field CLOPIDOGREL
Haematology · Haematology · Level 2
 TICAGRELOR
Haematology · Haematology · Level 2
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
Absorption

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

BA=40%
Protein binding

95% protein binding,

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Volume of distribution

Vd unknown

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Metabolism

- Hepatic CYP450 2C19 + Esterases to Inactive metab

Metabolized by CYP3A4
Excretion

- Renal and faecal elimination

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Half-life

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

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Adverse Effects Toxicity

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

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Class Group

Antiplatelet

Antiplatelet
Introduction

ADP Receptor Antagonist - Thienopyridine

ADP Receptor Antagonist - Thienopyridine
Legacy Cicm Level

Level 3

Level 3
Main Action

Platelet inhibition

Platelet inhibition