Pharmacopeia

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Field ASPIRIN
Haematology · Haematology · Level 2
ABCIXIMAB
Haematology · Haematology · Level 3
Mechanism of action

Non-specific Irreversible platelet cyclooxygenase inhibitor
(COX-1 and 2) via acetylation of serine residues → ↓formation PG precursors.
- Inhibits formation of thromboxane (TXA) → inhibit aggregation
- At higher doses prostacyclin (PFI2) synthesis also inhibited → vasoconstriction (but endothelium can regenerate COX)

Similar mechanism as tirofiban but monoclonal
antibody

Absorption

- PO. BA. 50%.
- 300mg Loading. 100mg maint.

—
Protein binding

85% protein binding, pKa 3

—
Volume of distribution

Vd 10L

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Metabolism

- Converted to salicylic acid in GI mucosa and liver
- Hepatic conjugation (saturable)

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

Excretion

- Renal as salicylate

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

Half-life

- T1/2b 15~20 mins when first order
- Dur: 4-6 hrs. (Effect on platelet aggregation will last life of current cohort of platelets (7-10 days)

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Adverse Effects Toxicity

Bleeding
Bronchospasm, Renal toxicity
Reye’s Syndrome, GI ulceration
Caution with other anticoagulants

Haemorrhage, thrombocytopenia, human antichimeric antibody development, allergic reaction

Class Group

Antiplatelet

Antiplatelet

Introduction

COX inhibitor

GP IIb/IIIA Inhibitor

Legacy Cicm Level

Level 1

Level 3

Main Action

Platelet inhibition

Platelet inhibition