Ticlopidine Hydrochloride

What it is and how it works

Ticlopidine is a prodrug whose active metabolite irreversibly blocks the P2Y12 ADP receptor on platelets, inhibiting ADP-induced activation of the glycoprotein IIb/IIIa complex and platelet aggregation for the lifespan of the platelet. Its onset of action takes several days.

Indications

Prevention of thrombotic stroke in patients with prior stroke or transient ischaemic attack who are intolerant of aspirin; prevention of thrombotic events in selected patients (e.g. peripheral arterial disease, after coronary stenting) where alternatives are unsuitable. Largely superseded by clopidogrel because of its haematological toxicity.

Dosage and administration (summary)

Orally, 250 mg twice daily with food.

Contraindications

Haematological disorders (neutropenia, thrombocytopenia, agranulocytosis) or history of them; active bleeding or conditions with high bleeding risk; severe hepatic impairment; acute stroke with haemorrhage.

Warnings and precautions

Can cause severe neutropenia/agranulocytosis, thrombotic thrombocytopenic purpura and aplastic anaemia, mostly within the first 3 months; a full blood count should be performed before treatment and every 2 weeks during the first 3 months. Discontinue several days before elective surgery. Concomitant anticoagulants, NSAIDs or other antiplatelets increase bleeding risk.

Pregnancy

Not recommended in pregnancy owing to insufficient data.

Storage and supply

Store below 25 °C, protected from moisture.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.