Prasugrel !

An oral thienopyridine that blocks P2Y12 irreversibly, more strongly than clopidogrel. Not used after a stroke or transient ischaemic attack.

Updated 2026-11-01

Class: Antiplatelet drugs
Receptor: P2Y12 ADP receptor on platelets
ATC code: B01AC22

P2Y12 ADP receptor on plateletsPrasugrel

The figure shows the human P2Y12 receptor with AZD1283, an experimental P2Y12 blocker. Prasugrel's active metabolite binds covalently and has no structure with the receptor.

Target in 3D: P2Y12 ADP receptor on platelets. PDB structure 4NTJ (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Prasugrel is a prodrug. In the gut it is quickly hydrolysed to a thiolactone, which liver enzymes (mainly CYP3A4 and CYP2B6) turn into the active metabolite in a single step. The metabolite binds P2Y12 irreversibly, blocking ADP-driven activation and aggregation for the rest of the platelet's life. Because its activation is simpler, common CYP2C19 variants do not change its effect.

Gut esterases turn prasugrel into a thiolactone
One liver step (CYP3A4, CYP2B6) makes the active metabolite
It binds P2Y12 irreversibly: platelets blocked for life

Pharmacokinetics

Absorption: Rapid; prasugrel itself is not detected in plasma.
Distribution: The active metabolite is about 98% bound to albumin.
Metabolism: Intestinal hydrolysis, then one step mainly by CYP3A4 and CYP2B6; CYP2C19 genotype has no relevant effect.
Half-life: About 7 hours for the active metabolite (range 2 to 15).
Onset and duration: About 90% of patients reach at least 50% platelet inhibition within 1 hour of a loading dose.

Indications

Acute coronary syndrome (unstable angina, NSTEMI or STEMI) managed with percutaneous coronary intervention, together with aspirin. Myocardial Infarction (Heart Attack) →

Adverse effects

Common

Bleeding, including nosebleeds and bruising
Anaemia
Headache, dizziness, back pain

Contraindications

Active pathological bleeding
Prior transient ischaemic attack or stroke
Hypersensitivity to prasugrel

Key interactions

Warfarin, NSAIDs and other drugs that raise bleeding risk: Increase the risk of bleeding.
Opioids such as morphine: Can delay and reduce platelet inhibition after the loading dose.

What is monitored

Signs of bleeding, especially after invasive procedures (suspect it with low blood pressure)
Haemoglobin
Platelet count and smear if TTP is suspected

Administration and safety

Oral, with or without food, together with aspirin
Generally not recommended from age 75, except in high-risk patients (diabetes or prior MI); low body weight increases exposure
Not started when urgent coronary bypass surgery is likely; stopped several days before surgery when possible, as planned by the team
Not stopped early without the cardiology team

Nursing care

Ask about previous stroke or transient ischaemic attack before the first dose: it is a contraindication
Note age and body weight, which change bleeding risk
Watch for bleeding and low blood pressure after catheterisation
Teach the patient to tell every dentist and surgeon and to report purple spots, fever or confusion

Pregnancy and breastfeeding

There are no human data in pregnancy; animal studies showed no malformations. Bleeding at delivery is a concern.

Test yourself

Think of the answer, then tap the question to see it.

Why does CYP2C19 genotype matter for clopidogrel but not for prasugrel?

Prasugrel becomes active through intestinal hydrolysis and one liver step, mainly CYP3A4 and CYP2B6; CYP2C19 variants have no relevant effect on its active metabolite.

Which history contraindicates prasugrel?

A previous stroke or transient ischaemic attack, because of the higher risk of intracranial bleeding.

In which patients is prasugrel generally not recommended because of bleeding?

People aged 75 or more (except high-risk cases such as diabetes or prior MI); low body weight also raises exposure and bleeding risk.

Add to my cards (3)

Myocardial Infarction (Heart Attack)

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - PRASUGREL tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); Prasugrel: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); 4NTJ: Structure of the human P2Y12 receptor in complex with an antithrombotic drug (RCSB Protein Data Bank, 2014).

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Representative model, for educational purposes only.