Prasugrel
An oral thienopyridine P2Y12 inhibitor used to prevent clots, including stent thrombosis, in acute coronary syndromes treated with PCI.
Drug card
- Class
- P2Y12 inhibitor
- How it works
- Blocking the platelet ADP receptor P2Y12, so platelets clump less
- Used for
- Acute coronary syndrome managed with PCI (stenting)
- Preventing stent thrombosis and further heart attacks
- Known for
- Bleeding, including fatal and intracranial
- Its name
- -grel-, -grel means an antiplatelet drug (mostly P2Y12 blocker)
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does prasugrel work?
A thienopyridine prodrug. The gut rapidly hydrolyzes it to a thiolactone, which mainly CYP3A4 and CYP2B6 turn into the active metabolite in a single step, with minor help from CYP2C9 and CYP2C19. This binds P2Y12 irreversibly, so ADP-driven aggregation is blocked for the platelet's remaining life.
Like other P2Y12 inhibitors: They block P2Y12, the platelet receptor for ADP. ADP then cannot switch on the glycoprotein IIb/IIIa complex, so fibrinogen does not bridge platelets together and aggregation falls. Clopidogrel and prasugrel are prodrugs whose active metabolites bind irreversibly, for the platelet's 7 to 10 day life; ticagrelor is active itself and binds reversibly, at a site apart from where ADP binds.
Uses
What is prasugrel used for?
- Acute coronary syndrome managed with PCI (stenting)
- Preventing stent thrombosis and further heart attacks
Side effects
Side effects of prasugrel
- Bleeding, including fatal and intracranialKnown forSerious
- Thrombotic thrombocytopenic purpura (TTP)Serious
- Angioedema and other allergic reactionsSerious
- Rash
- Headache
- Back pain
- Nausea
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Contraindicated after a prior stroke or TIA, because more strokes, including brain bleeds, occurred on it.
- Age 75 or over: generally not recommended (more fatal and brain bleeding), except in diabetes or after a previous heart attack.
- Body weight under 60 kg raises bleeding risk, so a lower maintenance dose is considered.
- Stop it at least 7 days before surgery, and do not start it when urgent bypass surgery (CABG) is likely.
Good to know: In PCI patients it prevented more heart attacks than clopidogrel (TRITON-TIMI 38) but caused more bleeding, including bleeding after bypass surgery.
Remember it
A way to remember it
Ticagrelor ticks on and off; clopidogrel and prasugrel lock on for life.
Ticagrelor binds P2Y12 reversibly. The active metabolites of clopidogrel and prasugrel bind it irreversibly, so their effect lasts the platelet's 7 to 10 day lifetime, which is why they are stopped days before surgery.
Written for biofideX
Its name
-grel-, -grel means antiplatelet drug (mostly P2Y12 blocker)
Clopidogrel, prasugrel and ticagrelor block the platelet P2Y12 (ADP) receptor. The stem may end the name or sit inside it, as in ticagrelor and cangrelor.
- Every drug name stem
Its class
P2Y12 inhibitors
Other P2Y12 inhibitors with a card:
Easily mixed up with non-steroidal anti-inflammatory drugs and direct factor Xa inhibitors.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Blood clots and cholesterol
Prasugrel is one of 19 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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