Ticagrelor
An oral, reversible P2Y12 inhibitor used with aspirin to lower the risk of heart attack, stroke and death in coronary disease and after stroke.
Drug card
- Class
- P2Y12 inhibitor
- How it works
- Blocking the platelet ADP receptor P2Y12, so platelets clump less
- Used for
- Acute coronary syndromes, including after stenting
- Preventing heart attack and stroke in coronary disease
- Lowering stroke risk after minor stroke or high-risk TIA
- Known for
- Bleeding, sometimes fatal
- Breathlessness (dyspnea)
- 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 ticagrelor work?
A cyclopentyltriazolopyrimidine, not a thienopyridine. It and its equally potent main metabolite bind P2Y12 reversibly, at a site apart from the ADP binding site, without needing activation. Platelet inhibition peaks at about 2 hours, is greater than with clopidogrel, and returns to baseline about 5 days after the last dose.
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 ticagrelor used for?
- Acute coronary syndromes, including after stenting
- Preventing heart attack and stroke in coronary disease
- Lowering stroke risk after minor stroke or high-risk TIA
Side effects
Side effects of ticagrelor
- Bleeding, sometimes fatalKnown forSerious
- Breathlessness (dyspnea)Known for
- Slow heart rhythms, pauses and AV blockSerious
- Raised uric acid
- Gout
- Central sleep apnea (Cheyne-Stokes breathing)
- Thrombotic thrombocytopenic purpura (TTP)Serious
- Angioedema and other allergic reactionsSerious
- Rash
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Contraindicated after any intracranial hemorrhage and with active pathological bleeding.
- Avoid strong CYP3A inhibitors (clarithromycin, ritonavir, ketoconazole) and strong inducers (rifampin, carbamazepine, phenytoin).
- Use it only with low-dose aspirin; higher aspirin doses are avoided.
- Sick sinus syndrome or high-grade AV block without a pacemaker: higher risk of bradyarrhythmias.
Good to know: Not a prodrug and binds reversibly, so it works within hours without needing activation; breathlessness is its best-known side effect.
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
Ticagrelor 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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