Ticagrelor

BRILINTA

Open Ticagrelor in the interactive console ↗

What it isReversible P2Y12 antagonist; acute coronary syndrome.

Why this oneIt needs no metabolic activation, so it works in CYP2C19 poor metabolizers where clopidogrel fails, and it acts faster and reverses sooner.

What limits itTwice-daily dosing, more bleeding than clopidogrel, and dyspnea in about one in seven. Aspirin above 100 mg reduces its benefit.

FDA-approved for

acute coronary syndrome (2011)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Bleeding risk: can cause significant, sometimes fatal bleeding; do not use with active pathological bleeding or history of intracranial hemorrhage; do not start before urgent CABG; stopping increases risk of subsequent CV events.

FDA dosing	Population	Start	Target
ACS or history of MI	Adults	180 mg load, then 90 mg BID x1 year	60 mg BID after 1 year
CAD, no prior stroke or MI	Adults	60 mg BID	60 mg BID
Acute ischemic stroke or TIA	Adults	180 mg load, then 90 mg BID	90 mg BID up to 30 days

Renal No adjustment needed

Hepatic Avoid in severe hepatic impairment; no adjustment in mild; caution in moderate

Instructions

Use with daily aspirin 75-100 mg; avoid aspirin doses above 100 mg
Give first maintenance dose 6-12 hours after loading dose
May crush tablets, mix with water, and drink or give via nasogastric tube
Do not co-administer with another oral P2Y12 inhibitor
If interrupted for surgery, stop 5 days before major-bleeding-risk surgery; resume when hemostasis achieved
Missed dose: take next dose at scheduled time

Contraindications

History of intracranial hemorrhage
Active pathological bleeding

Cautions

Bleeding risk
Dyspnea
Bradyarrhythmias including AV block
Avoid in severe hepatic impairment
Central sleep apnea/Cheyne-Stokes respiration
Thrombotic thrombocytopenic purpura (TTP) reported

Adverse reactions

Bleeding
Dyspnea
Dizziness, nausea, diarrhea

Pregnancy Human data have not identified a drug-associated risk; animal studies showed structural abnormalities at higher exposures

Lactation Breastfeeding not recommended during treatment

⚠ BOXED WARNINGS

Bleeding risk
Aspirin above 100 mg daily reduces effectiveness

Cost, est. cash$300–$800/month

Generic entry2025

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger3 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryB

Defining liabilityGI or intracranial bleeding, especially with anticoagulants, NSAIDs or serotonergic antidepressants.

Mechanism of action: Ticagrelor ballicule

Ticagrelor ballicule: receptor binding, kinetics and half-life diagram

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Memory aids: mascots and interaction avatars

Ticagrelor BRILINTA mascot mnemonic cartoon — **“Brilliant Tickle Grill”**
Blue platelet grilled

CYP3A4 substrate

Open Ticagrelor in the interactive console ↗