Drug reference

Ticagrelor

Antiplatelet · Antithrombotic

AntiplateletAntithrombotic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

Avoid; toxicity in animal studies

FDA category + note

Top interactionssee all 12 →

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Mechanism

Ticagrelor is a cyclopentyltriazolopyrimidine that directly and reversibly antagonizes the P2Y12 ADP receptor on platelets without requiring metabolic activation — distinguishing it from the thienopyridine prodrugs clopidogrel and prasugrel, which bind irreversibly. This reversible binding means platelet function recovers within 3-5 days of discontinuation (vs 7-10 days for thienopyridines), providing more flexibility around surgical timing. Ticagrelor also inhibits cellular adenosine reuptake via equilibrative nucleoside transporter 1 (ENT1), raising plasma adenosine levels — potentially contributing to its dyspnea side effect.

Indications

Prevention of atherothrombotic events in patients with acute coronary syndrome (in combination with aspirin for up to 12 months)Alternatives to clopidogrel in certain patients undergoing percutaneous coronary intervention (PCI) (off-label/unlicensed, in combination with aspirin)reduction in the risk of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome or a history of myocardial infarctionacute coronary syndrome with or without coronary interventionDual antiplatelet therapy (DAPT) with aspirin for ACS patients managed conservatively or with an early invasive strategyPrevention of thrombotic complications during Percutaneous Coronary Intervention (PCI)Component of dual antiplatelet therapy (DAPT) post-PCI

Dosing

Adult: ACS: loading 180 mg, then 90 mg BD for up to 12 months, with aspirin 75-150 mg daily. Extended post-MI: 60 mg BD (started after initial 12-month therapy or within 2 years of MI), with aspirin.
Renal adjustment: No adjustment needed
Hepatic adjustment: Avoid in severe hepatic impairment
Geriatric: No dose adjustment; assess bleeding risk
Max dose: 180 mg loading; 90 mg BD (ACS); 60 mg BD (extended)

Pharmacokinetics

Onset

more rapid onset of action than clopidogrel

Peak effect

more rapid offset of action than clopidogrel

Bioavailability

about 36%

Metabolism

hepatic CYP3A4

Contraindications

Active bleeding
History of intracranial haemorrhage
Severe hepatic impairment
history of prior intracranial bleeding

Side effects

Common

DyspnoeaHaemorrhageHeadacheDizzinessNauseaDiarrhoeaHyperuricaemia/goutdyspnea (17% of patients, often transient and not associated with pulmonary disease)BleedingDyspnea (up to 15% of patients, usually self-limiting and mild)Asymptomatic ventricular pausesDyspnea (often transient and infrequently serious)

Serious