Ticagrelor

Class
Antiplatelets
Subclass
P2Y12 inhibitors
Substance name
Ticagrelor
Brand names
Brilinta®
Common formulations
Tablet
Dosage and administration
Adults patients
Treatment
Cardiovascular mortality in patients with myocardial infarction
•
Loading: 180 mg PO once
•
Maintenance: 90 mg PO BID for 1 year
Prevention
Cardiovascular mortality in patients with acute coronary syndromes
•
Loading: 180 mg PO once
•
Maintenance: 90 mg PO BID for 1 year followed by 60 mg twice daily thereafter
Stroke in patients with AIS • NIH Stroke Scale score ≤ 5
•
Loading: 180 mg PO once
•
Maintenance: 90 mg PO BID a duration of up to 30 days
TIA
•
Loading: 180 mg PO once
•
Maintenance: 90 mg PO BID a duration of up to 30 days
Indications for use
Labeled indications
Adults
•
Treatment of cardiovascular mortality in patients with myocardial infarction
•
Treatment of coronary artery disease (prevention of first myocardial infarction and first stroke)
•
Prevention of cardiovascular mortality in patients with acute coronary syndromes
•
Prevention of stroke in patients with AIS (NIH Stroke Scale score ≤ 5)
•
Prevention of TIA
Safety risks
Boxed warnings
Exacerbation of bleeding
Contraindications
Hypersensitivity to ticagrelor or any of its components
Warnings and precautions
Cardiac arrhythmias, bradycardia
•
Use caution in patients with a history of sick sinus syndrome, second or third degree AV block, or syncope.
Dyspnea
•
Maintain a high level of suspicion, as mild to moderate intensity dyspnea has been observed in patients treated with ticagrelor.
Exacerbation of central sleep apnea, Cheyne-Stokes respirations
•
Use extreme caution in patients with pre-existing central sleep apnea.
Specific populations
Renal impairment
eGFR 0-90 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required.
Renal replacement therapy
Any modality
•
Use acceptable. No dose adjustment required.
Hepatic impairment
Child-Pugh A (mild)
•
Use acceptable. No dose adjustment required. Monitor for toxicity.
Child-Pugh B (moderate)
•
Use with caution. Monitor for toxicity. - Carefully weigh the risks versus the benefits of treatment, considering the probable increase in exposure to ticagrelor.
Child-Pugh C (severe)
•
Do not use.
Pregnancy and breastfeeding
Pregnancy
All trimesters
•
Use only if benefits outweigh potential risks. Evidence of fetal harm in animals. AU and UK: Use is not recommended.
•
US: Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
•
Furthermore, ticagrelor should be used with extreme caution near term and during labor and obstetric delivery because of the possibility of maternal postpartum hemorrhage.
•
tial risk to the fetus.
Breastfeeding
Consider alternative agents that may be safer.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
•
Dyspnea
Common 1-10%
•
AF, bleeding, bradycardia, hypertension, hypotension, back pain, chest pain, cough, diarrhea, dizziness, fatigue, headache, nausea, syncope
Uncommon < 1%
•
Gynecomastia, intracranial hemorrhage, intracranial hemorrhage, ↑ serum uric acid
Unknown frequency
•
Atrioventricular block, angioedema, apnea, cheyne-Stokes breathing, skin rash, thrombotic thrombocytopenic purpura
Interactions
Drug(s)
Check Interactions
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