Ticagrelor

General

• Type: Antiplatelet
• Dosage Forms: Pill
• Common Trade Names: Brilenta

Adult Dosing

• ACS: 180mg (two 90mg tablets) loading dose
  • PO vs OG vs NG (depending on mental status)
• ACS patients who have received a loading dose of Clopidogrel may be started on Ticagrelor
• Maintenance: 90mg twice daily

Pediatric Dosing

• Undetermined

Special Populations

• Pregnancy Rating: Category C
• Lactation: Undetermined
• Renal Dosing
  • Adult
  • Pediatric
• Hepatic Dosing
  • Adult
  • Pediatric

Contraindications

• Allergy to class/drug
• History of:
  • Intracranial hemorrhage
  • Active pathological bleeding, such as peptic ulcer or intracranial hemorrhage
  • Severe hepatic impairment

Adverse Reactions

Serious

• Major coronary artery bypass graft (CABG)–related bleeding (86%)
• Digoxin: Because of inhibition of the P-gp transporter, digoxin concentrations may be elevated, increasing the risk of toxicity.
  • Monitor digoxin concentrations with initiation of, or any change in, ticagrelor therapy

Common

• Cardiovascular
  • Ventricular pause (6%)
  • Atrial fibrillation
  • Hypertension (4%)
  • Chest pain
  • Hypotension(3%)
• CNS
  • Headache (7%)
  • Dizziness (5%)
  • Fatigue (3%)
  • Syncope/pre-syncope/loss of consciousness (2%)
• GI
  • Diarrhea, nausea (4%).
• Hematologic
  • Non–CABG-related bleeding (9%)
• Pulmonary
  • Dyspnea (14%)
  • Cough (5%)

Pharmacology

• Half-life: 7 hours (ticagrelor) and 9 hours (active metabolite)
• Metabolism: liver (CYP3A4)
• Excretion: 26% excreted in urine (less than 1% as ticagrelor and the active metabolite); 58% excreted in feces
• Mechanism of Action: Reversibly binds to the P2Y 12 class of adenosine diphosphate (ADP) receptors on platelets to prevent signal transduction and platelet activation

See Also

Antiplatelet

References

Authors

Aaron Snyder, Daniel Ostermayer, Ross Donaldson, Neil Young