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
    • No adjustment necessary
  • Pediatric
• Hepatic Dosing
  • Adult
    • Mild impairment - no adjustment necessary
    • Moderate impairment - not defined but use caution as undergoes hepatic metabolism
    • Severe impairment - avoid use
  • 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 medications
• Antiplatelet agent reversal

References

Ticagrelor: Drug information. UpToDate. www.uptodate.com. Accessed April 2, 2019.