Pharm

Ticagrelor

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Ticagrelor, Brilinta

  • Indications
  • Prevention of Thrombotic Events
  1. See Platelet ADP Receptor Antagonist
  2. See Antiplatelet Therapy for Vascular Disease
  3. Cerebrovascular Accident Prevention
  4. Coronary Artery Disease Prevention (especially if Aspirin Allergy)
  5. Post-ST Elevation MI (with or without reperfusion)
    1. Ticagrelor is recommended by ACA (2016) over Clopidogrel in Acute Coronary Syndrome and stenting
  • Contraindications
  1. Active Bleeding
  • Dosing
  1. Requires twice daily dosing (contrast with Clopidogrel which is once daily)
  2. Standard dosing
    1. Brilanta 90 mg orally twice daily
  3. Acute Myocardial Infarction with or without impending PCI
    1. Loading dose: Brilanta 180 mg orally once
    2. Then initiate standard 90 mg twice daily Brilanta dose
    3. Used with Aspirin 81 mg (Dual Antiplatelet Therapy) after PCI
  4. Dosing Adjustments
    1. No dosing adjustment needed in renal and mild hepatic Impairment
    2. Use caution in moderate liver disease and avoid in severe liver disease
  • Efficacy
  1. Per 1000 ACS patients, Ticagrelor prevents more adverse CV events than Clopidogrel
    1. Prevents 11 more cardiovascular deaths
    2. Prevents 11 more Myocardial Infarctions
    3. Prevents 6 more stent thromboses
  2. Majority of cardiovascular benefit is within first few weeks after Acute Coronary Syndrome
    1. Patients on Clopidogrel already will be unlikely to benefit from switch to Ticagrelor
    2. Discuss antiplatelet agent choice with cardiology at time of Acute Coronary Syndrome
  • Adverse Effects
  1. Gastrointestinal Bleeding
    1. Similar bleeding risk to Clopidogrel
  2. Dyspnea
    1. Occurs with Brilinta use for 1 in 27 patients
  3. Dizziness or Syncope
  4. Acute Kidney Injury
  5. Other less common adverse effects
    1. Angioedema or Hypersensitivity
    2. AV Block
    3. Bradycardia
    4. Skin rash
  • Safety
  1. Pregnancy Category C
  2. Unknown safety in Lactation
  • Drug Interactions
  1. Metabolized by CYP3A4
  2. Digoxin
  3. Morphine (and presumed other Opioids)
    1. Morphine decreased (35%) and delayed (2 hours) Ticagrelor absorption
    2. May affect acute STEMI management
    3. Kubica (2016) Int J Cardiol 215:201-8 [PubMed]
  4. Aspirin
    1. Doses >100 mg decrease Ticagrelor efficacy
  5. CYP3A4 Inhibitors (increased Ticagrelor effects and bleeding risk)
    1. Protease Inhibitors
    2. Clarithromycin
    3. Ketoconazole, Itraconazole or Voriconazole
  6. CYP3A4 Inducers (decreased Ticagrelor efficacy)
    1. Carbamazepine
    2. Phenobarbital
    3. Phenytoin
    4. Dexamethasone
    5. Rifampin
  7. Statins (e.g. Simvastatin, Lovastatin at doses >40 mg/day)
    1. Increased Statin related adverse effects
  • Management
  • Reversal
  1. See Platelet ADP Receptor Antagonist
  2. Stop 5 days before elective surgery
  • References
  1. (2012) Presc Lett 19(5): 27
  2. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  3. Filler and Lovecchio (2017) Crit Dec Emerg Med 31(7): 24
  4. Switaj (2017) Am Fam Physician 95(4): 232-40 [PubMed]