Ticagrelor

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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%)[1]
  • 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
  • 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

  1. http://www.drugs.com/cdi/ticagrelor.html -- Accessed April 2015