Ticagrelor

DEA Class; Rx

Common Brand Names; Brilinta

• Antiplatelet Agents, Cardiovascular

Hypersensitivity (eg, angioedema)

History of intracranial hemorrhage (ICH)

Active pathologic bleeding (eg, peptic ulcer, ICH)

Dyspnea (13.8%)

Bleeding (see specific data listed below)

Dizziness (4.5%)

Nausea (4.3%)

Diarrhea (3.7%)

Ventricular pauses (6%)

Bleeding

Non-CABG related bleeds (PLATO trial)

• Total bleeds (major + minor) (7.7%)

• Major bleeds

  • Major bleeds (3.9%)
  • Fatal/life-threatening (1.9%)
  • Fatal (0.2%)
  • Intracranial (fatal/life-threatening) (0.3%)

CABG related bleeds (PLATO trial)

• Total major bleeds (81.3%)
• Major bleeds when antiplatelet therapy stopped 5 days before CABG (75%)
• Fatal/life-threatening (43.8%)
• Fatal (0.8%)

Bleeding events (PEGASUS trial)

• TIMI major

  • TIMI major: 8 per 1000 patient years
  • Fatal: 1 per 1000 patient years
  • Intracranial hemorrhage: 2 per 1000 patient years

• TIMI major or minor

  • 11 per 1000 patient years

Bleeding events (THEMIS trial)

• TIMI major: 9 per 1000 patient years
• TIMI major or minor: 12 per 1000 patient years
• TIMI major or minor or requiring medical attention: 46 per 1000 patient years
• Fatal bleeding: 1 per 1000 patient years
• Intracranial hemorrhage: 3 per 1000 patient years

Inhibits platelet function, and thereby, increases bleeding risk; if possible, manage bleeding without discontinuing drug; stopping ticagrelor increases risk of subsequent cardiovascular events

Discontinuation of therapy will increase risk of myocardial infarction, stroke, and death in patients being treated for coronary artery disease; if drug must be temporarily discontinued (eg, to treat bleeding or for significant surgery), restart it as soon as possible; when possible, interrupt therapy for five days prior to surgery that has a major risk of bleeding and resume therapy as soon as hemostasis is achieved

Surgery: When possible, discontinue 5 days prior to surgery

Dyspnea reported; intensity described as usually mild-to-moderate and decreases/resolves during continued treatment; if dyspnea symptoms intolerable consider administering a different antiplatelet agent

Can cause ventricular pauses; bradyarrhythmias, including AV block reported; patients with history of sick sinus syndrome, 2nd or 3rd degree AV block, or bradycardia-related syncope who were not protected by a pacemaker were excluded from PLATO and PEGASUS and may be at increased risk of developing bradyarrhythmias with ticagrelor

Avoid use with severe hepatic impairment, which may increase ticagrelor serum levels

Reported to cause false-negative results in platelet functional tests (eg, HIPA assay for HIT)

Central sleep apnea (CSA) including Cheyne-Stokes respiration (CSR) reported in post-marketing setting, including recurrence or worsening of CSA/CSR following rechallenge; if central sleep apnea suspected, consider further clinical assessment

Available data from case reports on use in pregnant females have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

There are no data on presence of drug or metabolites in human milk, effect on breastfed infants, or on milk production