TYE-ka-GREL-or

• To reduce the risk of cardiovascular death, MI, and stroke in patients with acute coronary syndrome (ACS) or a history of MI. Also reduces the risk of stent thrombosis in patients who have received an intracoronary stent for ACS (in combination with aspirin).
• To reduce the risk of first MI or stroke in patients with coronary artery disease who are at high risk for such events (in combination with aspirin).
• To reduce the risk of stroke in patients with acute ischemic stroke (NIH Stroke Scale score 5) or high-risk transient ischemic attack (TIA) (in combination with aspirin).

• Both parent drug and its active metabolite inhibit platelet aggregation by reversibly interacting with platelet P2Y₁₂ADP-receptors, preventing signal transduction and platelet activation.

• Reduction in risk of cardiovascular death, MI, and stroke associated with ACS.
• Reduction in stent thrombosis
• Reduction in risk of first MI or stroke in high-risk patients with coronary artery disease.
• Reduction in risk of stroke in patients with acute ischemic stroke or TIA.

Absorption: 36% absorbed following oral administration.

Distribution: Well distributed to tissues.

Protein Binding: 99%.

Metabolism/Excretion: Mostly metabolized in the liver (CYP3A4 enzyme system, some metabolism by CYP3A5) with conversion to an active metabolite (AR-C124910XX); excretion primarily via biliary secretion; <1% excreted unchanged or as active metabolite in urine.

Half-life: Ticagrelor — 7 hr; Active metabolite — 9 hr.

Contraindicated in:

• Hypersensitivity
• Active bleeding
• History of intracranial bleeding
• Severe hepatic impairment (↑ risk of bleeding)
• Impending coronary artery bypass graft (CABG) surgery or other surgery (discontinue 5 days prior)
• Use of thrombolytics for treatment of acute ischemic stroke
• Strong inhibitors/inducers of CYP3A enzyme system (avoid concurrent use if possible)
• Lactation: Lactation.

Use Cautiously in:

• Moderate hepatic impairment
• History of sick sinus syndrome, 2nd or 3rd degree heart block, or bradycardia-related syncope in the absence of a pacemaker
• Hypotension following recent CABG or percutaneous coronary intervention (PCI) in patients receiving ticagrelor (consider bleeding as a cause)
• OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk
• Pedi: Safety and effectiveness not established in children
• Geri: Some older adults may be more sensitive to drug effects.

CV: bradycardia, heart block.

Endo: gynecomastia.

Hemat: BLEEDING.

Resp: dyspnea, central sleep apnea, Cheyne-Stokes respiration.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA).

Drug-Drug:

• Strong inhibitors of CYP3A4/5 including atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, and voriconazole↑ levels and the risk of bleeding and should be avoided.
• Potent inducers of CYP3A including carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampin may ↓ levels and effectiveness and should be avoided.
• P-glycoprotein (P-gp) inhibitors including cyclosporine may ↑ levels and the risk of bleeding
• Concurrent use of lovastatin or simvastatin in doses >40 mg/day ↑ risk of statin-related adverse reactions.
• Effectiveness is ↓ by aspirin >100 mg/day (maintain aspirin at 75–100 mg/day).
• May alter digoxin levels (monitoring recommended).
• Risk of bleeding ↑ by anticoagulants, fibrinolytics and chronic NSAIDs.
• Opioids may ↓ absorption of ticagrelor and its active metabolite and ↓ antiplatelet effects; consider using parenteral antiplatelet in patients with acute coronary syndrome if concurrent use of opioids needed.

Acute Coronary Syndrome or History of Myocardial Infarction

• PO (Adults): Loading dose — 180 mg; followed by maintenance dose — 90 mg twice daily for 1 yr, then 60 mg twice daily.

Coronary Artery Disease Without a History of Myocardial Infarction or Stroke

• PO (Adults): 60 mg twice daily.

Acute Ischemic Stroke or Transient Ischemic Attack

• PO (Adults): Loading dose — 180 mg; followed by maintenance dose — 90 mg twice daily for up to 30 days.

• PO: Administer without regard for food.
  • For patients unable to swallow, tablets can be crushed and mixed with water. Mixture can also be administered via a nasogastric tube.
  • Patients who have received a loading dose of clopidogrel may be started on ticagrelor.
  • For acute ischemic stroke or transient ischemic attack (TIA), administer a loading dose of aspirin (300–325 mg) and a daily maintenance dose of aspirin (75–100 mg) with ticagrelor.
  • Discontinue ticagrelor 5 days before planned surgical procedures with a major risk of bleeding. If ticagrelor must be temporarily discontinued, restart as soon as possible. Premature discontinuation of therapy may increase risk of myocardial infarction, stent thrombosis, and death.

Brilinta

Therapeutic Classification: antiplatelet agents

Pharmacologic Classification: platelet aggregation inhibitors

(Generic available)

• Tablets : 60 mg; 90 mg;

(inhibition of platelet aggregation)

† Following discontinuation.

• Assess patient for symptoms of stroke, peripheral vascular disease, or MI periodically during therapy.
• Observe patient for signs and symptoms of hypersensitivity reactions (rash, facial swelling, pruritus, laryngeal edema, wheezing). Discontinue drug and notify health care professional immediately if symptoms occur. Keep epinephrine, an antihistamine, and resuscitation equipment close by in case of anaphylactic reaction.

• May cause ↑ serum uric acid and ↑ serum creatinine.
  • May cause false negative results in heparin-induced platelet aggregation (HIPA) assay for patients with heparin-induced thrombocytopenia (HIT).

• Instruct patient to take ticagrelor exactly as directed. Take missed doses as soon as possible unless almost time for next dose; do not double doses. Do not discontinue ticagrelor without consulting health care professional; may increase risk of cardiovascular events. Advise patient to read the Medication Guide before starting therapy and with each Rx refill in case of changes.
• Advise patient that daily aspirin should not exceed 100 mg and to avoid taking other medications that contain aspirin.
• Inform patient that they will bleed and bruise more easily and it will take longer to stop bleeding. Advise patient to notify health care professional promptly if unusual, prolonged, or excessive bleeding or blood in stool or urine occurs.
• Inform patient that ticagrelor may cause shortness of breath which usually resolved during therapy. Advise patient to notify health care professional if unexpected or severe shortness of breath or symptoms of hypersensitivity reactions occur.
• Advise patient to notify health care professional of medication regimen prior to treatment or surgery or dental procedure. Prescriber should be consulted before stopping ticagrelor.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially aspirin or NSAIDs.
• Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy.

• Decreased thrombotic cardiovascular events in patients with ACS.
• Reduction in risk of first MI or stroke in high-risk patients with coronary artery disease.
• Reduction in risk of stroke in patients with acute ischemic stroke or TIA.

NDC Code^*

• 0186- AstraZeneca Pharmaceuticals LP
  • 0186-0776- BRILINTA
    • 0186-0776-60- 60 TABLET in 1 BOTTLE (0186-0776-60)

• 0186- AstraZeneca Pharmaceuticals LP
  • 0186-0776- BRILINTA
    • 0186-0776-94- 1 BLISTER PACK in 1 BOX, UNIT-DOSE (0186-0776-94) > 14 TABLET in 1 BLISTER PACK

• 0186- AstraZeneca Pharmaceuticals LP
  • 0186-0777- BRILINTA
    • 0186-0777-08- 8 TABLET in 1 BOTTLE (0186-0777-08)

• 0186- AstraZeneca Pharmaceuticals LP
  • 0186-0777- BRILINTA
    • 0186-0777-39- 10 BLISTER PACK in 1 BOX, UNIT-DOSE (0186-0777-39) > 10 TABLET in 1 BLISTER PACK

• 0186- AstraZeneca Pharmaceuticals LP
  • 0186-0777- BRILINTA
    • 0186-0777-60- 60 TABLET in 1 BOTTLE (0186-0777-60)

• 55154- Cardinal Health
  • 55154-9618- BRILINTA
    • 55154-9618-0- 10 BLISTER PACK in 1 BAG (55154-9618-0) > 1 TABLET in 1 BLISTER PACK

• 55154- Cardinal Health
  • 55154-9618- BRILINTA
    • 55154-9618-8- 1440 TABLET in 1 BOTTLE, PLASTIC (55154-9618-8)

• 69238- Amneal Pharmaceuticals NY LLC
  • 69238-1134- ticagrelor
    • 69238-1134-1- 100 TABLET in 1 BOTTLE (69238-1134-1)

• 69238- Amneal Pharmaceuticals NY LLC
  • 69238-1134- ticagrelor
    • 69238-1134-6- 60 TABLET in 1 BOTTLE (69238-1134-6)