Ticagrelor

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[edit] STRUCTURE

Ticagrelor.jpg

[edit] MECHANISM OF ACTION

Ticagrelor, is an inhibitor of platelet aggregation. This means that it helps to prevent blood clots from forming. When the blood clots, this is due to special cells in the blood, the platelets, sticking together (aggregating).

Ticagrelor acts as a selective and reversible antagonist of the adenosine diphosphate (ADP) P2Y12 receptor. it binds to the platelet P2Y12 receptors and prevents ADP-mediated platelet activation of the glycoprotein GPIIb/IIIa complex. As the glycoprotein GPIIb/IIIa complex is the major receptor for fibrinogen, its impaired activation prevents fibrinogen binding to platelets and inhibits platelet aggregation.

Ticagrelor, by reducing the risk of a blood clot forming, it helps to prevent a stroke or another heart attack.

In a study involving over 18,000 adults who had had a heart attack or had unstable angina, Ticagrelor was compared with clopidogrel (another inhibitor of platelet aggregation). The patients also took aspirin and were treated for up to a year. The main measure of effectiveness was based on the number of patients having another heart attack, a stroke or dying from a cardiovascular disease. In the main study, 9.3% of the patients taking Ticagrelor 90 mg twice daily had another heart attack, stroke or died from a cardiovascular disease compared with 10.9% of patients taking clopidogrel 75 mg daily.

[edit] INDICATIONS

Ticagrelor is used together with acetylsalicylic acid (ASA) to prevent atherothrombotic events such as heart attacks or strokes. It is used in adults who have had a heart attack or have unstable angina (chest pain caused by problems with the blood flow to the heart).

[edit] DOSAGE

The loading dose of Ticagrelor is 180 mg (two tablets) taken at once, followed by a regular dose of 90 mg (one tablet) taken twice a day. Patients should also be taking aspirin daily, unless specifically contraindicated. the initial loading dose of ASA is 325 mg and the daily maintenance dose should be 75-100 mg (Maintenance doses of aspirin above 100 mg decreased the effectiveness of Ticagrelor).

Treatment is recommended for up to 12 months unless discontinuation of Ticagrelor is clinically indicated. Experience beyond 12 months is limited.

Patients treated with clopidogrel can be directly switched to Ticagrelor if needed.

[edit] CONTRAINDICATIONS

  • Hypersensitivity to ticagrelor or any of the other ingredients.
  • Severe liver disease
  • Active pathological bleeding
  • History of intracranial hemorrhage

[edit] WARNINGS AND PRECAUTIONS

  • Ticagrelor increases the risk of bleeding
  • Dyspnea, usually mild to moderate in intensity and often resolves without need for treatment discontinuation. Patients with asthma/COPD may have an increased absolute risk of experiencing dyspnea with ticagrelor. Dyspnea was reported more frequently with ticagrelor than with clopidogrel.
  • Discontinuations: Patients who require discontinuation of Ticagrelor are at increased risk for cardiac events. Premature discontinuation of treatment should be avoided.

[edit] INTERACTIONS

  • Ticagrelor is primarily a CYP3A4 substrate. Avoid it in patients taking other medicines which are:
  • The concomitant use of Ticagrelor with doses of simvastatin or lovastatin greater than 40 mg is not recommended (ticagrelor increases simvastatin and lovastatin plasma levels)
  • Ticagrelor is a p-glycoprotein (P-gp) substrate and a weak inhibitor of P-gp. Close clinical and laboratory monitoring is recommended when giving narrow therapeutic index P-gp dependent drugs like digoxin concomitantly with Ticagrelor

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Ticagrelor should be used during pregnancy only if the potential benefit to the mother justifies any potential risks to the fetus.
  • It is not known whether Ticagrelor is excreted in human milk, as no clinical study has been conducted in lactating women. Studies in rats have shown that ticagrelor and its active metabolites are excreted in milk. Therefore, its use during breastfeeding is not recommended.

[edit] SIDE EFFECTS

The most common side effects with Ticagrelor are dyspnea (difficulty breathing) in 14% of patients, epistaxis (nose bleeds), gastrointestinal hemorrhage (bleeding in the stomach or gut), bleeding in the skin or below the skin, bruising, and bleeding at the procedural site (where a blood vessel has been punctured).

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