Ticagrelor

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Czech Republic: Brilique; Denmark: Brilique; Estonia: Brilique, Possia; Finland: Brilique; Germany: Brilique, Possia; Ireland: Brilique; Latvia: Brilique, Possia; Lithuania: Brilique, Possia; Luxembourg: Brilique, Possia; Malta: Brilique, Possia; Netherlands: Brilique, Possia; Portugal: Brilique, Possia; Slovakia: Brilique, Possia; Slovenia: Brilique, Possia; Sweden: Brilique, Possia; UK: Brilique.

Drug combinations

Chemistry

Ticagrelor: C~23~H~28~F~2~N~6~O~4~S. Mw: 522.57. (1S,2S,3R,5S)-3-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol. CAS-274693-27-5.

Pharmacologic Category

Antithrombotic Agents; Platelet-aggregation Inhibitors; Selective adenosine diphosphate (ADP) receptor antagonist. (ATC-Code: B01AC24).

Mechanism of action

Ticagrelor is a member of the chemical class cyclopentyltriazolopyrimidines (CPTP), which is a selective adenosine diphosphate (ADP) receptor antagonist acting reversibly on the platelet P2Y12 ADP-receptor that can prevent ADP-mediated platelet activation and aggregation. Ticagrelor does not interact with the ADP binding site itself, but interacts with platelet P2Y12 ADP-receptor to prevent signal transduction.

Therapeutic use

When co-administered with acetylsalicylic acid (ASA), indicated for the prevention of atherothrombotic events in adult patients with Acute Coronary Syndromes (ACS) such as unstable angina, non-ST elevation myocardial infarction [NSTEMI] or ST elevation myocardial infarction [STEMI]; including patients managed medically, and those who are managed with percutaneous coronary intervention (PCI) or coronary artery by-pass grafting (CABG).

Pregnancy and lactiation implications

Women of childbearing potential should use appropriate contraceptive measures to avoid pregnancy during therapy. Not recommended during pregnancy or lactation.

Unlabeled use

Contraindications

Hypersensitivity to the active substance or to any of the excipients. Active pathological bleeding. History of intracranial hemorrhage. Moderate-to-severe hepatic impairment. Co-administration of ticagrelor with strong CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin, nefazodone, ritonavir, and atazanavir) is contraindicated, as co-administration may lead to a substantial increase in exposure to ticagrelor.

Warnings and precautions

The use of ticagrelor in patients at known increased risk for bleeding should be balanced against the benefit in terms of prevention of atherothrombotic events. If clinically indicated, should be used with caution in patients with propensity to bleeding (e.g. due to recent trauma, recent surgery, coagulation disorders, active or recent gastrointestinal bleeding). Contraindicated in active pathological bleeding, history of intracranial hemorrhage, and in moderate-to-severe hepatic impairment. Caution in patients with concomitant administration of medicinal products that may increase the risk of bleeding (e.g. non-steroidal anti-inflammatory drugs [NSAIDs], oral anticoagulants and/or fibrinolytics) within 24 hours of ticagrelor dosing. Patients should be advised to inform physicians and dentists that they are taking ticagrelor before any surgery is scheduled and before any new medicinal product is taken. Caution should be exercised in patients with an increased risk of bradycardic events or when it is administered concomitantly with medicinal products known to induce bradycardia. Dyspnea has been reported (should be used with caution in patients with history of asthma and/or COPD; if a patient reports new, prolonged or worsened dyspnea, it may be necessary to stop treatment). Creatinine levels may increase during treatment (renal function should be checked after one month and it is recommended to pay special attention to patients ≥75 years, patients with moderate/severe renal impairment and those receiving concomitant treatment with an angiotensin receptor blocker). Patients on ticagrelor had a higher risk of hyperuricemia than those patients receiving clopidogrel (caution should be exercised when administering ticagrelor to patients with history of hyperuricemia or gouty arthritis; use of ticagrelor in patients with uric acid nephropathy is discouraged).

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