Kogavant (Ticagrelor)

• Ticagrelor is indicated for antiplatelet therapy in several cardiovascular conditions.
• Acute coronary syndrome: reduces risk of cardiovascular death, myocardial infarction and stroke.
• Myocardial infarction prevention: prevents recurrent myocardial infarction in patients with a prior MI.
• Post‑percutaneous coronary intervention (PCI) antiplatelet therapy: provides platelet inhibition after PCI to lower stent thrombosis risk.

• Ticagrelor binds reversibly to the platelet P2Y12 ADP receptor, blocking ADP‑mediated activation of the G_i protein pathway. This inhibition prevents the conformational change of the glycoprotein IIb/IIIa receptor, thereby reducing fibrinogen binding and platelet aggregation. Unlike thienopyridines, ticagrelor does not require metabolic activation, offering rapid and consistent antiplatelet effect. The drug’s rapid onset and offset allow clinicians to adjust therapy based on procedural timing and bleeding risk.

Ticagrelor may cause a range of adverse reactions, varying from mild to severe.

Common Side Effects

• Dyspnea: shortness of breath occurring in many patients.
• Headache: mild to moderate head pain.
• Dizziness: sensation of lightheadedness.
• Nausea: gastrointestinal upset.
• Bleeding: increased bruising or minor bleeding.
• Diarrhea: loose stools.

Serious or Rare Side Effects

• Intracranial hemorrhage: bleeding within the skull.
• Severe bleeding: gastrointestinal or internal hemorrhage requiring medical attention.
• Allergic reactions: rash, pruritus, or anaphylaxis.
• Hepatic injury: elevated liver enzymes or hepatitis.
• Thrombocytopenia: low platelet count.
• Bradyarrhythmia: abnormal slow heart rhythm.

• When prescribing ticagrelor, clinicians should observe several safety precautions to minimize bleeding and other risks.
• Assess bleeding risk: evaluate patient history for active or recent bleeding before initiating therapy.
• Monitor for dyspnea: watch for new or worsening shortness of breath during treatment.
• Avoid in active pathological bleeding: do not start or continue ticagrelor in patients with uncontrolled bleeding.
• Use caution in hepatic impairment: dose adjustments may be needed for moderate to severe liver disease.
• Discontinue before surgery: stop ticagrelor according to recommended interval prior to invasive procedures.
• Store at ambient temperature: keep tablets in the original container, protect from moisture and light.

Ticagrelor interacts with several medicines that can alter its antiplatelet effect or increase bleeding risk.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may raise ticagrelor levels and bleeding risk.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): may reduce efficacy and increase thrombotic risk.
• Concurrent use with other antiplatelet agents (e.g., aspirin, clopidogrel): significantly heightens bleeding potential.

Moderate Interactions (Monitor Closely)

• Statins metabolized by CYP3A4 (e.g., simvastatin, atorvastatin): may increase statin exposure; monitor for muscle symptoms.
• Digoxin: ticagrelor can raise digoxin concentrations; check serum levels.