Tikagrelor (Ticagrelorum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

Antiaggregants

Included in the formulation
  • Brilinta®
    pills inwards 
    AstraZeneca AB     Sweden
  • Brilinta®
    pills inwards 
    AstraZeneca AB     Sweden
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    B.01.A.C   Inhibitors of platelet aggregation (excluding heparin)

    B.01.A.C.24   Tikagrelor

    Pharmacodynamics:

    The selective and reversible antagonist of the P2Y12 receptor to adenosine diphosphate (ADP) prevents ADP-mediated activation and platelet aggregation.

    Pharmacokinetics:

    After oral administration, up to 36% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 1.5 hours. The connection with plasma proteins is more than 99%.

    Metabolism in the liver.

    The half-life is 7 hours. Elimination with feces (57%) and kidneys (43%).

    Indications:

    Used in combination with acetylsalicylic acid to prevent atherothrombotic complications in patients with stable angina, myocardial infarction, as well as in patients after percutaneous coronary intervention or coronary artery bypass grafting.

    ICD-10

    IX.I20-I25.I20   Angina pectoris [angina pectoris]

    IX.I20-I25.I21   Acute myocardial infarction

    IX.I26-I28.I26   Pulmonary embolism

    IX.I70-I79.I74   Embolism and thrombosis of the arteries

    IX.I80-I89.I82   Embolism and thrombosis of other veins

    XXI.Z80-Z99.Z95.1   Aortocoronary shunt transplant

    XXI.Z80-Z99.Z95.5   Presence of coronary angioplasty implant and graft

    Contraindications:

    Bleeding, severe hepatic insufficiency, individual intolerance.

    Carefully:

    Blood clotting disorders, hyperuricemia.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside. The loading dose: 180 mg, then 90 mg 2 times / day.

    The highest daily dose: 180 mg.

    The highest single dose: 180 mg.

    Side effects:

    Central and peripheral nervous system: headache, intracranial hemorrhage, confusion, paresthesia.

    Respiratory system: shortness of breath, hemoptysis, nosebleed.

    Digestive system: gingival, gastrointestinal, hemorrhoidal hemorrhages, diarrhea, constipation.

    Musculoskeletal system: rarely - hemarthrosis.

    Dermatological reactions: subcutaneous and dermal hemorrhages, bruising, itching.

    Sense organs: conjunctival, intraocular, retinal hemorrhages, vertigo.

    Reproductive system: metrorrhagia.

    Urinary system: hematuria.

    Local reactions: necrosis or bruising at the injection site.

    Allergic reactions.

    Overdose:

    Bleeding.

    Treatment is symptomatic.

    Interaction:

    The risk of bleeding increases with simultaneous use with salicylates, indirect coagulants, glucocorticoids, nonsteroidal anti-inflammatory drugs, antiaggregants.

    Simultaneous use with CYP3A4 inhibitors (nefazodone, ketoconazole, clarithromycin, atazanavir and ritonavir) leads to an increase in exposure to ticagrelyl.

    Simultaneous application with inductors CYP3A4 (dexamethasone, rifampicin, phenytoin, carbamazepine and phenobarbital) decreases the effectiveness of ticagrelyl.

    Special instructions:

    Monitoring the amount of peripheral blood platelets.

    It is recommended to cancel the drug 7 days before the scheduled operation.

    Instructions
    Up