Brilinta, pills 90 mg, 168 pcs.

Composition

1 table. contains ticagrelor 90 mgm auxiliary substances: mannitol 126 mg, calcium hydrophosphate 63 mg, sodium carboxymethyl starch 9 mg, hyprolose 9 mg, magnesium stearate 3 mg. composition of the film shell:hypromellose 2910 5,6 mg, titanium dioxide E 171 1,7 mg, talc 1,0 mg, macrogol 400 0,6 mg, iron oxide yellow dye E 172 0,1 mg

. Pharmacological action

Brilinta contains ticagrelor, a member of the cyclopentyltriazolopyrimidine chemical class, which is a selective and reversible antagonist of the P2Y12 adenosine diphosphate (ADP) receptor and can prevent ADP-mediated platelet activation and aggregation. Ticagrelor is active when taken orally and reversibly interacts with the P2Y12 ADP platelet receptor. Ticagrelor does not interact with the binding site of ADP itself, but its interaction with the P2Y12 platelet receptor for ADP prevents signal transduction. In patients with a stable course of coronary heart disease (CHD), ticagrelor begins to act quickly against the background of acetylsalicylic acid, which is confirmed by the results of determining the average value of platelet aggregation inhibition (IAT): 0.5 hours after taking a loading dose of 180 mg of ticagrelor, the average IAT value is approximately 41%, the maximum IAT value of 89% is reached 2-4 hours after taking the drug and is maintained for 2-8 hours. In 90% of patients, the final IAT value of more than 70% is reached 2 hours after taking the drug. When planning CABG, the risk of bleeding increases if ticagrelor is stopped less than 96 hours before the procedure.

Indications

Brilinta, used simultaneously with acetylsalicylic acid, is indicated for the prevention of atherothrombotic events in patients with acute coronary syndrome:

• Unstable angina pectoris.
• Non-ST-segment elevation myocardial infarction or ST-segment elevation myocardial infarction [STEMI]), including patients receiving drug therapy and patients undergoing percutaneous coronary intervention (PCI) or coronary artery bypass grafting (CABG)).

Contraindications

• Hypersensitivity to ticagrelor or any of the components of the drug.
• Active pathological bleeding.
• History of intracranial hemorrhage.
• Moderate or severe liver failure.
• Co-administration of ticagrelor with potent CYP3A4 inhibitors (e. g. ketoconazole, clarithromycin, nefazodone, ritonavir and atazanavir).
• Children under 18 years of age (due to the lack of data on the effectiveness and safety of use in this group of patients).

Side effects

According to the PLATO study, the most common reported adverse events in patients taking ticagrelor were shortness of breath, bruising, and nosebleeds. Adverse reactions are classified according to the frequency of development and the class of the organ system. The frequency of adverse reactions is determined using the following symbols: very common (≥1/10), common (≥1/100, Adverse drug reactions by frequency and class of organ system (SOC) – Metabolism and nutrition: Hyperuricemia (a*) (rare)- Nervous system: Intracranial hemorrhage (b*), headache, dizziness (infrequent), Paresthesia, confusion (rare) – Visual organs: Hemorrhages (intraocular, conjunctival, retinal) (infrequent)- Hearing organs: Ear hemorrhage, vertigo (rare)- Respiratory system: Shortness of breath (c*), nosebleedd (often), Hemoptysis (infrequently)- Digestive system: Gastrointestinal bleeding (d*) (common), Vomiting with blood, bleeding from a gastrointestinal ulcer (e*), hemorrhoidal bleeding, gastritis, oral bleeding (including gingival bleeding), vomiting, diarrhea, abdominal pain, nausea, dyspepsia (infrequent), Retroperitoneal bleeding, constipation (rare)- Skin and subcutaneous tissue: Subcutaneous or cutaneous hemorrhages (f*), bruises (g*) (common), Rash, itching (uncommon)- Musculoskeletal system: Hemarthrosis (rare) – Urinary system: Bleeding from the urinary tract (h*) (infrequent)- Reproductive system: Vaginal bleeding (including metrorrhagia) (infrequently)- Laboratory abnormalities: Increased blood creatinine (rarely) – Other: Bleeding at the procedure site (i*) (often), Bleeding after the procedure (infrequently), Bleeding from a wound, traumatic bleeding (rarely).

Interaction

Effects of other medicinal products on Brilinta®Drugs metabolized by the CYP3A4 isoenzyme CYP3A4 inhibitors * Potent CYP3A4 inhibitors: concomitant use of ketoconazole with ticagrelor increases the Cmax and AUC of ticagrelor by 2.4 and 7.3 times, respectively. Cmax and AUC of the active metabolite were reduced by 89% and 56%, respectively. Other potent CYP3A4 inhibitors (clarithromycin, nefazodone, ritonavir, and atazanavir) will have similar effects, so their combined use with Brilinta® is contraindicated (see sections “Contraindications”, “Special Instructions”). * Moderate CYP3A4 inhibitors: co-administration of diltiazem with ticagrelor increases the Cmax of ticagrelor by 69% and the AUC by 2.7 times, and reduces the Cmax of the active metabolite by 38%, but the AUC does not change. Ticagrelor does not affect the plasma concentrations of diltiazem. Other moderate CYP3A4 inhibitors (e. g., amprenavir, aprepitant, erythromycin, fluconazole) may be administered concomitantly with Brilinta. CYP3A4 inducers Co-administration of rifampicin with ticagrelor reduces the Cmax and AUC of ticagrelor by 73% and 86%, respectively. The Cmax of the active metabolite does not change, and the AUC decreases by 46%. Other CYP3A4 inducers (e. g. dexamethasone, phenytoin, carbamazepine, and phenobarbital)are likely to reduce exposure to Brilinta. Potent inducers of CYP3A4 may reduce the exposure and efficacy of Brilinta. According to the results of pharmacological interaction studies, concomitant use of ticagrelor with heparin, enoxaparin and acetylsalicylic acid or desmopressin does not affect the pharmacokinetics of ticagrelor, its active metabolite and ADP-dependent platelet aggregation. If there are clinical indications for the use of drugs that affect hemostasis, they should be used with caution in combination with Brilinta® (see the section “With caution”). There are no data on the concomitant use of Brilinta® with potent glycoprotein P inhibitors (for example, verapamil, quinidine and cyclosporine) that can increase the exposure of ticagrelor. If their combined use cannot be avoided, it should be carried out with caution (see the sections “With caution”, “Special instructions”). Effect of Brilinta® on other medicinal mediationsmedicines metabolized by the CYP3A4 isoenzyme * Simvastatin: concomitant use of ticagrelor and simvastatin increases the Cmax and AUC of simvastatin by 81% and 56%, respectively, and increases the Cmax and AUC of simvastatin acid by 64% and 52%, respectively, while in some cases these indicators increase 2-3 times. Concomitant use of simvastatin at a dose higher than 40 mg / day. treatment with ticagrelor may lead to the development of simvastatin side effects, and the potential risk-benefit ratio should be evaluated. * Non-moderate CYP3A4 inhibitors: co-administration of diltiazem with ticagrelor increases the Cmax of ticagrelor by 69% and the AUC by 2.7 times, and reduces the Cmax of the active metabolite by 38%, but the AUC does not change. Ticagrelor does not affect the plasma concentrations of diltiazem. Other moderate CYP3A4 inhibitors (e. g., amprenavir, aprepitant, erythromycin, fluconazole) may be administered concomitantly with Brilinta. CYP3A4 inducers Co-administration of rifampicin with ticagrelor reduces the Cmax and AUC of ticagrelor by 73% and 86%, respectively. The Cmax of the active metabolite does not change, and the AUC decreases by 46%. Other CYP3A4 inducers (e. g. dexamethasone, phenytoin, carbamazepine, and phenobarbital)are likely to reduce exposure to Brilinta. Potent inducers of CYP3A4 may reduce the exposure and efficacy of Brilinta.

How to take, course of administration and dosage

For oral administration. Brilinta can be taken regardless of food intake. The use of Brilinta should begin with a single loading dose of 180 mg (two tablets of 90 mg) and then continue taking 90 mg twice a day. Patients taking Brilinta should take acetylsalicylic acid daily (from 75 mg to 150 mg with constant intake), if there are no specific contraindications. Interruptions in therapy should be avoided. A patient who has missed taking Brilinta should only take one 90 mg tablet (the next dose) at the scheduled time. If necessary, patients taking clopidogrel can be transferred to Brilinta. It is recommended to carry out therapy with Brilinta for 12 months, except in cases of clinical need for early withdrawal of the drug. Data on the use of ticagrelor for more than 12 months are limited. In patients with acute coronary syndrome, early withdrawal of any antiplatelet therapy, including Brilinta, may increase the risk of cardiovascular death or myocardial infarction as a result of the underlying disease. Premature discontinuation of the drug should be avoided.

Overdose

Symptoms: In the only dose-increasing study, the adverse effects on the gastrointestinal tract were dose-limiting. Other clinically significant adverse events that may have occurred with overdose were dyspnea and ventricular pauses.In case of overdose, it is recommended to monitor for these adverse events and conduct ECG monitoring. : Brilinta is not excreted during hemodialysis, and the antidote is not known. In case of overdose, symptomatic therapy should be carried out in accordance with local standards. Due to platelet inhibition, an increase in the duration of bleeding is a suspected pharmacological effect of an overdose with Brilinta, so appropriate maintenance measures should be taken if bleeding develops.

Special instructions

In patients with acute coronary syndrome treated with Brilinta and acetylsalicylic acid, there was an increased risk of non-CABG major bleeding and bleeding requiring increased medical attention, such as large + small bleeding as defined by PLATO, but the risk of fatal/life-threatening bleeding did not increase. When prescribing Brilinta, the ratio of benefit from prevention of atherothrombotic events and risk in patients with an increased risk of bleeding should be evaluated.

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

2 years

Active ingredient

Ticagrelor

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Prevention of thrombosis, Angina pectoris, Prevention of heart attacks and strokes, Thrombophlebitis, Myocardial infarction

Weight

Weight: 250 gr.