Brilinta

Brilinta is a drug whose action is aimed at preventing the formation of blood clots in the blood.

As a result, the cells lose their ability to glue and form clots. The drug belongs to the pharmacological group of anticoagulants and antiplatelet agents.

On this page you will find all the information about Brilint: complete instructions for use for this drug, average prices in pharmacies, complete and incomplete analogues of the drug, as well as reviews of people who have already used Brilint. Want to leave your opinion? Please write in the comments.

Clinico-pharmacological group

Antiplatelet.

Pharmacy sales terms

It is released on prescription.

Prices

How much does Brilint cost? The average price in pharmacies is at 5,500 rubles.

Release form and composition

Brilin's drug dosage form is coated tablets. The main active ingredient of the drug is ticagrelor, the concentration of which in 1 tablet is 90 mg.

The composition of the shell covering the tablet includes such excipients:

  • Titanium dioxide E 171-1.7 mg.
  • Hypromellose 2910-5.6 mg.
  • Talc - 1.0 mg.
  • Dye iron oxide yellow E172 - 0.1 mg.
  • Macrogol 400 - 0.6 mg.

Also included excipients:

  • Calcium phosphate - 63 mg.
  • Mannitol - 126 mg.
  • Sodium carboxymethyl starch - 9 mg.
  • Magnesium stearate - 3 mg.
  • Giproloza - 9 mg.

The tablets are packaged in 56 and 112 pieces. The carton pack also contains instructions for use of the drug.

Pharmacological effect

The active substance of the drug, ticagrelor is an oral, selective and reversible antagonist of direct acting P2Y12 receptors, a member of the chemical class of cyclopentyl triazolopyrimidines and warning ADP (adenosine diphosphate) -mediated P2Y12-dependent platelet aggregation and activation. The interaction of ticagrelor with the P2Y12 platelet receptor interferes with ADP-induced signal transduction. Inhibiting platelet function, the drug helps reduce the risk of cardiovascular events such as stroke, myocardial infarction, and death.

Ticagrelor also has an additional mechanism of action by increasing local concentrations of endogenous adenosine by inhibiting the endogenous equilibrium nucleoside transporter type I (ENT-1). In patients with acute coronary syndrome (ACS) and in healthy volunteers, ticagrelor increased the effects of adenosine, such as vasodilatation, platelet function suppression and shortness of breath. However, the relationship of morbidity and mortality with elevated local concentrations of adenosine has not been proven.

Indications for use

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

  • Unstable angina.
  • Myocardial infarction without ST segment elevation or myocardial infarction with ST segment elevation STEMI), including patients who received drug therapy, and patients undergoing percutaneous coronary intervention (CKB) or coronary artery bypass surgery (CABG)).

Contraindications

Absolute contraindications

  • history of intracranial hemorrhage;
  • moderate or severe liver failure;
  • hypersensitivity to the active substance or to any excipient;
  • the presence of abnormal bleeding;
  • pregnancy and lactation;
  • combined use of ticagrelor with powerful inhibitors of CYP3A4 (for example, ketoconazole, clarithromycin, nefazodone, ritonavir, and atazanavir), since combined use can lead to a significant increase in the effects of ticagrelor.

Relative (Brilint should be taken with caution):

  • concomitant therapy with drugs that increase the risk of bleeding with nonsteroidal anti-inflammatory drugs (NSAIDs), oral anticoagulants and / or fibrinolytic agents, for 24 hours before taking ticagrelor;
  • susceptibility to the development of bleeding (recent injuries, recent operations, bleeding disorders, active or recent gastrointestinal bleeding);
  • combined use with drugs that cause bradycardia;
  • chronic obstructive pulmonary disease (COPD) and bronchial asthma (in case of prolonged dyspnea, the occurrence of a new episode or worsening of dyspnea, an examination is required, in case of intolerance, treatment with ticagrelor must be stopped);
  • increased risk of developing bradycardia, sick sinus syndrome (patients without a pacemaker), atrioventricular block II or III, fainting associated with bradycardia, because clinical experience Brilints is insufficient;
  • moderate to severe renal failure;
  • concomitant therapy with angiotensin receptor antagonists;
  • a history of hyperuricemia or gouty arthritis (use of ticagrelor with hyperuricemic nephropathy should be avoided);
  • combined use with powerful inhibitors of P-glycoprotein (quinidine and verapamil), because there are no data from clinical observations;
  • combined use with digoxin when indicated, careful clinical and laboratory monitoring of heart rate (HR), electrocardiogram (ECG) and plasma concentration of digoxin is recommended;
  • age of 75 years and older.

Combined use of Brilints with ASA in a high maintenance dose exceeding 300 mg is not recommended.

Use during pregnancy and lactation

The drug should not be prescribed to pregnant women.

Active metabolites and active substance are excreted in breast milk, so breastfeeding should be stopped.

Instructions for use

The instructions for use indicate that Brilinta are taken orally, regardless of the meal.

  1. The use of the drug should begin with a single loading dose of 180 mg (2 tab. 90 mg) and then continue taking 90 mg 2 times / day.
  2. At the same time, in the absence of specific contraindications, acetylsalicylic acid is prescribed (from 75 mg to 150 mg with a constant intake) daily.
  3. For patients with difficulty swallowing a pill (or 2 tablets - in the case of receiving a loading dose) should be crushed to the state of fine powder, mix into 1/2 cup of drinking water and immediately drink the resulting suspension. Mix the rest with an additional 1/2 cup of drinking water and drink the resulting suspension. A suspension can also be administered via a nasogastric tube (CH8 or larger). After the introduction of the suspension, it is necessary to wash the nasogastric tube with water so that the dose of the drug is completely in the stomach of the patient.
  4. Breaks in therapy should be avoided. In case of missing a dose of Brilint, the patient should take only one 90 mg tablet (next dose) at the scheduled time.

If necessary, patients taking clopidogrel, can be transferred to the drug Brilint. It is recommended to conduct Brillint therapy 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 is limited. In patients with acute coronary syndrome, early cancellation of any antiplatelet therapy, including Brilint, may increase the risk of cardiovascular death or myocardial infarction as a result of the underlying disease. Avoid premature discontinuation of the drug.

Side effects

  1. Musculoskeletal system: hemarthrosis;
  2. Exchange processes: hyperuricemia;
  3. Sense organs: intraocular, retinal and conjunctival hemorrhages, vertigo, ear hemorrhages;
  4. Nervous system: headaches, paresthesias, intracranial hemorrhage, dizziness, confusion;
  5. Respiratory system: hemoptysis, shortness of breath, nosebleed;
  6. Skin lesions: rash, hemorrhage, itching, bruising;
  7. Urinary system: bleeding from the urinary tract;
  8. The digestive system: gastritis, constipation or diarrhea, nausea or vomiting, abdominal pain, dyspepsia, bleeding;
  9. The results of laboratory studies: an increase in the level of creatinine in the blood;
  10. Reproductive system: metrorrhagia, vaginal bleeding.

Overdose

Symptoms: In a single study with an increase in dose, the adverse effect on the gastrointestinal tract was dose-limiting. Other clinically significant adverse events that may have occurred during an overdose were dyspnea and ventricular pauses. In case of overdose, it is recommended to monitor for these undesirable effects and monitor the ECG.

  • Treatment: Brilinta is not eliminated during hemodialysis, the antidote is not known.

In case of overdose, symptomatic therapy should be carried out in accordance with local standards. In connection with the inhibition of platelets, an increase in the duration of bleeding is the intended pharmacological action of Brilint's overdose, therefore, with the development of bleeding, it is necessary to carry out appropriate supportive measures.

Special instructions

  1. Before starting treatment with Brilinta, a thorough assessment of the balance between the benefits of preventing atherothrombotic events and the possible threat of bleeding is required.
  2. Dyspnea that occurs during treatment is usually mild or moderate and takes place during therapy.
  3. The use of recombinant activated factor VIIa and / or antifibrinolytic treatment (aminocaproic or tranexamic acid) can lead to increased hemostasis. After determining the cause of bleeding and its relief, it is possible to resume taking Brilints.
  4. There is no data confirming the hemostatic efficacy of platelet transfusions during the use of ticagrelor. Brilinta is able to inhibit transfused platelets in the blood.
  5. During CABG, the incidence of major bleeding during the use of ticagrelor was the same as when taking clopidogrel all the days after cessation of therapy, except for the first day, when the likelihood of major bleeding was higher with Brilints.
  6. Before the start of a planned surgery or the use of new drugs, the attending physician should be informed about ticagrelor therapy. If surgical intervention is prescribed in which the antithrombotic effect is not desirable, taking Brilinta should be canceled 7 days before the operation.
  7. During treatment with Brilinto, an increase in the level of creatinine is possible, and therefore it is recommended to use the drug with particular caution (evaluating renal function) with concomitant treatment with angiotensin receptor antagonists.

Drug interactions

When taking the drug should consider the following drug interactions:

  • powerful inducers of CYP3A4 (phenobarbital, carbamazepine, phenytoin, dexamethasone, rifampicin) - reducing the effectiveness and exposure of the drug;
  • powerful inhibitors of CYP3A4 (atazanavir, ritonavir, nefazodone, clarithromycin, ketoconazole) - a significant increase in the exposure of ticagrelor;
  • moderate CYP3A4 inhibitors — 69% increase in Cmaxtiagrelore, a 2.7 times AUC, while the active metabolite decreases by 38% Cmax;
  • lovastatin together with simvastatin more than 40 mg - an increase in the AUC of atorvastatinic acid metabolites and Cmax, respectively, by 36%;
  • simvastatin at a dose of more than 40 mg / day s - the occurrence of side effects of simvastatin, it is recommended to evaluate the feasibility before use;
  • ethinyl estradiol and levonorgestrel - a 20% increase in the exposure to ethinyl estradiol;
  • cisapride, ergot alkaloids - increasing their exposure.

Reviews

We picked up some feedback from people about Brilint:

  1. Sergei. Grandfather made jokes and prescribed to drink Brillint. We, of course, despite the price, immediately agreed, if we must then find the money. Although it is not clear how much to drink it and how much it will fly to us, but the fact itself! When Yeltsin was doing shunting, the whole country stood on his ears for almost a month. And then the grandfather with a heart attack immediately on the table, bypass. And now these pills along with ascorbic (!), So that there are no blood clots. Grandfather, of course, a real colonel, hardening, training and other physical training there, but still. What medicine has come to! When the doctor wrote out the prescription, he warned, of course, that the treatment would be long. But I say the same fact! The fact that a heart attack is like this is famously once - and they have stopped and are now being treated - no money is worth it.
  2. Misha Of course, prices are deadly for retirees, but who cares? Now everyone lives on his level and sees only his own problems.

Analogs

Analogs of Brilint tablets regarding therapeutic action are Clopidogrel, Aspigrel. Acetylsalicylic acid-based drugs that are used in cardiology as antiplatelet agents - Cardiomagnyl, Aspecard, Aspirin-Cardio have a similar effect, but an excellent mechanism of action.

Before using analogues consult your doctor.

Storage conditions and shelf life

The shelf life of the drug is 2 years, it is recommended to be stored in a dry, warm place at 30 degrees in a place protected from children.

Watch the video: ESC: Short DAPT with Ticagrelor Doesn't Improve Outcomes - Medpage Today (November 2019).

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