BRILLINTA PILLS 90MG

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BRILLINTA PILLS 90MG - 168 TABS

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Adverse Effects

According to the PLATO study, the most frequent adverse reactions reported in patients receiving ticagrelor were shortness of breath, bruises and nosebleeds.

Undesirable reactions are classified according to the frequency of development and the class of the organ system. The frequency of undesirable reactions is determined using the following conventions: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 (10,000, <1/1000).

Undesirable drug reactions in terms of developmental frequency and organ system class

Metabolism

Hyperuricemiaa

The nervous system

Intracranial Hemorrhageb
Headache
Dizziness

Paresthesia
Confusion

On the part of the organ of vision

Hemorrhages (intraocular, conjunctival, retinal)

The organ of hearing

Ear hemorrhage
Vertigo

On the part of the respiratory system

Dyspneac
Nasal
bleeding

Hemoptysis

From the digestive system

Gastrointestinal bleedingd

Vomiting of blood, bleeding from ulcers in the digestive tracte
Hemorrhoidal bleeding
Gastritis
Bleeding in the oral cavity (including gingival bleeding)
Vomiting
Diarrhea
Abdominal pain
Nausea
dyspepsia

Retroperitoneal bleeding
Constipation

Skin and Subcutaneous Tissues

Subcutaneous or dermal
hemorrhagesf
Bruisesg

Rash, itching

From the musculoskeletal system

Hemarthrosis#

On the part of the urinary system

Urinary tract bleedingh

From the reproductive system

Vaginal bleeding (including metrorrhagia)

Deviations of laboratory results

Increased creatinine levels

Other

Bleeding at the treatment sitei

Bleeding after the procedure

Bleeding from a wound, traumatic bleeding

a hyperuricemia, an increase in the concentration of uric acid in the blood (see the section "Deviations of Laboratory Results" below);

cerebral hemorrhage, intracranial hemorrhage, hemorrhagic stroke;

with shortness of breath, dyspnea on exertion, dyspnea at rest, night dyspnea;

dGastrointestinal bleeding, rectal bleeding, intestinal bleeding, melena, positive test for occult blood;

e bleeding from gastrointestinal ulcer, bleeding from gastric ulcer, bleeding from duodenal ulcer, bleeding from peptic ulcer;

f subcutaneous hematoma, skin and subcutaneous hemorrhages, petechiae;

contusion, hematoma, ecchymosis, increased tendency to bruises, traumatic hematoma;

hematuria, bleeding from the urinary tract;

bleeding from the puncture site of the vessel, hematoma at the puncture site of the vessel, bleeding from the injection site, bleeding from the puncture site, bleeding from the place of catheterization;

# in patients taking ticagrelor in the PLATO study (n = 9235), no cases of hemarthrosis were noted.The frequency of hemarthrosis was calculated using the upper limit of 95% CI for the expected frequency (according to the formula 3 / X, where X is the number of patients receiving ticagrelor, ie 9235). The estimated frequency of hemarthrosis is 3/9235, which corresponds to the frequency of "rare".

Description of some undesirable reactions

Bleeding

The following definitions of bleeding were used in the PLATO study:

— Major fatal / life threatening bleeding: lethal, or intracranial hemorrhage, or bleeding into the pericardial cavity with cardiac tamponade; or hypovolemic shock or severe hypotension caused by bleeding and requiring the use of vasoconstrictors or surgery, or clinically overt bleeding, accompanied by a decrease in hemoglobin level of more than 50 g / l, or requiring transfusion of 4 or more units of whole blood or red blood cells.

- Large other bleeding: causing significant incapacity of the patient (for example, intraocular hemorrhage with irreversible loss of vision), or clinically obvious bleeding, accompanied by a decrease in hemoglobin level by 30-50 g / l, or requiring a transfusion of 2-3 units of whole blood or erythrocytes.

- Minor bleeding: requires medical intervention to stop or treat bleeding (for example, nosebleeds that require a hospital visit for a tamponade of the nose).

Brilinta® and clopidogrel did not differ in the incidence of major bleeding as a whole according to the PLATO criteria (11.6% / year and 11.2% / year, respectively), fatal / life-threatening bleeding according to the PLATO criteria (5.8% / year in both groups).However, the frequency of the combination of large and small bleeding according to the PLATO criteria was higher in the ticagrelor group (16.1%) compared with clopidogrel (14.6%, p = 0.0084).

Age, gender, body weight, race, geographical region, comorbidities, concomitant therapy, history, including previous stroke and transient ischemic attack, did not affect the incidence of major bleeding in general and not associated with the procedures according to the PLATO criteria. No groups with an increased risk of bleeding have been identified.

Bleeding associated with CABG. In the PLATO study, 42% of 1584 patients (12% of the cohort) undergoing CABG developed large lethal / life-threatening bleeding without significant differences in both treatment groups. Lethal bleeding associated with CABG was observed in 6 patients in each treatment group.

Bleeding that is not associated with CABG and bleeding that is not associated with procedures. Brilinta® and clopidogrel did not differ in the frequency of cases of major fatal / life-threatening bleeding that was not associated with CABG by the criteria of PLATO, but with Brillinta® major bleeding was more common as a whole according to the definition of the PLATO study (4.5% / year compared to 3.8% / year; p = 0.0264). If you remove the cases of development of bleeding associated with CABG, more bleeding was observed in the ticagrelor group (3.1% / year) than in the clopidogrel group (2.3% / year; p = 0.0058). Termination of treatment due to non-procedure-related bleeding was more frequent with ticagrelor (2.9%) compared with clopidogrel (1.2%, p <0.001).

Intracranial hemorrhage. In the ticagrelor group, more intracranial bleeding was not associated with the procedures (n = 27 bleeding in 26 patients, 0.3%) than in the clopidogrel group (n = 14 bleeding, 0.2%), of which 11 bleeding on ticagrelor and 1 clopidogrel were fatal. However, there were no significant differences in the total number of fatal bleeding.

Dyspnea

Adverse events in the form of dyspnea (dyspnea, dyspnea at rest, dyspnea on exertion, paroxysmal night dyspnea and dyspnea in combination) developed in 13.8% of patients who received Brillinta®, and in 7.8% of patients taking clopidogrel. The researchers found that in 2.2% of patients in the ticagrelor group, shortness of breath was associated with therapy. Most cases of dyspnea were mild or moderate in intensity and were single episodes immediately after the start of therapy.

Approximately 30% of all cases of dyspnea resolved within 7 days. More often, dyspnea developed in elderly patients, in patients with congestive heart failure, COPD or bronchial asthma at the beginning of the study. 0.9% of patients stopped taking Brillinta® due to shortness of breath. Dyspnea was not associated with the development of a new or worsening existing heart or lung disease.

Brilin's preparation® does not affect the performance of respiratory function.

Deviations of laboratory results

Serum creatinine concentration increased by more than 30% in 25.5% of patients and more than 50% in 8.3% of patients receiving Brillinta®. More than 50% increase in creatinine was more common in patients older than 75 years, in patients with severe renal failure when enrolled in the study, and in patients receiving angiotensin receptor antagonist therapy. The total number of renal adverse events was 4.9% in patients on ticagrelor, but the researchers attributed them to taking the drug in 0.6% of cases.

The serum uric acid concentration increased above VGN in 22% of patients receiving Brillinta®. Adverse events associated with hyperuricemia were reported in 0.5% of cases on ticagrelor, of which researchers attributed to ticagrelor 0.05% of cases. Gouty arthritis was observed in 0.2% of patients receiving ticagrelor, none of these cases was regarded by the researcher as being related to taking the drug.

Post-marketing application

Below are the adverse reactions that have been noted during post-marketing use of Brilint's drug.®. Since messages are received spontaneously from a population of an unspecified size, it is not always possible to reliably estimate the frequency of development.

On the part of the immune system: hypersensitivity reactions, including angioedema.

Contraindications

- active pathological bleeding;

- history of intracranial hemorrhage;

- moderate or severe liver failure;

- combined use of ticagrelor with powerful inhibitors of CYP3A4 (for example, KetoconazoleClarithromycin, nefazodone, ritonavir and atazanavir);

- children's and teenage age up to 18 years (due to the lack of data on the efficacy and safety of use in this group of patients);

- hypersensitivity to the drug.

WITH caution the drug should be used in patients with a predisposition to the development of bleeding (for example, in connection with a recent injury, a recent operation, bleeding disorders, active or recent gastrointestinal bleeding); in patients with concomitant therapy with drugs that increase the risk of bleeding (ie, NSAIDs, oral anticoagulants and / or fibrinolytics) for 24 hours before taking Brillinta®; in patients with an increased risk of developing bradycardia (for example, patients with SSS without a pacemaker, with AV block II or III; fainting associated with bradycardia) due to insufficient experience with the clinical use of Brillinta®; together with drugs that cause bradycardia; in patients with bronchial asthma and COPD (if the patient reports a new episode of dyspnea, prolonged dyspnea or worsening dyspnea, an examination should be conducted, and in case of intolerance, treatment with ticagrelor should be stopped).

Against the background of the use of the drug Brillinta® an increase in serum creatinine is possible, therefore it is necessary to evaluate the renal function in accordance with routine clinical practice,paying particular attention to patients aged 75 and older, patients with moderate to severe renal insufficiency, patients receiving therapy with angiotensin receptor antagonists.

Caution is needed in patients with a history of hyperuricemia or gouty arthritis. As a preventive measure, the use of ticagrelor in patients with hyperuricemic nephropathy should be avoided.

The combined use of ticagrelor and acetylsalicylic acid in a high maintenance dose (more than 300 mg) is not recommended.

With the combined use of Digoxin and Brillinta drug® Recommended careful clinical and laboratory monitoring (heart rate, in the presence of clinical indications also ECG and concentration of digoxin in the blood).

There are no data on the joint use of ticagrelor with powerful inhibitors of glycoprotein P (for example, Verapamil and quinidine), so simultaneous therapy with these drugs should be carried out with caution.

Use during pregnancy and lactation

Data on the use of the drug Brillinta® pregnant women are absent or limited. Brilin's preparation® not recommended for use during pregnancy.

Since the risk for a newborn / infant cannot be ruled out, Brillinta is not recommended.® during breastfeeding.

AT experimental studies In animals, ticagrelor caused a slight decrease in the weight gain of the mother, a decrease in the viability of the newborn and its body weight, and a slowdown in growth.Available pharmacodynamic, toxicological data in animals have shown that ticagrelor and its active metabolites are excreted in breast milk.

Application for violations of the liver

For patients with hepatic impairment mild dose adjustment is not required. No studies have been conducted on Brillinta® at patients with moderate or severe hepatic impairmenttherefore, use in this category of patients is contraindicated.

Application for violations of kidney function

Patients with renal failure no dose adjustment required. No information on the use of the drug Brillinta® at hemodialysis patientstherefore, its use in these patients is not indicated.

Use in children

Safety and efficacy of Brillinta® at children and teenagers under 18 years old according to the testimony approved in adults not established.

Use in elderly patients

Elderly patients dose adjustment is not required. Against the background of the use of the drug Brillinta® An increase in serum creatinine levels is possible, and therefore it is necessary to evaluate renal function in accordance with routine clinical practice, paying particular attention to patients aged 75 years and older.

special instructions

Risk of bleeding

In patients with acute coronary syndrome who received Brillint therapy® and acetylsalicylic acid,There was an increased risk of non-CABG-related major bleeding and bleeding that required increased medical attention, such as major + small bleeding, as defined by PLATO, but did not increase the risk of fatal / life-threatening bleeding.

When prescribing Brillinta® the ratio of the benefits of prophylaxis of atherothrombotic events and risk in patients with an increased likelihood of bleeding should be evaluated.

In the presence of clinical evidence of the drug Brillinta® should be used with caution in the following groups of patients:

- predisposition of patients to the development of bleeding (for example, in connection with a recent injury, a recent operation, bleeding disorders, active or recent bleeding from the gastrointestinal tract). Use of Brillinta® contraindicated in patients with active pathological bleeding, intracranial hemorrhage in history, moderate or severe liver failure;

- concomitant use of drugs that may increase the risk of bleeding (for example, NSAIDs, oral anticoagulants and / or fibrinolytics taken 24 hours before taking Brillinta®).

There are no data on the hemostatic efficacy of platelet transfusions with Brillinta.®; Brilinta® can inhibit transfused platelets in the blood. Since with the concomitant use of the drug Brillinta® and desmopressin did not decrease standardized bleeding time, it is unlikely that desmopressin will effectively stop bleeding.

Antifibrinolytic therapy (aminocaproic acid or tranexamic acid) and / or recombinant factor Vlla may enhance hemostasis. After determining the cause of the bleeding and its relief, you can resume therapy with Brillinta®.

Surgery

Before a planned operation or the start of taking new drugs, the patient should inform the doctor about taking Brillint's drug.®. In patients undergoing CABG, the incidence of major bleeding with Brillinta® was the same as when clopidogrel was used on all days after discontinuation of therapy, except for day 1, when the incidence of large bleeding was higher when Brillinta was taken®.

If the patient undergoes a planned operation and the antithrombotic effect is not desirable, then Brillint therapy® should stop 7 days before surgery.

Patients at risk for bradycardia

In connection with the discovery in the earlier clinical study, mainly asymptomatic pauses, patients with an increased risk of developing bradycardia (for example, patients without a pacemaker who have been diagnosed with SSS, AV-blockade of the heart of the second or third degree; syncope associated with bradycardia) did not were included in the main study to assess the safety and efficacy of Brillinta®. Therefore, due to the limited clinical experience of using the drug in these patients, it is recommended that Brillinta be prescribed with caution.® to such patients.

Extra caution is needed when Brillinta use the drug together.® with drugs that can cause bradycardia. However, there were no clinically significant side effects when combined with one or more drugs that can cause bradycardia (for example, 96% beta-blockers, 33% Calcium channel blockers, including diltiazem and verapamil, and 4% digoxin).

In the course of the sub-study using daily ECG Holter monitoring in the ticagrelor group compared with clopidogrel, more patients in the acute phase of acute coronary syndrome (ACS) had ventricular pauses> 3 seconds. The increase in the number of ventricular pauses recorded by daily monitoring of Holter, while receiving ticagrelor was observed more often in patients with chronic heart failure compared with the general population in the acute phase of ACS, but not in the first month. The pauses in these patients were not accompanied by subsequent undesirable clinical consequences (fainting and installation of a pacemaker).

Dyspnea

Shortness of breath when using Brillinta® usually mild or moderate in intensity, often disappearing as therapy continues. Patients with asthma / COPD may have an increased absolute risk of shortness of breath when taking Brillinta®. In patients with asthma / COPD, ticagrelor should be used with caution. The mechanism of dyspnea when taking ticagrelor is not clear. If a patient has developed a new episode of dyspnea, dyspnea persists or is worse during the use of Brillinta®then it is necessary to conduct a full examination, and in case of intolerance, the drug should be stopped.

Creatinine increase

When taking the drug Brillinta® creatinine levels may increase. The mechanism of this effect is not known. Assessment of renal function should be made one month after the start of the drug, and subsequently in accordance with routine clinical practice, paying particular attention to patients aged 75 years and older, patients with moderate or severe renal failure and receiving angiotensin receptor antagonists.

Increased uric acid levels

Patients receiving ticagrelor have a higher risk of hyperuricemia than taking clopidogrel. Care must be taken in patients with a history of hyperuricemia or gouty arthritis. As a preventive measure, the use of ticagrelor in patients with hyperuricemic nephropathy should be avoided.

Other indications

Based on the observed interaction between acetylsalicylic acid at a maintenance dose and the effectiveness of ticagrelor compared to clopidogrel, the combined use of acetylsalicylic acid at a high maintenance dose (more than 300 mg) and Brillinta® Not recommended.

Combined use of Brillinta® with powerful inhibitors of CYP3A4 (for example, ketoconazole, clarithromycin, nefazodone, ritonavir, and atazanavir) is contraindicated because it can lead to a significant increase in ticagrelor exposure.

Combined use of Brillinta® with powerful inducers of CYP3A4 (for example, rifampicin, phenytoin, Carbamazepine and phenobarbital) is not recommended, because taking them together can reduce the exposure and effectiveness of ticagrelor.

Combined use of Brillinta® and substrates of CYP3A4 with a narrow therapeutic index (for example, cisapride and ergot alkaloids) are not recommended, since ticagrelor may increase the exposure of these drugs. Combined use of Brillinta® with Simvastatin or lovastatin at a dose of more than 40 mg is not recommended.

With the combined use of digoxin and Brillinta drug® Recommended careful clinical and laboratory monitoring (heart rate, and in the presence of clinical indications also ECG and concentration of digoxin in the blood).

There are no data on the combined use of ticagrelor with potent glycoprotein P inhibitors (for example, verapamil and quinidine), which can increase the exposure of ticagrelor. If this combination cannot be avoided, treatment should be carried out with caution.

Influence on ability to drive motor transport and control mechanisms

No research has been conducted on the effect of Brillinta® on the ability to drive vehicles and control mechanisms. Brilinta® does not affect or slightly affects the ability to drive vehicles and machinery. During the treatment of acute coronary syndrome, dizziness and confusion have been reported. In the case of the development of these phenomena, patients should be careful when driving and other mechanisms.

Effects of other drugs on Brillinta®

Drugs metabolized by CYP3A4 isoenzyme

Inhibitors of CYP3A4. Potent inhibitors of CYP3A4: combined use of ketoconazole with ticagrelor increases Cmax and AUC of ticagrelor 2.4 and 7.3 times, respectively. WITHmax and the AUC of the active metabolite are reduced by 89% and 56%, respectively.Other potent inhibitors of CYP3A4 (clarithromycin, nefazodone, ritonavir, and atazanavir) will have the same effects, so their combined use with Brillinta® contraindicated.

Moderate CYP3A4 inhibitors: co-administration of diltiazem with ticagrelor increases Cmax ticagrelor by 69%, a AUC 2.7 times, while reducing Cmax active metabolite by 38%, a AUC does not change. Ticagrelor does not affect diltiazem plasma concentrations. Other moderate inhibitors of CYP3A4 (for example, amprenavir, aprepitant, Erythromycin, fluconazole) can be administered simultaneously with Brillinta®.

Cyclosporine (an inhibitor of P-gp and CYP3A4). The combined use of cyclosporine (at a dose of 600 mg) with ticagrelor increases Cmax and AUC of ticagrelor 2.3 and 2.8 times respectively. At the same time, there is an increase in the AUC of the active metabolite by 32% and a decrease in Cmax by 15%. Ticagrelor does not affect the plasma concentration of cyclosporine.

Inductors CYP3A4. The combined use of rifampicin with ticagrelor reduces Cmax and AUC of ticagrelor by 73% and 86%, respectively. WITHmax active metabolite does not change, a AUC decreases by 46%. Other inducers of CYP3A4 (for example, phenytoin, carbamazepine, and phenobarbital) are likely to decrease the exposure of Brillinta®. Powerful inducers of CYP3A4 can reduce the exposure and effectiveness of Brilint's drug®.<

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