Concor, pills 5mg 50pcs

Composition

1 film-coated tablet,5 mg contains: Nuclear Active ingredient: Bisoprolol fumarate 2: 1 (bisoprolol hemifumarate) – 5 mgsupport substances: colloidal anhydrous silicon dioxide, magnesium stearate, crospovidone, microcrystalline cellulose, corn starch, anhydrous calcium hydrophosphate. Shell: Dye iron oxide yellow (E 172), dimethicone 100, macrogol 400, titanium dioxide (E 171), hypromellose 2910/15.

Pharmacological action

Beta-1-adrenoblocker selective

ATX code:  C 07 AB 07

Pharmacotherapeutic properties

Pharmacodynamics

Selective beta-1-adrenoblocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. Reduces the activity of blood plasma renin, reduces the need for myocardial oxygen, reduces the heart rate (HR) (at rest and during exercise). It has antihypertensive, antiarrhythmic and antianginal effects.

Blocking the beta – 1-adrenergic receptors of the heart in low doses, it reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular flow of calcium ions, and has a negative chrono -, dromo -, batmo-and inotropic effect (inhibits conduction and excitability, slows down atrioventricular conduction).

When the dose is increased above the therapeutic dose, it has a beta-2-adrenoblocking effect.

The total peripheral vascular resistance at the beginning of the drug use, in the first 24 hours, slightly increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors), which returns to the initial value after 1-3 days, and decreases with prolonged use.

The hypotensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (which is of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure (BP), and an effect on the central nervous system (CNS). With arterial hypertension, the effect occurs in 2-5 days, stable effect – in 1-2 months.

The antianginal effect is due to a decrease in the myocardial oxygen demand as a result of a decrease in heart rate, a slight decrease in contractility, an elongation of the diastole, and an improvement in myocardial perfusion. The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and a slowdown in atrioventricular (AV) conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular node) and along additional pathways.

When used in medium therapeutic doses, unlike non-selective beta-blockers, it has a less pronounced effect on the organs containing beta-2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause sodium (Na+) ion retention in the body.

Pharmacokinetics

Suction.

Bisoprolol is almost completely (>90%) absorbed from the gastrointestinal tract. Its bioavailability due to insignificant metabolism “at the first pass” through the liver (at the level of approximately 10% -15%) is approximately 85-90% after oral use. Food intake does not affect bioavailability. Bisoprolol exhibits linear kinetics, and its plasma concentrations are proportional to the administered dose in the dose range from 5 to 20 mg. The maximum concentration in the blood plasma is reached in 2-3 hours.

Distribution.

Bisoprolol is distributed fairly widely. The volume of distribution is 3.5 l / kg. Binding to plasma proteins reaches approximately 35%; uptake by blood cells is not observed.

Metabolism.

It is metabolized by the oxidative pathway without subsequent conjugation. All metabolites have a strong polarity and are excreted by the kidneys. The main metabolites found in blood plasma and urine do not show pharmacological activity. Data obtained from experiments with human liver microsomes in vitro show that bisoprolol is primarily metabolized by CYP3A4 (about 95%), and CYP2D6 plays only a small role.

Output.

The clearance of bisoprolol is determined by the balance between its excretion through the kidneys as an unchanged substance (about 50%) and oxidation in the liver (about 50%) to metabolites, which are then also excreted by the kidneys. The total clearance is 15.6 ± 3.2 l / h, and the renal clearance is 9.6±1.6 l / h. The elimination half-life is 10-12 hours.

Indications

Use during pregnancy and lactation

During pregnancy, Concor® should only be recommended if the benefit to the mother outweighs the risk of side effects in the fetus. As a rule, beta-blockers reduce blood flow in the placenta and can affect the development of the fetus. Blood flow in the placenta and uterus should be closely monitored, as well as the growth and development of the unborn child, and in case of dangerous manifestations in relation to pregnancy or the fetus, alternative therapeutic measures should be taken. The newborn should be carefully examined after delivery. In the first three days of life, symptoms of a decrease in blood glucose and heart rate may occur. There are no data on the excretion of bisoprolol in breast milk or the safety of exposure to bisoprolol in infants. Therefore, Concor is not recommended for women who are breast-feeding.

Contraindications

Concor®preparation it should not be used to treat patients with the following conditions:

With caution: hepatic insufficiency, chronic renal failure, Prinzmetal angina pectoris; myasthenia gravis, thyrotoxicosis, diabetes mellitus, atrioventricular block I degree, depression (including in the anamnesis), psoriasis, elderly age.

Side effects

The frequency of adverse reactions listed below was determined according to the following: – very common: ≥1/10; – common: >1/100. ><1/10; – infrequent: >1/1000. <1/10; – infrequent: ><1/100: – rare: >1/10 LLC. <1/1000: – very rare: including individual messages. The cardiovascular system is very common: decreased heart rate (bradycardia, especially in patients with chronic heart failure); Often: hypotension (especially in patients with chronic heart failure), angiospasm (increased peripheral circulatory disorders. sensation of cold in the extremities (paresthesia); Infrequently: violation of atrioventricular conduction, orthostatic hypotension, decompensation of heart failure with the development of peripheral edema. Nervous system At the beginning of the course of treatment, disorders of the central nervous system may temporarily appear, infrequently: dizziness, headache, asthenia, increased fatigue, sleep disorders, as well as mental disorders (infrequently-depression, rare hallucinations, nightmares, convulsions). Usually, these symptoms are mild and disappear, usually within 1-2 weeks after the start of treatment. Organs of vision Rare: visual impairment, reduced tear production (should be considered when wearing contact lenses): very rare: conjunctivitis. Respiratory systemarea: allergic rhinitis. Infrequently: bronchospasm in patients with bronchial asthma or obstructive airway diseases. Gastrointestinal tract Infrequently: nausea, vomiting, diarrhea, constipation, dryness of the oral mucosa; rarely: hepatitis. Musculoskeletal system Often: muscle weakness, cramps in the calf muscles, arthralgia. Allergic reactionsreferences: hypersensitivity reactions, such as itching of the skin, redness of the skin, sweating, rash. Very rare: allopecia. Beta-blockers can exacerbate the course of psoriasis. Urogenital system is very rare: disorders of potency. Laboratory indicators Redko: increased levels of liver enzymes in the blood (ACT, ALT), increased levels of triglycerides in the blood. In some cases: thrombocytopenia, agranulocytosis.

Interaction

The effectiveness and tolerability of medications may be affected by taking other medications at the same time. Such an interaction can also occur in cases where two drugs are taken after a short period of time. You should inform your doctor that you are taking other medications, even if you are taking them without a prescription.Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol. Iodine-containing radiopaque diagnostic agents for intravenous use increase the risk of developing anaphylactic reactions. Phenytoin with intravenous use, drugs for inhaled general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of lowering blood pressure. The effectiveness of insulin and oral hypoglycemic drugs may change during treatment with bisoprolol (masks the symptoms of developing hypoglycemia: tachycardia, increased blood pressure). Clearance of lidocaine and xanthines (except diphylline) may decrease due to a possible increase in their concentration in blood plasma, especially in patients with an initially increased clearance of theophylline under the influence of smoking. Nonsteroidal anti-inflammatory drugs, glucocorticosteroids and estrogens weaken the hypotensive effect of bisoprolol (Na + retention, blockade of prostaglandin synthesis by the kidneys). Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), amiodarone and other antiarrhythmic agents increase the risk of developing or worsening bradycardia, atrioventricular block, cardiac arrest and heart failure. Nifedipine can lead to a significant decrease in blood pressure. Diuretics, clonidine, sympatholytics, hydralazine, and other antihypertensive drugs can lead to an excessive decrease in blood pressure. The effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins may be prolonged during treatment with bisoprolol. Tri-and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and sleeping pills increase CNS depression. Concomitant use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect. A break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days. Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders. Ergotamine increases the risk of developing peripheral circulatory disorders; sulfasalazine increases the concentration of bisoprolol in blood plasma; rifampicin shortens the half-life.

How to take, course of use and dosage

Tablets should be taken with a small amount of liquid in the morning before breakfast, during or after it. Tablets should not be chewed or ground into powder. Treatment of arterial hypertension and angina pectorisin all cases, the mode of use and dosage is selected by the doctor for each patient individually, in particular, taking into account the patient’s heart rate and condition. Usually, the initial dose is 5 mg (1 tablet of Concor® 5 mg) once a day. If necessary, the dosage can be increased to 10 mg once a day. In the treatment of arterial hypertension and angina pectoris, the maximum recommended dose is 20 mg Concor® once a day. Treatment of chronic heart failure. Initiation of treatment of chronic heart failure with Concor® requires a special titration phase and regular medical monitoring. The prerequisites for Concor® treatment are as follows:

• chronic heart failure without signs of exacerbation in the previous six weeks,
• almost unchanged basic therapy in the previous two weeks,
• treatment with optimal doses of ACE inhibitors (or other vasodilators in case of intolerance to ACE inhibitors), diuretics and, optionally, cardiac glycosides.

Treatment of chronic heart failure with Concor® begins according to the following titration schedule. However, individual adjustment may be required depending on how well the patient tolerates the prescribed dose, i. e. the dose can only be increased if the previous dose was well tolerated.

* To ensure the above dosage regimen, Concor® is recommended for subsequent stages of treatment. The maximum recommended dose for the treatment of chronic heart failure is 10 mg Concor®once a day. Patients are recommended to take the dose of the drug selected by the doctor, if no adverse reactions occur. After starting treatment with the drug at a dose of 1.25 mg (1/2 tablet of Concor KOR), the patient should be monitored for about 4 hours (heart rate control, blood pressure, conduction disturbances, signs of worsening heart failure). During or after the titration phase, there may be a temporary worsening of heart failure, fluid retention, hypotension, or bradycardia. In this case, it is recommended, first of all, to pay attention to the selection of the dosage of concomitant basic therapy (optimize the dose of a diuretic and/or ACE inhibitor) before reducing the dosage of Concor®. Concor® treatment should only be interrupted if absolutely necessary. After stabilization of the patient’s condition, repeat titration should be performed, or continue treatment. Duration of treatment for all indications. Concor® treatment is usually a long-term therapy. If necessary, treatment can be interrupted and resumed in compliance with certain rules. Treatment should not be interrupted abruptly, especially in patients with coronary artery disease. If it is necessary to stop treatment, then the dosage of the drug should be reduced gradually. Special patient groups Impaired renal or hepatic function:Treatment of arterial hypertension or angina pectoris:

• Mild or moderate hepatic or renal impairment usually does not require dose adjustment.
• In patients with severe renal impairment (creatinine clearance less than 20 ml / min) and in patients with severe liver disease, the maximum daily dose is 10 mg.

Elderly patients:No dose adjustment is required.

Description

Light yellow, heart-shaped, biconvex tablets, film-coated, with a risk on both sides.

Special instructions

Do not abruptly discontinue treatment and do not change the recommended dosage without first consulting your doctor, as this may lead to temporary deterioration of heart activity. Treatment should not be interrupted abruptly, especially in patients with coronary artery disease. If discontinuation of treatment is necessary, the dosage should be reduced gradually. Monitoring of the condition of patients taking Concor® should include measuring heart rate and blood pressure (at the beginning of treatment – daily, then 1 time in 3 – 4 months), ECG, blood glucose determination in patients with diabetes mellitus (1 time in 4-5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months). The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min. Before starting treatment, it is recommended to conduct a study of the function of external respiration in patients with a burdened bronchopulmonary history. Patients who use contact lenses should take into account that during treatment, there may be a decrease in the production of tear fluid. When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if an effective alpha-adrenoblockade is not previously achieved). In thyrotoxicosis, Concor® can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, since it can increase symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels. If clonidine is co-administered, it may be discontinued only a few days after Concor is discontinued. It is possible to increase the severity of the hypersensitivity reaction and the lack of effect from conventional doses of epinephrine against the background of a burdened allergic history. If elective surgical treatment is necessary, the drug should be discontinued 48 hours before general anesthesia. If the patient took the drug before surgery, he should choose a drug for general anesthesia with minimal negative inotropic effect.Reciprocal activation of the vagus nerve can be eliminated by intravenous use of atropine (1-2 mg). Medications that reduce the supply of catecholamines (including reserpine) can increase the effect of beta-blockers, so patients taking such combinations of medications should be constantly monitored by a doctor for a pronounced decrease in blood pressure or bradycardia. Patients with bronchospastic diseases can be prescribed cardioselective adrenoblockers in case of intolerance and / or ineffectiveness of other antihypertensive agents. If the dose of the drug is exceeded, there is a risk of developing bronchospasm. In case of increasing bradycardia (heart rate less than 50 beats/min), marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular block in elderly patients, it is necessary to reduce the dose or discontinue treatment. It is recommended to stop therapy if depression develops. Do not abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction. Discontinuation of the drug is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days). The drug should be discontinued before testing the content of catecholamines, normetanephrine and vanillinmindalic acid in the blood and urine; titers of antinuclear antibodies. Effect on the ability to drive a car and complex mechanismsi Bisoprolol does not affect the ability to drive a car in the study of patients suffering from coronary vascular diseases of the heart. However, due to individual reactions, the ability to drive a car or work with technically complex mechanisms may be impaired. This should be paid special attention at the beginning of treatment, after changing the dose, as well as when drinking alcohol at the same time.

Storage conditions

Store at a temperature not exceeding 30°C. Keep out of reach of children.

Shelf

life is 5 years. Do not use after the expiration date.

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets