Bisomor pills 5mg, 30pcs

Composition

Active ingredient: bisoprolol fumarate – 5 mg. Auxiliary substances: mannitol – 146.50 mg, microcrystalline cellulose-21.10 mg, croscarmellose sodium-1.80 mg, magnesium stearate-3.60 mg. Shell composition: Wincoat dye WT AQ 01069 (orange) – 3.6 mg. The composition of the dye Wincoat WT-AQ-01069 orange per 100 mg: hypromellose-61.00 mg, macrogol 400-9.50 mg, titanium dioxide-17.20 mg, talc – 4.77 mg, macrogol 6000 -6.02 mg, aluminum varnish sunny sunset yellow-1.51 mg

Pharmacological action

Pharmacotherapy group: Beta-1-adrenoblocker Selektivnyatx:  

C. 07. A. B Selective beta-1-blockers

C. 07. A. B. 07 Bisoprolol

Pharmacodynamics : Selective beta-1-adrenoblocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. Reduces the activity of renin in the blood plasma, reduces the need for oxygen in the myocardium, reduces the heart rate (HR). It has antihypertensive, antiarrhythmic and antianginal effects. Blocking the beta-1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular flow of calcium ions, and has a negative chrono -, dromo -, batmo – and inotropic effect (inhibits conduction and excitability, slows down atrioventricular (AV) conduction). When the dose is increased above the therapeutic dose, it has a beta-2-adrenoblocking effect. 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 alpha-adrenergic activity and elimination of beta-2-adrenergic stimulation), which returns to its original value after 1-3 days, and decreases with prolonged use. The antihypertensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, and a decrease in the activity of the sympathoadrenal system. (CAC) (of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure (BP) and effects 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 need for oxygen in the myocardium as a result of a decrease in contractility and other functions of the myocardium, an elongation of the diastole, and an improvement in myocardial perfusion. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the ventricular muscle fibers, the myocardial oxygen demand may increase, especially in patients with chronic heart failure (CHF). 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 AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the AV node) and along additional pathways. When used in medium therapeutic doses, in contrast to 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 ion retention in the body. Pharmacokinetics: Absorption Bisoprolol is almost completely (> 90%) absorbed from the gastrointestinal tract (GIT), food intake does not affect absorption. Bisoprolol shows linear kinetics, and its plasma concentrations are proportional to the administered dose in the range from 5 to 20 mg. Maximum bisoprolol concentration (Cmax) In the blood plasma is reached in 2-3 hours. Distributionthe volume of distribution (Vd) is 3.5 l/kg. The connection with plasma proteins is about 30%. Metabolismmetabolized via the oxidative pathway without subsequent conjugation; slightly metabolized during the “primary passage” through the liver (approximately 10-15%). All metabolites are polar. The main metabolites found in blood plasma and urine do not show pharmacological activity. Data obtained as a result of experiments with human liver microsomes in vitro show that bisoprolol is primarily metabolized with the participation of the CYP3A4 isoenzyme (about 95%), and the CYP2D6 isoenzyme plays only a small role. Excretionisoprolol is excreted in two ways,50% of the dose is metabolized in the liver with the formation of inactive metabolites. About 98% is excreted by the kidneys, of which 50% is unchanged, and less than 2% is excreted through the intestines (with bile). Total clearance is 12-18 l / h, with a renal clearance of 8-11 l/h, and a half – life (T 1/2) of 10-12 hours. Blood-brain and placental barrier permeability is low. The pharmacokinetics of bisoprolol are linear and independent of age. In patients with CHF, the plasma concentration of bisoprolol is higher, and T 1/2 is longer than in healthy volunteers.

Indications

-arterial hypertension;- coronary heart disease: prevention of stable angina attacks;- chronic heart failure (CHF).

Use during pregnancy and lactation

During pregnancy, the drug should be recommended for use only if the benefits of treatment for the mother outweigh the risk of side effects in the fetus and / or child. As a rule, beta-blockers reduce blood flow in the placenta and can affect the development of the fetus. It is necessary to monitor blood flow in the placenta and uterus, as well as monitor the growth and development of the unborn child, and in case of adverse events in relation to pregnancy and/or the fetus, switch to alternative methods of therapy. If beta-blockers are used during pregnancy, the newborn should be carefully examined after delivery. In the first three days of life, symptoms of bradycardia and hypoglycemia may occur. There are no data on the excretion of bisoprolol in breast milk. Therefore, taking Bisomor is not recommended during breast-feeding. If taking the drug during lactation is necessary; breastfeeding should be discontinued.

Contraindications

-hypersensitivity to bisoprolol or any of the components, as well as to other beta-blockers;- acute heart failure;- CHF in the stage of decompensation, requiring inotropic therapy;- cardiogenic shock; – collapse; – grade II and III AV block without pacemaker; – sinus node weakness syndrome; – sinoatrial block; – bradycardia (heart rate less than 60 beats / min);- severe arterial hypotension (systolic blood pressure less than 100 mm Hg); – a history of severe bronchial asthma and chronic obstructive pulmonary disease (COPD) ;- severe peripheral circulatory disorders, Raynaud’s syndrome; – pheochromocytoma (without simultaneous use of alpha-blockers);- metabolic acidosis;- cardiomegaly (no signs of heart failure);- simultaneous use of monoamine oxidase (MAO)inhibitors (with the exception of MAO type B inhibitors); – concomitant use of floctafenin and sultopride; – age up to 18 years (efficacy and safety have not been established). With caution: – bronchial asthma and COPD; – simultaneous desensitizing therapy;- Prinzmetal’s angina pectoris; – hyperthyroidism;- diabetes mellitus;- Grade I AV block; – severe renal insufficiency (creatinine clearance less than 20 ml / min);- severe liver function disorders;- psoriasis;- restrictive cardiomyopathy; – congenital heart defects or heart valve disease with severe hemodynamic disorders; – CHF with myocardial infarction in the last 3 months;- strict diet; – depression (including in the anamnesis).

Side effects

The frequency of adverse reactions listed below was determined according to the following classification: – very often ≥ 1/10; – often ≥1/100, <1/10; – infrequently ≥ 1/1000, <1/100; – rarely≥ 1/10 000, ;- very rarely From the cardiovascular system:

• Very common: bradycardia (in patients with CHF).
• Often: worsening of symptoms of the course of CHF (in patients with CHF), a feeling of coldness or numbness in the extremities, a marked decrease in blood pressure, especially in patients with CHF.
• Infrequently: violation of AV conduction; bradycardia (in patients with arterial hypertension or angina pectoris); worsening of symptoms of CHF (in patients with arterial hypertension or angina pectoris), orthostatic hypotension.

From the central nervous system:

• Often: dizziness, headache.
• Rare: loss of consciousness.

Mental disorders:

• Infrequently: depression, insomnia.
• Rare: hallucinations, nightmares.

From the side of the visual organ:

• Rarely: reduced lacrimation (should be considered when wearing contact lenses).
• Very rare: conjunctivitis.

Hearing disorders: Rare: hearing disorders. Respiratory system disorders:

• Infrequently: bronchospasm in patients with a history of bronchial asthma or airway obstruction.
• Rare: allergic rhinitis.

From the digestive system:

• Often: nausea, vomiting, diarrhea, constipation.
• Rare: hepatitis.

Musculoskeletal disorders: Infrequently: muscle weakness, muscle cramps. From the side of the skin:

• Rarely: hypersensitivity reactions, such as pruritus, rash, or hyperemia of the skin.
• Very rare: alopecia; beta-blockers may exacerbate the symptoms of psoriasis or cause a psoriasis-like rash.

From the side of the reproductive system: Rarely: violation of potency. General violations:

• Common: asthenia (in patients with CHF), increased fatigue.
• Infrequently: asthenia (in patients with arterial hypertension or angina pectoris).

Laboratory parameters: Rarely: increased triglyceride concentration and activity of “hepatic” transaminases in the blood (aspartate aminotransferase and alanine aminotransferase). In patients with hypertension or angina, these symptoms appear more often at the beginning of the course of treatment, are usually mild in nature and usually disappear within 1-2 weeks after the start of treatment.

Interaction

Treatment of CHF Class I antiarrhythmic agents (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone) when used concomitantly with bisoprolol may reduce AV conduction and myocardial contractility. For all indications, verapamil-type slow calcium channel blockers (BMCC) and, to a lesser extent, diltiazem, when used concomitantly with bisoprolol, can lead to a decrease in myocardial contractility and impaired AV conduction. In particular, intravenous use of verapamil to patients taking beta-blockers may lead to severe hypotension and AV block. Antihypertensive agents of central action (such as clonidine, methyldopa, moxonidine, rilmenidine) can lead to a decrease in heart rate and a decrease in cardiac output, as well as to vasodilation due to a decrease in central sympathetic tone. Abrupt withdrawal, especially before beta-blockers are discontinued, may increase the risk of developing “rebound” hypertension. Combinations that should be used with caution in arterial hypertension and stable angina pectoris. Class I antiarrhythmic agents (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone) may reduce AV conduction and myocardial contractility when used concomitantly with bisoprolol. Dihydropyridine derivatives (e. g., nifedipine, felodipine, amlodipine) may increase the risk of hypotension in all indications of BMCC. In patients with CHF, the risk of subsequent deterioration of myocardial contractility cannot be excluded. Class III antiarrhythmic agents (such as amiodarone) may increase the violation of AV conduction. Beta-blockers for topical use (for example, eye drops for the treatment of glaucoma) may increase the systemic effects of bisoprolol (lowering blood pressure, lowering heart rate). Parasympathomimetics when used concomitantly with bisoprolol may increase the violation of AV conduction and increase the risk of bradycardia. The hypoglycemic effect of insulin or oral hypoglycemic agents may be enhanced. Signs of hypoglycemia, such as tachycardia, may be masked or suppressed. Such interactions are more likely to occur with non-selective beta-blockers. General anaesthetic agents may increase the risk of cardiodepressive effects, leading to a marked decrease in blood pressure (see section “Special instructions”). Cardiac glycosides, when used concomitantly with bisoprolol, can lead to an extension of the pulse conduction time, and thus to the development of bradycardia. Nonsteroidal anti-inflammatory drugs (NSAIDs) may reduce the hypotensive effect of bisoprolol. Concomitant use of bisoprolol with beta-adrenomimetics (for example, isoprenaline, dobutamine) may lead to a decrease in the effect of both drugs. The combination of bisoprolol with adrenomimetics that affect beta-and alpha-adrenergic receptors (for example, norepinephrine, epinephrine) can increase the vasoconstrictor effects of these drugs that occur with the participation of alpha-adrenergic receptors, leading to an increase in blood pressure. Such interactions are more likely to occur with non-selective beta-blockers. Antihypertensive agents, as well as other agents with a possible antihypertensive effect (for example, tricyclic antidepressants, barbiturates, phenothiazines) may increase the antihypertensive effect of bisoprolol. Mefloquine, when co-administered with bisoprolol, may increase the risk of developing bradycardia. MAO inhibitors (with the exception of MAO B inhibitors) may enhance the antihypertensive effect of beta-blockers. Simultaneous use can also lead to the development of a hypertensive crisis.

How to take, course of use and dosage

Bisomor should be taken orally with a small amount of liquid in the morning before breakfast, during or after it. Tablets should not be chewed or ground into powder. In all cases, the dosage and use regimen is selected by the doctor for each patient individually, in particular, taking into account the patient’s heart rate and condition. Treatment of arterial hypertension and stable angina pectorisas a rule, the initial dose is 5 mg 1 time / day. If necessary, the dose can be increased to 10 mg 1 time/day. In the treatment of arterial hypertension and angina pectoris, the maximum recommended dose is 20 mg 1 time/day. Patients with mild or moderate hepatic or renal impairment, as well as elderly patients, usually do not need to adjust the dosage regimen. For patients with severe renal impairment (creatinine clearance less than 20 ml/min) and patients with severe hepatic impairment, the maximum daily dose is 10 mg. Chronic heart failure At the beginning of treatment of chronic heart failure requires a special titration phase and regular medical monitoring. A prerequisite for treatment with Bisomor is stable CHF without signs of exacerbation. Treatment of chronic heart failure begins in accordance with the following scheme, but individual adaptation 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. The recommended initial dose of Bisomor is 1.25 mg (1/2 tablet 2.5 mg) 1 time/day. Depending on individual tolerance, the dose should be gradually increased to 2.5 mg,3.75 mg (VA tablets of 2.5 mg),5 mg,7.5 mg (1 tablet of 5 mg, tablet of 2.5 mg) and 10 mg once a day at intervals of at least 2 weeks or more. The maximum recommended dose of Bisomor in the treatment of chronic heart failure is 10 mg 1 time / day. If an increase in the dose of the drug is poorly tolerated by the patient, it is possible to reduce the dose. During titration, regular monitoring of blood pressure, heart rate, and symptoms of increasing CHF is recommended. Worsening of the symptoms of CHF is possible from the first day of use of the drug. During or after the titration phase, there may be a temporary deterioration in the course of CHF, hypotension, or bradycardia. In this case, it is recommended, first of all, to pay attention to the selection of the dose of concomitant standard therapy. You may also need to temporarily reduce the dose of Bisomor or discontinue treatment. After the patient’s condition stabilizes, the dose should be re-titrated or the treatment should be continued. To date, there are insufficient data on the use of Bisomor in patients with CHF associated with type 1 diabetes mellitus, severe renal and/or liver dysfunction, restrictive cardiomyopathy, congenital heart defects, and hemodynamically significant heart disease. Also, until now, not enough data have been obtained on patients with CHF with myocardial infarction in the last 3 months. Duration of treatment for all indications, the cure is usually long. If necessary, treatment can be interrupted and resumed in compliance with certain rules. Treatment should not be interrupted abruptly, especially in patients with CHD. If it is necessary to stop treatment, then the dose of the drug should be reduced gradually.

Overdose

Symptoms The most common symptoms of overdose are AV block, severe bradycardia, severe BP reduction, bronchospasm, acute heart failure, and hypoglycemia. Sensitivity to a single high dose of bisoprolol varies greatly among individual patients, and it is likely that patients with CHF have a higher sensitivity. Treatmentsupportive and symptomatic therapy. For severe bradycardia: intravenous use of atropine. If its effect is insufficient, a remedy with a positive chronotropic effect can be administered with caution. Sometimes it may be necessary to temporarily install an artificial pacemaker. With a marked decrease in blood pressure: intravenous use of plasma-substituting solutions and vasopressors. With AV block: patients should be constantly monitored and treated with beta-adrenomimetics, such as epinephrine. If necessary, an artificial pacemaker can be installed. In acute heart failure: intravenous use of diuretics, drugs with a positive inotropic effect, as well as vasodilators. In case of bronchospasm: use of bronchodilators, including beta-2-adrenomimetics and / or aminophylline. Hypoglycemia: intravenous use of dextrose (glucose).

Special instructions

Monitoring of patients taking Bisomor should include measurement of heart rate and blood pressure (at the beginning of treatment – daily, then 1 time in 3-4 months), ECG, determination of blood glucose in patients with diabetes mellitus (1 time in 4-5 months). In elderly patients, it is recommended to monitor kidney 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 60 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. 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. When taking clonidine at the same time, it can be stopped only a few days after the withdrawal of Bisomor. In case of detection of increasing bradycardia (less than 60 beats/min), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade 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). At the initial stages of treatment with Bisomor, patients need constant monitoring. Patients with bronchospastic diseases can be prescribed cardioselective beta-blockers in case of intolerance and / or ineffectiveness of other antihypertensive agents. If the dose of Bisomor is exceeded, there is a risk of developing bronchospasm. 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. Patients who use contact lenses should take into account that during treatment with Bisomor, the production of tear fluid may decrease. When performing general anesthesia during drug treatment, the risk of beta-adrenergic blockage should be taken into account. If it is necessary to stop therapy with Bisomor before surgery, discontinuation of the drug is carried out gradually, and is completed 48 hours before general anesthesia. If the patient took the drug before surgery, he should choose a general anesthesia drug with a minimal negative inotropic effect. You should warn the anesthesiologist about treatment with Bisomor. In patients with pheochromocytoma, the drug can be prescribed only against the background of the use of alpha-blockers. When treated with Bisomor, the symptoms of hyperthyroidism (hyperthyroidism) may be masked (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase symptoms. It should be canceled before testing the content of catecholamines, normetanephrine and vanillinmindalic acid in the blood and urine, and titers of antinuclear antibodies. In “smokers”, the effectiveness of beta-blockers is lower. Influence on the ability to drive vehicles and mechanisms:During treatment with Bisomor, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not take after the expiration date indicated on the package.

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets