Biprol, pills 5mg 50pcs

Composition

Active ingredient: Bisoprolol fumarate 5,000 mg/10,000 mg; excipients: Microcrystalline cellulose 44,500 mg / 62,400 mg; Ludipress LCE (lactose monohydrate 94.7-98.3%, povidone 3-4%) 40,000 mg/ 38,500 mg; Corn starch 8,000 mg/ 11,000 mg; Colloidal silicon dioxide 0.500 mg/ 0.600 mg;Crospovidone (Collidone CL) 1,000 mg/ 1,250 mg;Magnesium Stearate 1,000 mg/ 1,250 mg; Shell: Titanium dioxide 0.287 mg / 0.430 mg; Macrogol (polyethylene glycol 4000) 0.287 mg/ 0.430 mg; Hypromellose 1.320 mg/ 1.968 mg; talc 0.106 mg/ 0.172 mg

Pharmacological action

Selective beta-1-adrenoblocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. 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 from adenosine triphosphate, reduces the intracellular flow of calcium ions, has a negative chrono -, dromo -, batmo-and inotropic effect, reduces atrioventricular (AV) conduction and excitability. If the therapeutic dose is exceeded, it has a beta-2-adrenoblocking effect. Total peripheral vascular resistance at the beginning of the drug use (in the first 24 hours) increases (as a result of a reciprocal increase in alpha-adrenergic activity and elimination of beta-2-adrenergic stimulation), which returns to the initial value after 1-3 days, and decreases with prolonged use. The antihypertensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin-aldosterone system (it is of great importance for patients with transient renin hypersecretion), restoration of sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and an effect on the central nervous system. With arterial hypertension, the effect develops 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 and reduced myocardial contractility, prolongation of diastole, and improvement of myocardial perfusion. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for myocardial oxygen, 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 content of cyclic adenosine monophosphate, 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 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; it does not cause sodium ion retention in the body. Pharmacokineticsabsorption. Absorption — 80-90%, food intake does not affect the absorption of the drug. The maximum concentration in the blood plasma is observed after 1-3 hours. Bioavailability is about 90%. The connection with plasma proteins is about 30%. Distribution. The volume of distribution is 3.5 l / kg. Permeability through the blood-brain and placental barriers is low. Metabolism. It is metabolized in the liver with the participation of isoenzymes CYP3A4 (up to 95%) and CYP2D6. The effect of “primary passage” through the liver is insignificant (about 10%). Biotransformation of bisoprolol is not accelerated in patients with hyperthyroidism. Output. Total clearance is 15.6±3.2 l / h, renal clearance is 9.6±1.6 l / h. The balanced clearance of bisoprolol is determined by the balance between its excretion through the kidneys unchanged (about 50%) and oxidation in the liver (about 50%) to inactive metabolites, which are then also excreted by the kidneys; less than 2% is excreted through the intestine (with bile). It does not accumulate in the body. The elimination half-life is 9-12 hours. The dose-dependent pharmacokinetics of bisoprolol are linear. The pharmacokinetics of bisoprolol are stable, independent of the patient’s age and gender. Pharmacokinetics in special clinical casesrenal insufficiency. In the case of severe renal impairment (creatinine clearance less than 20 ml / min) and in patients with anuria, the half-life may increase by more than 2 times. Liver failure. In the case of severe hepatic insufficiency, the half-life is increased to 13-15 hours. Chronic heart failure. In patients with chronic heart failure (NYHA functional class III), the concentration of bisoprolol in blood plasma is higher than in healthy volunteers, and the half-life increases to 17 hours.

Indications

• Arterial hypertension.
• Coronary heart disease: prevention of stable angina attacks.

Use during pregnancy and lactation

The use of Biprol during pregnancy and lactation is possible if the benefit to the mother exceeds the risk of side effects in the fetus and child.

Contraindications

Hypersensitivity to bisoprolol, other components of the drug and other beta-blockers; shock (including cardiogenic); pulmonary edema; acute heart failure or CHF in the decompensation stage, requiring inotropic therapy; AV block II-III degree, without pacemaker;sinoatrial block; sinus node weakness syndrome; bradycardia (heart rate less than 60 beats/min); Prinzmetal angina pectoris; cardiomegaly (without signs of heart failure);severe arterial hypotension (systolic blood pressure less than 100 mm Hg), especially in myocardial infarction; severe bronchial asthma and chronic obstructive pulmonary disease (COPD) in the anamnesis;simultaneous use of floctafenin, sultoprid, monoamine oxidase inhibitors (MAO), with the exception of MAO type B; simultaneous intravenous use of verapamil or diltiazem; severe peripheral circulatory disorders, Raynaud’s syndrome; pheochromocytoma (without simultaneous use of alpha-blockers); metabolic acidosis; age up to 18 years (efficacy and safety have not been established). Lactase deficiency, lactose intolerance, lactose/isomaltose malabsorption syndrome (the drug contains lactose). With caution, severe hepatic insufficiency, severe renal insufficiency (creatinine clearance less than 20 ml / min), myasthenia gravis, thyrotoxicosis, diabetes mellitus (may mask the symptoms of hypoglycemia), burdened allergic anamnesis, grade I AV block, depression (including in the anamnesis), psoriasis, bronchial asthma, COPD, peripheral circulatory disorders, strict diet.

Side effects

the Frequency of the following side effects are in accordance with the who classification: very often — more than 10%; often — more than 1% and less than 10%; infrequently — more than 0.1% and less than 1%; rarely — less than 0.01% and less than 0.1%; very rarely — less than 0.01%, including isolated cases. Central and peripheral nervous system disorders: often — increased fatigue, asthenia, dizziness, headache. Usually these phenomena develop at the beginning of treatment, as a rule, they are expressed slightly and pass within 1-2 weeks; infrequently-sleep disorders, depression; rarely-nightmares, hallucinations, loss of consciousness. From the cardiovascular system: very often — bradycardia, palpitation sensation; often — marked decrease in blood pressure (especially in patients with CHF), manifestations of angiospasm (increased peripheral circulatory disorders, cold sensation in the extremities (paresthesia); infrequently — violation of AV conduction (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, worsening of CHF treatment with the development of peripheral edema (swelling of the ankles, feet) and shortness of breath, orthostatic hypotension, chest pain. From the digestive system: often — nausea, vomiting, diarrhea, abdominal pain, constipation, dryness of the oral mucosa; rarely-hepatitis, increased activity of “liver” transaminases (alanine aminotransferase, aspartate aminotransferase), increased bilirubin concentration. Respiratory system disorders: infrequently-laryngospasm and bronchospasm in patients with bronchial asthma or obstructive airway diseases; rarely-allergic rhinitis, nasal congestion. From the musculoskeletal system: infrequently — muscle weakness, cramps in the calf muscles, arthralgia. From the side of the senses: rarely-visual impairment, reduced tear production (should be considered when wearing contact lenses), hearing impairment, changes in taste;very rarely — dry and painful eyes, conjunctivitis. From the side of the skin: rarely-increased sweating, psoriasis-like skin reactions; very rarely-alopecia, exacerbation of psoriasis. From the endocrine system: rarely-hypoglycemia. From the genitourinary system: rarely-violation of potency, weakening of libido. From the immune system: rarely-the appearance of antinuclear antibodies with unusual clinical symptoms of lupus-like syndrome, which disappear after the end of treatment. Allergic reactions: rarely-hyperemia of the skin, pruritus, skin rash, urticaria. Laboratory parameters: rarely-hypertriglyceridemia; very rarely-thrombocytopenia, agranulocytosis, leukopenia. Other services: rarely — “withdrawal” syndrome (increased angina attacks, increased blood pressure).

Interaction

of Floctafenin.In the case of shock or hypotension caused by floctafenin, beta-blockers cause a decrease in compensatory cardiovascular reactions (co-use is contraindicated). Sultoprid. Due to the additive effect, severe bradycardia may develop (co-use is contraindicated). MAO inhibitors. Concomitant use is not recommended (with the exception of MAO type B), since there is a high probability of a significant increase in the antihypertensive effect. A break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days. Slow calcium channel blockers (diltiazem and verapamil). This combination should be avoided. Intravenous use of verapamil or diltiazem or other antiarrhythmic drugs is contraindicated during treatment with Biprol. Due to the synergism of the action, a sharp decrease in blood pressure, violations of automatism (pronounced bradycardia, sinus node arrest), violations of AV conduction, heart failure are possible. If necessary, the appointment of such a combination requires careful clinical and electrocardiographic monitoring of patients, especially the elderly and at the beginning of treatment. Class I antiarrhythmic agents (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone) with simultaneous use may reduce the electrical conductivity and contractility of the myocardium (combination with bisoprolol should be avoided). Class III antiarrhythmic drugs (for example, amiodarone). When combined with bisoprolol, contractility, automatism and conduction may be impaired due to suppression of sympathetic compensatory mechanisms (this combination should be avoided). Antihypertensive agents of central action (clonidine, apraclonidine, alpha-methyldopa, guangfangzin, moxonidine, rilmenidine). When used together, there is an increased risk of developing severe bradycardia, sinus node arrest, impaired AV conduction, a sharp decrease in blood pressure, and heart failure (synergistic effect). This combination should be avoided. If necessary, careful clinical and electrocardiographic monitoring is required, especially in elderly patients and at the beginning of treatment. A significant increase in blood pressure when the central antihypertensive drug is abruptly discontinued. Cardiac glycosides. Decreased heart rate, impaired conduction. Beta-blockers for topical use (for example, eye drops for the treatment of glaucoma) can increase the systemic effect of bisoprolol (lowering blood pressure, lowering heart rate). Calcium channel blockers (for example, nifedipine). Excessive lowering of blood pressure may occur. Parasympathomimetics. When used together, the risk of developing bradycardia. Mefloquine. Combined use with bisoprolol increases the risk of developing bradycardia (additive effect). Phenytoin with intravenous use, drugs for inhaled general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of lowering blood pressure. Concomitant use 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) may increase the vasoconstrictor effect of these agents, which occurs 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. Bisoprolol can change the effectiveness of insulin and hypoglycemic agents for oral use, mask the symptoms of developing hypoglycemia (tachycardia, increased blood pressure). Bisoprolol reduces the clearance of lidocaine and xanthines (except diphylline)and increases their plasma concentrations, especially in patients with initially elevated theophylline clearance due to smoking. The antihypertensive effect is weakened by nonsteroidal anti-inflammatory drugs (sodium ion retention and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (sodium ion retention). Diuretics, sympatholytics, hydralazine and other antihypertensive drugs. Risk of excessive lowering of blood pressure. Bisoprolol prolongs the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins. Tri-and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and sleeping pills — when combined with bisoprolol, increased central nervous system depression. 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 plasma. Rifampicin reduces the elimination half-life of bisoprolol. 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 anaphylactic reactions.

How to take, course of use and dosage

The drug Biprol is taken orally, in the morning,1 time a day with a small amount of liquid, before breakfast, during or after it. Tablets should not be chewed or ground into powder. In all cases, the mode of use and dose is selected by the doctor for each patient individually, in particular, taking into account the patient’s heart rate and condition. In case of arterial hypertension and coronary heart disease, the drug is prescribed 5 mg 1 time a day. If necessary, the dose is increased to 10 mg once a day. In the treatment of arterial hypertension and angina pectoris, the maximum daily dose is 20 mg once a day. For patients with severe renal impairment (creatinine clearance less than 20 ml / min) or with severe hepatic impairment, the maximum daily dose is 10 mg once a day. Increasing the dose in such patients should be carried out with extreme caution. No dose adjustment is required in elderly patients.

Overdose

Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, severe lowering of blood pressure, acute heart failure, hypoglycemia, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, convulsions. Treatment: gastric lavage, use of adsorbents, symptomatic therapy. With severe bradycardia-intravenous use of atropine. If the effect is insufficient, you can use caution to introduce a drug that has a positive chronotropic effect. Sometimes it may be necessary to temporarily install an artificial pacemaker. If AV block develops, intravenous use of 1-2 mg of atropine, epinephrine, or the installation of a temporary pacemaker — For ventricular extrasystole — lidocaine (class IA drugs are not used). With a marked decrease in blood pressure, the patient should be transferred to the Trendelenburg position; if there are no signs of edema — intravenous use of plasma-substituting solutions, if they are ineffective-the introduction of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic effects and eliminate a pronounced decrease in blood pressure). For hypoglycemia, intravenous use of a dextrose (glucose) solution may be indicated. In case of heart failure-cardiac glycosides, diuretics. For convulsions-intravenous diazepam. In case of bronchospasm — inhaled beta-2-adrenomimetics.

Special instructions

Treatment with the drug is usually long-term. Before starting treatment, it is recommended to conduct a study of the function of external respiration in patients with a burdened bronchopulmonary history. Patients with bronchospastic diseases can be prescribed bisoprolol in case of intolerance and/or ineffectiveness of other antihypertensive drugs, while strictly monitoring the dose of the drug. Overdose is dangerous for the development of bronchospasm. Monitoring of patients taking bisoprolol should include monitoring of heart rate, blood pressure (at the beginning of treatment — daily, then once every 3-4 months), electrocardiograms, blood glucose concentration in blood plasma in patients with diabetes mellitus (once every 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 the heart rate and instructed about the need for medical consultation if it is reduced to less than 60 beats / min. Beta-blockers are ineffective in approximately 20% of patients with angina pectoris. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats / min) and an increase in the final diastolic volume of the left ventricle, which disrupts subendocardial blood flow. In “smokers”, the effectiveness of beta-blockers is lower. 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 was not previously achieved). In thyrotoxicosis, bisoprolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as 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.With simultaneous use of clonidine, its use can be stopped only a few days after the withdrawal of bisoprolol. 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 it is necessary to carry out a planned surgical intervention, the drug is canceled 48 hours before the start of general anesthesia. If the patient has taken the drug before surgery, they should choose a general anesthesia medication with minimal negative inotropic effects. Reciprocal activation of the vagus nerve can be eliminated by intravenous use of atropine (1-2 mg). Medications that reduce the supply of catecholamines (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of medications should be constantly monitored by a doctor for hypotension or bradycardia. If elderly patients develop increasing bradycardia (less than 60 beats/min), hypotension (systolic blood pressure below 100 mm Hg), AV block, bronchospasm, ventricular arrhythmias, severe liver and kidney function disorders, the dose should be reduced or treatment should be discontinued. Do not abruptly interrupt treatment with bisoprolol due to the risk of developing severe arrhythmias and myocardial infarction. Withdrawal is carried out gradually, reducing the dose for 2 weeks or more (the dose is reduced by 25% in 3-4 days). It is recommended to stop therapy (with a gradual decrease in the dose) with the development of depression caused by taking the drug. The drug should be discontinued before testing the blood and urine levels of catecholamines, normetanephrine and vanillinmindalic acid, and the titer of antinuclear antibodies. Influence on the ability to drive vehicles and work with mechanisms During treatment, care should be taken when driving vehicles and performing other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Film-coated tablets,5 mg and 10 mg. 10 tablets each in a contour cell pack made of polyvinyl chloride film and aluminum foil. 3,5 or 10 contour cell packs together with the instructions for use in a cardboard pack.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

3 years

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Arrhythmia, Hypertension, Heart Failure