Biprol, pills 5mg 30pcs

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

. Characteristics

Round, biconvex tablets, film-coated in white or almost white color. On a cross-section, the core is white or white with a barely noticeable creamish tinge of color.

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.

Active ingredients

Bisoprolol

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. From the central and peripheral nervous system: 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 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: rarely – “withdrawal” syndrome (increased angina attacks, increased blood pressure).

Interaction

The use of allergens used for immunotherapy or allergen extracts for skin tests against the background of Biprol therapy increases the risk of severe systemic allergic reactions or anaphylaxis.

When iodine-containing X-ray contrast drugs for intravenous use are used simultaneously with bisoprolol, the risk of anaphylactic reactions increases.

When phenytoin is co-administered with bisoprolol for intravenous use, drugs for inhaled general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of lowering blood pressure.

When used concomitantly, bisoprolol changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia ( tachycardia, increased blood pressure).

When used concomitantly, bisoprolol reduces the clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentrations, especially in patients with an initially increased clearance of theophylline under the influence of smoking.

The antihypertensive effect of bisoprolol is reduced by NSAIDs (Na + retention and blockade of prostaglandin synthesis by the kidneys), corticosteroids and estrogens (Na + ion retention).

Concomitant use of cardiac glycosides, methyldopa, reserpine and guanfacine, calcium channel blockers Other antiarrhythmic medications (verapamil, diltiazem ), amiodarone, and other antiarrhythmic medications increase the risk

of developing or worsening bradycardia, AV block, cardiac arrest, and heart failure.

When used concomitantly with bisoprolol, nifedipine can lead to a significant decrease in blood pressure.

When used concomitantly with bisoprolol, diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in 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 increase the depressing effect of bisoprolol on the central nervous system.

Concomitant use of bisoprolol with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect (the interval between taking MAO inhibitors and bisoprolol should be at least 14 days).

When used concomitantly with bisoprolol, non-hydrogenated ergot alkaloids and ergotamine increase the risk of developing peripheral circulatory disorders.

Simultaneous use of sulfasalazine increases the concentration of bisoprolol in plasma.

When used concomitantly, rifampicin reduces T 1/2 of bisoprolol.

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:

arrhythmias, ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, chronic heart failure, cyanosis of the fingernails and palms, shortness of breath, bronchospasm, dizziness, fainting, convulsions.

Treatment: 

gastric lavage, use of adsorbents. If necessary, symptomatic therapy is performed: if AV block develops, intravenous use of atropine (1-2 mg), epinephrine, or setting up a temporary pacemaker; with ventricular extrasystole, lidocaine (Class I A drugs are not used).

With a decrease in blood pressure, the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema, intravenous plasma-substituting solutions are administered; if ineffective, epinephrine, dopamine, dobutamine are administered (to maintain chronotropic and inotropic effects and eliminate a pronounced decrease in blood pressure).

For heart failure, cardiac glycosides, diuretics, glucagon are prescribed ; for convulsions, intravenous diazepam; for bronchospasm, beta-2-adrenostimulants are inhaled.

Description

Round, biconvex tablets, film-coated in white or almost white color. On a cross-section, the core is white or white with a barely noticeable creamish tinge of color.

Functional features

Suction. 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 cases of renal failure. 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.

Complete set

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.

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

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Heart Failure, Arrhythmia, Hypertension