Bidop tablets 5mg, No. 28

Inside. BidopЃ tablets should be taken 1 time / day with a small amount of liquid in the morning before breakfast, during or after it. The tablets should not be chewed or powdered. Arterial hypertension and stable angina pectoris In all cases, the regimen and dose are selected by the doctor for each patient individually, in particular, taking into account the heart rate and the patient's condition. Usually, the initial dose is 5 mg of BidopЃ 1 time / day. If necessary, the dose can be increased to 10 mg 1 time / day. In the treatment of arterial hypertension and stable angina pectoris, the maximum recommended dose is 20 mg of BidopЃ 1 time / day. Chronic heart failure The standard treatment regimen for CHF includes the use of ACE inhibitors or angiotensin II receptor antagonists (in case of intolerance to ACE inhibitors), beta-blockers,diuretics and, optionally, cardiac glycosides. The beginning of CHF treatment with BidopЃ requires a special titration phase and regular medical supervision. A precondition for treatment with BidopЃ is stable chronic heart failure without signs of exacerbation. Treatment of stable chronic heart failure with BidopЃ begins according to the following titration schedule. In this case, individual adaptation may be required depending on how well the patient tolerates the prescribed dose, i.e., the dose can be increased only if the previous dose was well tolerated. To ensure an appropriate titration process at the initial stages of treatment, it is recommended to use bisoprolol in a dosage form: 2.5 mg tablets.The recommended starting dose is 1.25 mg once a day. To ensure the specified dosing regimen, bisoprolol drugs should be used (for example, BidopЃ Cor tablets 2.5 mg or drugs from other manufacturers) at a dosage of 2.5 mg 1/2 tablet 1 time / day. Depending on individual tolerance, the dose should be gradually increased to 2.5 mg, 3.75 mg, 5 mg, 7.5 mg and 10 mg 1 time / day. Each subsequent dose increase should be carried out at least 2 weeks later. If an increase in the dose of the drug is poorly tolerated by the patient, a dose reduction is possible. The maximum recommended dose for the treatment of CHF is 10 mg of BidopЃ 1 time / day. During titration, regular monitoring of blood pressure, heart rate and the severity of CHF symptoms is recommended.Aggravation of the symptoms of CHF is possible from the first day of using the drug. If the patient does not tolerate the maximum recommended dose of the drug, a gradual dose reduction should be considered. During the titration phase or after it, a temporary worsening of the course of CHF, arterial hypotension or bradycardia may occur. In this case, it is recommended, first of all, to adjust the doses of concomitant therapy drugs. You may also need to temporarily reduce the dose of BidopЃ or cancel it. After stabilization of the patient's condition, the dose should be re-titrated, or treatment should be continued.During the titration phase or after it, a temporary worsening of the course of CHF, arterial hypotension or bradycardia may occur. In this case, it is recommended, first of all, to adjust the doses of concomitant therapy drugs. You may also need to temporarily reduce the dose of BidopЃ or cancel it. After stabilization of the patient's condition, the dose should be re-titrated, or treatment should be continued.During the titration phase or after it, a temporary deterioration in the course of CHF, arterial hypotension or bradycardia may occur. In this case, it is recommended, first of all, to adjust the doses of concomitant therapy drugs. You may also need to temporarily reduce the dose of BidopЃ or cancel it. After stabilization of the patient's condition, titration of the dose should be repeated, or treatment should be continued.

Duration of treatment for all indications

Treatment with BidopЃ is usually a long-term therapy.

Special patient groups

Patients with impaired renal or hepatic function: in case of impaired liver or kidney function, mild to moderate dosage adjustment is usually not required. In severe renal impairment (CC less than 20 ml / min) and in patients with severe liver disease, the maximum daily dose is 10 mg. Increasing the dose in these patients should be done with extreme caution. Elderly patients (over 65 years of age): dose adjustment is not required. Children and adolescents: since there is insufficient data on the use of bisoprolol in children and adolescents, it is not recommended to prescribe the drug to children under 18 years of age. To date, there is insufficient data on the use of BidopЃ in patients with CHF in combination with type 1 diabetes mellitus, severe renal and / or liver dysfunction, restrictive cardiomyopathy,congenital heart defects or heart valve disease with severe hemodynamic disturbances. There is also insufficient data on the use of BidopЃ in patients with CHF and myocardial infarction during the last 3 months.

active substance:

bisoprolol fumarate

hypersensitivity to bisoprolol or any of the excipients; acute heart failure, chronic heart failure in the stage of decompensation, requiring inotropic therapy; cardiogenic shock; AV block II and III degree without a pacemaker; SSSU; sinoatrial blockade; severe bradycardia (heart rate less than 60 beats / min); severe arterial hypotension (systolic blood pressure less than 100 mm Hg); severe forms of bronchial asthma and COPD; severe peripheral arterial circulation disorders or Raynaud's syndrome; pheochromocytoma (without the simultaneous use of alpha-blockers); metabolic acidosis; age up to 18 years (insufficient data on efficacy and safety in this age group); lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Carefully

Conducting desensitizing therapy, Prinzmetal angina, hyperthyroidism, type 1 diabetes mellitus and diabetes mellitus with significant fluctuations in blood glucose concentration, grade I AV block, severe renal failure (CC less than 20 ml / min), severe liver dysfunction, psoriasis, restrictive cardiomyopathy , congenital heart defects or heart valve disease with severe hemodynamic disturbances, CHF with myocardial infarction within the last 3 months, strict diet.

pharmachologic effect

Selective beta1-blocker without intrinsic sympathomimetic activity, does not have a membrane stabilizing effect. It has only a slight affinity for ?2-adrenergic receptors of smooth muscles of the bronchi and blood vessels, as well as for ?2-adrenergic receptors involved in the regulation of metabolism. Consequently, bisoprolol in general does not affect airway resistance and metabolic processes in which ?2-adrenergic receptors are involved. The selective effect of the drug on ?1-adrenergic receptors persists beyond the therapeutic range. Bisoprolol does not have a pronounced negative inotropic effect. The maximum effect of the drug is achieved 3-4 hours after ingestion. Even with the use of bisoprolol 1 time per day, its therapeutic effect lasts for 24 hours due to the 10-12-hour half-life from blood plasma.Typically, the maximum reduction in blood pressure is achieved 2 weeks after starting treatment. Bisoprolol reduces the activity of the sympathoadrenal system (SAS) by blocking the ? 1-adrenergic receptors of the heart. With a single oral administration in patients with coronary artery disease without signs of chronic heart failure (CHF), bisoprolol slows down the heart rate, reduces the stroke volume of the heart and, as a result, reduces the ejection fraction and myocardial oxygen demand. With long-term therapy, the initially increased OPSS decreases. A decrease in renin activity in blood plasma is considered as one of the components of the hypotensive action of beta-blockers.With a single oral administration in patients with coronary artery disease without signs of chronic heart failure (CHF), bisoprolol slows down the heart rate, reduces the stroke volume of the heart and, as a result, reduces the ejection fraction and myocardial oxygen demand. With long-term therapy, the initially increased TPR decreases. A decrease in renin activity in blood plasma is considered as one of the components of the hypotensive action of beta-blockers.With a single oral administration in patients with coronary artery disease without signs of chronic heart failure (CHF), bisoprolol slows down the heart rate, reduces the stroke volume of the heart and, as a result, reduces the ejection fraction and myocardial oxygen demand. With long-term therapy, the initially increased TPR decreases. A decrease in renin activity in blood plasma is considered as one of the components of the hypotensive action of beta-blockers.

Pharmacokinetics

Absorption Bisoprolol is almost completely (more than 90%) absorbed from the gastrointestinal tract. The bioavailability of bisoprolol due to insignificant metabolism during the 'first pass' through the liver (at about 10%) is about 90% after oral administration. Food intake does not affect bioavailability. Bisoprolol demonstrates linear kinetics, and its plasma concentrations are proportional to the dose taken in the range from 5 to 20 mg. Cmax in blood plasma is reached after 2-3 hours.

Distribution

Bisoprolol is widely distributed. The volume of distribution is 3.5 l / kg. Plasma protein binding reaches approximately 30%.

Metabolism

It is metabolized by the oxidative pathway without subsequent conjugation. All metabolites are polar (water-soluble) and are excreted by the kidneys. The main metabolites found in blood plasma and urine do not show pharmacological activity. The data obtained as a result of studies with human liver microsomes in vitro show that bisoprolol is metabolized primarily by the CYP3A4 isoenzyme (about 95%), and the CYP2D6 isoenzyme plays only a minor role.

Withdrawal

The clearance of bisoprolol is determined by the balance between excretion by the kidneys unchanged (about 50%) and metabolism in the liver (about 50%) to metabolites, which are also excreted by the kidneys. The total ground clearance is 15 l / h. T1 / 2 from blood plasma is 10-12 hours.

Pharmacokinetics in selected patient groups

There is no information on the pharmacokinetics of bisoprolol in patients with CHF and simultaneous impaired liver or kidney function.

Side effect

The adverse drug reactions listed below are presented by systemic organ classes in accordance with the MedDRA classification and with the frequency of occurrence: very often (? 1/10); often (? 1/100, <1/10); infrequently (? 1/1000, <1/100); rarely (? 1/10 000, <1/1000); very rare (<1/10 000). From the nervous system: often - dizziness *, headache *; rarely - loss of consciousness. Mental disorders: infrequently - depression, insomnia; rarely - hallucinations, nightmares. From the side of the organ of vision: rarely - a decrease in lacrimation (should be taken into account when wearing contact lenses); very rarely - conjunctivitis. From the side of the organ of hearing and labyrinth disorders: rarely - hearing impairment. From the side of the cardiovascular system: very often - bradycardia (in patients with CHF); often - aggravation 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), aggravation of symptoms of the course of CHF (in patients with arterial hypertension or angina pectoris), orthostatic hypotension. From the respiratory system: infrequently - bronchospasm in patients with bronchial asthma or a history of airway obstruction; rarely, allergic rhinitis. From the digestive system: often - nausea, vomiting, diarrhea, constipation; rarely - hepatitis. From the musculoskeletal system: infrequently - muscle weakness, muscle cramps. On the part of the skin and subcutaneous tissues: rarely - hypersensitivity reactions, such as itching, rash, hyperemia of the skin; very rare: alopecia.Beta-blockers can aggravate the symptoms of psoriasis or cause a psoriasis-like rash. On the part of the genitals and mammary gland: rarely - violation of potency.

General reactions: often - asthenia (in patients with CHF), increased fatigue *; infrequently - asthenia (in patients with arterial hypertension or angina pectoris).

Application during pregnancy and lactation

During pregnancy, BidopЃ should be used only if the benefits to the mother outweigh the risk of side effects in the fetus and / or child. Typically, beta-blockers reduce blood flow to the placenta and can affect fetal development. Blood flow in the placenta and uterus should be monitored, as well as the growth and development of the unborn child should be monitored, and in the event of adverse events in relation to pregnancy and / or the fetus, alternative therapies should be used. 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 penetration of bisoprolol into breast milk. Taking BidopЃ is not recommended for women during breastfeeding. If taking the drug during lactation is necessary, breastfeeding should be discontinued.

Application for violations of liver function

It should be used with caution in liver failure. For patients with impaired liver function, the maximum daily dose is 10 mg.

Application for impaired renal function

It should be used with caution in chronic renal failure. For patients with impaired renal function with CC less than 20 ml / min, the maximum daily dose is 10 mg.

Application in children

Contraindicated in children and adolescents under 18 years of age.

Use in elderly patients

It should be used with caution in elderly patients.

special instructions

The patient should not abruptly interrupt treatment with BidopЃ and not change the recommended dose without first consulting a doctor, because this can lead to a temporary deterioration in the activity of the heart. Treatment should not be interrupted abruptly, especially in patients with coronary artery disease. If discontinuation of treatment is necessary, the dose should be reduced gradually. At the initial stages of treatment with BidopЃ, patients need constant monitoring. The drug should be used with caution in the following cases: diabetes mellitus with significant fluctuations in the concentration of glucose in the blood - symptoms of a pronounced decrease in glucose concentration (hypoglycemia), such as tachycardia, palpitations or excessive sweating, can be masked; strict diet; desensitizing therapy; AV blockade of the 1st degree; Prinzmetal's angina;mild to moderate peripheral arterial circulation disorders (at the beginning of therapy, an increase in symptoms may occur); psoriasis (including history). Respiratory system: with bronchial asthma or COPD, the simultaneous use of bronchodilators is indicated. In patients with bronchial asthma, an increase in airway resistance is possible, which requires a higher dose of beta2-adrenergic agonists. Allergic reactions: beta-blockers, including BidopЃ, can increase the sensitivity to allergens and the severity of anaphylactic reactions due to the weakening of adrenergic compensatory regulation under the action of beta-blockers. Epinephrine (adrenaline) therapy does not always give the expected therapeutic effect. General anesthesia:when carrying out general anesthesia, the risk of beta-adrenergic blockade should be taken into account. If it is necessary to discontinue therapy with BidopЃ before surgery, this should be done gradually and completed 48 hours before general anesthesia. The patient must warn the anesthesiologist about taking BidopЃ. Pheochromocytoma: in patients with adrenal tumor (pheochromocytoma), BidopЃ can be prescribed only against the background of the use of alpha-blockers. Hyperthyroidism: When treated with BidopЃ, symptoms of hyperthyroidism (hyperthyroidism) may be masked.The patient should warn the anesthesiologist about taking BidopЃ. Pheochromocytoma: in patients with adrenal tumor (pheochromocytoma), BidopЃ can be prescribed only against the background of the use of alpha-blockers. Hyperthyroidism: When treated with BidopЃ, the symptoms of hyperthyroidism (hyperthyroidism) may be masked.The patient must warn the anesthesiologist about taking BidopЃ. Pheochromocytoma: in patients with adrenal tumor (pheochromocytoma), BidopЃ can be prescribed only against the background of the use of alpha-blockers. Hyperthyroidism: When treated with BidopЃ, symptoms of hyperthyroidism (hyperthyroidism) may be masked.

Influence on the ability to drive vehicles and mechanisms

According to the study results, BidopЃ does not affect the ability to drive vehicles in patients with coronary artery disease. However, due to individual reactions, the ability to drive vehicles and complex mechanisms may be impaired. This should be paid special attention to at the beginning of treatment, after changing the dose, as well as with the simultaneous use of alcohol.

Overdose

Symptoms: the most common symptoms of an overdose are AV blockade, severe bradycardia, a marked decrease in blood pressure, bronchospasm, acute heart failure, hypoglycemia. The sensitivity to a single dose of a high dose of bisoprolol varies greatly among individual patients and, probably, patients with CHF are highly sensitive. Treatment: in case of an overdose, first of all, it is necessary to stop taking the drug and begin supportive symptomatic therapy. With severe bradycardia: intravenous administration of atropine. If the effect is insufficient, then with caution, you can enter an agent with a positive chronotropic effect. Temporary pacemaker placement may sometimes be required. With a pronounced decrease in blood pressure: in / in the introduction of plasma-substituting solutions and vasopressor drugs. With AV block:patients should be monitored continuously and treated with beta-agonists such as epinephrine. If necessary, install an artificial pacemaker. With exacerbation of CHF: intravenous administration of diuretics, drugs with a positive inotropic effect, as well as vasodilators. With bronchospasm: the appointment of bronchodilators, incl. beta2-adrenergic agonists and / or aminophylline. With hypoglycemia: intravenous administration of dextrose (glucose).With hypoglycemia: intravenous administration of dextrose (glucose).With hypoglycemia: intravenous administration of dextrose (glucose).

Drug interactions

The efficacy and tolerability of bisoprolol may be affected by the simultaneous administration of other drugs. This interaction can also occur when two drugs are taken over a short period of time. The doctor must be informed about taking other drugs, even if they are taken without a doctor's prescription (i.e. over-the-counter drugs). Combinations not recommended Treatment of chronic heart failure Class I antiarrhythmics (eg, quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conduction and contractility of the heart.All indications for the use of BidopЃ Slow calcium channel blockers (BMCC) such as verapamil and, to a lesser extent, diltiazem, when used simultaneously with bisoprolol, can lead to a decrease in myocardial contractility and impairment of AV conduction. In particular, intravenous administration of verapamil to patients taking beta-blockers can lead to severe arterial hypotension and AV blockade. Centrally acting antihypertensives (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 the withdrawal of beta-blockers, may increase the risk of developing 'rebound' arterial hypertension. Combinations,requiring special care Treatment of arterial hypertension and angina pectoris Class I antiarrhythmics (for example, quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conductivity and myocardial contractility. All indications for the use of BidopЃ BMCC, dihydropyridine derivatives (for example, nifedipine, felodipine, amlodipine), when used simultaneously with bisoprolol, may increase the risk of arterial hypotension. In patients with CHF, the risk of subsequent deterioration of the contractile function of the heart cannot be excluded. Class III antiarrhythmics (eg, amiodarone) may increase AV conduction disturbances. The action of beta-blockers for topical use (for example,eye drops for the treatment of glaucoma) can enhance the systemic effects of bisoprolol (lowering blood pressure, lowering heart rate). Parasympathomimetics, when used concomitantly with bisoprolol, can increase the violation of AV conduction and increase the risk of developing bradycardia. The hypoglycemic effect of insulin or oral hypoglycemic agents may be enhanced. Signs of hypoglycemia, in particular tachycardia, can be masked or suppressed. Such interactions are more likely with the use of non-selective beta-blockers. Agents for general anesthesia can increase the risk of cardiodepressive action, leading to arterial hypotension (see section 'Special instructions'). Cardiac glycosides, when used simultaneously with bisoprolol, can lead to an increase in pulse conduction time and, thus,to the development of bradycardia. NSAIDs can reduce the antihypertensive effect of bisoprolol. The simultaneous use of the drug BidopЃ with beta-adrenergic agonists (for example, isoprenaline, dobutamine) can lead to a decrease in the effect of both drugs. The combination of bisoprolol with adrenergic agonists that affect beta and alpha-adrenergic receptors (for example, norepinephrine, epinephrine) can enhance the vasoconstrictor effects of these drugs, which occur with the participation of alpha-adrenergic receptors, leading to an increase in blood pressure. Such interactions are more likely with the use of non-selective beta-blockers. Antihypertensive drugs, as well as other drugs with a possible antihypertensive effect (for example, tricyclic antidepressants, barbiturates, phenothiazines), can enhance the antihypertensive effect of bisoprolol.Mefloquine, when used simultaneously with bisoprolol, may increase the risk of developing bradycardia. MAO inhibitors (with the exception of MAO B inhibitors) can enhance the antihypertensive effect of beta-blockers. Simultaneous use can also lead to the development of a hypertensive crisis.