Bisoprolol-LF tab. p/o 2.5 mg №10×6

Name:
Bisoprolol-LF. Forms of release Tablets. INNBisoprolol. FTGBeta1-blocker selective.
Description:
: White film-coated tablets – dosage of 2.5 mg, blue – dosage of 5 mg, pink color – dosage of 10 mg, with a doubly convex surface, with a notch. The cross section shows two layers (for doses of 5 mg and 10 mg). Composition One tablet contains: active substance – bisoprolol fumarate – 2.5 mg; 5 mg or 10 mg; excipients – microcrystalline cellulose, calcium hydrophosphate dihydrate, corn starch, anhydrous colloidal silicon dioxide, magnesium stearate, sodium starch glycolate (type A), opad-rai II (including polyvinyl alcohol, partially hydrolyzed, talc, macrogol 3350, coloring white pigment (contains titanium dioxide E 171) – for a dosage of 2.5 mg, coloring pigment pink (contains titanium dioxide E 171, carmine E 120, indigo carmine E 132, iron oxide black E 172) – for a dosage of 10 mg or coloring blue pigment (contains titanium dioxide E 171, indigo carmine E 132, yellow quinoline E 104) – for a dosage of 5 mg. Pharmacotherapeutic group Selective beta-blockers. ATC code: C07AB07 activity.It has only a slight affinity for beta2-adrenergic ptoram smooth muscles of the bronchi and blood vessels, as well as to beta2-adrenergic receptors involved in the regulation of metabolism. Therefore, bisoprolol generally does not affect airway resistance and metabolic processes, which involve beta2-adrenergic receptors. 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 appointment of bisoprolol 1 time per day, its therapeutic effect persists for 24 hours due to the 10-12-hour half-life from blood plasma. As a rule, the maximum reduction in blood pressure (BP) is achieved 2 weeks after the start of treatment. With a single use in patients with coronary heart disease (CHD), bisoprolol reduces heart rate and stroke volume of the heart and, as a result, reduces cardiac output and oxygen consumption. With long-term administration, initially increased total peripheral vascular resistance decreases. A decrease in plasma renin activity is considered as one of the mechanisms of the antihypertensive action of beta-blockers. Bisoprolol reduces the activity of the sympathoadrenal system (SAS) by blocking the beta1-adrenergic receptors of the heart. This leads to a slowdown in the contraction of the heart and a decrease in contractility, and, as a result, to a decrease in oxygen consumption. The reduction in oxygen consumption is a desirable effect of therapy in patients with angina pectoris as a manifestation of CAD. Pharmacokinetics Absorption and distribution. Absorption – 80-90%, food intake does not affect absorption. Cmax in blood plasma is observed after 1-3 hours. Communication with blood plasma proteins is about 30%. It passes through the BBB and the placental barrier to a small extent, in small amounts it is excreted in breast milk. Metabolism and excretion. 50% of the dose is metabolized in the liver to form inactive metabolites. T½ – 10-12 hours. About 98% is excreted in the urine – 50% unchanged, less than 2% – with bile. Indications for use For a dosage of 2.5 mg. Treatment of compensated chronic heart failure with impaired left ventricular systolic function, in addition to therapy with angiotensin-converting enzyme (ACE) inhibitors, diuretics, and cardiac glycosides. For dosages of 5 and 10 mg. Arterial hypertension, ischemic heart disease (stable angina pectoris). Contraindications – hypersensitivity to bisoprolol or to any of the excipients of the drug; – acute heart failure or chronic heart failure in a state of decompensation, when intravenous inotropic therapy is required; – cardiogenic shock; – atrioventricular block II or III degree (in the absence of an artificial pacemaker); – sinus node weakness syndrome; – sinoatrial blockade; – symptomatic bradycardia (heart rate less than 60 beats per minute); – arterial hypotension (systolic blood pressure below 100 mm Hg); – severe form of bronchial asthma or chronic obstructive pulmonary disease; – severe forms of occlusive disorders of the peripheral circulation, Raynaud’s disease; – untreated pheochromocytoma; – metabolic acidosis. Dosage and administration Arterial hypertension and stable angina Doses. Treatment with the drug must begin with low doses and then gradually increase the daily dose. In all cases, the regimen and dose is selected by the doctor for each patient individually, in particular, taking into account the heart rate and the patient’s condition. Arterial hypertension The recommended dose is 5 mg bisoprolol once a day. With mild arterial hypertension (diastolic blood pressure up to 105 mm Hg), a dose of 2.5 mg may be sufficient to adequately control the disease. If necessary, the dose can be increased to 10 mg once a day. Further increase in dose is possible only in exceptional cases. The maximum recommended dose is 20 mg once daily. Ischemic heart disease (stable angina) The recommended dose is 5 mg bisoprolol once a day. If necessary, the dose can be increased to 10 mg once a day. Further increase in dose is possible only in exceptional cases. The maximum recommended dose is 20 mg once daily. Chronic heart failure The standard treatment regimen for chronic heart failure (CHF) includes the use of an ACE inhibitor (or angiotensin II receptor antagonists in case of intolerance to ACE inhibitors), a beta-blocker, diuretics, and, when necessary, cardiac glycosides. At the beginning of treatment with the drug, patients should be in a stable condition (without acute insufficiency). It is recommended that the attending physician has experience in the treatment of CHF. During the titration phase or after it, a temporary worsening of the course of heart failure, arterial hypotension or bradycardia may occur. Doses. Treatment of CHF with Bisoprolol requires a mandatory titration phase. Treatment with bisoprolol should begin with a gradual increase in dose according to the following scheme: 1.25 mg once a day for 1 week. If well tolerated, increase to 2.5 mg once daily for the next week. If well tolerated, increase to 3.75 mg once daily for the next week. If well tolerated, increase to 5 mg once daily for the next 4 weeks. If well tolerated, increase to 7.5 mg once daily for the next 4 weeks, if well tolerated, increase to 10 mg once daily as maintenance therapy. The maximum recommended dose is 10 mg once daily. During the titration phase, close monitoring of vital signs (heart rate, blood pressure) and symptoms of progression of heart failure is necessary. Symptoms may appear as early as the first day after the start of therapy. Adjustment of treatment In case of poor tolerance of the maximum recommended dose, a gradual dose reduction should be considered. In the event of a temporary worsening of the course of heart failure, arterial hypotension or bradycardia, it is recommended to reconsider the dosage of concomitant therapy drugs. You may also need to temporarily reduce the dose of bisoprolol or cancel it. After stabilization of the patient’s condition, the possibility of re-appointment and / or titration of the dose of bisoprolol with its increase should always be considered. When deciding to stop taking, a gradual dose reduction is recommended, since abrupt withdrawal can lead to an acute impairment of the patient’s condition. Treatment of CHF with bisoprolol is usually long-term. Patients with impaired hepatic or renal function In patients with impaired hepatic or renal function of mild or moderate degree, dose adjustment is usually not required in the treatment of arterial hypertension and coronary artery disease. With severe renal dysfunction (creatinine clearance less than 20 ml / min.) And in patients with severe liver disease, the maximum daily dose should not exceed 10 mg. Experience with the use of bisoprolol in patients on dialysis is limited. There are no data indicating the need to change the dosing regimen. Information regarding the pharmacokinetics of bisoprolol in patients with CHF with concomitant impaired liver or kidney function is not available. In this regard, increasing the dose in these groups of patients should be carried out with additional precautions. Elderly patients Dose adjustment is not required in elderly patients. Children Due to the lack of experience with the use of bisoprolol in children, its administration to patients under 18 years of age is not recommended. Method of application Bisoprolol tablets should be taken once a day in the morning. May be taken with food. Tablets should be swallowed with a small amount of liquid, without chewing. Duration of treatment for all indications for use The duration of treatment is not limited and depends on the cause and severity of the disease. Treatment with bisoprolol should not be interrupted suddenly, especially in patients with coronary artery disease, as abrupt withdrawal can lead to an acute impairment of the patient’s condition. If it is necessary to stop treatment, the daily dose should be reduced gradually (for example, halving at weekly intervals). Side effects Side effects are classified by frequency of occurrence: very often (> 1/10), often (> 1/100, <1/10), sometimes (> 1/1000 and <1/100), rarely (> 1/10000 and <1/1000), very rarely (<1/10000). From the nervous system. Often: dizziness, headache (especially at the beginning of treatment, usually disappear within 1-2 weeks). Sometimes: sleep disturbances, depression. Rarely hallucinations, paresthesias. From the organs of vision. Rare: lacrimation disorder (take into account when wearing contact lenses). Very rare: conjunctivitis. From the hearing organs. Rare: hearing disorders. From the side of the cardiovascular system. Very common: bradycardia (in patients with heart failure). Often: a feeling of coldness or immobility of the limbs, signs of worsening of the course of heart failure at the beginning of treatment (in patients with chronic heart failure). Sometimes: violations of atrioventricular conduction (in patients with arterial hypertension and coronary heart disease), orthostatic hypotension. From the respiratory system. Sometimes: bronchospasm in patients with a history of bronchial asthma and chronic obstructive airways disease. Rare: allergic rhinitis. From the gastrointestinal tract. Often: nausea, vomiting, diarrhea, constipation. From the side of the liver. Rarely: metabolic disorders (increased blood triglycerides), increased activity of liver enzymes in blood plasma (ACT, ALT), hepatitis. From the skin and musculoskeletal system. Sometimes: muscle weakness, convulsions. Rarely: hypersensitivity reactions (itching, excessive sweating, rashes). Very rare: hair loss, in the treatment of beta-receptor blockers, there may be a worsening of the condition of patients with psoriasis in the form of a psoriatic rash. From the genitourinary system. Rarely: violation of potency. General disorders. Often: asthenia (in patients with chronic heart failure), fatigue (especially at the beginning of treatment, usually mild and disappears within 1-2 weeks). Sometimes: asthenia (in patients with arterial hypertension and coronary heart disease). OverdoseSymptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV blockade, marked decrease in blood pressure, chronic heart failure, cyanosis of fingernails or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions. Treatment: gastric lavage and administration of adsorbents; symptomatic therapy: with developed AV blockade - in / in the introduction of 1-2 mg of atropine, epinephrine or setting up a temporary pacemaker; with ventricular extrasystole - lidocaine (class IA 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, if ineffective - the introduction of epinephrine, dopamine, dobutamine; in heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam; with bronchospasm, beta-agonists are inhaled. Hypoglycemia: intravenous administration of glucose. Bisoprolol is poorly excreted from the body during dialysis. Precautions: Treatment with compensated chronic heart failure begins with dose titration. The initiation of treatment requires constant monitoring. In the absence of absolute indications, drug therapy should not be stopped abruptly, this may lead to a transient deterioration in cardiac function. This is especially true for patients with ischemic heart disease. There is no experience of therapeutic use of the drug in patients with heart failure with such diseases and conditions: - insulin-dependent diabetes mellitus (type I); - severe renal dysfunction; - severe liver dysfunction; - restrictive cardiomyopathy; - hemodynamically significant organic lesion of the heart valves; - myocardial infarction that has developed within the last three months. Bisoprolol should be used with caution in: - diabetes mellitus with marked fluctuations in blood glucose levels; the effects of bisoprolol (eg tachycardia, palpitations or profuse sweating) may mask the symptoms of hypoglycemia; - strict fasting; - specific hyposensitizing therapy. Like other beta-blockers, bisoprolol is able to increase the body's sensitivity to allergens and increase anaphylactic reactions. Adrenaline therapy does not always provide the desired therapeutic effect; - atrioventricular block I degree; - Prinzmetal's angina; - occlusive lesions of peripheral arterial vessels. There may be an increase in clinical manifestations (more often at the beginning of therapy with bisoprolol). Patients with psoriasis and patients with a history of psoriasis should only receive beta-blockers (including bisoprolol) after a careful benefit/risk assessment. Therapy with the drug can mask the symptoms of thyrotoxicosis. In the treatment of patients with pheochromocytoma, bisoprolol therapy should not be started before the use of alpha-blockers. Blockade of beta-adrenergic receptors reduces the likelihood of developing cardiac arrhythmias and myocardial ischemia during the induction of anesthesia and tracheal intubation, as well as in the postoperative period. Today it is recommended to continue maintenance therapy with beta-blockers in the preoperative period. The anesthesiologist should be aware that the patient is receiving beta-blockers, since the interaction of beta-blockers with other drugs can lead to the development of bradyarrhythmias, inhibition of reflex tachycardia and suppression of the reflex ability to compensate for blood loss. If it is considered that therapy with beta-blockers should be stopped in the preoperative period, then the withdrawal should be carried out gradually and completed approximately 48 hours before anesthesia. Patients with bronchial asthma. Although selective beta1-blockers may have a lesser effect on lung function than non-selective beta-blockers, their use, like any other beta-blocker, should be avoided in patients with obstructive airway disease, unless clear clinical need. When such grounds exist, bisoprolol may be used with caution. In patients with obstructive airways disease, treatment with bisoprolol should be started at the lowest possible dose, and patients should be closely monitored for new symptoms (eg, shortness of breath, exercise intolerance, cough). In bronchial asthma or other chronic obstructive pulmonary diseases that can cause such symptoms, the simultaneous use of bronchodilators is indicated. In patients with bronchial asthma, there may be a periodic increase in airway resistance, which may require a higher dose of beta2-adrenergic agonists. The combination of bisoprolol with calcium antagonists such as verapamil or diltiazem, with class I antiarrhythmic drugs and with centrally acting antihypertensive agents is usually not recommended (for more information, see the section "Interaction with other drugs"). The use of bisoprolol may cause positive results during doping control. Use during pregnancy and lactation Pregnancy. The pharmacological effects of bisoprolol may have harmful effects on pregnancy and/or the fetus/newborn. In general, beta-adrenergic blockers reduce placental blood flow, which can lead to growth retardation, fetal death, abortion, or preterm birth. Adverse reactions (eg, hypoglycemia and bradycardia) may occur in the fetus and newborn. If treatment with a beta-blocker is necessary, it is desirable that it be a selective beta1-blocker. Bisoprolol should not be used during pregnancy unless there is a clear clinical need for it. If treatment with bisoprolol is regarded as necessary, uteroplacental blood flow should be monitored, as well as the growth and development of the fetus should be monitored. In the event of adverse effects on pregnancy and/or the fetus, alternative treatments should be considered. The newborn should be carefully examined after delivery. In the first three days of life, symptoms of bradycardia and hypoglycemia may occur. Lactation. Breastfeeding is not recommended during therapy with bisoprolol. Children The drug is not recommended for the treatment of children. Influence on the ability to drive vehicles and control mechanisms In individual cases, at the beginning of treatment and when replacing the drug, as well as when interacting with alcohol, the ability to drive a car or work with mechanisms may be reduced. Interactions with other medicinal products Combinations not recommended Class I antiarrhythmic drugs (eg quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone). There may be an increase in the effect on AV conduction time and an increase in the negative inotropic effect. Calcium channel blockers from the verapamil group and, to a lesser extent, from the diltiazem group. Negative effect on contractility and AV conduction. The introduction of verapamil to patients receiving therapy with beta-blockers may be accompanied by the development of severe arterial hypotension and AV blockade. Centrally acting antihypertensives (eg clonidine, methyldopa, moxonidine, rilmenidine). The simultaneous use of centrally acting antihypertensive drugs can further reduce the sympathetic tone of the central nervous system and, as a result, reduce heart rate and cardiac output, and also cause vasodilation. Abrupt discontinuation of therapy, especially in conditions of prior withdrawal of beta-blockers, may increase the risk of developing a rebound effect (arterial hypertension). Combinations to be used with caution Dihydropyridine-type calcium channel blockers (eg felodipine and amlodipine). It cannot be ruled out that concomitant use may increase the risk of arterial hypotension and a decrease in ventricular pumping function in patients with heart failure. Class III antiarrhythmic drugs (eg, amiodarone). There may be an increased effect on AV conduction time. Parasympathomimetics. Simultaneous use may increase the time of AV conduction and increase the risk of bradycardia. Beta-blockers intended for topical use (for example, eye drops for the treatment of glaucoma). It is possible to potentiate the systemic effects of bisoprolol. Insulin and oral sugar-lowering drugs. Strengthening the hypoglycemic effect. Blockade of beta-adrenergic receptors may mask the symptoms of hypoglycemia. Anesthetics. Inhibition of reflex tachycardia and increased risk of arterial hypotension. Digitalis preparations. Increase in atrioventricular conduction time, decrease in heart rate. Non-steroidal anti-inflammatory drugs (NSAIDs). May suppress the hypotensive effects of bisoprolol. Beta-sympathomimetics (eg isoprenaline, dobutamine). The combination with bisoprolol can suppress the effects of both drugs. Sympathomimetics acting on both beta- and alpha-adrenergic receptors (for example, norepinephrine, epinephrine). The combination with bisoprolol may enhance the alpha-adrenergic receptor-mediated vasoconstriction effect of these drugs, which leads to an increase in blood pressure levels and exacerbation of intermittent claudication. Such an interaction is more likely with the use of non-selective beta-blockers. Combinations requiring clarification Mefloquine, when used simultaneously with bisoprolol, may increase the risk of developing bradycardia. Monoamine oxidase (MAO) inhibitors (with the exception of MAO-B inhibitors) may increase the hypotensive effect of beta-blockers, but may also increase the risk of developing a hypertensive crisis. The concomitant use of antihypertensive drugs or other drugs that lower blood pressure (for example, tricyclic antidepressants, barbiturates, phenothiazines) may increase the risk of arterial hypotension. Upakovka10 tablets in a blister pack of PVC film and aluminum foil. 3 or 6 blister packs together with a leaflet in a pack of cardboard (packaging No. 10 × 3, No. 10 × 6). Storage conditions In a place protected from light and moisture, at a temperature not exceeding 25 ºС. Keep out of the reach of children. Shelf life 2 years. Do not use after the expiration date. Conditions for dispensing from pharmacies By prescription. Buy Bisoprolol-LF tab. p / o 2.5 mg No. 10x6 Price for Bisoprolol-LF tab. p / o 2.5 mg No. 10x6 Instructions for use for Bisoprolol-LF tab. p/o 2.5 mg №10x6