Expiration date: 01/2025
Release form and composition:
Tablets, coated yellow, biconvex in cross section are visible two layers, the inner layer white or white with a barely noticeable kremovatym color.
1 tablet contains bisoprolol fumarate 5 mg
Excipients: cellulose microcrystalline, ludipress, corn starch, silicon dioxide colloidal (Aerosil), kollidon CL (crospovidone), magnesium stearate.
The composition of the shell: titanium dioxide, polyethylene glycol 4000, hydroxypropyl methylcellulose (hypromellose), talc, tropeolin O.
10 PCs. - packaging sells contoured (3) - packs cardboard.
10 PCs. - packaging sells contoured (5) - packs of cardboard.
10 PCs. - packaging sells contoured (10) - packs of cardboard.
100 PCs banks polymer (1) - packs of cardboard.
Tablets, film-coated dark yellow color, lenticular in cross section are visible two layers, the inner layer white or white with a barely noticeable kremovatym color.
1 tablet contains bisoprolol fumarate 10 mg
Excipients: cellulose microcrystalline, ludipress, corn starch, silicon dioxide colloidal (Aerosil), kollidon CL (crospovidone), magnesium stearate.
The composition of the shell: titanium dioxide, polyethylene glycol 4000, hydroxypropyl methylcellulose (hypromellose), talc, tropeolin O.
10 PCs. - packaging sells contoured (3) - packs cardboard.
10 PCs. - packaging sells contoured (5) - packs of cardboard.
10 PCs. - packaging sells contoured (10) - packs of cardboard.
100 PCs banks polymer (1) - packs of cardboard.
Pharmacological action:
Selective beta1-blocker without intrinsic sympathomimetic activity, has membrane stabilizing properties.
Reduces plasma renin activity, reduces the need heart of oxygen, reduces the heart rate at rest and during exercise. It has hypotensive, antiarrhythmic and antianginal effects. When used in low doses blocks beta1-adrenergic receptors of the heart, reduces catecholamines stimulated camp formation from ATP, reduces intracellular current of calcium ions, has a negative Chrono-, dromo-, batmo - and inotropic action, oppressing conductivity and anxiety, decreases airway diseases.
When used in high doses, it has a beta2-adrenoblokirtee action.
The CSO at the start of application of the drug (in the first 24 h) increases (as a result of reciprocal increase in activity of apha-adrenergic receptors and eliminate stimulation of beta2-adrenergic receptors), then through 1-3 day returns to the source, and with long-term use of the drug is reduced.
Hypotensive effect is associated with a decrease in minute volume of blood, sympathetic stimulation of peripheral vessels, decreased activity of the renin-angiotensin system (is of great significance for patients with initial hypersecretion of renin), restoring sensitivity in response to decreased blood pressure and effects on the Central nervous system. When hypertension the initial effect occurs in 2-5 days, stable in 1-2 months.
Antianginal effect is due to reduction of requirement of a myocardium for oxygen by reducing the heart rate and decrease contractility, lengthening of diastole, improved myocardial perfusion. By increasing end-diastolic pressure in the left ventricle and increase the tension of the muscle fibers of the ventricles can increase the need for myocardial oxygen, especially in patients with chronic heart failure.
Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased camp content, arterial hypertension), reduced rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing AV conduction (mainly in the antegrade and to a lesser extent, in the retrograde directions through the AV node) and on additional ways.
When used in high therapeutic doses, unlike nonselective beta-blockers, has a less pronounced effect on bodies containing beta2-adrenergic receptors (pancreas, skeletal muscle, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause the delay of sodium ions (Na+) in the body the severity of the atherogenic actions is not different from the action of propranolol. When used in high doses (200 mg or more) has a blocking effect on both subtypes of beta-adrenergic receptors mainly in the bronchi and vascular smooth muscle.
Pharmacokinetics:
Absorption and distribution
The ingestion well absorbed from the gastrointestinal tract (absorption is 80-90%) food intake does not affect absorption. C max in plasma achieved through 1-3 h. Linking blood plasma proteins is about 30%. In small amounts, permeates through GEB, placental barrier, excreted in breast milk.
Metabolism and excretion
Metabolized in liver, T1/2 - 10-12 hours Excreted by the kidneys (50% in unaltered), less than 2% is excreted in the bile.
Indications:
— arterial hypertension
— Coronary artery disease: prevention of angina attacks.
Dosing regimen:
Taken orally, in the morning, on an empty stomach tablets do not chew.
The drug is administered in a dose of 5 mg 1 times/day. If necessary, increase the dose to 10 mg 1 times/day. The maximum daily dose of 20 mg.
In patients with impaired renal function when KK less 20 ml/min or with acute human liver the maximum daily dose - 10 mg.
Side effects:
CNS and peripheral nervous system: fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia, paresthesia in the extremities (in patients with the syndrome of intermittent claudication and Raynaud's syndrome ), tremor.
On the part of the organ of vision: visual disturbances, reduced secretion of tear fluid, dryness and soreness of eyes, conjunctivitis.
From the side of cardiovascular system: sinus bradycardia, palpitations, impaired conductivity infarction, AV-blockade (up to the development of a complete transverse blockade and heart failure), arrhythmia, weakening of myocardial contractility, development (the aggravation of) chronic heart failure (swelling of ankles, feet shortness of breath), reducing AD, orthostatic hypotension, manifestation of angiospasm (increased peripheral circulatory disorders, cold lower extremities, Raynaud's syndrome), chest pain, withdrawal syndrome (increased angina, increased blood pressure).
From the digestive system: dry mucous membranes of the mouth, nausea, vomiting, abdominal pain, constipation or diarrhea, a change in the activity of liver enzymes (increased ALT and ACT), bilirubin, human liver (dark urine, yellowness of the sclera or skin, cholestasis), changing taste.
The respiratory system: nasal congestion, difficulty breathing in the appointment of high doses (loss of selectivity) and/or prone patients - laringo - and bronchospasm.
From the endocrine system: hyperglycemia (in patients with diabetes mellitus type 2), hypoglycemia (in patients, receiving insulin), hypothyroid state.
Allergic reactions: skin itching, rash, hives.
Dermatological reactions: increased sweating, hyperemia of skin, exanthema, psoriasiform skin reactions, exacerbation of psoriasis symptoms.
With the hematopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.
From the reproductive system: reduced libido, reduced potency.
Other: back pain, arthralgia, changes in the level of triglycerides.
Contraindications:
— shock (including cardiogenic)
— the collapse
— pulmonary edema
acute heart failure
— chronic cardiac insufficiency of the decompensation
— AV blockade II-III degree
— sinoatrial block
syndrome sick sinus
— expressed aetiology
— Prinzmetal's angina
— cardiomegaly (with no signs of heart failure)
— hypotension (systolic BP less than 100 mm Hg.St., especially in myocardial infarction)
— bronchial asthma and chronic obstructive pulmonary disease in anamnesis
— simultaneous reception of MAO inhibitors (except for MAO inhibitors of type B)
— late stage human peripheral blood circulation (Raynaud's disease)
— pheochromocytoma (without the simultaneous use of alpha-blockers)
— metabolic acidosis
— the age 18 years (effectiveness and safety have not been established)
— hypersensitivity to the medication and other beta-blockers.
With caution is prescribed to patients with hepatic insufficiency, chronic renal insufficiency, myasthenia gravis, thyrotoxicosis, diabetes, AV blockade degree I, depression (including in history), psoriasis, and the elderly.
Pregnancy and lactation:
The use of the drug during pregnancy and lactation is possible in the case if the benefit to the mother outweighs the risk of side effects in the fetus and child.
On the background of the use of the drug can cause intrauterine growth retardation, hypoglycemia, bradycardia in the fetus.
Special instructions:
Status monitoring of patients receiving, Bipra should include measurement of HR and AD (at the beginning of treatment - daily, then 1 once in 3-4 mo), the ECG, determination of blood glucose in patients with diabetes mellitus (1 once in 4-5 mo). In elderly patients it is recommended to monitor kidney function (1 once in 4-5 mo).
Before treatment is recommended study of respiratory function in patients with respiratory diseases in history.
It should teach the patient methods of calculating heart rate and instruct on the need of medical advice if heart rate less than 50 beats/min.
Approximately 20% of patients with angina beta-blockers are ineffective. The main reason - severe coronary atherosclerosis with the low threshold of ischemia (heart rate less than 100 beats/min) and increased end-diastolic volume of the left ventricle that violate the upper subendocardialnah blood flow.
In smokers the effectiveness of beta-adrenoblokatorov below.
Patients using contact lenses should be aware that the treatment may decrease the production of tear fluid.
When used in patients with pheochromocytoma there is a risk of paradoxical hypertension (if not previously achieved an effective blockade of the apha-adrenergic receptors).
Thyrotoxicosis, Bipra may mask certain clinical signs of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, because in such a case may increase symptoms.
Diabetes drug may mask the tachycardia, caused by hypoglycemia. Unlike nonselective beta-blockers hardly enhances insulin-induced hypoglycemia and delay recovery of the glucose concentration in the blood to normal levels.
At the same time taking clonidine its reception can be terminated only a few days after discontinuation Bipola.
Perhaps the increased severity of hypersensitivity reactions and lack of effect of conventional doses of epinephrine in patients with allergic history.
In case of the need for planned surgical treatment elimination of the drug is carried out for 48 h before General anesthesia. If the patient has taken the drug before surgery, he should choose drug for General anesthesia with minimal negative inotropic effects.
Reciprocal activation of the vagus nerve can eliminate/atropine (1-2 mg).
Medicines, reducing stocks of catecholamines (e.g. reserpine), may enhance the action of beta-adrenoblokatorov, therefore, patients, accepting such combination drugs, should be under constant supervision of a doctor to identify expressed downward AD or bradycardia.
Patients with bronchospastic conditions or diseases, you can assign a cardioselective blocker in case of intolerance and/or ineffectiveness of other antihypertensive drugs. Overdose is dangerous development of bronchospasm.
In the case of elderly patients increasing bradycardia (less 50 beats/min), expressed lower AD (systolic BP below 100 mm Hg.St.), AV-blockade, it is necessary to reduce the dose or stop the treatment.
It is recommended to discontinue therapy in the development of depression.
Do not abruptly discontinue the treatment because of the risk of severe arrhythmias and myocardial infarction. Lifting a gradually reducing the dose over 2 weeks or more (25% in 3-4 day).
The drug should be discontinued before the examination of blood and urine catecholamines, normetanephrine and vanillylmandelic acid, titles of antinuclear antibodies.
Effects on ability to drive vehicles and management mechanisms
During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and psychomotor speed reactions.
Overdose:
Symptoms: arrhythmia, ventricular arrythmia, expressed aetiology, AV-blockade, expressed lower AD, chronic heart failure, acrocyanosis, shortness of breath, bronchospasm, dizziness, fainting, seizures.
Treatment: gastric lavage, appointment of adsorbents. If necessary, symptomatic therapy: with advanced AV-blockade-in/in the introduction of atropine (1-2 mg), epinephrine or staging a temporary pacemaker with ventricular arrhythmia - lidocaine (drugs I And class does not apply). When blood pressure decrease, the patient should be in Trendelenburg position if there are no signs of pulmonary edema introducing/plasma-substituting solutions in case of inefficiency - epinephrine, dopamine, dobutamine (for maintaining chronotropic and inotropic actions and resolve expressed lower AD). In heart failure prescribed cardiac glycosides, diuretics, glucagon in convulsions – in/diazepam with bronchospasm - beta2-agonists inhalation.
Drug interactions:
The application of the therapy Bipolor allergens, used for immunotherapy, or extracts of allergens for skin tests increases the risk of severe systemic allergic reactions or anaphylaxis.
While the use of bisoprololum radiopaque iodine-containing drugs for at/in the introduction increases the risk of anaphylactic reactions.
When concomitant administration with phenytoin bisoprololum for/in the introduction, drugs for inhalation General anesthesia (derivatives of hydrocarbons) increase the intensity of cardiodepressive actions and reduce the likelihood of AD.
While the use of bisoprolol modifies the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, the AD).
While the use of bisoprolol reduces the clearance of lidocaine and xantinov (except difillina) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of Smoking.
The hypotensive effect of bisoprolol reduce NSAIDs (delay of Na+ and the blockade of prostaglandin synthesis by the kidney), corticosteroids and estrogens (delay of Na+ions).
With simultaneous use of cardiac glycosides, methyldopa, reserpine, and guanfacine, calcium channel blockers (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or exacerbating bradycardia, AV-blockade, heart failure and heart failure.
While the use of bisoprolol nifedipine can lead to significant reduction of HELL.
While the use of bisoprololum diuretics, clonidine, sympatholytic, hydralazine, and other antihypertensive medicines can cause excessive reduction of HELL.
Bisoprolol prolongs the action of non-depolarizing muscle relaxants and anticoagulant effect of coumarins.
Three - and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics drugs increase inhibitory effect of bisoprolol on the Central nervous system.
Not recommended simultaneous application of bisoprolol with MAO inhibitors because of significant increase gipotenzivnogo actions (the interval between receiving MAO inhibitors and bisoprolol must be not less than 14 days).
While the use of bisoprololum non-hydrogenated ergot alkaloids, ergotamine increases risk of peripheral circulatory disorders.
While the use of sulfasalazine bisoprolol improves concentration in plasma.
With simultaneous use of rifampicin reduces T1/2 of bisoprolol.
Terms and conditions of storage:
List B. the Drug should be stored out of the reach of children, dry place at temperature not exceeding 25°C. shelf Life - 3 years.
