Description
Release form
Film-coated tablets, 5 mg and 10 mg.
10 tablets in blister packs of a film of polyvinyl chloride and aluminum foil.
For 3, 5 or 10 blister packs with instructions for use in a cardboard box.
Packing
30 pcs.
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 degree II-III block block, without electrocardiosis Sinus node weakness syndrome bradycardia (heart rate less than 60 beats / min) Prinzmetal angina pectoris cardiomegaly (without signs of heart failure) Single hypotension (systolic blood pressure less than 100 torr), especially in myocardial infarction severe bronchial asthma and chronic obstructive pulmonary disease (COPD) simultaneous reception history floctafenine, sultopride, monoamine oxidase inhibitors (MAO) with the exception of MAO type B, simultaneous intravenous administration of verapamil or diltiazem severe peripheral circulatory disorders, Raynaud’s pheochromocytoma syndrome (without the simultaneous use of alpha-blockers) metabolic acidosis under 18 years of age (efficacy and safety have not been established).
Lactase deficiency, lactose intolerance, lactose / isomaltose malabsorption syndrome (the drug contains lactose).
Precautions
Severe liver failure, severe renal failure (creatinine clearance less than 20 ml / min), myasthenia gravis, thyrotoxicosis, diabetes mellitus (can mask the symptoms of hypoglycemia), aggravated allergic history, AV block I degree, depression (including history ), psoriasis, bronchial asthma, COPD, peripheral circulatory disorders, strict diet.
Use during pregnancy and lactation
Use Biprol during pregnancy and lactation is possible if the benefit to the mother outweighs the risk of side effects in the fetus and the baby.
Special instructions
Treatment with the drug is usually long-term.
Before treatment, a study of the function of external respiration in patients with a history of bronchopulmonary history is recommended. Patients with bronchospastic diseases can be prescribed bisoprolol in case of intolerance and / or ineffectiveness of other antihypertensive drugs, and the dose of the drug should be strictly monitored. An overdose is dangerous for the development of bronchospasm.and plasma glucose in patients with diabetes mellitus (1 time in 4-5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months). The patient should be taught the method of calculating heart rate and instructed on the need for medical advice if it is reduced to less than 60 beats / min.
In approximately 20% of patients with angina pectoris, beta-blockers are ineffective. 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 using contact lenses should consider that tear fluid production may be reduced during treatment.
When used in patients with pheochromocytoma, there is a risk of developing paradoxical hypertension (unless effective alpha adrenoblockade has been previously achieved).
With thyrotoxicosis, bisoprolol may mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can enhance symptoms.
With diabetes, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels.
With the simultaneous use of clonidine, its administration 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 of the usual doses of epinephrine against the background of a burdened allergic history.
If it is necessary to carry out planned surgical intervention, the drug
cancellation is carried out 48 hours before the start of general anesthesia. If the patient took the drug before surgery, he should choose a drug for general anesthesia with minimal negative inotropic effect.
Reciprocal vagus nerve activation can be eliminated by intravenous administration of atropine (1-2 mg).
Catecholamine-lowering drugs (such as reserpine) can enhance the effects of beta-blockers, so patients taking these drug combinations should be under the constant supervision of a doctor to detect arterial hypotension or bradycardia.
In the case of elderly patients with increasing bradycardia (less than 60 beats / min), arterial hypotension (systolic blood pressure below 100 mmHg), AV block, bronchospasm, ventricular arrhythmias, severe liver and kidney function impairment, it is necessary to reduce the dose or stop treatment.
Do not abruptly interrupt bisoprolol treatment because of the danger of developing severe arrhythmias and myocardial infarction. Cancellation 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 discontinue therapy (with a gradual dose reduction) in case of development of depression caused by taking the drug. The drug should be discontinued before examining the content of catecholamines in the blood and urine, normetanephrine and vanillinindic acid, antinuclear antibody titer.
Effect on the ability to drive vehicles and work with mechanisms
During the treatment period, care must be taken when driving vehicles and performing other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
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 8,000 mg / 11,000 mg silicon colloidal 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.
Dosage and administration
The drug Biprol is taken orally, in the morning, 1 time per 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 regimen and dose are selected by the doctor individually for each patient, in particular, taking into account the heart rate and the patient’s condition.
With arterial hypertension and coronary heart disease, the drug is prescribed 5 mg 1 time per day. If necessary, increase the dose 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.
In elderly patients, dose adjustment is not required.
Side effects
The frequency of the following side effects is indicated according to the WHO classification: very often – more than 10% often – more than 1% and less than 10% infrequently – more than 0.1% and less
1% rarely – more 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 – fatigue, asthenia, dizziness, headache. Typically, these phenomena develop at the beginning of treatment, as a rule, they are slightly expressed and pass within 1-2 weeks infrequently – sleep disturbances, depression rarely – nightmares, hallucinations, loss of consciousness.
From the cardiovascular system: very often – bradycardia, palpitations often – a pronounced decrease in blood pressure (especially in patients with heart failure), manifestations of angiospasm (increased peripheral circulatory disorders, sensation of coldness in the extremities (paresthesia) infrequently – violation of AV conduction (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, aggravated
of CHF 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, dry oral mucosa rarely – hepatitis, increased activity Liver transaminases (alanine aminotransferase, aspartate aminotransferase), increased bilirubin concentration.
From the respiratory system: infrequently – laryngo- and bronchospasm in patients with
bronchial asthma or obstructive airways diseases rarely –
allergic rhinitis, nasal congestion.
From the musculoskeletal system: infrequently – muscle weakness, cramps in the calf muscles, arthralgia.
On the part of the sensory organs: rarely – visual impairment, decreased lacrimation (to be considered when wearing contact lenses), hearing impairment, taste change
very rarely – dry and sore 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 – impaired potency, weakening of libido.
On the part of the immune system: rarely – the appearance of antinuclear antibodies with unusual clinical symptoms of lupus-like syndrome, which disappear after treatment.
Allergic reactions: rarely – flushing of the skin, itchy skin, skin rash, urticaria.
Laboratory indicators: rarely – hypertriglyceridemia very rarely – thrombocytopenia, agranulocytosis, leukopenia.
Other: rarely – withdrawal syndrome (increased angina attacks, increased blood pressure).
Drug Interactions
Flactafenin. In the case of shock or arterial hypotension due to flactaphenin, beta-blockers cause a decrease in compensatory cardio-vascular reactions (combined use is contraindicated).
Suloprid. Due to the additive effect, the development of severe bradycardia is possible (combined use is contraindicated).
MAO inhibitors. The simultaneous use is not recommended (with the exception of MAO type B), since there is a high probability of a significant increase in antihypertensive effect. The 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. During treatment with Biprol, intravenous administration of verapamil or diltiazem, other antiarrhythmic drugs is contraindicated. Due to the synergism of action, a sharp decrease in blood pressure, impaired automatism (severe bradycardia, sinus node stop), impaired AV conduction, and 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 drugs (e.g., quinidine, disopyramide, lidocaine, phenytoin flecainide, propafenone) with simultaneous use, a decrease in
AV conduction and myocardial contractility is possible (combination with bisoprolol should be avoided).
Class III antiarrhythmic drugs (e.g., amiodarone). When combined with bisoprolol, contractility, automatism, and conduction may be impaired due to inhibition of sympathetic compensatory mechanisms (this combination should be avoided).
Antihypertensive agents of central action (clonidine, apraclonidine, alpha – methyldopa, guanfancin, moxonidine, rilmenidine). When used together, the increased risk of developing severe bradycardia, stopping the sinus node, impaired AV conduction, a sharp decrease in blood pressure, 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 with a sharp abolition of the central antihypertensive drug.
Cardiac glycosides. Decreased heart rate, impaired conduction.
Topical beta-blockers (for example, eye drops for the treatment of glaucoma) can enhance the systemic effect of bisoprolol (lowering blood pressure, decreasing heart rate).
Calcium channel blockers (e.g., nifedipine). An excessive decrease in blood pressure is possible.
Parasympathomimetics. When used together, the risk of developing bradycardia.
Mefloquine. Joint use with bisoprolol increases the risk of developing bradycardia (additive effect).
Phenytoin when administered intravenously, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.
Concomitant use 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 affecting beta and alpha adrenoreceptors (for example, norepinephrine, epinephrine) can enhance the vasoconstrictor effect of these drugs, which occurs with the participation of alpha adrenergic receptors, leading to an increase in blood pressure. Such interactions are more likely when using non-selective beta-blockers.
Bisoprolol can change the effectiveness of insulin and hypoglycemic agents for oral administration, mask the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).
Bisoprolol reduces the clearance of lidocaine and xanthines (except diphillin) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking.
Non-steroidal anti-inflammatory drugs (sodium ion retention and prostaglandin synthesis blockade by the kidneys), glucocorticosteroids and estrogens (sodium ion retention) weaken the antihypertensive effect.
Diuretics, sympatholytics, hydralazine and other antihypertensive drugs. The risk of an excessive decrease in blood pressure.
Bisoprolol prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.
Tri- and tetracyclic antidepressants, antipsychotic drugs (antipsychotics), ethanol, sedatives and hypnotics – when combined with bisoprolol, an increase in central nervous system depression.
Non-hydrogenated ergot alkaloids increase the risk of peripheral circulation disorders.
Ergotamine increases the risk of developing peripheral circulatory disorders.
Sulfasalazine increases the concentration of bisoprolol in plasma.
Rifampicin decreases the 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 administration increase the risk of anaphylactic reactions.
Overdose
Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV blockade, severe blood pressure, acute heart failure, hypoglycemia, acrocyanosis, difficulty breathing, bronchial obstruction.
Treatment: gastric lavage, appointment of adsorbing agents, symptomatic therapy. In severe bradycardia – intravenous atropine. If the effect is insufficient, it is possible to enter with caution the positive chronotropic action with caution. Occasional staging of an artificial rhythm driver may be required.
With advanced AV blockade, intravenous administration 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 position of Trendelenburg if there is no evidence of pulmonary edema – intravenous administration of plasma-replacement solutions, with their inefficiency – the introduction of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and elimination of arterioles).
In hypoglycemia, intravenous dextrose (glucose) may be indicated. In case of heart failure – cardiac glycosides, diuretics. In convulsions – intravenous diazepam. In bronchospasm – inhalation beta2-adrenomimetics.
Storage Conditions
In a dry, dark place at a temperature not exceeding 25 ° C.
Shelf life
3 years.
Deystvuyushtee substance
Bisoprolol
dosage form
tablets
Appointment
Appointment
Adult
