Biprol, 5 mg 50 pcs.
€4.75 €4.22
A selective beta1-adrenoblocker with no sympathomimetic activity of its own, has no membrane stabilizing effect.
It has antihypertensive, antiarrhythmic and antianginal action.
By blocking in low doses beta1-adrenoreceptors of the heart it decreases stimulated by catecholamines formation of cyclic adenosine monophosphate from adenosine triphosphate, decreases intracellular ion flux.br>
calcium, has negative chrono-, dromo-, batmo- and inotropic effects, reduces atrioventricular (AV) conduction and excitability.
In case of therapeutic dose it has beta2-adrenoblocking action.
The total peripheral vascular resistance at the beginning of the drug administration (during the first 24 hours) increases (as a result of reciprocal increase of activity of alpha-adrenoreceptors and elimination of
stimulation of beta2-adrenoreceptors) that after 1-3 days returns to the initial level, and decreases after the long-term administration.
Antihypertensive effect is associated with reduction of the minute blood volume, sympathetic stimulation of peripheral vessels, reduction of renin-angiotensin-aldosterone system activity (of great importance for patients with
initial renin hypersecretion), restoration of sensitivity of aortic arch baroreceptors (there is no increase of their activity in response to a decrease in blood pressure) and the effect on the central nervous system.
In case of arterial hypertension the effect is developed in 2-5 days, its stable effect – in 1-2 months.
Antianginal action is determined by the decrease of myocardial oxygen demand due to slow heart rate and decreased myocardial contractility, prolongation of diastole, improvement of myocardial perfusion.
By increasing end diastolic pressure in the left ventricle and increasing ventricular muscle fiber stretch may increase myocardial oxygen demand, especially in patients with chronic heart failure (CHF).
Antiarrhythmic action is due to the elimination of arrhythmogenic factors (tachycardia, increased sympathetic nervous system activity, increased cyclic adenosine monophosphate,
arterial hypertension), decreased rate of spontaneous excitation of sinus and ectopic pacemakers, and deceleration of AV conduction (predominantly antegrade and, to a lesser extent, retrograde) through the atrioventricular node and along accessory pathways.
In contrast to non-selective beta-adrenoblockers, when administered in medium therapeutic doses it has less pronounced effect on organs containing beta2-adrenoreceptors (pancreas, skeletalbr>
muscles, smooth muscles of peripheral arteries, bronchi and uterus) and carbohydrate metabolism; does not cause sodium ion retention in the body.
Pharmacokinetics
Absorption. Absorption is 80-90%, food intake does not affect absorption of the drug. Maximal concentration in blood plasma is observed after 1-3 hours.
Bioavailability is about 90%. Binding with blood plasma proteins – about 30%.
Distribution.
Distribution volume is 3.5 l/kg. Permeability through the blood-brain and placental barriers is low.
Metabolism. Metabolized in the liver with the participation of CYP3A4 (up to 95%) and CYP2D6 isoenzymes. The e
ffekt “primary passage” through the liver is insignificant (about 10%). Bisoprolol biotransformation is not accelerated in patients with thyroid hyperfunction.
Excretion.
Total clearance is 15.6±3.2 l/hour, renal clearance is 9.6±1.6 l/hour.
Balanced clearance of bisoprolol is determined by the balance between its excretion through the kidneys in unchanged form (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. Half-life period is 9-12 hours.
Dependence of bisoprolol pharmacokinetics on dose is linear.
Pharmacokinetics of bisoprolol is stable, independent of patient age and sex.
Pharmacokinetics in special clinical cases
Renal insufficiency. In case of marked renal function impairment (creatinine clearance less than 20 ml/min) and in patients with anuria half-life period may increase more than 2 times.
Hepatic insufficiency.
In case of severe hepatic insufficiency half-life period is increased up to 13-15 hours.
Chronic heart failure.
In patients with chronic heart failure (functional class III according to the NYHA classification), the plasma concentration of bisoprolol is higher than in healthy volunteers, and the half-life is increased to 17 hours.
Indications
Heart failure, Heart palpitations, Tachycardia, Cardialgia (pain in the heart), Hypertension (high blood pressure), Arrhythmia
- Arterial hypertension.
- Ischemic heart disease: prevention of attacks of stable angina.
.
Active ingredient
Bisoprolol
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 silica 0,500 mg/ 0,600 mg;
Crospovidone (Collidon CL) 1,000 mg/ 1,250 mg;
Magnesium stearate 1,000 mg/ 1,250 mg;
Cover:
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.
How to take, the dosage
Biprol is taken orally, in the morning, once a day with some liquid, before, during or after breakfast.
Tablets should not be chewed or crushed into powder. In all cases the mode of administration and the dose are determined individually by the physician taking into account the heart rate and the patient’s condition.
In arterial hypertension and coronary heart disease the drug is administered by 5 mg once a day.
If necessary the dose is increased up to 10 mg once a day.
In treatment of arterial hypertension and angina pectoris the maximum daily dose is 20 mg 1 time per day.
For patients with severe renal dysfunction (creatinine clearance less than 20 ml/min) or with severe liver dysfunction the maximum daily dose is 10 mg 1 time per day.
Increasing the dose in such patients should be done with extreme caution.
In elderly patients no dose adjustment is required.
Interaction
Floktaphenin. In case of shock or arterial hypotension caused by floktafenin, beta-adrenoblockers cause reduction of compensatory cardiovascular reactions (co-administration is contraindicated).
Sultopride. Due to the additive effect, pronounced bradycardia is possible (combined use is contraindicated).
MAO inhibitors. Concomitant use is not recommended (except for MAO type B), because there is high probability of significant increase of antihypertensive effect.
Treatment interval between 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 or other antiarrhythmic drugs is contraindicated.
Due to synergistic action sharp decrease of arterial pressure, automatism disorders (expressed bradycardia, sinus node arrest), AV conduction disorders, cardiac insufficiency are possible.
If it is necessary to prescribe this combination it is required careful clinical and electrocardiographic monitoring of patients, especially of the elderly and at the beginning of treatment.
Antirhythmic agents of class I (e.g., quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone) when used simultaneously may decrease
AV conduction and myocardial contractility (avoid combination with bisoprolol).
Antiarrhythmic agents of class III (e.g., amiodarone).
When combined with bisoprololol impairment of contractility, automaticity and conduction due to inhibition of sympathetic compensatory mechanisms (this combination should be avoided).
Antihypertensive agents of central action (clonidine, apraclonidine, alpha – methyldopa, guanfancine, moxonidine, rilmenidine).
If used concomitantly the risk of significant bradycardia, sinus node arrest, AV dysfunction, rapid decrease of blood pressure, heart failure increases (synergistic effect).
This combination should be avoided. Close clinical and electrocardiographic monitoring is required, especially in elderly patients and at the beginning of treatment.
Significant increase in blood pressure with abrupt withdrawal of a centrally acting antihypertensive.
Cardiac glycosides. Decreased heart rate, impaired conduction.
Beta-adrenoblockers for topical use (e.g. eye drops for glaucoma) may increase the systemic effects of bisoprolol (decrease in blood pressure, decreased heart rate).
Calcium channel blockers (e.g. nifedipine). An excessive decrease of blood pressure is possible.
Parasympathomimetics. When used together there is a risk of bradycardia.
Mefloquine. Concomitant use with bisoprolol increases the risk of bradycardia (additive effect).
Phenytoin when administered intravenously, drugs for inhalation general anesthesia
(hydrocarbon derivatives) increase the severity of cardiodepressive effects and the possibility of decreased blood pressure.
Simultaneous use with beta-adrenomimetics (e.g. isoprenaline, dobutamine) may decrease the effect of both drugs.
Combination of bisoprolol with adrenomimetics affecting beta- and alpha-adrenoreceptors (e.g. norepinephrine, epinephrine) may increase vasoconstrictor effect of these drugs that occurs with alpha-adrenoreceptors, leading to increased blood pressure.
Such interaction is more likely during the use of non-selective beta-adrenoblockers.
Bisoprolol can change the effectiveness of insulin and hypoglycemic agents for oral administration, mask the symptoms of hypoglycemia (tachycardia, increased blood pressure).
Bisoprolol decreases clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentrations, especially in patients with initially increased clearance of theophylline under the influence of smoking.
Antihypertensive effect is weakened by nonsteroidal anti-inflammatory drugs (sodium ion retention and blockade of prostaglandin synthesis by kidneys), glucocorticosteroids and estrogens (sodium ion retention).
Diuretics, sympatholytics, hydralazine and other hypotensive drugs. Risk of excessive reduction of blood pressure.
Bisoprolol prolongs the effect of nondepolarizing myorelaxants and anticoagulant effect of coumarins.
Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol,
sedative and hypnotic drugs – when combined with bisoprolol, increased depression of the central nervous system.
Non-hydrogenated ergot alkaloids increase the risk of peripheral circulatory disorders.
Ergotamine increases the risk of peripheral circulatory disorders.
Sulfasalazine increases the plasma concentration of bisoprolol.
Rifampicin decreases the half-life of bisoprolol.
Allergens used for immunotherapy or allergen extracts for skin testing increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprololol.
Iodine-containing radiopaque diagnostic agents for intravenous administration increase the risk of anaphylactic reactions.
Special Instructions
Treatment with the drug is usually long-term.
Before starting treatment, it is recommended to conduct a study of external respiratory function in patients with a history of bronchopulmonary problems.
Patients with bronchospastic disorders may be prescribed bisoprololol in case of intolerance and/or ineffectiveness of other hypotensive drugs, and the dose of the drug should be strictly monitored.
Supervision of patients receiving bisoprolol should include monitoring of heart rate, blood pressure (at the beginning of treatment – daily, then once in 3-4 months),
electrocardiogram, plasma glucose concentration in patients with diabetes (once in 4-5 months).
In elderly patients it is recommended to monitor renal function (once every 4-5 months). The patient should be taught the method of counting the heart rate and instructed to consult a physician if the heart rate falls below 60 bpm.
In about 20% of patients with angina pectoris, beta-adrenoblockers are ineffective.
The main reasons are severe coronary atherosclerosis with low ischemia threshold (heart rate less than 100 bpm) and increased left ventricular end-diastolic volume, which impairs subendocardial blood flow. In “smokers” the efficacy of beta-adrenoblockers is lower.
Patients who use contact lenses should consider that against the background of treatment there may be a decrease in tear fluid production.
When used in patients with pheochromocytoma there is a risk of paradoxical arterial hypertension (if effective alpha-adrenoblockade has not been previously achieved).
In thyrotoxicosis bisoprolol may mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it may exacerbate the symptoms.
In diabetes mellitus, it may mask tachycardia caused by hypoglycemia. Unlike non-selective beta-adrenoblockers, it practically does not increase insulin-induced hypoglycemia and does not delay recovery of blood glucose concentration to normal levels.
If clonidine is used simultaneously, its use can be discontinued only a few days after bisoprolol withdrawal.
The severity of hypersensitivity reactions may increase and the lack of effect of usual doses of epinephrine against the background of a history of aggravated allergology.
If it is necessary to perform a planned surgical intervention the drug should be canceled 48 hours before the start of general anesthesia.
If the patient took the drug before the surgical procedure, he should choose a drug for general anesthesia with minimal negative inotropic effect.
Reciprocal activation of the vagus nerve can be eliminated by intravenous injection of atropine (1-2 mg).
Drugs that reduce catecholamine stores (e.g., reserpine) may enhance the effects of beta-adrenoblockers, so patients taking such drug combinations should be under constant medical supervision for arterial hypotension or bradycardia.
In elderly patients with increasing bradycardia (less than 60 bpm), arterial hypotension (systolic blood pressure below 100 mmHg.), AV blockade, bronchospasm, ventricular arrhythmias, severe hepatic and renal dysfunctions it is necessary to reduce the dose or discontinue treatment.
Bisoprolol treatment should not be abruptly interrupted because of the risk of severe arrhythmias and myocardial infarction. Discontinuation is carried out gradually, reducing the dose over 2 weeks or more (the dose is reduced by 25% every 3 to 4 days).
It is recommended to discontinue therapy (with gradual dose reduction) if depression caused by taking the drug. The drug should be discontinued before testing the content of catecholamines, normetanephrine and vanillinmindalic acid in the blood and urine, the titer of antinuclear antibodies.
Influence on the ability to drive vehicles and operate machinery
During treatment, caution should be exercised when driving vehicles and performing other potentially dangerous activities that require increased concentration and rapid psychomotor reactions.
Contraindications
Hypersensitivity to bisoprolol, other drug components and other beta-adrenoblockers; shock (including cardiogenic); pulmonary edema; acute heart failure or CHF in decompensation stage,
requiring inotropic therapy; AV block of II-III degree, without pacemaker;
sinoatrial block; sinus node weakness syndrome; bradycardia (heart rate less than 60 bpm); Prinzmetal’s angina; cardiomegaly (without signs of heart failure);
severe arterial hypotension (systolic BP less than 100 mm.Hg.
severe arterial hypotension (systolic BP less than 100 mm Hg), especially in myocardial infarction; severe bronchial asthma and chronic obstructive pulmonary disease (COPD) in anamnesis;
concomitant use of floktafenine, sultopride, monoamine oxidase inhibitors (MAO), except for MAO type B; Simultaneous intravenous administration of verapamil or diltiazem; severe disorders of
peripheral circulation, Raynaud’s syndrome; pheochromocytoma (without simultaneous use of alpha-adrenoblockers); metabolic acidosis; age under 18 years (effectiveness and safety have not been established).
Lactase deficiency, lactose intolerance, lactose/isomaltose malabsorption syndrome (the drug contains lactose).
With caution
Severe hepatic impairment, severe renal insufficiency (creatinine clearance less than 20 ml/min), myasthenia, thyrotoxicosis, diabetes (may mask the symptoms of hypoglycemia), aggravated
allergic reactions.
allergic history, 1st degree AV blockade, depression (including in anamnesis), psoriasis, bronchial asthma, COPD, peripheral circulatory disorders, strict diet.
Side effects
Frequency of the following side effects is given in accordance with the WHO classification: very common – more than 10%; common – more than 1% and less than 10%; infrequent – more than 0.1% and less than
1%; rare – more than 0.01% and less than 0.1%; very rare – less than 0.01%, including individual cases.
Central and peripheral nervous system:
often – increased fatigue, asthenia, dizziness, headache. Usually these phenomena occur at the beginning of treatment, are usually insignificant and disappear within 1-2 weeks; rarely – sleep disturbances, depression; rarely – nightmares, hallucinations, loss of consciousness.
Cardiovascular system:
very common – bradycardia, sensation of palpitations; often – marked decrease in blood pressure (especially in patients with CHF), manifestations of angiopasm (worsening of peripheral circulation disorders,
feeling of cold in the extremities (paresthesias); infrequent – AV conduction disorders (up to complete transverse blockade and cardiac arrest), arrhythmias, worsening
CHF course with the development of peripheral edema (edema of ankles, feet) and dyspnea, orthostatic hypotension, chest pain.
Digestive system disorders:
often – nausea, vomiting, diarrhea, abdominal pain,
constipation, dry mouth mucosa; rarely – hepatitis, increased activity of “liver” transaminases (alanine aminotransferase, aspartate aminotransferase), increased concentration of bilirubin.
Respiratory system:
infrequent – laryngo- and bronchospasm in patients with
bronchial asthma or obstructive airway disease; rarely –
allergic rhinitis, nasal congestion.
Musculoskeletal system:
infrequent – muscle weakness, cramps in the calf muscles, arthralgia.
Senses:
rarely – visual impairment, decreased tear production (should be considered while wearing contact lenses), hearing impairment, changes in taste;
very rarely – dry and painful eyes, conjunctivitis.
Skin:
rarely – increased sweating, psoriasis-like skin reactions, very rare – alopecia, exacerbation of psoriasis.
Endocrine system:
rarely – hypoglycemia.
Urinary system disorders:
rarely – impaired potency, weakening of libido.
On the side of the immune system:
rarely – appearance of antinuclear antibodies with unusual clinical symptomatology of lupus-like syndrome, which disappear after the end of treatment.
Allergic reactions:
rarely – skin hyperemia, skin itching, skin rash, urticaria.
Laboratory parameters:
rarely – hypertriglyceridemia; very rarely – thrombocytopenia, agranulocytosis, leukopenia.
Other:
rarely – withdrawal syndrome (increased angina pectoris attacks, increased blood pressure).
Overdose
Symptoms: arrhythmia, ventricular extrasystole, marked bradycardia, AV block, marked decrease in blood pressure, acute heart failure, hypoglycemia, acrocyanosis, difficulty in breathing, bronchospasm, dizziness, syncope, seizures.
Treatment: gastric lavage, administration of adsorbents, symptomatic therapy. In case of marked bradycardia – intravenous injection of atropine.
If the effect is insufficient, drugs with a positive chronotropic effect may be administered with caution. Sometimes a temporary artificial pacemaker may be required.
In developed AV blockade – intravenous injection of 1-2 mg of atropine, epinephrine or placement of a temporary pacemaker.
In ventricular extrasystole – lidocaine (Class IA drugs are not used). With a marked decrease in blood pressure the patient should be transferred to Trendelenburg; if there are no signs of pulmonary edema
– intravenous administration of plasma substitute solutions, if they are ineffective – administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and to eliminate a marked decrease in blood pressure).
In hypoglycemia intravenous injection of dextrose (glucose) solution may be indicated.
In case of cardiac insufficiency – cardiac glycosides and diuretics.
In convulsions – intravenous diazepam. In bronchospasm – inhaled beta2-adrenomimetics.
Pregnancy use
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.
Similarities
Niperten, Concor, Bisogamma, Concor Cor, Coronal, Bidop, Bisoprolol-Teva, Bisoprolol, Biprolol, Bidop Cor
Weight | 0.020 kg |
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Shelf life | 3 years |
Conditions of storage | In a dry, light-protected place at a temperature not exceeding 25 °C |
Manufacturer | Chemopharm LLC, Russia |
Medication form | pills |
Brand | Chemopharm LLC |
Other forms…
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