Bisomor
Bisomor: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Bisomor
ATX code: C07AB07
Active ingredient: bisoprolol (Bisoprolol)
Producer: Edge Pharma Private, Limited (India)
Description and photo update: 2019-11-07
Prices in pharmacies: from 158 rubles.
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Bisomor is a selective beta1-blocker.
Release form and composition
Dosage form - film-coated tablets: round, biconvex, light yellow (dosage 2.5 mg), light orange (dosage 5 mg) or orange (dosage 10 mg), two layers are visible on the fracture - the core from almost white to white and sheathed; in tablets of 2.5 mg on one of the sides there is a dividing risk (10 pcs. in a blister, in a cardboard box for consumer packaging 3 blisters and instructions for use of Bisomor).
Composition of 1 tablet:
- active substance: bisoprolol fumarate - 2.5; 5 or 10 mg;
- auxiliary components: croscarmellose sodium, microcrystalline cellulose, magnesium stearate, mannitol;
- film shell: 2.5 mg tablets - Winkout WT-AQ-01530 yellow dye (titanium dioxide, macrogol 6000, talc, macrogol 400, hypromellose, quinoline yellow aluminum varnish), 5 mg tablets - WT-AQ-01069 orange Winkout dye (titanium dioxide, macrogol 6000, talc, macrogol 400, hypromellose, aluminum varnish, sunset yellow), tablets 10 mg - dye Winkout WT-AQ-01620 orange (titanium dioxide, macrogol 6000, talc, macrogol 400, hypromellose, aluminum varnish sunset yellow).
Pharmacological properties
Pharmacodynamics
Bisoprolol fumarate is a selective beta1-blocker that does not have its own sympathomimetic activity and membrane stabilizing effect.
The drug slows down heart rate (heart rate), reduces myocardial oxygen demand and renin activity in blood plasma. It has hypotensive, antianginal and antiarrhythmic effects. In low doses, it blocks beta1-adrenergic receptors of the heart, which entails a decrease in the catecholamine-stimulated formation of cAMP (cyclic adenosine monophosphate) from ATP (adenosine triphosphate), a decrease in the intracellular current of calcium ions, as well as the development of batmo-, dromo-, chromo- and inotropic action [slowing down of atrioventricular AV-) conduction, suppression of excitability and conduction]. When used in a dose exceeding the therapeutic dose, it has a beta2-adrenergic blocking effect.
In the first 24 hours after taking Bisomor, the OPSS (volume of peripheral vascular resistance) slightly increases, which is due to a reciprocal increase in the activity of α-adrenergic receptors and elimination of stimulation of beta2-adrenergic receptors. After 1-3 days, this indicator returns to its original value, and with prolonged use of the drug, it decreases.
The antihypertensive effect of bisoprolol is due to sympathetic stimulation of peripheral vessels, a decrease in the minute blood volume, a decrease in the activity of the sympathoadrenal system (this is especially important for patients with initial renin hypersecretion), the effect on the central nervous system (central nervous system), as well as restoration of sensitivity in response to a decrease in blood pressure (arterial pressure). The antihypertensive effect is observed after 2–5 days of therapy, a stable therapeutic effect develops within 1–2 months.
The antianginal effect is explained by a decrease in myocardial oxygen demand (due to a decrease in contractility and other myocardial functions), an improvement in myocardial perfusion and a prolongation of diastole. An increase in the end diastolic pressure in the left ventricle and an increase in the stretching of the muscle fibers of the ventricles can cause an increase in myocardial oxygen demand, especially in CHF (chronic heart failure).
The antiarrhythmic action of Bisomor is based on the elimination of arrhythmogenic factors (such as arterial hypertension, tachycardia, increased cAMP content, increased activity of the sympathetic nervous system), a decrease in the rate of spontaneous excitation of ectopic and sinus pacemakers, a slowdown in AV conduction (mainly in the antegrade direction, less - in the retrograde direction through the AV node) and conduction along additional pathways.
In contrast to non-selective beta-blockers, bisoprolol in medium therapeutic doses has a less pronounced effect on carbohydrate metabolism and on organs that contain beta2-adrenergic receptors (skeletal muscles, pancreas, smooth muscles of peripheral arteries, bronchi, uterus). In addition, it does not contribute to the retention of sodium ions in the body.
Pharmacokinetics
The main pharmacokinetic parameters of bisoprolol:
- absorption: the drug is absorbed from the gastrointestinal tract to a high degree (more than 90%). Simultaneous food intake does not affect absorption. Linear kinetics of the drug was noted, with the plasma concentration proportional to the administered dose in the range of 5–20 mg. C max (maximum concentration) in plasma is reached within 2–3 h;
- distribution: Vd (volume of distribution) of bisoprolol is 3.5 l / kg. About 30% of the dose is bound to plasma proteins. In small quantities, it penetrates the blood-brain and placental barriers;
- metabolism: bisoprolol is insignificantly (10–15%) exposed to the effect of the first passage through the liver. It is predominantly metabolized by the oxidative pathway (it does not undergo further conjugation). All the resulting metabolites are polar. The main metabolites found in plasma and urine have no pharmacological activity. According to the data obtained in experiments with human liver microsomes in vitro, CYP3A4 isoenzymes are mainly involved in the metabolism of bisoprolol (~ 95%). The CYP2D6 isoenzyme is involved to a small extent;
- excretion: bisoprolol is excreted in two ways. About 50% of the dose is biotransformed in the liver with the formation of inactive metabolites. Approximately 98% is excreted by the kidneys (unchanged - about 50%), no more than 2% - with bile (through the intestines). The total clearance of the drug is 12–18 l / h, renal clearance is 8–11 l / h. The half-life is 10-12 hours.
The pharmacokinetics of bisoprolol is linear and does not depend on the patient's age. With CHF, the plasma concentration of the drug and the half-life increase (in comparison with healthy volunteers).
Indications for use
- arterial hypertension;
- chronic heart failure;
- ischemic heart disease (for the prevention of attacks of stable angina pectoris).
Contraindications
Absolute:
- simultaneous administration of monoamine oxidase (MAO) inhibitors, with the exception of type B MAO inhibitors;
- the combined appointment of sultopride, floktaphenin;
- pheochromocytoma (without the simultaneous use of alpha-blockers);
- severe peripheral circulatory disorders, Raynaud's syndrome;
- a history of severe bronchial asthma and chronic obstructive pulmonary disease (COPD);
- metabolic acidosis;
- bradycardia (heart rate <60 beats / min);
- decompensated chronic heart failure requiring inotropic therapy;
- acute heart failure;
- AV block II and III degree without a pacemaker;
- sinoatrial blockade;
- cardiogenic shock;
- cardiomegaly (no signs of heart failure);
- sick sinus syndrome;
- collapse;
- severe arterial hypotension (systolic blood pressure <100 mm Hg);
- age up to 18 years;
- lactation period;
- hypersensitivity to bisoprolol, other beta-blockers or any auxiliary component of the drug.
Relative (Bisomor tablets are used with caution):
- depression (current or history);
- psoriasis;
- diabetes;
- hyperthyroidism;
- adherence to a strict diet;
- bronchial asthma and COPD;
- severe liver dysfunction;
- severe renal failure [creatinine clearance (CC) <20 ml / min];
- CHF in patients who have had myocardial infarction in the previous 3 months;
- AV block I degree;
- restrictive cardiomyopathy;
- Prinzmetal's angina;
- congenital heart defects or heart valve disease with severe hemodynamic disturbances;
- the period of the desensitizing therapy;
- pregnancy.
Bisomor, instructions for use: method and dosage
Bisomor tablets are taken orally: they are swallowed whole (you cannot chew the tablets or grind them into powder) and drink plenty of liquid. The recommended time of taking is in the morning before, during or after breakfast.
The optimal dose is selected by the doctor individually, taking into account the general condition of the patient and his heart rate.
With arterial hypertension and stable angina pectoris, treatment is usually started with a daily dose of 5 mg. If necessary, it is increased to 10 mg, maximum up to 20 mg.
For patients with CHF, the drug can be prescribed only if the condition is stable, without signs of exacerbation. The initial recommended dose is 1.25 mg (1/2 tablet at a dosage of 2.5 mg). With good tolerance of Bisomor, it is gradually (no more than once every 2 weeks) increased first to 2.5 mg (1 tablet 2.5 mg), then to 3.75 mg (1½ tablets 2.5 mg), to 5 mg (1 tablet 5 mg or 2 tablets 2.5 mg), up to 7.5 mg (1 tablet 5 mg and 1 tablet 2.5 mg). The maximum allowable daily dose is 10 mg.
If, after increasing the dose of the drug, poor tolerance is noted in the patient, the dose is reduced. During the titration period, blood pressure, heart rate and symptoms of an increase in CHF should be monitored. Worsening of the course of CHF is possible from the first day of treatment with Bisomor.
When titrating the dose and after the end of the phase of the selection of the dosage regimen, the development of arterial hypotension and bradycardia, a temporary aggravation of the symptoms of CHF is possible. If necessary, reduce the dose of Bisomor for a certain period or cancel it. It is also required to consider the possibility of adjusting the dosing regimen of concomitant therapy. After stabilization of the patient's condition, the dose can be re-titrated or continued therapy with the drug.
Treatment with a beta1-blocker is usually long-term. If necessary, the drug can be interrupted and later resumed. However, the abolition of Bisomor should be gradual, especially with coronary heart disease.
Side effects
Classification of the frequency of side effects: ≥ 1/10 - very often, from ≥ 1/100 to <1/10 - often, from ≥ 1/1000 to <1/100 - infrequently, from ≥ 1/10000 to <1/1000 - rare, <1/10000 - very rare.
Possible adverse reactions of Bisomor:
- laboratory parameters: rarely - an increase in the activity of hepatic transaminases and the concentration of triglycerides;
- on the part of the cardiovascular system: very often in patients with CHF - bradycardia; often - a marked decrease in blood pressure (especially in patients with CHF), a feeling of numbness or coldness in the extremities, aggravation of symptoms of CHF in patients with CHF; infrequently - orthostatic hypotension, bradycardia in patients with arterial hypertension or angina pectoris, impaired AV conduction, aggravation of symptoms of CHF in patients with angina pectoris or arterial hypertension;
- from the respiratory system: rarely in patients with bronchial asthma or a history of airway obstruction - bronchospasm; rarely - allergic rhinitis;
- on the part of the musculoskeletal system: infrequently - muscle weakness, muscle cramps;
- from the digestive system: often - constipation, diarrhea, nausea, vomiting; rarely - hepatitis;
- from the reproductive system: rarely - violation of potency;
- from the senses: rarely - hearing impairment, decreased lacrimation; very rarely - conjunctivitis;
- on the part of the skin: rarely - hypersensitivity reactions (rash, itching, hyperemia of the skin); very rarely - alopecia, exacerbation of the course of psoriasis or the appearance of a psoriasis-like rash;
- from the central nervous system and psyche: headache *, dizziness *; infrequently - insomnia, depression; rarely - nightmares, hallucinations;
- others: often - increased fatigue *, asthenia in patients with CHF; infrequently in patients with arterial hypertension or angina pectoris - asthenia.
* The described symptoms in patients with angina pectoris and arterial hypertension often develop at the beginning of treatment, are usually mild and go away on their own within 1–2 weeks of therapy.
Overdose
In case of an overdose, bisomor can cause a pronounced decrease in blood pressure, the development of significant bradycardia, AV blockade, acute heart failure, hypoglycemia and bronchospasm.
To a single dose of Bisomor in a high dose, the sensitivity varies greatly from patient to patient. It is assumed that more pronounced sensitivity is present in patients with CHF.
Overdose treatment is symptomatic and supportive.
Severe bradycardia is eliminated by intravenous atropine. If the effect is insufficient, a drug with a positive chronotropic effect is used with caution. In some cases, temporary setting of an artificial pacemaker (IVP) is required.
With a significant decrease in blood pressure, vasopressor agents and plasma-substituting solutions are administered intravenously.
If AV block develops, the patient is prescribed beta-adrenomimetics (for example, epinephrine), and IVR may be required.
In acute heart failure, diuretics, vasodilators and drugs with a positive inotropic effect are administered intravenously.
Bronchospasm is treated with bronchodilators (aminophylline and / or beta2-adrenomimetics can be used).
The resulting hypoglycemia is eliminated by intravenous administration of dextrose (glucose).
special instructions
Close medical supervision of patients is recommended at an early stage of treatment.
Against the background of therapy with Bisomor, blood pressure and heart rate should be monitored (at the initial stage - daily, then - once every 3-4 months) and an electrocardiogram should be performed. In patients with diabetes mellitus, it is necessary to determine the blood glucose level every 4–5 months. In the elderly, it is also recommended to monitor kidney function (every 4–5 months).
The doctor should teach each patient the method of self-calculating the heart rate and inform about the need for immediate medical attention if this indicator is below 60 beats / min.
Before prescribing the drug to patients with a burdened bronchopulmonary history, it is recommended to conduct a study of the function of external respiration.
For patients with bronchospastic diseases, Bisomor can be prescribed if other antihypertensive drugs are ineffective or intolerant. Do not exceed the dose of the drug recommended by the doctor, since in this case the risk of developing bronchospasm increases.
Bisomor can mask hypoglycemia-induced tachycardia in diabetic patients. Unlike non-selective beta-blockers, this drug practically does not induce an increase in insulin-induced hypoglycemia. In addition, it does not interfere with the restoration of blood glucose concentration to normal values.
The drug is also able to mask the symptoms of hyperthyroidism (in particular tachycardia), so it is contraindicated to abruptly stop taking it, otherwise the symptoms may increase.
If depression develops, treatment with Bisomor is stopped.
In patients with a burdened allergic history, the drug can increase the severity of the hypersensitivity reaction and reduce the effect of conventional doses of epinephrine.
Bisoprolol is able to reduce the production of tear fluid, which must be taken into account by people wearing contact lenses.
With concomitant pheochromocytoma, a beta1-blocker can be prescribed only against the background of maintenance therapy with an alpha-blocker.
The effectiveness of beta-blockers is reduced by smoking.
General anesthesia in patients receiving Bisomor can cause the development of β-adrenergic receptor blockade. Before surgery, it is recommended to discontinue the drug: gradually reduce the dose and complete the intake completely 48 hours before the operation using general anesthesia. In the event of an emergency surgical intervention, the patient should warn the doctor about taking bisoprolol so that he selects a drug for anesthesia with a minimal negative inotropic effect.
In the case of joint use with clonidine, it is allowed to stop taking it no earlier than a few days after the cancellation of Bisomor.
If it is necessary to conduct tests for the content of vanillin mandelic acid, normetanephrine, catecholamines and antinuclear antibody titers in the blood and urine, the drug should be discontinued.
With a sharp cessation of beta1-blocker intake, the risk of developing severe arrhythmias and myocardial infarction increases, therefore, Bisomor must be canceled gradually, reducing the dose by 25% every 3-4 days.
Currently, there is insufficient data on the safety of bisoprolol use in patients with CHF and such concomitant diseases as congenital heart disease, hemodynamically significant heart disease, restrictive cardiomyopathy, type 1 diabetes mellitus, severe functional disorders of the liver and / or kidneys. Also, to date, the necessary information has not been obtained to confirm the effectiveness of drug therapy in patients with CNS who have had myocardial infarction in the previous 3 months.
Influence on the ability to drive vehicles and complex mechanisms
Bisomor can cause undesirable reactions from the central nervous system and psyche, therefore patients need to be careful when engaging in potentially hazardous activities that require quick reactions and increased attention (including when driving a car).
Application during pregnancy and lactation
Bisomor during pregnancy is allowed to be prescribed only for the treatment of women in whom the use of the drug is absolutely necessary. It has been established that beta-blockers are able to reduce uteroplacental blood flow, which may lead to fetal development disorders. In this regard, it is necessary to carefully monitor the blood flow in the placenta and uterus, the development and growth of the fetus. If undesirable phenomena appear, it is recommended to switch to an alternative method of therapy.
Newborns whose mothers received bisoprolol during pregnancy should be carefully examined and observed in the first days after childbirth. There is a risk of developing symptoms of hypoglycemia and bradycardia.
There is no data on the penetration of the drug into breast milk. If during lactation a woman needs treatment with Bisomor, breastfeeding should be abandoned.
Pediatric use
Bisomor, due to the lack of data on safety and efficacy in pediatrics, is not used in patients under 18 years of age.
With impaired renal function
- mild and moderate functional disorders of the kidneys: no need to change the dosage regimen of Bisomor;
- severe disorders (CC <20 ml / min): the drug should be used with caution and do not exceed a daily dose of 10 mg.
For violations of liver function
Bisomor with pronounced functional disorders of the liver should be used with caution.
Use in the elderly
In old age, correction of the beta1-blocker dosing regimen is usually not required, but treatment should be carried out with caution.
In the case of a pronounced decrease in blood pressure (systolic blood pressure <100 mm Hg), the development of increasing bradycardia (heart rate <60 beats / min) or AV blockade, it is necessary to reduce the dose of Bisomor or replace it with alternative therapy.
Drug interactions
Combinations not recommended
When combined with bisoprolol, blockers of slow calcium channels (especially like verapamil, to a lesser extent diltiazem) can cause a decrease in myocardial contractility and a violation of AV conduction. Simultaneous intravenous use of verapamil during therapy with beta-blockers can provoke severe arterial hypotension and AV block.
Centrally acting antihypertensive drugs (for example, moxonidine, methyldopa, rilmenidine, clonidine) can slow heart rate, reduce cardiac output, cause vasodilation, reducing central sympathetic tone. Their abrupt cancellation, especially before discontinuation of bisoprolol, increases the risk of developing rebound arterial hypertension.
In patients receiving Bisomor for CHF, class I antiarrhythmics (including lidocaine, quinidine, flecainide, phenytoin, disopyramide, propafenone) are able to reduce AV conductivity and myocardial contractility.
Careful combinations
General anesthetics increase the risk of a cardiodepressant effect, which leads to a marked decrease in blood pressure.
Local beta-blockers (for example, eye drops for the treatment of glaucoma) can enhance the systemic effects of bisoprolol, which is manifested by a decrease in heart rate and a decrease in blood pressure.
Non-steroidal anti-inflammatory drugs have the ability to reduce the antihypertensive activity of bisoprolol.
With the combined use of Bisomor and cardiac glycosides, it is possible to lengthen the time of the impulse and, as a result, to develop bradycardia.
The risk of bradycardia increases with the simultaneous use of mefloquine.
Parasympathomimetics are able to increase the disturbance of AV conduction and increase the risk of developing bradycardia.
MAO inhibitors (with the exception of type B) can increase the hypotensive effect. There is also a risk of developing a hypertensive crisis.
With the combined use of beta-adrenergic agonists (for example, dobutamine or isoprenaline), a mutual decrease in the effects is possible. Bisoprolol is able to enhance the vasoconstrictor effects of adrenergic agonists that affect α- and β-adrenergic receptors (for example, norepinephrine, epinephrine), which leads to an increase in blood pressure. Such drug interactions are more likely when non-selective beta-blockers are taken, however, such a risk cannot be completely ruled out with the simultaneous use of selective beta-blockers.
The effect of bisoprolol can be enhanced by antihypertensive drugs and other drugs with a potential antihypertensive effect, such as barbiturates, tricyclic antidepressants, phenothiazines, etc.
Slow calcium channel blockers, which are derivatives of dihydropyridine (amlodipine, nifedipine, felodipine), increase the likelihood of arterial hypotension. In patients with CHF, there is a risk of further deterioration of myocardial contractile function.
Class III antiarrhythmics (for example, amiodarone) can increase the violation of AV conduction.
Bisoprolol can increase the hypoglycemic effect of insulin and oral hypoglycemic agents, and mask or suppress the symptoms of hypoglycemia (in particular tachycardia).
In patients receiving Bisomor for arterial hypertension or stable angina pectoris, class I antiarrhythmic drugs (including lidocaine, quinidine, flecainide, phenytoin, disopyramide, propafenone) are able to reduce AV conduction and myocardial contractility.
Analogs
Bisomor's analogues are Aritel, Atenolol, Betakard, Betalok, Bisogamma, Bisoprolol, Breviblok, Coronal, Metoprolol, Nebivolol, Nebilong, Niperten, Tirez, Egilok, Estecor, etc.
Terms and conditions of storage
Store in a dry, out of reach of children and protected from light, at a temperature not exceeding 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Bisomore
There are practically no reviews about Bisomore on forums and social networks. However, there are many reports of preparations that also contain bisoprolol as an active substance. It is an inexpensive beta-blocker that effectively reduces high blood pressure and normalizes heart rate. However, it should be taken as directed by a doctor and strictly under his supervision.
In isolated reviews, patients note that during therapy with Bisomor, such side effects as vomiting developed, in addition, the drug has many contraindications.
Price for Bisomor in pharmacies
At the moment, the price of Bisomor, film-coated tablets, is for 30 pcs. in the package is approximately: dosage 5 mg - 120 rubles; dosage of 10 mg - 145-156 rubles.
Bisomor: prices in online pharmacies
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Drug name Price Pharmacy |
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Bisomor 5 mg film-coated tablets 30 pcs. 158 RUB Buy |
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Bisomor 10 mg film-coated tablets 30 pcs. 214 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
