Bisoprolol indications for use reviews. Cardiological drug Bisoprolol: how to take pills with high blood pressure and other diseases of the cardiovascular system? Special instructions during admission

Floors 04.01.2021
Floors

1 tablet contains bisoprolol fumarate 2.5 mg or 5 mg or 10 mg;

Bisoprolol reduces the activity of renin in the blood plasma, reduces myocardial oxygen demand, and slows down the heart rate (HR). It has hypotensive, antiarrhythmic and antianginal effects.

The hypotensive effect is associated with a decrease in the minute blood volume and sympathetic stimulation of peripheral vessels. The antianginal effect is due to a decrease in myocardial oxygen demand and a decrease in contractility, an increase in diastole, and an improvement in myocardial perfusion.

Binding of bisoprolol to blood plasma proteins is 35%. The drug passes through the blood-brain and placental barriers to an insignificant extent, and is found in small quantities in breast milk. The half-life is about one day.

What is Bisoprolol prescribed for?

Indications for the use of the drug are:

  • Arterial hypertension;
  • Ischemic heart disease (CHD),
  • Exertional angina,
  • Myocardial infarction (secondary prevention),
  • Chronic heart failure (CHF).

Additionally, bisoprolol is prescribed for cardiac arrhythmias - sinus tachycardia, supraventricular and ventricular premature beats. As part of the therapy of arrhythmias against the background of mitral valve prolapse, thyrotoxicosis.

With arterial hypertension, the therapeutic effect is manifested in 2-5 days, a stable effect is expected in 1-2 months.

How quickly do the tablets appear? After taking the drug, blood pressure is normalized within 3-4 hours and remains stable for more than a day. Two-week treatment leads to the normalization of the functions of the cardiovascular system (CVS).

I hope I answered the question from what these tablets (bisoprolol). Do not go astray and consider them a cure for pressure.

Bisoprolol - instructions for use, dosage

The use of bisoprolol tablets - inside, without chewing. Therapeutic daily dosage is 5-10 mg, the maximum daily dose is 20 mg.

In case of impaired renal or liver function (creatinine clearance less than 20 ml / min), the dose of Bisoprolol should not exceed 10 mg once a day (the dosage can be divided into two doses).

In some patients, especially in patients with bronchopulmonary disease, it is recommended to start treatment with bisoprolol with half the dose - 2.5 mg - 1 time per day. A doctor's consultation is required.

Abrupt cancellation is prohibited - when the use of Bisoprolol is canceled, the dosage is reduced gradually over 10-14 days.

With CHF, the use of Bisoprolol is possible only by patients who have been in a state of stabilization during the last 6 weeks.

Important! Do not use bisoprolol tablets for self-treatment of hypertension and heart problems! Drugs affecting the heart muscle are categorically not recommended to be prescribed on their own or on the "advice of girlfriends / friends", for example, to drink bisoprolol from pressure.

Instructions for use Bisoprolol 2.5 is similar to the 5 mg version, the difference in the dosage of the active substance. It is worth choosing pills depending on the prescribed daily dose.

Overdose

If you take bisoprolol not according to the instructions, the following overdose symptoms may occur:

  • bradycardia,
  • arterial hypotension,
  • heart failure,
  • bronchospasm,
  • hypoglycemia.

When signs appear, gastric lavage and activated carbon are taken. Further treatment depends on the symptoms.

In case of an overdose, treatment with bisoprolol should be discontinued and the doctor should be immediately informed.

Bisoprolol - features and side effects

Bisoprolol can cause undesirable body reactions in the form of headache, depression, ECG changes, drowsiness or insomnia, dizziness, visual or hearing impairment, dryness of the conjunctiva, etc.

Other undesirable consequences of treatment: flushing of the face and head, sexual dysfunctions, allergic reactions, aggravation of the manifestations of diabetes mellitus.

Bisoprolol can cause drowsiness - do not drive a car or operate equipment while taking this medicine. Alcohol when using bisoprolol tablets is categorically contraindicated.

Contraindications:

Bradycardia with a heart rate of less than 60 beats per minute before starting therapy, sick sinus syndrome, severe sinoatrial blockade.

  • severe arterial hypotension (pressure less than 100 mm);
  • cardiogenic shock; age up to 18 years (efficacy and safety have not been established);
  • hypersensitivity to amlodipine, other dihydropyridine derivatives, bisoprolol and / or any of the excipients.

The drug should be prescribed with caution in liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes mellitus, AV block of the 1st degree, depression (including a history), psoriasis, as well as in elderly patients.

Bisoprolol analogues, list

One of the analogues of Bisoprolol is Bisoprolol Prana. The medicine is available in the form of tablets, each of which contains 10 mg of bisoprolol. It is taken taking into account the amount of active substance contained in 1 tablet.

Other analogs for the active substance:

Niperten, Aritel, Bidop, Biol, Bidop Cor, Biprol, Bisokard, Bisogamma, Bisoprolol-OBL, Bisomor, Bisoprolol, Bisoprolol-LEXVM®, Cordinorm Cor, Bisoprolol-SZ, Bisoprolol Pranaeva, Bisoprololisopar-L , Cordinorm, Bisoprolol fumarate, Bisoprolol fumarate-Pharmaplant, Concor, Concor Cor, Aritel Cor, Corbis, Coronal, Tirez.

Instructions for use, the price of Bisoprolol and analogues are different - this instruction cannot be applied to other drugs with a similar active substance (analogues). A dosage adjustment is required depending on the AB content and other indicators.

Storage conditions

Store at a temperature not exceeding 25 ° C in its original packaging, protected from moisture and light, out of reach of children.
The medicinal product must not be used after the expiration date.

Lekpharm, SOOO

Country of origin

Republic of Belarus

Product group

Cardiovascular drugs

Selective beta1-blocker

Release forms

  • 30 tab per pack

Description of the dosage form

  • Film-coated tablets, yellow, round, biconvex; at the break - the core is white or almost white.

Pharmacokinetics

Absorption - 80-90%, food intake does not affect absorption. Cmax in blood plasma is achieved after 2-4 hours. Plasma protein binding is 26-33%. Bisoprolol slightly crosses the BBB and the placental barrier; excreted in breast milk. Metabolized in the liver. T1 / 2 - 9-12 hours. It is excreted by the kidneys - 50% unchanged, less than 2% - with bile.

Special conditions

Use with caution in psoriasis and with indications of psoriasis in a family history, diabetes mellitus in the decompensation phase, with a predisposition to allergic reactions. With pheochromocytoma, the use of bisoprolol is possible only after taking alpha-blockers. Avoid sudden cancellation of bisoprolol, the course of treatment should be completed slowly with a gradual dose reduction. Before surgery, the anesthesiologist should be informed about bisoprolol treatment. Bisoprolol at a dose of more than 10 mg / day should be used only in exceptional cases. Do not exceed this dose in renal failure (CC less than 20 ml / min) and severe liver dysfunction. During the period of treatment, avoid alcohol consumption. Influence on the ability to drive vehicles and control mechanisms Use with caution in patients whose activities are associated with the need for concentration and high speed of psychomotor reactions.

Composition

  • 1 tab.
  • bisoprolol fumarate 5 mg
  • Excipients: magnesium stearate - 1.2 mg, colloidal silicon dioxide - 1.2 mg, crospovidone - 1.2 mg, corn starch - 15.6 mg, microcrystalline cellulose - up to 120.0 mg.
  • The composition of the film shell: opadry II yellow - up to 123.6 mg (titanium dioxide - 0.46296 mg, talc - 0.5328 mg, macrogol - 0.7272 mg, iron oxide yellow dye - 0.01404 mg, quinoline yellow dye - 0.42048 mg, orange yellow dye - 0.00252 mg ). polyvinyl alcohol - 1.44 mg.

Bisoprolol indications for use

  • -arterial hypertension
  • - ischemic heart disease (prevention of exertional angina attacks)
  • - chronic heart failure. ...
  • Bisoprolol is used with caution when:.
  • 1.Treatment of patients with diabetes mellitus with significant fluctuations in blood sugar. Symptoms of hypoglycemia can be masked.
  • 2. Strict diet.
  • 3. Treating patients with metabolic acidosis.
  • 4. Treatment of patients with a history of severe hypersensitivity reactions
  • 5. Conducting desensitizing therapy.
  • 6. Atrio-ventricular blockade of the 1st degree.
  • 7. Vasospastic angina (Prinzmetal's angina).
  • Application during pregnancy and during breastfeeding
  • You should not use Bisoprolol during pregnancy and during lactation, as well as for the treatment of children, since there is not enough experience for these cases. If Bisoprolol is used in exceptional cases during pregnancy, then treatment with it should be discontinued 72 hours before the expected due date due to the possibility

Bisoprolol contraindications

  • Acute heart failure, chronic heart failure in the stage of decompensation, cardiogenic shock, collapse, AV block II and III degree (without a pacemaker), SSSU; sinoatrial block, severe bradycardia (heart rate

Bisoprolol dosage

Bisoprolol side effects

  • From the nervous system: weakness, fatigue, dizziness, headache, sleep disorders, mental disorders (depression, rarely hallucinations), a feeling of cold and paresthesia in the extremities.
  • On the part of the cardiovascular system: orthostatic hypotension, bradycardia, impaired AV conduction, the appearance of symptoms of heart failure, aggravation of intermittent claudication and the main clinical symptoms in Raynaud's syndrome.
  • From the side of the organ of vision: a decrease in the secretion of lacrimal fluid, conjunctivitis.
  • From the digestive system: diarrhea, constipation, nausea, abdominal pain.
  • On the part of the musculoskeletal system: muscle weakness, muscle cramps.
  • On the part of the skin and subcutaneous tissues: itching; in some cases - increased manifestations of psoriasis, the appearance of psoriasis-like rashes.
  • From the respiratory system: in predisposed patients, symptoms of bronchial obstruction may appear.
  • Others: sweating, hot flashes, impaired potency, decreased glucose tolerance in patients with diabetes mellitus, allergic reactions.

Drug interactions

With the simultaneous use of antacids and antidiarrheals, it is possible to reduce the absorption of beta-blockers. With the simultaneous use of antiarrhythmic drugs, a sharp decrease in blood pressure, a decrease in heart rate, the development of arrhythmias and / or heart failure are possible. With the simultaneous use of antihypertensive drugs, an increase in the antihypertensive effect is possible. With the simultaneous use of cardiac glycosides, conduction disturbances are possible. With the simultaneous use of sympathomimetics (including those included in the composition of cough suppressants, nose drops, eye drops), the effectiveness of bisoprolol decreases. With the simultaneous use of verapamil, diltiazem, a sharp decrease in blood pressure, a decrease in heart rate, the development of arrhythmia and / or heart failure is possible. With the simultaneous use of guanfacine, severe bradycardia, conduction disturbances are possible. With the simultaneous use of insulin, hypoglycemic agents for oral administration, the effect of insulin or other hypoglycemic agents increases (regular monitoring of plasma glucose levels is required). With the simultaneous use of clonidine, severe bradycardia, arterial hypotension, conduction disturbances are possible. In the case of a sudden withdrawal of clonidine in patients receiving bisoprolol, a sharp increase in blood pressure is possible. With the simultaneous use of nifedipine, other calcium channel blockers, dihydropyridine derivatives, the antihypertensive effect of bisoprolol is enhanced. With the simultaneous use of reserpine, alpha-methyldopa, severe bradycardia is possible. With the simultaneous use of rifampicin, a slight decrease in T1 / 2 of bisoprolol is possible. With the simultaneous use of derivatives of ergotamine (including agents for the treatment of migraines containing ergotamine), symptoms of impaired peripheral circulation increase.

Beta 1 -adrenergic blocker

Active substance

Bisoprolol fumarate (bisoprolol)

Release form, composition and packaging

Film-coated tablets from beige-yellow to beige, round, biconvex; at the break of white or almost white.

Excipients: croscarmellose sodium (primellose), (medium molecular weight polyvinylpyrrolidone), pregelatinized starch (starch 1500), colloidal silicon dioxide (aerosil), talc, microcrystalline cellulose, lactose (milk sugar), magnesium stearate.

Film casing composition: opadry II (polyvinyl alcohol, partially hydrolyzed, titanium dioxide, talc, macrogol (polyethylene glycol 3350), iron oxide (II) dye).

10 pieces. - contour cell packages (3) - cardboard packs.
30 pcs. - dark glass jars (1) - cardboard packs.
30 pcs. - polymer cans (1) - cardboard packs.
30 pcs. - polymer bottles (1) - cardboard packs.

pharmachologic effect

Selective beta 1 -adrenergic blocker, without its own sympathomimetic activity, does not have a membrane stabilizing effect. Reduces blood renin activity, reduces myocardial oxygen demand, reduces heart rate (at rest and during exercise).

It has hypotensive, antiarrhythmic and antianginal effects. Blocking in low doses beta 1 -adrenergic receptors of the heart, reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular flow of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect, inhibits conductivity and excitability of the myocardium, reduces AV-conductivity.

When the dose is increased above the therapeutic dose, it has a beta 2 -adrenoceptor blocking effect.

OPSS at the beginning of the drug, in the first 24 hours, increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and elimination of stimulation of beta 2 -adrenergic receptors), which returns to the initial one after 1-3 days, and decreases with prolonged administration.

The hypotensive effect is associated with a decrease in the minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (it is of great importance for patients with initial renin hypersecretion), restoration of sensitivity in response to a decrease in blood pressure and an effect on the central nervous system . With arterial hypertension, the effect occurs after 2-5 days, a stable effect - after 1-2 months.

The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate and a decrease in contractility, an increase in diastole, and an improvement in myocardial perfusion. By increasing the end-diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, oxygen demand can increase, especially in patients with chronic heart failure.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and a slowdown in AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions) through the AV node) and along additional paths.

When used in moderate therapeutic doses, in contrast to non-selective doses, it has a less pronounced effect on organs containing beta 2 -adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause sodium ion retention (Na +) in the body; the severity of atherogenic action does not differ from the action of propranolol.

Pharmacokinetics

Absorption and distribution

Absorption - 80-90%, food intake does not affect absorption. C max in blood plasma is observed after 1-3 hours.

The connection with blood plasma proteins is about 30%. Passes through the BBB and the placental barrier to an insignificant extent, in small amounts excreted in breast milk.

Metabolism and excretion

50% of the dose is metabolized in the liver to form inactive metabolites.

T 1/2 - 10-12 hours. About 98% is excreted in the urine - 50% unchanged, less than 2% - with bile.

Indications

- arterial hypertension;

- IHD: prevention of angina attacks.

Contraindications

- shock (including cardiogenic);

- collapse;

- pulmonary edema;

- acute insufficiency;

- chronic heart failure in the stage of decompensation;

- AV block II and III degree;

- sinoatrial blockade;

- severe bradycardia;

- Prinzmetal's angina;

- cardiomegaly (without signs of heart failure);

- arterial hypotension (systolic blood pressure less than 100 mm Hg, especially in myocardial infarction);

- Severe forms of bronchial asthma and a history of chronic obstructive pulmonary disease;

- simultaneous administration of MAO inhibitors (except for MAO-B);

- late stages of peripheral circulation disorders, Raynaud's disease;

- pheochromocytoma (without the simultaneous use of alpha-blockers);

- metabolic acidosis;

- age up to 18 years (efficacy and safety have not been established);

- hypersensitivity to drug components and other beta-blockers.

FROM caution the drug should be prescribed for hepatic failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes mellitus, degree I AV block, depression (including a history), psoriasis, as well as elderly patients.

Dosage

The drug is taken orally, in the morning, on an empty stomach, without chewing, at an initial dose of 5 mg 1 time / day. If necessary, the dose is increased to 10 mg 1 time / day. The maximum daily dose is 20 mg / day.

In patients with impaired renal function with CC less than 20 ml / min or with severe liver dysfunction the maximum daily dose should be 10 mg.

Dose adjustments in elderly patients not required.

Side effects

From the side of the central nervous system:increased fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesia in the extremities (in patients with intermittent claudication and Raynaud's syndrome), tremor.

From the senses:blurred vision, decreased secretion of lacrimal fluid, dry and sore eyes, conjunctivitis.

On the part of the cardiovascular system:sinus bradycardia, palpitations, myocardial conduction disturbances, AV blockade (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakening of myocardial contractility, development (worsening) of chronic heart failure (swelling of the ankles, feet, shortness of breath), lowering blood pressure, orthostatic hypotension, manifestation of angiospasm (increased impairment of peripheral circulation, cooling of the lower extremities, Raynaud's syndrome), chest pain.

From the digestive system:dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, liver dysfunction (dark urine, yellowness of the sclera or skin, cholestasis), taste changes.

From the respiratory system:nasal congestion, difficulty breathing when prescribed in high doses (loss of selectivity) and / or in predisposed patients - laryngo- and bronchospasm.

From the endocrine system:hyperglycemia (in patients with non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroidism.

Allergic reactions:itching, rash, urticaria.

Dermatological reactions:increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms.

On the part of laboratory parameters:thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in the activity of liver enzymes (increased ALT, ACT), bilirubin, triglycerides.

Effect on the fetus:intrauterine growth retardation, hypoglycemia, bradycardia.

Others:back pain, arthralgia, weakening of libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

Overdose

Symptoms: arrhythmia, ventricular premature beats, severe bradycardia, AV blockade, marked reduction in blood pressure, chronic heart failure, cyanosis of fingernails or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: gastric lavage and the appointment of adsorbents; symptomatic therapy: with developed AV blockade - intravenous injection of 1-2 mg, epinephrine or setting a temporary pacemaker; with ventricular premature beats - 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 - IV, if ineffective - the introduction of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate a pronounced decrease in blood pressure); with heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - intravenous diazepam; with bronchospasm, beta-adrenostimulants are inhaled.

Drug interactions

Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.

When administered intravenously, phenytoin, drugs for inhalation general anesthesia (derivatives of hydrocarbons) increase the severity of the cardiodepressant effect and the likelihood of lowering blood pressure.

Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Reduces the clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentration, especially in patients with an initially increased clearance of theophylline under the influence of smoking.

The antihypertensive effect is weakened by NSAIDs (Na + delay and blockade of renal prostaglandin synthesis), GCS and estrogens (Na + ion delay).

Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), amiodorone, and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV block, cardiac arrest, and heart failure.

Nifedipine can lead to a significant decrease in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.

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 increase CNS depression.

Simultaneous use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect, the break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days.

Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.

Ergotamine increases the risk of developing impaired peripheral circulation; sulfasalazine increases the plasma concentration of bisoprolol; rifampicin shortens the half-life.

special instructions

Monitoring patients taking Bisoprolol should include measuring heart rate and blood pressure (at the beginning of treatment - daily, then - once every 3-4 months), ECG, determination of blood glucose levels 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 trained in the method of calculating the heart rate and instructed on the need for medical consultation with a heart rate of less than 50 beats / min.

Beta-blockers are ineffective in about 20% of patients with angina pectoris. The main reasons are severe coronary atherosclerosis with a low ischemic threshold (heart rate less than 100 bpm) and an increased end-diastolic volume of the left ventricle, which disrupts subendocardial blood flow.

In smoking patients, the effectiveness of beta-blockers is lower.

Patients using contact lenses should take into account that during treatment, it is possible to reduce the production of tear fluid.

When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if an effective alpha-blockade is not previously achieved).

In case of thyrotoxicosis, Bisoprolol can mask certain clinical signs of thyrotoxicosis, for example, tachycardia. Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can increase the symptoms.

In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. In contrast to non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels.

With the simultaneous use of clonidine, its reception can be stopped only a few days after the cancellation of Bisoprolol.

It is possible that the severity of the hypersensitivity reaction and the lack of effect from usual doses of zpinephrine against the background of a burdened allergic history are possible. If it is necessary to carry out planned surgical treatment, the drug is discontinued 48 hours before the start of general anesthesia. If the patient has taken the drug before surgery, he should select a drug for general anesthesia with a minimally negative inotropic effect.

Reciprocal activation of the vagus nerve can be eliminated by IV administration of atropine (1-2 mg).

Medicines that reduce the reserves of catecholamines (including reserpine) can enhance the action of beta-blockers, therefore, patients taking such combinations of medicines should be under constant medical supervision for detecting a pronounced decrease in blood pressure or bradycardia.

Patients with bronchospastic diseases can be prescribed cardioselective adrenergic blockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs. Overdose is dangerous for the development of bronchospasm.

In case of detection in elderly patients of growing bradycardia (less than 50 beats / min.), A pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade, it is necessary to reduce the dose or stop treatment.

You can not abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose over 2 weeks or more (reduce the dose by 25% in 3-4 days). Should be canceled before testing the content of catecholamines, normetanephrine and vanillin mandelic acid in the blood and urine, antinuclear antibody titers.

List B. The drug should be stored in a dry, dark place, out of the reach of children, at a temperature not exceeding 25 ° C. The shelf life is 3 years.

With high pressure, the patient must be prescribed drugs to reduce it. One of the most inexpensive and affordable means is Bisoprolol.

Bisoprolol - description and action

Bisoprolol tablets are an antihypertensive drug, widely used in the treatment of hypertension and a number of other diseases of the heart and blood vessels. The tool belongs to the group of selective beta-blockers, available in two dosages:

  • 0.005 g (5 mg);
  • 0.01 g (10 mg).

The product is produced by various pharmaceutical companies - Teva, Pranafarm, Vertex, Atoll, Severnaya Zvezda and many others. Tablets are very inexpensive - in pharmacies you can find a package of 30 pieces of 10 mg each for 40-50 rubles.

The composition of the drug is represented by the active substance - bisoprolol fumarate, a number of auxiliary components (magnesium stearate, cellulose, starch, colloidal dioxide).

It is undesirable to divide the tablets, since they are film-coated.

Like other beta-blockers, the drug has a positive effect on blood vessels in arterial hypertension. Its purpose is to remove signs of high blood pressure, but the exact mechanism of operation has not yet been established. When taking bisoprolol, the amount and activity of renin in the blood decreases, and this leads to a decrease in the oxygen demand of the heart muscle. The pills also help to reduce the heart rate. Thus, three main effects of the drug are achieved:

At the very beginning of the intake, the drug causes an increase in the general vascular resistance. Already after 1-3 days of application, the indicator returns to the initial one, and even later decreases. With regular intake of Bisoprolol tablets, they help from hypertension in 2-5 days, and full pressure stabilization occurs in 30-60 days.

Indications of the drug and contraindications

The main purpose of the remedy is the treatment of arterial hypertension. Since it helps to improve the functional state of the heart, it is most often recommended for the combination of hypertension and coronary heart disease (CHD). In complex therapy, the medicine is indicated for:


The drug, when taken regularly, serves as a prophylactic agent against attacks of angina pectoris, they may not occur for months or years. The drug is used in monotherapy for primary hypertension, with the initial degree of the disease with a slight and moderate increase in pressure. In more difficult stages, it is usually recommended in complex therapy. Contraindications for taking the drug are as follows:

Take the drug with caution if there is a history of abnormal reactions to other beta-blockers.

Reception instructions

The medication should be taken strictly according to the indications. The method is as follows: they drink tablets in the dosage prescribed by the doctor in the morning, before meals (15-30 minutes).

It is also possible to take the drug during breakfast, after breakfast. Take a tablet with a small amount of water. Reception is once / day.

It is forbidden to bite, chew, grind bisoprolol tablets into powder.

The dosage is always chosen individually, it depends on the severity of the disease, the duration of the course of the disease, on the presence of additional pathologies and the cause of hypertension. Heart rate is also taken into account. Usually the order of therapy is as follows:

In case of impaired renal function in a patient with glomerular filtration below 20 ml / minute, the maximum amount of Bisoprolol is 10 mg. Increasing the dosage is highly undesirable, since the excretion of metabolites occurs with the participation of the kidneys.

If the dosage regimen is violated, the probability of an overdose is high. It is manifested by heart rhythm disturbances (blockade, extrasystole). The patient may have a sharp decrease in pressure, blood sugar, there is a risk of seizures, fainting, bronchospasm. In severe cases, acute heart failure is possible. Treatment - gastric lavage, the introduction of symptomatic agents (epinephrine, etc.).

How to properly stop taking bisoprolol

The drug Bisoprolol has a specific dosage regimen:

  • the first 7 days - 1/4 tablet 5 mg;
  • the next 7 days, the dosage is doubled - 1/2 tablet (2.5 mg bisoprolol fumarate);
  • after 14 days, the dosage will be 3/4 tablet;
  • then the dose is increased to 1 tablet, which contains 5 mg of the active substance;
  • within 5 weeks, take 7.5 mg;
  • at 6 weeks, the maximum dosage is prescribed - 10 mg.

This treatment regimen can only be followed if the medication is well tolerated. But in any case, only a doctor should determine the scheme and dosage. No matter how long the therapy with Bisoprolol lasts, you cannot abruptly stop taking the medicine. They finish it gradually, as they started. To do this, you need to reduce the dosage from 10 mg to 1.25 mg. Only during the therapeutic course should the deterioration of health be prevented. It is necessary to reduce the dosage of the drug within 10-14 days.

If it is necessary to prevent critical conditions, implying disturbances in the work of the heart, as well as to control blood pressure, then take Bisoprolol 1 tablet per day, regardless of the meal.

Compared with cheap artificial counterparts, the medication does not adversely affect men's health, metabolic processes in the body are not disturbed and rarely leads to the development of side effects. But nevertheless, the following symptoms may develop: headache, depression, changes in the ECG, drowsiness or insomnia, dizziness, blurred vision or hearing, dryness of the conjunctiva. If you could not avoid them, then you need to urgently call an ambulance. While the doctors arrive, you need to rinse your stomach and drink activated charcoal to cleanse your internal organs.

Side effects - what to fear?

The most common side effects relate to changes in heart rate and are observed at the initial stage of therapy. Subsequently, the condition stabilizes. People with heart failure have bradycardia - a slow heartbeat. In the same category of patients, a strong decrease in pressure, angiospasm, atrioventricular conduction disorders, and edema are more often observed.

In severe cases, transverse blockade with asystole was recorded.

Against the background of the treatment, there may be sensations of "goose bumps", cold in the legs, hands. Sometimes there is chest pain, shortness of breath. Side effects from the nervous system are dizziness, sleep disturbances, depression, drowsiness, tremors.

Almost all of these signs go away on their own within 14 days from the start of treatment. Less common were visual impairments, dry eyes, conjunctivitis, hearing loss.

Bisoprolol analogs and substitutes

Bisoprolol analogs include drugs - beta-blockers. Their action is based on neutralizing the receptors of the heart and blood vessels that are sensitive to adrenaline and norepinephrine. The first of this pharmaceutical group was the original patented drug containing the active substance bisoprolol (manufactured by Merc, Germany). Generics of Concor are Bidop, Niperten, Bisoprolol Teva, Aritel, Bisogamma, Biol, Cordinorm Cor and other preparations containing bisoprolol.

Other beta-blockers - bisoprolol analogues:

Tradename Active substance Release form and dosage Manufacturers Price
Metoprolol Metoprolol tartroate 50 and 100 mg tablets "Ozone", "Biochemist", "Marbiopharm", "Organics" (Russia); Hemopharm (Serbia); Zentiva (Slovakia); Adipharm (Bulgaria); Ratiopharm (Germany) From 33 rubles
Atenolol 25, 50 and 100 mg tablets Atoll (Russia); Ipca Laboratories (India); Shreya Life Sciences (India); Tatkhimfarmpreparaty (Russia); "Renewal" (Russia); Nycomed Danmark (Denmark) From 17 rubles
Propranalol hydrochloride 10 and 40 mg tablets Tatkhimfarmpreparaty, Irbitskiy Khimfarmzavod, Biosintez, Sintez (Russia); "Health" (Ukraine), "Olainfarm" (Latvia) From 15 rubles
Nebilet Nebivolol hydrochloride 5 mg tablets Berlin-Chemie, Germany From 500 rubles
Carvedilol 6.25, 12.5 and 25 mg tablets "VERTEX", "Ozone" "Active component" (Russia); Polpharma (Poland); Moehs Catalana S.A. (Spain); G. Amphray Laboratories (India); Teva FP (Israel) From 101 rubles
Locren Betaxolol Tablets 20 mg Sanofi-Winthrop Industrie, France From 720 rubles

Bisoprolol substitutes - calcium antagonists

Substitutes are medicines that give a similar result, but have a different principle of action. These include slow calcium channel blockers (BMCC), or calcium antagonists. The principle of action is to block the channels through which calcium ions pass into the cells, causing a spasm of the vascular wall. By expanding the coronary vessels, calcium antagonists improve the nutrition of the heart muscle. The result of using BMCC is a decrease in blood pressure, a decrease in cardiac output and myocardial oxygen demand.

The most popular drugs BMCC:

Preparations - ACE inhibitors

Another group of antihypertensive drugs - bisoprolol substitutes - angiotensin-converting enzyme inhibitors. The hypotensive effect is achieved by suppressing the synthesis of the enzyme angiotensin II, which causes vasospasm. ACE inhibitors have the same cumulative effect as beta blockers and are prescribed for continuous use.

A special group of ACE inhibitors are sartans. These are advanced modern drugs that have a minimum of contraindications and side effects compared to other antihypertensive drugs. Sartans do not adversely affect cardiac activity.

The most popular drugs in this group:

It is important to know

During therapy, it is important to regularly measure blood pressure readings. At the beginning of the course, it is important to conduct an ECG at least once every 3 months. Patients with diabetes mellitus need to measure the concentration of sugar in the peripheral blood daily, take urine tests every 3-4 months to monitor kidney function. You should also regularly measure the pulse (heart rate), if it drops to less than 50 beats per minute, immediately consult a doctor.

In patients with bronchial asthma, dynamic control of the respiratory system is performed. During therapy, a decrease in the production of tear fluid is possible, which must be taken into account when wearing contact lenses.

Bisoprolol is a drug that, along with metoprolol and atenolol, belongs to the group of beta-blockers. This remedy is indispensable for cardiovascular diseases (coronary artery disease and high blood pressure).

Other names and classification

This medicine contains the following medicines:

  • Concor;
  • Coronal;
  • Concor Cor;
  • Aritel;
  • Bidop;
  • Cordinorm;
  • Tyrez;
  • Bisangil (a complex preparation containing bisoprolol fumarate and hydrochlorothiazide);
  • Biol;
  • Biprol.

In the anatomical-therapeutic-chemical classification of medicines, the code for this medication is C07AB07. If the drug is combined with thiazide diuretics, then the code is C07BB07.

Russian name

In Russian, the medicine is called Bisoprolol.

Latin name

The name in Latin is Bisoprolol.

Trade names

Trade names of the drug are Metoprolol-Teva, Prana, OBL, Lexvm and Lugal. These are synonyms.

CAS code

It is a drug numerical code that is registered with the American Chemical Society.

Composition and form of release

The medicine is available only in the form of film-coated tablets for oral administration. They are round in shape with two bulges. Color from beige to slightly yellowish. The components of the medicine are:

  • beta1-blocker;
  • primellose;
  • starch;
  • povidone;
  • cellulose;
  • talc;
  • milk sugar;
  • aerosil;
  • magnesium stearate.

The shell contains polyvinyl alcohol, iron oxide (is a dye), talc, macrogol and titanium dioxide.

Pharmacological group

The medicine belongs to the group of cardiovascular drugs. It is a selective blocker of beta1-adrenergic receptors, which are localized in the tissues of the heart.

pharmachologic effect

A beta blocker has the following effects on a person with hypertension or angina:

  1. Helps reduce blood pressure. A beta blocker reduces ventricular arterial blood output and sympathetic nervous system activity. The release of catecholamines (adrenaline and norepinephrine, which are synthesized by the adrenal glands) also decreases and renin activity decreases. Acts slowly. Blood pressure decreases after 3-5 days. A persistent drop in pressure is observed one month after the start of therapy.
  2. It has an antianginal effect (improves oxygen saturation of the myocardium). This is achieved by lowering the heart rate (heart rate), which helps to reduce myocardial oxygen demand, reduce the contraction force of the heart muscle, increase the diastole period and improve blood distribution (perfusion).
  3. Eliminates arrhythmia. The drug inhibits the conduction of a nerve impulse through the atrioventricular (atrioventricular) node. A beta blocker removes tachycardia and decreases cAMP production.
  4. To a lesser extent, it affects the organs in which there are beta2-adrenergic receptors (lungs, uterus, muscles, peripheral vessels).

What is Bisoprolol for?

There are the following indications for the appointment of Bisoprolol:

  • primary and secondary hypertension (high blood pressure);
  • angina attacks;
  • chronic heart failure.

How to take Bisoprolol

The tablets should be taken orally whole, 5 mg or 10 mg once a day (in the morning).

With arrhythmia

The tablets are taken once a day. For arrhythmias, the maximum allowable dose may be 20 mg. This creates an increased concentration of the active substance in the blood. The drug is used for ventricular tachycardia and atrial fibrillation. In atrial fibrillation, a beta-blocker controls the ventricular rate at rest and during exercise.

Quickly about drugs. Bisoprolol

With heart failure

The drug is not prescribed for AHF (acute form of heart failure) and CHF in the decompensation phase. After 4 hours from the start of CHF therapy with bisoprolol at a dose of 1.25 mg, the heart rate and blood pressure are monitored. Often these tablets are combined with other drugs (angiotensin-converting enzyme inhibitors, diuretics or cardiac glycosides). In this case, it is recommended to start therapy with angiotensin-converting enzyme inhibitors. With CHF, the drug is prescribed for life. In case of side effects, it is required to reduce the dosage or replace the tablets with analogues.

With increased pressure

Treatment may start with a low dose of 5 mg. If necessary, it is increased. Treatment with high doses of drugs is not used because of the high risk of a pronounced decrease in blood pressure.

With ischemic heart disease

The medicine eliminates the symptoms of myocardial ischemia with a stable form of angina pectoris. With this form of ischemic heart disease, the drug can be taken simultaneously with calcium channel blockers. This medication is more effective than Nifedipine.

special instructions

When treating with Bisoprolol it is necessary:

  • Select the dose individually, taking into account contraindications and the severity of the disease.
  • Monitor vital signs of body functioning. In the early stages of treatment, blood pressure and heart rate are measured every day, and then once every 3-4 months.
  • Monitor renal function in elderly patients. For this purpose, ultrasound and general clinical urinalysis are performed.
  • To assess the function of external respiration in patients with diseases of the lungs and bronchi.
  • Consult an ophthalmologist, as taking bisoprolol increases the risk of developing dry eye syndrome. The reason is a decrease in the production of tear fluid.
  • Do not abruptly stop treatment in the presence of thyrotoxicosis. In such people, after discontinuation of the drug, an increase in blood pressure is possible.
  • In the case of taking medications based on clonidine, they should not be canceled immediately, only a few days after the end of therapy with Bisoprolol.
  • Constantly monitor patients taking reserpine in parallel.
  • Suspend treatment in case of a sharp deterioration in mood (depression).
  • Observe safety precautions when working with dangerous equipment and when driving a machine.

Application during pregnancy and lactation

A beta1-blocker is prescribed only when the benefit to the mother outweighs the possible harm to the unborn child. The active substance can cross the placenta and complicate the course of pregnancy.

Side effects

During therapy with Bisoprolol, the following undesirable effects are possible:

  • Dysfunction of the nervous system. It manifests itself as weakness, headache, impaired consciousness, depression, difficulty sleeping at night, hallucinations, memory impairment up to its loss, tremors (tremors) and sensitive disorders in the form of paresthesias.
  • Signs of eye damage (watery eyes, redness, dryness, pain, and decreased vision). Conjunctivitis is common. It is most commonly seen in patients who wear contact lenses.
  • Respiratory problems (difficulty breathing).
  • Endocrine disorders (increased blood sugar in people with type 2 diabetes, hypoglycemia in people with type 1 diabetes, decreased production of thyroid hormones).
  • Allergy (exanthema, urticaria, itching).
  • Signs of lesions of the skin and appendages (increased sweating, rash, skin redness, exacerbation of psoriasis).
  • Changes in the blood picture (bleeding and hemorrhage due to a decrease in platelet count, leukopenia, increased ALT and AST, bilirubinemia and increased triglycerides).
  • Cardiovascular disorders (sinus bradycardia, impaired arterial circulation, atrioventricular block, cardiac arrest, palpitations, edema of the lower extremities, shortness of breath, a sharp drop in blood pressure, vascular spasm and chest pain).
  • Manifestations of dysfunction of the digestive system (pain in the abdomen or hypochondrium, stool disturbance, dry mouth, nausea, vomiting, dark urine, yellowness of the skin, taste disturbance).
  • Signs of fetal damage (when taking pills during pregnancy). Includes bradycardia (a rare heartbeat), developmental delay, and decreased blood glucose.
  • Withdrawal syndrome.
  • Joint and back pain.

Effect of bisoprolol on potency

Taking Bisoprolol often leads to a violation of potency in men and a decrease in libido in both sexes.

Contraindications

Medicines based on bisoprolol are not prescribed for:

  • heart valve disease;
  • blockade of the sinoatrial node;
  • intolerance to the components;
  • heart shock;
  • collapse;
  • pulmonary edema;
  • decompensated heart failure;
  • prinzmetal's angina;
  • sick sinus syndrome;
  • an enlarged heart (cardiomegaly);
  • atrioventricular blockade of the 3rd and 4th degrees;
  • severe bronchial asthma;
  • low blood pressure;
  • raynaud's disease;
  • COPD;
  • pheochromocytoma;
  • simultaneous administration of MAO inhibitors (monoamine oxidase);
  • metabolic acidosis.

The medicine is contraindicated in children.

Overdose

Overdose is manifested by a deterioration in the general condition of the patient. There are:

  • bradycardia;
  • violation of the rhythm of the heartbeat;
  • hypotension;
  • spasm of the bronchi (characterized by shortness of breath or attacks of suffocation);
  • acrocyanosis;
  • convulsions;
  • dizziness;
  • fainting.

Help consists in gastric lavage, the use of sorbents (activated carbon, Polysorb) and calling an ambulance. The doctor prescribes symptomatic agents (Epinephrine, Atropine, plasma substitutes, Lidocaine, Diazepam, cardiac glycosides). In the case of bronchospasm, beta2-adrenergic agonists are administered by inhalation.

Interoperability and compatibility

Preparations with bisoprolol are incompatible with the following medicines:

  • iodine-containing preparations used as dyes during radiography;
  • medicines for general anesthesia;
  • other antiarrhythmic drugs;
  • Methyldopa;
  • Reserpine;
  • antipsychotics;
  • ethanol;
  • antidepressants;
  • ergot alkaloids;
  • ergotamine.

When Bisoprolol is combined with diuretics, sympatholytics and clonidine, an excessive decrease in blood pressure is possible. With the simultaneous use of calcium slow-channel blockers and glycosides, there is a risk of cardiac arrest.

Manufacturers

The manufacturers of Aritel Cor, Aritel, Biprol, Bisangil and Aritel Plus tablets are Russian pharmaceutical companies. The producers of Bidop and Bidop Cor are Hungary and Ireland. Biol and Biprol Plus tablets are produced by Switzerland, Germany and Slovenia.

Analogs

Bisoprolol analogs and substitutes are:

  1. Concor. Contains a beta-blocker in the form of fumarate at a dosage of 10 mg.
  2. Lisinopril. Substitute for bisoprolol. The main active ingredient is lisinopril dihydrate. This is a representative of the group of ACE inhibitors, used for hypertension and angina pectoris. Contraindicated in pregnancy, children and during breastfeeding.
  3. Amlodipine. A drug from the group of calcium channels. It has antihypertensive and antianginal effects. Unlike bisoprolol, it can be prescribed for Prinzmetal's angina.
  4. Metoprolol. Beta1-blocker. The effects are similar to those of bisoprolol. The medicine can be prescribed both for cardiac pathology, and for migraine and hyperthyroidism. The antihypertensive effect is due to a decrease in renin activity.
  5. Terms of sale

    The sale of pills should only be carried out with a prescription.

    Price

    The cost of tablets with bisoprolol ranges from 30 to 260 rubles (for Bisangil). The price depends a lot on the manufacturer.

    Storage conditions and periods

    Medicines based on bisoprolol are included in list B. Tablets are stored in a dry place, protected from light and children. Storage temperature should not exceed 25ºC. Medicines for oral administration are valid for 3 years from the date of manufacture.

We recommend reading

Up