Bisoprolol-Prana

The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.

Before starting treatment, it is recommended to conduct a study of external respiratory function in patients with a burdened bronchopulmonary history. In approximately 20% of patients with angina, β-blockers are ineffective. The main reasons: severe coronary atherosclerosis with a low ischemic threshold (heart rate less than 100 beats/min) and increased end-diastolic volume of the left ventricle, disrupting subendocardial blood flow.

In smokers, the effectiveness of β-blockers is lower.

Patients using contact lenses should take into account that during treatment the production of tear fluid may decrease.

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

In thyrotoxicosis, bisoprolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms.

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

When taking clonidine at the same time, it can be discontinued only a few days after discontinuation of the drug BISOPROLOL-PRANA.

It is possible that the severity of the hypersensitivity reaction may increase and there will be no effect from usual doses of epinephrine against the background of a burdened allergic history.

If planned surgical treatment is necessary, the drug should be discontinued 48 hours before the start of general anesthesia. If the patient took the drug before surgery, he should choose a drug for general anesthesia with minimal negative inotropic effect.

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

Medicines that reduce the supply of catecholamines (including reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a pronounced decrease in blood pressure or bradycardia.

Patients with bronchospastic diseases can be prescribed cardioselective β-blockers in case of intolerance and/or ineffectiveness of other antihypertensive drugs. An overdose is dangerous due to the development of bronchospasm.

If increasing bradycardia (less than 50 beats/min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), or AV blockade is detected in elderly patients, it is necessary to reduce the dose or stop treatment.

It is recommended to discontinue therapy if depression develops.

It should be discontinued before testing the content of catecholamines, normetanephrine and vanillinmandelic acid in the blood and urine, and titers of antinuclear antibodies.

Bisoprolol-Prana, 10 mg, film-coated tablets, 30 pcs.

Monitoring of patients taking the drug BISOPROLOL-PRANA should include measuring heart rate and blood pressure (at the beginning of treatment - daily, then - once every 3-4 months), conducting an ECG, determining the concentration of glucose in the blood in patients with diabetes mellitus (once every 4 months). -5 months). In elderly patients, it is recommended to monitor renal function (once every 4–5 months).

The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.

Before starting treatment, it is recommended to conduct a study of external respiratory function in patients with a burdened bronchopulmonary history.

In approximately 20% of patients with angina, β-blockers are ineffective. The main reasons: severe coronary atherosclerosis with a low ischemic threshold (heart rate less than 100 beats/min) and increased end-diastolic volume of the left ventricle, disrupting subendocardial blood flow.

In smokers, the effectiveness of β-blockers is lower.

Patients using contact lenses should take into account that during treatment the production of tear fluid may decrease.

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

When taking clonidine at the same time, it can be discontinued only a few days after discontinuation of the drug BISOPROLOL-PRANA.

It is possible that the severity of the hypersensitivity reaction may increase and there will be no effect from usual doses of epinephrine against the background of a burdened allergic history.

Reciprocal activation of the vagus nerve can be reversed by intravenous atropine (1–2 mg).

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

It is recommended to discontinue therapy if depression develops.

Treatment should not be abruptly interrupted due to the risk of developing withdrawal syndrome (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). It should be discontinued before testing the content of catecholamines, normetanephrine and vanillylmandelic acid in the blood and urine, and titers of antinuclear antibodies.

Effect on the ability to drive a car and other mechanical means

The question of the possibility of engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions should be decided only after assessing the patient’s individual response to the drug (especially at the beginning of treatment, due to the possibility of developing dizziness).

Bisoprolol

Bisoprolol is a selective (cardioselective) beta-1 blocker with antihypertensive, antiarrhythmic and antianginal effects. The drug reduces the need for oxygen in the heart muscle, slows the heart rate, and “disarms” renin circulating in the blood plasma. Good tolerance by patients, high efficiency and the ability to prevent the development of a number of negative consequences of arterial hypertension have elevated beta blockers to the rank of permanent participants in the “battle” against cardiovascular diseases, which is waged today with varying success in modern cardiology. The discovery of subtypes of beta-1 and beta-2 adrenergic receptors at the end of the 60s of the last century prompted scientists to think about selective blockade of the former, because It is they, interacting with catecholamines, that create a favorable background for moving the tonometer needle beyond the WHO-recommended borderline readings of “140/90”. Selectivity (or cardioselectivity) has little effect on the hypotensive and antianginal effects of beta-blockers, while reducing the likelihood of a number of unpleasant side effects associated with stimulation of beta-2 adrenergic receptors (for example, bronchospasm or peripheral vasoconstriction).

Among all beta blockers known today, bisoprolol is endowed with the greatest selectivity and effectiveness. The antihypertensive effect of bisoprolol is comparable to that of calcium channel blockers and angiotensin-converting enzyme inhibitors. Distinctive features of this drug are also high (about 90%) bioavailability, long elimination period and “elusiveness” for proteins, with which no more than 30% of the active substance of the drug binds.

Moreover, these purely positive qualities of bisoprolol are characteristic of it regardless of the dose, which makes it possible to reduce the frequency of administration to a minimum - once a day. Having the advantages of both lipophilic (high absorption rate) and hydrophilic (long elimination time, insignificant biotransformations after the first passage through the liver) beta blockers, bisoprolol can be used in patients with liver and kidney diseases without changing the dose. As already mentioned, bisoprolol has the highest degree of cardioselectivity and only minimally affects beta-2 adrenergic receptors. This allows the drug to be prescribed to patients with chronic bronchial obstruction, bronchial asthma and atherosclerosis of peripheral vessels. Bisoprolol does not interfere with the processes of carbohydrate and lipid metabolism, and therefore does not cause increased insulin resistance. Regular and long-term use of bisoprolol for arterial hypertension, angina pectoris, chronic heart failure allows not only to curb “unleashed” blood pressure, reduce the frequency of angina manifestations, prevent or stop the progression of heart failure, but also significantly reduce the development of severe cardiovascular complications, thereby improving health prognosis patient and increasing his life expectancy.

Bisoprolol-Prana tablets ppo 5mg No. 30

Compound

Active substance: bisoprolol fumarate - 5 mg. Excipients: corn starch, microcrystalline cellulose (type 102), magnesium stearate, crospovidone, colloidal silicon dioxide, anhydrous calcium hydrogen phosphate.

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 penetrates to a small extent through the BBB and the placental barrier; excreted in breast milk.

Metabolized in the liver.

T1/2 - 9-12 hours. Excreted by the kidneys - 50% unchanged, less than 2% - with bile.

Indications for use

Arterial hypertension, prevention of angina attacks, chronic heart failure.

Contraindications

hypersensitivity to the components of the drug and other β-blockers;
shock (including cardiogenic);
collapse;
pulmonary edema;
acute heart failure, chronic heart failure in the stage of decompensation;
atrioventricular (AV) block II-III degree, sinoatrial block;
sick sinus syndrome;
severe bradycardia;
Prinzmetal's angina;
cardiomegaly (without signs of heart failure);
arterial hypotension (systolic blood pressure less than 100 mm Hg, especially with myocardial infarction);
severe forms of bronchial asthma and chronic obstructive pulmonary disease (COPD) in history;
simultaneous use of monoamine oxidase inhibitors (MAO) (with the exception of MAO-B);
late stages of peripheral circulatory disorders;
Raynaud's disease;
pheochromocytoma (without simultaneous use of α-blockers);
metabolic acidosis;
age under 18 years (efficacy and safety have not been established).

Directions for use and doses

Inside, in the morning on an empty stomach, without chewing, once.

Arterial hypertension and coronary heart disease: prevention of angina attacks

It is recommended to take 5 mg once. If necessary, the dose is increased to 10 mg 1 time per day. The maximum daily dose is 20 mg.

In all cases, the dosage regimen and dosage are selected by the doctor individually for each patient, in particular, taking into account heart rate values and therapeutic response.

In patients with impaired renal function with creatinine clearance (CC) less than 20 ml/min, or with severe liver dysfunction, the maximum daily dose is 10 mg.

No dose adjustment is required in elderly patients.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25°C.

Keep out of the reach of children.

Best before date

3 years. Do not use after the expiration date stated on the package.

special instructions

Use with caution for psoriasis and when there is a family history of psoriasis, diabetes mellitus in the decompensation phase, or with a predisposition to allergic reactions. In case of pheochromocytoma, the use of bisoprolol is possible only after taking alpha-blockers. Avoid abrupt withdrawal of bisoprolol; the course of treatment should be completed slowly with a gradual reduction in dose. Before surgery, the anesthesiologist should be informed about treatment with bisoprolol.

Bisoprolol at a dose of more than 10 mg/day should be used only in exceptional cases.

This dose should not be exceeded in case of renal failure (creatinine clearance less than 20 ml/min) and severe liver dysfunction.

During the treatment period, avoid drinking alcohol.

Description

Beta1-blocker.

Dosage form

Light yellow film-coated tablets, round, biconvex, scored; On a cross section, two layers are visible, the inner layer is white or almost white.

Use in children

Contraindicated for people under 18 years of age.

Pharmacodynamics

A selective beta1-blocker without internal sympathomimetic activity and does not have membrane stabilizing activity. Reduces plasma renin activity, reduces myocardial oxygen demand, reduces heart rate (at rest and during exercise) and cardiac output, while stroke volume does not decrease significantly. Inhibits AV conduction. Has antianginal and hypotensive effects. In high doses (200 mg or more) it can cause blockade of β2-adrenergic receptors, mainly in the bronchi and vascular smooth muscles.

The hypotensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (of greater importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure and an effect on the central nervous system.

The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate and decreased contractility, prolongation of diastole, and improved myocardial perfusion.

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 via the AV node) and along additional paths.

Side effects

From the nervous system: weakness, fatigue, dizziness, headache, sleep disorders, mental disorders (depression, rarely hallucinations), feeling of cold and paresthesia in the extremities.

From the cardiovascular system: orthostatic hypotension, bradycardia, impaired AV conduction, the appearance of symptoms of heart failure, worsening intermittent claudication and the main clinical symptoms of Raynaud's syndrome.

From the organ of vision: decreased secretion of tear fluid, conjunctivitis.

From the digestive system: diarrhea, constipation, nausea, abdominal pain.

From the musculoskeletal system: muscle weakness, muscle cramps.

From the skin and subcutaneous tissues: skin 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.

Other: sweating, hot flashes, impaired potency, decreased glucose tolerance in patients with diabetes, allergic reactions.

Use during pregnancy and breastfeeding

Use during pregnancy and lactation is not recommended and is possible only in cases where the expected benefit to the mother outweighs the potential risk of side effects in the fetus and child.

In exceptional cases of use during pregnancy, bisoprolol should be discontinued 72 hours before the expected due date due to the possibility of bradycardia, arterial hypotension, hypoglycemia and respiratory depression in the newborn. If discontinuation is not possible, then the condition of the newborn must be carefully monitored for 72 hours after birth.

If it is necessary to use bisoprolol during lactation, breastfeeding should be stopped.

Interaction

With the simultaneous use of antacids and antidiarrheals, the absorption of beta-blockers may be reduced.
With the simultaneous use of antiarrhythmic drugs, a sharp decrease in blood pressure, a decrease in heart rate, and the development of arrhythmia and/or heart failure are possible.
With the simultaneous use of antihypertensive drugs, the antihypertensive effect may be enhanced.
With the simultaneous use of cardiac glycosides, conduction disturbances are possible.
With the simultaneous use of sympathomimetics (including those included in cough suppressants, nasal drops, eye drops), the effectiveness of bisoprolol decreases.
With the simultaneous use of verapamil and diltiazem, a sharp decrease in blood pressure, a decrease in heart rate, and the development of arrhythmia and/or heart failure are possible.
With simultaneous use of guanfacine, severe bradycardia and conduction disturbances are possible.
With the simultaneous use of insulin and hypoglycemic agents for oral administration, the effect of insulin or other hypoglycemic agents is enhanced (regular monitoring of plasma glucose levels is necessary).
With simultaneous use of clonidine, severe bradycardia, arterial hypotension, and conduction disturbances are possible.
In case of 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 and alpha-methyldopa, severe bradycardia is possible.
With simultaneous use of rifampicin, a slight decrease in T1/2 of bisoprolol is possible.
With the simultaneous use of ergotamine derivatives (including drugs for the treatment of migraines containing ergotamine), symptoms of peripheral circulatory disorders increase.

Overdose

Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, chronic heart failure, cyanosis of fingernails or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: gastric lavage and administration of adsorbents; symptomatic therapy:

in case of developed AV block - intravenous administration of 1-2 mg of atropine, epinephrine or temporary placement of a pacemaker;
for ventricular extrasystole - lidocaine (class IA drugs are not used);
when blood pressure decreases, the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema, intravenous administration of plasma-substituting solutions; if ineffective, administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic effects and eliminate a pronounced decrease in blood pressure);
for heart failure - cardiac glycosides, diuretics, glucagon;
for convulsions - intravenous diazepam;
for bronchospasm - β2-adrenergic stimulants by inhalation.

Release form

Film-coated tablets, 5 mg No. 30.

Impact on the ability to drive vehicles and operate machinery

Use with caution in patients whose activities require concentration and high speed of psychomotor reactions.