Biol, pills 2.5mg 30pcs

Composition

1 tablet contains:

Active ingredient:

bisoprolol hemifumarate 2.5 mg

excipients:

MCC;

calcium hydrophosphate;

corn starch;

croscarmellose sodium;

magnesium stearate;

colloidal anhydrous silicon dioxide

film shell:

lactose monohydrate; hypromellose; titanium dioxide; macrogol 4000; iron (III) oxide yellow dye; iron (III) oxide red dye (for a dosage of 10 mg)

Pharmacological action

Pharmacodynamics

Bisoprolol-a selective beta_-1-adrenoblocker, without its own sympathomimetic activity-does not have a membrane-stabilizing effect. As with other beta_-1blockers, the mechanism of action in hypertension is unclear. At the same time, it is known that bisoprolol reduces the activity of renin in blood plasma, reduces the need for myocardial oxygen, and reduces heart rate. It has antihypertensive, antiarrhythmic and antianginal effects.

By blocking the beta_-1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular flow of calcium ions, inhibits all heart functions, and reduces AV conduction and excitability. If the therapeutic dose is exceeded, it has a beta_-2-adrenoblocking effect. OPSS at the beginning of the drug use, in the first 24 hours, increases (as a result of a reciprocal increase in alpha-adrenergic activity and elimination of beta_-2— adrenergic stimulation), returns to its initial value after 1-3 days, and decreases with prolonged use. The antihypertensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the sympathoadrenal system (SAS) (which is of great 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. With arterial hypertension, the effect develops in 2-5 days, a stable effect is noted in 1-2 months.

The antianginal effect is due to a decrease in the myocardial oxygen demand as a result of reduced contractility and other myocardial functions, prolongation of diastole, and improvement of myocardial perfusion. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the ventricular muscle fibers, oxygen demand may increase, especially in patients with chronic heart failure (CHF).

When used in the medium therapeutic doses, unlike nonselective beta-blockers, has a less pronounced effect on the organs containing the beta₂-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus), and carbohydrate metabolism; it does not cause the delay of sodium ions in the body; the manifestation of atherogenic action is different from the action of propranolol.

Bisoprolol is almost completely absorbed from the gastrointestinal tract, food intake does not affect absorption. Bioavailability is about 90%.

T_max is 2-4 hours after oral use. Binding to plasma proteins is 26-33%. Metabolized in the liver, bisoprolol metabolites do not have pharmacological activity. T_1/2 is 9-12 hours, which makes it possible to use the drug once a day.

It is excreted by the kidneys-50% unchanged, less than 2% – through the intestines.

Permeability through the blood-brain and placental barrier is low, and small amounts are excreted in breast milk.

Indications

• arterial hypertension;
• IHD (prevention of stable angina attacks);
• CHF (as part of combination therapy).

Contraindications

• hypersensitivity to the medication and other beta-blockers;
• acute heart failure and CHF decompensation requiring inotropic therapy;
• cardiogenic shock;
• collapse;
• AV blockade of II–III degree, without pacemaker
• sinoatrial block;
• sick sinus syndrome node;
• bradycardia (heart rate before treatment less than 50 beats/min);
• severe hypotension (SBP less than 90 mm Hg. St. )
• cardiomegaly (without signs of heart failure);
• severe forms of bronchial asthma and COPD in history;
• severe peripheral circulatory disorders;
• Raynaud’s syndrome;
• metabolic acidosis;
• pheochromocytoma (without the simultaneous use of alpha-blockers);
• concomitant use floctafenine and sultopride;
• age to 18 years (efficacy and safety not established).

With caution:

• conducting desensitizing therapies;
• hyperthyroidism;
• diabetes mellitus type 1 and diabetes mellitus, with significant fluctuations in the concentration of glucose in the blood;
• severe renal insufficiency (Cl creatinine less than 20 ml/min);
• severe disturbances of liver function;
• psoriasis;
• AV blockade of I degree;
• Prinzmetal’s angina;
• restrictive cardiomyopathy;
• congenital heart defect or heart valve with severe hemodynamic disorders
• of CHF with myocardial infarction within the last 3 months;
• depression (including in history);
• pheochromocytoma (required the simultaneous use of alpha-blockers);
• a strict diet.

Side effects

the Frequency of adverse reactions listed below is defined as follows (the classification of who): very often — at least 10%; often — not less than 1% but < 10%; infrequently — no more than 0.1% but < 1%; rarely — not less than 0.01%, but less than 0.1%; very rarely — less than 0.01%, including individual messages.

From the cardiovascular system: very often — a decrease in heart rate (bradycardia, especially in patients with CHF), palpitation sensation; often — a pronounced decrease in blood pressure (especially in patients with CHF), angiospasm (increased peripheral circulatory disorders, a feeling of cold in the extremities (paresthesia); infrequently — violation of AV conduction (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, orthostatic hypotension, worsening of the course of CHF with the development of peripheral edema (swelling of the ankles, feet, shortness of breath), chest pain.

From the nervous system: often — dizziness, headache, asthenia, increased fatigue, sleep disorders, depression, anxiety; rarely-confusion or short-term memory loss, nightmares, hallucinations, myasthenia gravis, tremor, muscle cramps. Usually, these phenomena are mild and usually disappear within 1-2 weeks after the start of treatment.

From the sensory organs: rarely-visual impairment, reduced tear production (should be taken into account when wearing contact lenses), tinnitus, hearing loss, ear pain; very rarely — dry and painful eyes, conjunctivitis, taste disorders.

From the respiratory system: infrequently-bronchospasm in patients with bronchial asthma or obstructive airway diseases; rarely-allergic rhinitis; nasal congestion.

From the digestive system: often — nausea, vomiting, diarrhea, constipation, dryness of the oral mucosa, abdominal pain; rarely-hepatitis, increased activity of liver enzymes (ALT, AST), increased bilirubin concentration, taste changes.

From the musculoskeletal system: infrequently-arthralgia, back pain.

From the genitourinary system: very rarely — violation of potency, weakening of libido.

Laboratory parameters: rarely-an increase in the concentration of triglycerides in the blood; in some cases — thrombocytopenia, agranulocytosis, leukopenia.

Allergic reactions: rarely-skin pruritus, rash, urticaria.

From the skin: rarely-increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions; very rarely-alopecia; beta-blockers can exacerbate the course of psoriasis.

Other: withdrawal syndrome (increased frequency of angina attacks, increased blood pressure).

Interaction

Class I antiarrhythmic agents (e. g. quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone) may reduce AV conduction and myocardial contractility when used concomitantly with bisoprolol. Class III antiarrhythmic agents (such as amiodarone) may increase the violation of AV conduction. The action of beta-blockers for topical use (for example, eye drops for the treatment of glaucoma) may increase the systemic effects of bisoprolol (lowering blood pressure, lowering heart rate).

Parasympathomimetics, when used concomitantly with bisoprolol, may increase the violation of AV conduction and increase the risk of bradycardia.

Concomitant use of Biol® with beta-adrenomimetics (for example, isoprenaline, dobutamine) may lead to a decrease in the effect of both drugs. The combination of bisoprolol with adrenomimetics that affect beta-and alpha-adrenergic receptors (for example, norepinephrine, epinephrine) may increase the vasoconstrictor effects of these agents that occur with the participation of alpha-adrenergic receptors, leading to an increase in blood pressure. Such interactions are more likely to occur with non-selective beta-blockers.

Mefloquine, when co-administered with bisoprolol, may increase the risk of developing bradycardia.

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

Iodine-containing radiopaque diagnostic agents for intravenous use increase the risk of anaphylactic reactions.

Phenytoin with intravenous use, means for inhalation anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive effects and the likelihood of lowering blood pressure. The effectiveness of insulin and hypoglycemic agents for oral use may change during treatment with bisoprolol (masks the symptoms of developing hypoglycemia: tachycardia, increased blood pressure).

Clearance of lidocaine and xanthines (other than theophylline) may decrease due to a possible increase in their concentration in blood plasma, especially in patients with an initially increased clearance of theophylline under the influence of smoking. The antihypertensive effect is weakened by NSAIDs (sodium ion retention and blockade of PG synthesis by the kidneys), corticosteroids and estrogens (sodium ion retention).

Cardiac glycosides, methyldopa, reserpine and guanfacine, BMCC (verapamil, diltiazem), amiodarone and other antiarrhythmic agents 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 agents may lead to an excessive decrease in blood pressure. The effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins may be prolonged during treatment with bisoprolol.

Tricyclic and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and sleeping pills increase CNS depression.

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

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

Sulfasalazine increases the concentration of bisoprolol in the blood plasma.

Rifampicin shortens T_1/2 bisoprolol.

How to take, course of use and dosage

Inside, in the morning, on an empty stomach (before breakfast), during breakfast or after it 1 time a day with a small amount of liquid. Tablets should not be chewed or ground into powder.

In all cases, the mode of use and dose is selected by the doctor for each patient individually, in particular, taking into account the patient’s heart rate and condition.

Arterial hypertension and CHD

In patients with arterial hypertension and coronary heart disease, Biol® is used 5 mg once a day. If necessary, the dose is increased to 10 mg once a day.

In the treatment of arterial hypertension and angina pectoris, the maximum daily dose is 20 mg 1 time/day.

CHF

Starting treatment for CHF with Biol® requires a special titration phase and regular medical monitoring.

A prerequisite for treatment with Biol® is stable CHF without signs of exacerbation.

Treatment of CHF with Biol ® begins according to the following titration schedule. This may require individual adjustment, depending on how well the patient tolerates the prescribed dose, i. e. the dose can only be increased if the previous dose was well tolerated.

To ensure an appropriate titration process at the initial stages of treatment, it is recommended to use the drug in smaller doses.

The recommended starting dose is 1.25 mg (1/4 tablet of 5 mg) once a day. Depending on individual tolerance, the dose should be gradually increased to 2.5 mg (1/2 table of Biol® 5 mg),3.75 mg (3/4 table of 5 mg),5 mg (1 table of Biol® 5 mg or 1/2 table of 10 mg),7.5 mg (3/4 table of 10 mg) and 10 mg once a day with an interval of at least 2 weeks.

If an increase in the dose of the drug is poorly tolerated by the patient, it is possible to reduce the dose.

The maximum daily dose for the treatment of CHF is 10 mg once a day.

During titration, regular monitoring of blood pressure, heart rate, and symptoms of increasing CHF severity is recommended. Worsening of the symptoms of CHF is possible from the first day of use of the drug.

During or after the titration phase, there may be a temporary deterioration in the course of CHF, hypotension, or bradycardia. In this case, it is recommended to first pay attention to the selection of the dose of concomitant standard therapy. It may also be necessary to temporarily reduce the dose of Biol® 5 mg or discontinue treatment. After the patient’s condition stabilizes, the dose should be re-titrated or the treatment should be continued.

Impaired kidney or liver function

Mild or moderate hepatic or renal impairment usually does not require dose adjustment. In patients with severe renal impairment (creatinine clearance less than 20 ml / min) and in patients with severe liver disease, the maximum daily dose is 10 mg. Increasing the dose in such patients should be carried out with extreme caution.

Elderly patients

No dose adjustment is required.

To date, there are insufficient data on the use of Biol® 5 mg in patients with CHF associated with type 1 diabetes mellitus, severe renal and/or liver dysfunction, restrictive cardiomyopathy, congenital heart defects or hemodynamically caused heart disease. Also, until now, insufficient data have been obtained on patients with CHF with myocardial infarction during the last 3 months.

Overdose

Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, acute heart failure, hypoglycemia, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: if an overdose occurs, first of all it is necessary to stop taking the drug, conduct gastric lavage, take adsorbents, and conduct symptomatic therapy.

With severe bradycardia-IV use of atropine. If the effect is insufficient, you can use caution to introduce a drug that has a positive chronotropic effect. Sometimes it may be necessary to temporarily install an artificial pacemaker.

With a pronounced decrease in blood pressure, intravenous use of plasma — substituting solutions and vasopressors is recommended. In case of hypoglycemia, intravenous use of glucagon or dextrose (glucose) may be indicated. With AV block, patients should be constantly monitored and treated with beta-adrenomimetics, such as epinephrine. If necessary, an artificial pacemaker can be installed.

If the course of CHF worsens, intravenous diuretics, drugs with a positive inotropic effect, as well as vasodilators are administered.

With bronchospasm-the appointment of bronchodilators, including beta-adrenomimetics and / or aminophylline.

Special instructions

Do not abruptly discontinue treatment with Biol® due to the risk of developing severe arrhythmias and myocardial infarction. Withdrawal is carried out gradually, reducing the dose by 25% every 3-4 days.

Monitoring of the condition of patients taking Biol® should include measuring heart rate and blood pressure (at the beginning of treatment — daily, then — 1 time in 3-4 months), performing an ECG, determining the concentration of blood glucose in patients with diabetes mellitus (1 time in 4-5 months).

In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months).

The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.

In case of increasing bradycardia (heart rate less than 50 beats/min), marked decrease in blood pressure (sBP less than 100 mm Hg), AV blockade in elderly patients, it is necessary to reduce the dose or discontinue treatment. Before starting treatment, it is recommended to conduct a study of the function of external respiration in patients with a burdened bronchopulmonary history.

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

When using Biol® in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if effective alpha-adrenergic blockade is not achieved beforehand).

In hyperthyroidism, bisoprolol may mask certain clinical signs of hyperthyroidism (for example, tachycardia). Abrupt withdrawal of the drug in patients with hyperthyroidism is contraindicated, since it can increase symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal values. With simultaneous use of clonidine, its use can be stopped only a few days after the withdrawal of Biol®.

It is possible to increase the severity of the hypersensitivity reaction and the lack of effect from conventional doses of epinephrine against the background of a burdened allergic history.

If elective surgical treatment is necessary, the drug should be discontinued 48 hours before 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 use of atropine (1-2 mg). Drugs that deplete the catecholamine depot (including reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be constantly monitored by a doctor for a pronounced decrease in blood pressure or bradycardia.

Patients with bronchospastic diseases may be cautiously prescribed cardioselective beta-blockers in case of intolerance and/or ineffectiveness of other antihypertensive agents. Against the background of taking beta-blockers in patients with concomitant bronchial asthma, airway resistance may increase. If the dose of Biol® is exceeded, such patients are at risk of developing bronchospasm.

If patients show increasing bradycardia (heart rate less than 50 beats / min), a marked decrease in blood pressure (sBP less than 100 mm Hg), AV blockade, it is necessary to reduce the dose or discontinue treatment.

It is recommended to discontinue therapy with Biol® if depression develops.

Do not abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction. Discontinuation of the drug is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days).

The drug should be discontinued before testing the concentration of catecholamines, normetanephrine, vanillinmindalic acid, and anti-nuclear antibody titers in the blood and urine. In smokers, the effectiveness of beta-blockers is lower.

Influence on the ability to drive vehicles and perform other activities that require concentration of attention and speed of psychomotor reactions. During treatment with Biol®, care should be taken when driving vehicles and performing other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Film-coated tablets

Storage conditions

At a temperature not exceeding 25 °C.

Shelf

life is 4 years.

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Heart Failure, Hypertension, Arrhythmia