Bisoprolol-Teva

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Bisoprolol-Teva: 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: Bisoprolol-Teva

ATX code: C07AB07

Active ingredient: bisoprolol (Bisoprolol)

Manufacturer: TEVA Pharmaceutical Plant Private, Ltd. Co. (TEVA Pharmaceutical Works Private, Ltd. Co.) (Hungary)

Description and photo update: 2019-11-07

Prices in pharmacies: from 88 rubles.

Buy

Bisoprolol-Teva is a drug of hypotensive, antianginal and antiarrhythmic action.

Release form and composition

The drug is produced in the form of film-coated tablets: biconvex, round, almost white or white, engraved on one side with "BISOPROLOL 5" or "BISOPROLOL 10", depending on the dosage of tablets (10 pcs. In an aluminum blister foil and PVC / PVDC film, in a cardboard box 3 or 5 blisters and instructions for the use of Bisoprolol-Teva).

1 tablet contains:

active substance: bisoprolol fumarate - 5 or 10 mg;
additional components: magnesium stearate, mannitol, croscarmellose sodium, microcrystalline cellulose;
film shell: hypromellose, macrogol 6000, titanium dioxide; it is possible to use the finished casing OPADRY 03F280038 white.

Pharmacological properties

Pharmacodynamics

Bisoprolol belongs to selective β ₁ -adrenergic blockers that do not exhibit membrane stabilizing properties and do not possess their own sympathomimetic activity.

The mechanism of action of the drug in arterial hypertension, as well as for drugs from the group of β ₁ -adrenoceptor blockers, is unclear. At the same time, it was found that bisoprolol contributes to a weakening of renin activity in blood plasma, a decrease in the oxygen demand of the heart muscle, and a decrease in the heart rate (HR). Demonstrates hypotensive, antiarrhythmic and antianginal properties. The active substance, blocking in small doses β ₁ -adrenergic receptors of the heart, reduces the production of cyclic adenosine triphosphate (ATP) stimulated by catecholamines from adenosine triphosphate (cAMP), helps to weaken the intracellular current of calcium ions, and reduces atrioventricular (AV) excitability and conductivity.

When used in doses exceeding therapeutic ones, bisoprolol exhibits β ₂ -adrenoceptor blocking effect. During the first 24 hours after taking Bisoprolol-Tev, the total peripheral vascular resistance increases (due to a reciprocal increase in the activity of α-adrenergic receptors and the exclusion of stimulation of β ₂ -adrenergic receptors), after 1-3 days it returns to its original value, and decreases with prolonged use.

The antihypertensive effect is due to a decrease in the minute blood volume and sympathetic stimulation of peripheral vessels, as well as a weakening of the activity of the sympathoadrenal system (SAS) (which is especially important for people with initial hypersecretion of renin), influencing the central nervous system (CNS) and restoration of sensitivity as a result of a decrease in arterial pressure (BP). Against the background of arterial hypertension, the effect of the drug after administration develops after 2–5 days, and a stable effect is recorded after 1–2 months.

The antianginal activity of bisoprolol is associated with a decrease in myocardial oxygen demand (due to a weakening of the contractile and other functions of the heart muscle), lengthening of the diastole period, and normalization of myocardial perfusion. The increase in the end diastolic pressure in the left ventricle provided by the drug and an increase in the stretching of the fibers of the ventricular muscles can increase the need for oxygen, especially in patients with chronic heart failure (CHF).

When used in moderate therapeutic doses, as opposed to non-selective β-blockers, Bisoprolol-Teva exhibits a less potent effect on β ₂ -adrenoceptor- containing organs and tissues, such as skeletal muscle, pancreas, smooth muscles of the bronchi, uterus and peripheral arteries, and on the metabolism of carbohydrates. Bisoprolol does not lead to a delay of sodium ions in the body, the severity of its atherogenic effect does not differ from that of propranolol.

Pharmacokinetics

The active substance is almost completely absorbed in the gastrointestinal tract (GIT), regardless of food intake. The effect of the first passage through the liver is observed to an insignificant extent, which provides a high bioavailability of the drug - 90%.

The metabolic transformation of bisoprolol is carried out by oxidation without further conjugation. All metabolites of the basic substance are strongly polarized and excreted by the kidneys. The main metabolites detected in blood plasma and urine do not demonstrate pharmacological activity. According to the data obtained in experiments with human liver microsomes in vitro, bisoprolol is biotransformed mainly with the participation of the CYP3A4 isoenzyme (approximately 95%), and to a small extent - with the CYP2D6 isoenzyme.

It binds to plasma proteins by approximately 30%, the total clearance is on average 15 l / h, the volume of distribution is 3.5 l / kg. The maximum concentration (C _max) of bisoprolol in the blood plasma is observed 2-3 hours after administration. Through the blood-brain barrier (BBB) and the placenta, Bisoprolol-Teva weakly penetrates. The half-life (T _1/2) from plasma is 10-12 hours, which allows the drug to show its effect within 24 hours after using 1 daily dose.

Up to 50% of the dose taken is metabolized in the liver, resulting in the formation of inactive metabolites. Bisoprolol is excreted from the body in two ways: approximately 98% of the drug is eliminated by the kidneys, of which 50% is in unchanged form; less than 2% - with bile through the intestines.

In patients with CHF, when compared with healthy volunteers, the plasma level of bisoprolol is higher, and T _1/2 is longer.

The pharmacokinetics of the drug is linear and not affected by age.

Indications for use

ischemic heart disease (CHD): attacks of stable angina pectoris (prevention);
arterial hypertension (treatment).

Contraindications

Absolute:

AV block II – III degree, without a pacemaker;
acute heart failure; CHF in the stage of decompensation, which requires the appointment of inotropic therapy;
sinoatrial blockade;
collapse; cardiogenic shock;
cardiomegaly (without existing signs of heart failure);
severe arterial hypotension (systolic blood pressure below 100 mm Hg);
bradycardia (recorded before starting treatment, heart rate less than 60 beats / min);
sick sinus syndrome;
Raynaud's syndrome;
severe disorders of peripheral circulation;
metabolic acidosis;
a history of chronic obstructive pulmonary disease (COPD) and severe bronchial asthma;
pheochromocytoma (without the combined use of α-blockers);
age up to 18 years;
concomitant therapy with floktaphenin and sultopride;
the simultaneous use of monoamine oxidase inhibitors (MAOIs), except for MAOI type B;
hypersensitivity to the constituents of the drug and other β-blockers.

Relative (use Bisoprolol-Teva tablets with caution):

AV block I degree;
Prinzmetal's angina;
diabetes;
desensitizing therapy;
a history of indications of bronchospasm;
the development of allergic reactions in history;
depression (including history);
thyrotoxicosis;
psoriasis;
severe functional disorders of the liver and / or kidneys [creatinine clearance (CC) below 20 ml / min];
elderly age.

Bisoprolol-Teva, instructions for use: method and dosage

Bisoprolol-Teva tablets are taken orally 1 time per day in the morning, before, during or after breakfast.

The tablets should be swallowed whole, without chewing or grinding into powder, with a small amount of liquid. The attending physician sets the regimen and dose of the agent individually, taking into account the patient's condition and heart rate.

In the treatment of ischemic heart disease and arterial hypertension, the recommended daily dose of Bisoprolol-Teva is 5 mg, if necessary, an increase in the dose to 10 mg is allowed.

In the treatment of angina pectoris and arterial hypertension, the maximum dose should not exceed 20 mg, taken 1 time per day.

Side effects

respiratory system: infrequently - bronchospasm (in the presence of bronchial asthma or obstructive respiratory diseases); rarely - nasal congestion, allergic rhinitis;
nervous system: often - sleep disturbances, headache, increased fatigue, dizziness, asthenia, anxiety, depression; rarely - nightmares, tremors, short-term memory loss or confusion, hallucinations, myasthenia gravis, muscle cramps (as a rule, these effects are mild and usually resolve within 1–2 weeks after starting the course of therapy);
cardiovascular system: very often - a feeling of palpitations, decreased heart rate (bradycardia, mainly in patients with CHF); often - a significant decrease in blood pressure (especially in patients with CHF), a feeling of coldness in the extremities (paresthesia) and aggravation of peripheral circulatory disorders (manifestations of angiospasm); infrequently - chest pain, orthostatic hypotension, arrhythmias, worsening of CHF with the appearance of peripheral edema - swelling of the ankles / feet, shortness of breath; violation of AV conduction, including the development of complete transverse blockade and cardiac arrest;
sensory organs: rarely - a decrease in lacrimation (must be taken into account when using contact lenses), visual impairment, tinnitus, ear pain, hearing impairment; extremely rare - taste disturbances, conjunctivitis, dryness and soreness of the eyes;
digestive system: often - dryness of the oral mucosa, nausea, diarrhea, vomiting, abdominal pain, constipation; rarely - a change in taste, an increase in the activity of liver enzymes (aspartate aminotransferase, alanine aminotransferase), an increase in the level of bilirubin, hepatitis;
genitourinary system: extremely rarely - weakening of libido, violation of potency;
musculoskeletal system: infrequently - back pain, arthralgia;
skin: rarely - skin flushing, increased sweating, psoriasis-like skin reactions, exanthema; extremely rare - alopecia, exacerbation of the course of psoriasis;
allergic reactions: rarely - rash, pruritus, urticaria;
laboratory indicators: rarely - an increase in the content of triglycerides in the blood; in some cases - leukopenia, thrombocytopenia, agranulocytosis;
others: withdrawal syndrome - increased blood pressure, increased frequency of angina attacks.

Overdose

Symptoms of an overdose of Bisoprolol-Teva can be: dizziness, difficulty breathing, hypoglycemia, acrocyanosis, bronchospasm, acute heart failure, a significant decrease in blood pressure, arrhythmia, AV block, severe bradycardia, fainting, ventricular extrasystole, convulsions.

In the event of the development of this condition, it is necessary to urgently stop taking the drug, rinse the stomach, take adsorbents, and carry out symptomatic treatment.

When severe bradycardia appears, intravenous (IV) administration of atropine is prescribed. If the positive reaction to the introduction is insufficient, with caution, the use of a drug with a positive chronotropic effect is allowed. In some cases, temporary placement of an artificial pacemaker may be necessary.

If there is a pronounced decrease in blood pressure, IV administration of vasopressors and plasma-substituting solutions is recommended. In hypoglycemia, IV glucagon / dextrose (glucose) may be prescribed.

With AV block, careful observation of the patient's condition and therapy with β-adrenergic agonists, including epinephrine, and, if necessary, the setting of a pacemaker are indicated. In case of exacerbation of CHF, intravenous diuretics, drugs with a positive inotropic effect, as well as vasodilators are administered.

For the treatment of bronchospasm, bronchodilators are prescribed, including β ₂ -adrenomimetics and / or aminophylline.

special instructions

Against the background of therapy with Bisoprolol-Teva, it is necessary to monitor the heart rate and blood pressure, conduct an electrocardiogram (ECG), in the presence of diabetes mellitus, determine the blood glucose level (once every 4–5 months).

In patients with a history of bronchospasm, it is recommended to conduct a study of the function of external respiration before starting the course of therapy.

Patients with pheochromocytoma can be prescribed Bisoprolol-Teva only after an effective blockade of α-adrenergic receptors has been previously achieved, since otherwise the risk of paradoxical arterial hypertension increases.

Drug therapy can mask some signs of thyrotoxicosis, for example, tachycardia. In patients with thyrotoxicosis, abrupt withdrawal of the drug is contraindicated, since in this case, there may be an increase in the symptoms of this disease.

Against the background of diabetes mellitus, Bisoprolol-Teva can also mask tachycardia caused by hypoglycemia. The drug practically does not increase insulin-induced hypoglycemia, and does not interfere with the restoration of blood glucose levels to normal, in contrast to non-selective β-blockers.

With concomitant therapy with clonidine, its reception should be completed only a few days after the termination of the use of Bisoprolol-Teva.

With a burdened allergic history, there may be an increase in the severity of the hypersensitivity reaction and the ineffectiveness of epinephrine administered in usual doses.

If a surgical procedure is planned, Bisoprolol-Teva must be canceled 48 hours before general anesthesia is performed. If the drug was used before surgery, the drug with the least negative inotropic effect should be selected for general anesthesia.

The elimination of reciprocal activation of the vagus nerve can be ensured by intravenous administration of atropine (at a dose of 1-2 mg).

Drugs that deplete the depot of catecholamines (reserpine) can provoke an increase in the effect of β-blockers, as a result of which, when using Bisoprolol-Teva with such drugs, constant medical supervision is necessary to detect a possible sharp decrease in blood pressure or the development of bradycardia.

In the presence of bronchospastic diseases, cardioselective β-blockers can be used with extreme caution only when there is intolerance and / or ineffectiveness of other antihypertensive drugs. In patients with bronchial asthma, when using β-blockers, an increase in airway resistance is possible. If the dose of Bisoprolol-Teva is exceeded, patients in this group are at risk of developing bronchospasm.

If patients have an increasing bradycardia (heart rate below 50 beats / min), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV block, it is necessary to reduce the dose of Bisoprolol-Tev or cancel it.

It is impossible to abruptly interrupt drug therapy because of the risk of severe arrhythmias and myocardial infarction. It is recommended to withdraw the drug gradually, reducing the dose for 14 days or more - decreasing by 25% in 3-4 days.

Smokers have a lower effectiveness of β-blockers.

Before carrying out studies of the content in blood and urine of normetanephrine, vanillin mandelic acid, catecholamines, antinuclear antibody titers, the drug should be discontinued.

Influence on the ability to drive vehicles and complex mechanisms

Bisoprolol-Teva should be used with caution in patients driving vehicles or working with complex mechanisms, especially at the beginning of the course of therapy, after adjusting the dose, as well as with the combined use of ethanol-containing drinks.

Application during pregnancy and lactation

Despite the fact that bisoprolol does not show direct mutagenic, cytotoxic and teratogenic effects, it can lead to pharmacological effects that can have a negative effect on the course of pregnancy and / or on the development of the fetus and the health of the newborn. As a rule, β-blockers reduce placental perfusion, which causes growth retardation or intrauterine fetal death, as well as miscarriages or premature birth. The fetus / newborn may have hypoglycemia, bradycardia, intrauterine growth retardation.

Bisoprolol-Teva should not be used during pregnancy, it is possible to take it only when the benefits to the mother significantly outweigh the threat of developing adverse reactions in the fetus and / or child. If drug treatment is necessary for a pregnant woman, it is required to control blood flow in the placenta and uterus, as well as the growth and development of the fetus. If harmful effects on pregnancy and / or fetus are found, alternative treatments should be considered. After childbirth, the newborn is subject to careful examination. As a rule, symptoms of hypoglycemia and bradycardia can be observed during the first three days of life.

Since there are no data on the excretion of bisoprolol in breast milk, taking the drug during breastfeeding is not recommended. If it is necessary to prescribe Bisoprolol-Teva during lactation, it is required to transfer the child to artificial feeding.

Pediatric use

For patients under 18 years of age, drug therapy is contraindicated, since its effectiveness and safety in children and adolescents have not been established.

With impaired renal function

In the presence of renal failure (with CC below 20 ml / min), the daily dose of Bisoprolol-Teva should not exceed 10 mg. Increasing the dose in patients from this risk group should be done with extreme caution.

For violations of liver function

In the presence of severe violations of hepatic function, Bisoprolol-Teva should be taken in a daily dose not exceeding 10 mg. Increasing the dose in patients with hepatic insufficiency should be done with great caution.

Use in the elderly

Individual selection of doses of Bisoprolol-Teva is not required for elderly patients, however, therapy with the drug in patients from this age group should be carried out with caution, monitoring renal function once every 4-5 months.

Drug interactions

β-blockers for local use (including eye drops for the treatment of glaucoma): it is possible to increase the systemic effects of bisoprolol, such as a decrease in heart rate, a decrease in blood pressure;
lidocaine, quinidine, phenytoin, disopyramide, propafenone, flecainide and other class I antiarrhythmics: AV conduction and myocardial contractility are weakened;
class III antiarrhythmics, including amiodarone: impairment of AV conduction is aggravated;
dobutamine, isoprenaline and other β-adrenergic agonists: when any of these drugs are combined with bisoprolol, a mutual decrease in the effect is possible;
parasympathomimetics: impairment of AV conduction increases and the risk of bradycardia is aggravated;
adrenergic agonists that affect β- and α-adrenergic receptors, including norepinephrine and epinephrine: the vasoconstrictor effect of these drugs is potentiated, which occurs with the participation of α-adrenergic receptors, which causes an increase in blood pressure; the likelihood of such interactions increases with the use of non-selective β-blockers;
iodine-containing radiopaque diagnostic preparations for intravenous administration: the threat of anaphylactic reactions is aggravated;
allergens used for immunotherapy or allergen extracts used for skin tests: increases the risk of severe systemic allergic reactions or anaphylaxis;
lidocaine and xanthines (except theophylline): the clearance of these drugs may decrease as a result of a likely increase in their plasma concentration in the blood, mainly with an initially increased clearance of theophylline in smokers;
mefloquine: the risk of bradycardia increases;
phenytoin (intravenous injection), means for inhalation anesthesia (hydrocarbon derivatives): the likelihood of lowering blood pressure and the severity of cardiodepressive effects increases;
reserpine and guanfacine, methyldopa, slow calcium channel blockers (diltiazem, verapamil), cardiac glycosides, amiodarone and other antiarrhythmic agents: the threat of the development / aggravation of bradycardia, AV blockade, heart failure and cardiac arrest increases;
clonidine, hydralazine, nifedipine, sympatholytics, diuretics and other antihypertensive drugs: a significant decrease in blood pressure is possible;
coumarins: the anticoagulant effect of these drugs is prolonged;
glucocorticosteroids and estrogens, non-steroidal anti-inflammatory drugs (NSAIDs): the hypotensive effect is weakened due to the retention of sodium ions and (for NSAIDs) blockade of renal prostaglandin production;
non-depolarizing muscle relaxants: the effect of these funds is lengthened;
antipsychotics (neuroleptics), tetracyclic and tricyclic antidepressants, sedatives and hypnotics, ethanol: there is an increase in central nervous system depression;
MAOIs: the hypotensive effect is significantly enhanced; this combination is contraindicated, the interval between taking Bisoprolol-Teva and MAO inhibitors should be at least 14 days;
sulfasalazine: the plasma concentration of bisoprolol in the blood increases;
ergotamine: the risk of peripheral circulatory disorders is aggravated;
non-hydrogenated ergot alkaloids: increased risk of peripheral circulatory disorders;
rifampicin: shortens the T _{1/2 of} bisoprolol.

Analogs

Analogs of Bisoprolol-Teva are Concor, Bisoprolol, Niperten, Bisogamma, Aritel, Bisomor, Coronal, Bisoprolol Velpharm, Bidop Cor, etc.

Terms and conditions of storage

Store at a temperature not exceeding 25 ° C, out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Bisoprolol-Teva

According to many reviews of Bisoprolol-Teva, left on medical sites, it is an affordable, inexpensive and effective drug that normalizes blood pressure, lowers heart rate, eliminates arrhythmia, improves blood circulation, and prevents the development of attacks of stable angina pectoris. All patients recommend taking the remedy only after consulting the attending physician, in an individually selected optimal dose. It is often noted that in order to achieve a positive result from therapy, careful titration of the dose of bisoprolol is required.

At the same time, other patients who took Bisoprolol-Teva claim that it is effective, but not safe. A long-term consequence of a decrease in pressure can be a deterioration in cardiac activity. In elderly people, in isolated cases, relatives noted an excessive decrease in blood pressure and the appearance of senile dementia, which were associated with drug therapy.

Price for Bisoprolol-Teva in pharmacies

The price for Bisoprolol-Teva 5 mg is 110-130 rubles, 10 mg - 170-190 rubles. per pack of 30 film-coated tablets.

Bisoprolol-Teva: prices in online pharmacies

Drug name

Price

Pharmacy

Bisoprolol-Teva 5 mg film-coated tablets 30 pcs.

RUB 88

Buy

Bisoprolol-Teva 10 mg film-coated tablets 30 pcs.

91 rbl.

Buy

Bisoprolol-Teva 10 mg film-coated tablets 50 pcs.

RUB 128

Buy

Bisoprolol-Teva tablets p.o. 5mg 30 pcs.

129 RUB

Buy

Bisoprolol-Teva 5 mg film-coated tablets 50 pcs.

143 r

Buy

Bisoprolol-Teva tablets p.o. 10mg 30 pcs.

159 r

Buy

Bisoprolol-Teva tablets p.o. 10mg 50 pcs.

RUB 291

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!