Bidop Cor - instructions for use, dose, side effects, contraindications

White, oblong tablets, with a risk on both sides and labeling "BI"to the left of the risks and the figure" 2.5 "to the right of the risks on one side.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B Selective beta-blockers

C.07.A.B.07 Bisoprolol

Pharmacodynamics:

Bisoprolol - selective β₁-adrenoceptor without its own sympathomimetic activity, does not possess membrane-stabilizing action. Bisoprolol has only a slight affinity for β₂-adrenoceptors of smooth muscles of bronchi and vessels, as well as to p2adrenoreceptors involved in the regulation of metabolism. Consequently, bisoprolol in general, does not affect the resistance of the respiratory tract and the metabolic processes involved β₂-adrenoceptors. Selective action of the drug on β₁-adrenoceptors persists beyond the therapeutic range.

In a single application in patients with coronary heart disease (CHD) without signs of chronic heart failure (CHF) bisoprolol reduces the heart rate (heart rate), stroke volume of the heart and, as a result, reduces the ejection fraction and the need for myocardium in oxygen. With prolonged therapy, initially increased total peripheral vascular resistance (OPSS) is reduced.

Pharmacokinetics:

Suction

Bisoprolol is almost completely (more than 90%) absorbed from the gastrointestinal tract. Its bioavailability due to an insignificant metabolism "during primary passage" through the liver (about 10%) is about 90% after ingestion. Eating does not affect bioavailability. Bisoprolol demonstrates linear kinetics, and its concentrations in the blood plasma are proportional to the dose taken in the dose range from 5 to 20 mg. The maximum concentration in the blood plasma is achieved 2-3 hours after ingestion.

Distribution

Bisoprolol is distributed quite widely. The volume of distribution is 3.5 l / kg. The connection with plasma proteins is approximately 30%.

Metabolism

Bisoprolol is metabolized along the oxidative pathway without subsequent conjugation. All metabolites are polar (water-soluble) and excreted by the kidneys.The main metabolites found in blood plasma and urine, do not show pharmacological activity. Data obtained as a result of experiments with microsomes of human liver in vitro, show that bisoprolol is metabolized primarily by isoenzyme CYP3A4 (about 95%), and isoenzyme CYP2D6 plays only a small role.

Excretion

Bisoprolol clearance is determined by the balance between excretion by the kidneys in unchanged form (about 50%) and metabolism in the liver (about 50%) to metabolites, which are also excreted by the kidneys. The total ground clearance is 15 l / h. The half-life is 10-12 hours.

There is no information on the pharmacokinetics of bisoprolol in patients with CHF and simultaneous impairment of liver or kidney function.

Indications:

Chronic heart failure.

Contraindications:

- Hypersensitivity to bisoprolol or to any of the excipients (see section "Composition");

- acute heart failure, chronic heart failure in the stage of decompensation, requiring inotropic therapy;

- cardiogenic shock;

- atrioventricular (AV) of blockade II and III degree in patients without an electrocardiostimulator;

- syndrome of weakness of the sinus node;

- sinoatrial blockade;

- bradycardia (heart rate less than 60 beats / min);

- severe arterial hypotension (systolic blood pressure less than 100 mm Hg);

- severe forms of bronchial asthma or chronic obstructive pulmonary disease (COPD);

- severe peripheral arterial circulation or Raynaud's syndrome;

- pheochromocytoma (without simultaneous application of α-blockers);

- metabolic acidosis;

- age 18 years (clinical application experience in children is absent);

- lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Carefully:

Conducting desensitizing therapy, Prinzmetal angina, hyperthyroidism, diabetes type I and diabetes with considerable fluctuations in blood glucose concentration, AV blockade I extent severe renal failure (creatinine clearance (CC) of less than 20 ml / min) expressed by human liver, psoriasis, restrictive cardiomyopathy, congenital heart defects, or defect of a heart valve with severe hemodynamic disorders, chronic heart failure myocardial infarction within the past 3 months, a strict diet.

Pregnancy and lactation:

Pregnancy

The use of Bidop®Kor during pregnancy is possible only if the intended benefit of therapy for the mother exceeds the potential risk of side effects in the fetus and / or the child.

As a rule, β-adrenoblockers reduce blood flow in the placenta and can affect fetal development. Blood flow in the placenta and uterus should be monitored, and the growth and development of the unborn child should be monitored, and alternative therapeutic measures taken if pregnancy and / or fetus are undesirable.

You should carefully examine the newborn after delivery. In the first three days of life, bradycardia and hypoglycemia may occur.

Breastfeeding period

There is no data on whether the bisoprolol in breast milk. Therefore, taking Bidop®Cor is not recommended for women during lactation. If it is necessary to use the drug, breastfeeding should be discontinued.

Dosing and Administration:

Bidop®Kor should be taken orally once a day with a small amount of liquid in the morning before breakfast, during or after it. Tablets should not be chewed or ground into a powder.

The standard treatment regimen for CHF includes the use of angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists (in the case of intolerance to ACE inhibitors), β-blockers, diuretics and, optionally, cardiac glycosides. The initiation of treatment with CHD with Bidop®Cor requires mandatory special phase titration and regular medical supervision. A prerequisite for the treatment with Bidop ® Cor is stable CHF without signs of exacerbation.

Treatment of CHF with Bidop®Kor begins with the following titration scheme. Individual adaptation may be required depending on how well the patient tolerates the prescribed dose, i.e., the dose can be increased only if the previous dose is well tolerated.

The recommended initial dose is 1.25 mg (¹/₂ tablets of 2.5 mg) once a day. Depending on the individual tolerability, the dose should be gradually increased to 2.5 mg, 3.75 mg (1¹/₂ 2.5 mg tablets), 5 mg, 7.5 mg (3 tablets of 2.5 mg or 1¹/₂ 5 mg bisoprolol tablets with a risk) and 10 mg (2 tablets of bisoprolol 5 mg or 1 tablet of bisoprolol 10 mg) once a day.To ensure the given dosage regimen, you can use Bidop®Cor. Each subsequent increase in dose should be carried out not less than two weeks later.

If the increase in the dose of the drug is poorly tolerated by the patient, a dose reduction is possible. The maximum recommended dose for CHF is 10 mg of Bidop® Corp. once a day.

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

If the patient does not tolerate the maximum recommended dose of the drug, a gradual dose reduction is possible.

During the titration phase or after it, temporary worsening of the course of CHF, arterial hypotension or bradycardia may occur. In this case, it is recommended first of all to correct the doses of concomitant therapy. It may also be necessary to temporarily reduce the dose of Bidop®Cor or cancel it.

After stabilization of the patient's condition, a repeated titration of the dose should be performed or the treatment should be continued.

Duration of treatment

Treatment with Bidop®Cor is usually a long-term therapy.

Special patient groups

Impaired renal or hepatic function

- If the liver or kidney function is mild or moderate, usually no dose adjustment is required.

- At the expressed infringements of function of kidneys (KK less than 20 ml / mines) and at patients with serious diseases of a liver the maximum daily dose makes 10 mg.

Increasing the dose in such patients should be carried out with extreme caution.

Elderly patients

Correction of the dose is not required.

Children

It is not recommended to prescribe Bidop®Kor for children under 18 years of age, due to the fact that the experience of clinical use of the drug in children is absent.

To date, there is insufficient data on the use of bisoprolol in patients with CHF in combination with type 1 diabetes mellitus, marked kidney and / or liver dysfunction, restrictive cardiomyopathy, congenital heart disease or heart valve disease with severe hemodynamic disorders. Also, sufficient data have not yet been obtained regarding patients with CHF with myocardial infarction during the last 3 months.

Side effects:

The incidence of adverse reactions is determined as follows: very often ≥ 1/10; often ≥1 / 100, <1/10; infrequently ≥ 1/1000, <1/100; rarely ≥ 1/10000, <1/1000; very rarely <1/10000.

Disturbances from the nervous system

Often: dizziness, headache;

Rarely: loss of consciousness.

Disorders of the psyche

Infrequently: depression, insomnia;

Rarely: hallucinations, nightmares.

Disturbances on the part of the organ of sight

Rarely: decreased lacrimation (should be considered when wearing contact lenses);

Very rarely: conjunctivitis.

Hearing disorders and labyrinthine disorders

Rarely: hearing impairment.

Violations from the heart and blood vessels

Very often: a bradycardia;

Often: exacerbation of symptoms of CHF, a feeling of cold or numbness in the limbs, a pronounced decrease in blood pressure;

Infrequently: violation AV conduction, orthostatic hypotension.

Disturbances from the respiratory system, chest and mediastinal organs

Infrequent: bronchospasm in patients with bronchial asthma or airway obstruction in anamnesis;

Rarely: allergic rhinitis.

Disorders from the gastrointestinal tract

Often: nausea, vomiting, diarrhea, constipation;

Rarely: hepatitis.

Disturbances from musculoskeletal and connective tissue

Infrequently: muscle weakness, muscle cramps.

Disturbances from the skin and subcutaneous tissues

Rarely: hypersensitivity reactions, such as pruritus, rash, hyperemia of the skin;

Very rarely: alopecia.

β-blockers can exacerbate the symptoms of psoriasis or cause a psoriasis-like rash.

Violations of the genitals and mammary gland

Rarely: a violation of potency.

General disorders and disorders at the site of administration:

Often: asthenia, increased fatigue.

Impact on the results of laboratory and instrumental studies

Rarely: hypertriglyceridemia, increased activity of "hepatic" transaminases (alanine aminotransferase (ALT), aspartate aminotransferase (ACT)).

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms

The most common symptoms of an overdose are: AV blockade, pronounced bradycardia, marked decrease in blood pressure, bronchospasm, acute heart failure and hypoglycemia. The sensitivity to a single dose of a high dose of bisoprolol varies greatly among individual patients, and probably patients with CHF have high sensitivity.

Treatment

In case of an overdose, first of all, it is necessary to stop taking the drug and begin supporting symptomatic therapy.

With a pronounced bradycardia: intravenous administration of atropine. If the effect is insufficient, with caution you can enter a drug that has a positive chronotropic effect. Sometimes it may be necessary to temporarily set up an artificial pacemaker.

With a pronounced decrease in blood pressure: intravenous injection of plasma-substituting solutions and vasopressor preparations.

When AV blockade: patients should be under constant observation and receive treatment with β-adrenomimetics, such as epinephrine. If necessary - staging an artificial pacemaker.

With exacerbation of CHF flow: intravenous injection of diuretics, drugs with a positive inotropic effect and vasodilators.

When bronhospazme: use of bronchodilators, including β₂adrenomimetics and / or aminophylline.

With hypoglycemia: intravenous dextrose (glucose).

Interaction:

Simultaneous administration of other medications may affect the efficacy and tolerability of bisoprolol.This interaction can also occur in cases where two drugs are taken in a short time. The physician should be informed about taking other medications, even if they are taken without the doctor's prescription (ie, drugs that are dispensed without a prescription).

Unrecommended combinations

Antiarrhythmic drugs of the first class (for example, quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone) with simultaneous application with bisoprolol may reduce AV conduction and contractility of the myocardium.

The blockers of "slow" calcium channels (BCCC) such as verapamil and to a lesser extent diltiazem with simultaneous application with bisoprolol may lead to a decrease in myocardial contractility and disruption AV conductivity. In particular, intravenous administration of verapamil to patients taking beta-blockers can lead to severe arterial hypotension and AV blockade.

Hypotensive agents of central action (such as clonidine, methyldopa, moxonidine, rilmenidine) can lead to a decrease in heart rate and a decrease in cardiac output, as well as to vasodilation due to a decrease in the central sympathetic tone.Abrupt withdrawal, especially before the abolition of β-blockers, may increase the risk of developing "ricochet" arterial hypertension.

Combinations requiring special care

BCCC, dihydropyridine derivatives (for example, nifedipine, felodipine, amlodipine), with simultaneous use with bisoprolol may increase the risk of developing arterial hypotension. In patients with heart failure, the risk of subsequent deterioration of the contractile function of the heart can not be ruled out.

Antiarrhythmic drugs of the III class (for example, amiodarone) can increase the violation AV conductivity.

The action of β-blockers for topical application (eg, eye drops for the treatment of glaucoma) can enhance the systemic effects of bisoprolol (lowering blood pressure, decreasing heart rate).

Parasympatomimetics with simultaneous use with bisoprolol may increase the disruption AV conductivity and increase the risk of developing a bradycardia.

The hypoglycemic effect of insulin or hypoglycemic agents for oral ingestion may be enhanced. Symptoms of hypoglycemia, in particular tachycardia, can be masked or suppressed. Similar interactions are more likely when using non-selective β-blockers.

Means for general anesthesia may increase the risk of cardiodepressive action, leading to hypotension (see section "Special instructions").

Cardiac glycosides with simultaneous application with bisoprolol may lead to an increase in the time of the impulse and, thus, to the development of bradycardia.

Non-steroidal anti-inflammatory drugs (NSAIDs) can reduce the antihypertensive effect of bisoprolol.

The simultaneous use of the Bidop®Cor with β-adrenomimetics (eg, isoprenaline, dobutamine) can lead to a decrease in the effect of both drugs.

The combination of bisoprolol with adrenomimetics that affect β- and α-adrenergic receptors (for example, norepinephrine, epinephrine) can enhance the vasoconstrictor effects of these drugs that occur with the participation of α-adrenoreceptors, leading to an increase in blood pressure. Similar interactions are more likely when using non-selective β-blockers.

Hypotensive drugs, as well as other agents with a possible antihypertensive effect (for example, tricyclic antidepressants, barbiturates, phenothiazines) can enhance the antihypertensive effect of bisoprolol.

Mefloquine with simultaneous application with bisoprolol may increase the risk of developing bradycardia.

Inhibitors of monoamine oxidase (MAO) (with the exception of MAO B inhibitors) can enhance the antihypertensive effect of β-blockers. Simultaneous application can also lead to the development of hypertensive crisis.

Rifampicin: a slight decrease in the half-life of bisoprolol is possible due to rifampicin induction of hepatic isoenzymes of cytochrome P-450. Usually dose adjustment is not required.

Derivatives of ergotamine: possibly aggravation of peripheral blood circulation.

Special instructions:

Do not interrupt treatment drastically and do not change the recommended dose without first consulting a doctor, since this can lead to a temporary worsening of the heart. Treatment should not be interrupted suddenly, especially in patients with ischemic heart disease. If cessation of treatment is necessary, then the dose should be reduced gradually.

At the initial stages of treatment with Bidop ® Cor, patients need constant monitoring.

The drug should be used with caution in the following cases:

- diabetes mellitus with significant fluctuations in blood glucose concentration: symptoms of marked decrease in glucose concentration (hypoglycemia), such as tachycardia, palpitations or excessive sweating, may be masked;

- strict diet;

- conducting desensitizing therapy;

- AV blockade of the 1st degree;

- angina of Prinzmetal;

- violations of peripheral arterial blood flow of mild and moderate degree (at the beginning of therapy there may be an increase in symptoms);

- psoriasis (including in the anamnesis).

Respiratory system: with bronchial asthma or COPD simultaneous application of bronchodilating agents is shown. In patients with bronchial asthma, an increase in airway resistance may be required, which requires a higher dose of β₂- adrenomimetics.

Allergic reactions: β-adrenoblockers, including Bidop ® Cor, can increase sensitivity to allergens and severity of anaphylactic reactions due to weakening of adrenergic compensatory regulation under the action of β-blockers. Epinephrine (epinephrine) therapy does not always produce the expected therapeutic effect.

General anesthesia: when conducting general anesthesia, the risk of blockade of β-adrenergic receptors should be considered. If it is necessary to discontinue therapy with Bidop.RTM before surgery, it should be done gradually and completed 48 hours before the general anesthesia. An anesthesiologist should be warned that you are taking Bidop®Cor.

Pheochromocytoma: in patients with a tumor of the adrenal glands (pheochromocytoma) Bidop ® Cor can be prescribed only against the background of the use of α-adrenoblockers.

Hyperthyroidism: when treated with Bidop®Cor, symptoms of hyperthyroidism (hyperthyroidism) may be masked.

Effect on the ability to drive transp. cf. and fur:Bisoprolol does not affect the ability to drive vehicles according to the results of the study in patients with ischemic heart disease. However, due to individual reactions, the ability to control vehicles and mechanisms can be disrupted. This should be paid special attention at the beginning of treatment, after changing the dose, as well as with the simultaneous use of alcohol.

Form release / dosage:

Tablets, 2.5 mg.

Packaging:

For 14 tablets in a blister of Al / PVC / PVDC.

For 1, 2 or 4 blisters in a cardboard box together with instructions for use.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002689

Date of registration:31.10.2014 / 02.02.2016

Expiration Date:31.10.2019

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER-RUS, CJSC Russia

NICHE GENERICS, Limited Ireland

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp25.01.2017

Illustrated instructions

Instructions

Bidop® Cor (Bidop® Cor)