Bisoprolol-Astrafarm 10 mg Pills No. 30 *

Bisoprolol (BISOPROLOL) Instructions for use

Composition:

active ingredient : bisoprolol; 1 tablet contains 5 mg or 10 mg bisoprolol fumarate;
auxiliary substances: lactose, monohydrate; sodium croscarmellose; microcrystalline cellulose; magnesium stearate

Dosage form

Tablets.

Basic physical and chemical properties:

Pills of white color, flat-cylindrical shape with beveled edges and risk on one side.

Pharmacotherapeutic group

Selective β-adrenergic blockers. Code АТХ С07А В07.

Pharmacological properties

Pharmacodynamics.

Bisoprolol is a highly selective β1-adrenergic blocker. When applied in therapeutic doses, it does not exhibit internal sympathomimetic activity and clinically expressed membrane-stabilizing properties. It has antianginal and hypotensive effects. Reduces myocardial oxygen demand by reducing heart rate and cardiac output and lowering blood pressure, increasing myocardial oxygen supply by reducing diastolic blood pressure and diastolic elongation. The drug has a very low affinity with the β2 receptors of smooth muscle of the bronchi and vasculature, as well as with the β2-receptors of the endocrine system.

The maximum effect of bisoprolol occurs 3-4 hours after ingestion. The half-life of the blood plasma is 10-12 hours, which provides a 24-hour efficacy after a single dose. The maximum antihypertensive effect is achieved after 2 weeks of administration.

Pharmacokinetics.

Suction After ingestion bisoprolol is well adsorbed from the digestive tract. Bioavailability is about 90% after oral administration and does not depend on food intake. The pharmacokinetics of bisoprolol and plasma concentration are linear in the range of doses ranging from 5 to 20 mg. The maximum concentration in blood plasma is reached in 2-3 hours.

Distribution. The volume of distribution is 3.5 l / kg. Binding to plasma proteins is about 30%.

Metabolism and elimination. Bisoprolol is excreted from the body in two ways: 50% biotransformed into the liver with the formation of inactive metabolites and is excreted by the kidneys, 50% is excreted by the kidneys in the unaltered form. In vitro studies using human liver microsomes have shown that bisoprolol is metabolised with CYP3A4 (~ 95%), and CYP2D6 plays only a minor role. The total clearance of bisoprolol is 15 l / h. The half-life is 10-12 hours.

Clinical characteristics

Indications

• Arterial hypertension;
• ischemic heart disease (angina pectoris);
• chronic heart failure with systolic dysfunction of the left ventricle in combination with ACE inhibitors, diuretics, if necessary - cardiac glycosides.

Contraindications

• Acute heart failure or heart failure in the stage of decompensation requiring inotropic therapy;
• cardiogenic shock;
• atrioventricular blockade of degrees II and III (except for patients with an artificial rhythm driver);
• syndrome of weakness of the sinus node;
• pronounced synodrial blockade;
• symptomatic bradycardia;
• symptomatic arterial hypotension;
• severe form of bronchial asthma or severe chronic obstructive pulmonary disease;
• late stages of disturbance of peripheral circulation or Raynaud's disease;
• untreated pheochromocytoma;
• metabolic acidosis;
• hypersensitivity to bisoprolol or to other components of the drug.

Interaction with other drugs and other types of interactions

Combinations that are not recommended for use

Treatment of chronic heart failure.

Class I antiarrhythmics (eg, quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone) can potentiate the effect of atrioventricular conductivity and increase the negative inotropic effect.

All indications

Calcium antagonists (verapamil groups, to a lesser extent, diltiazem) adversely affect the contractile function of the myocardium and atrioventricular conductivity. Intravenous administration of verapamil in patients taking β-blockers may result in pronounced arterial hypotension and atrioventricular blockade.

Hypotensive drugs with a central mechanism of action (clonidine, methyldopa, moxonidine, rilmenidine) may impair cardiac failure due to a decrease in central sympathetic tone (decreased heart rate and cardiac output, vasodilation).Abrupt withdrawal of the drug, especially if it is preceded by the abolition of β-blockers, may increase the risk of rectal hypertension.

Combinations that should be used with caution

Treatment for arterial hypertension or coronary heart disease (angina pectoris).

Class A antiarrhythmics (eg quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone): it is possible to potentiate the effect with regard to atrioventricular conductivity and to increase the negative inotropic effect.

All indications.

Calcium antagonists of the dihydropyridine type (e.g. nifedipine, felodipine, amlodipine) may increase the risk of arterial hypotension. The possibility of an increase in the negative influence on the inotropic function of the myocardium in patients with heart failure is not excluded.

Antiarrhythmic drugs of Class III (eg amiodarone): potentiation of the effect on atrioventricular conduction is possible.

Locally acting β-blockers (for example, which are contained in eye drops for the treatment of glaucoma) can increase the systemic effects of bisoprolol.

Parasympathomimetics can increase the time of atrioventricular conduction and increase the risk of bradycardia.

Insulin and oral hypoglycemic agents enhance hypoglycemic effects. The blockade of β-adrenergic receptors may mask the symptoms of hypoglycaemia.

Means for anesthesia increase the risk of depression of the function of the myocardium and the occurrence of arterial hypotension (see section "Peculiarities of application").

Cardiac glycosides: reduce heart rate, increase atrioventricular conduction time.

Nonsteroidal anti-inflammatory drugs: possibly the attenuation of the hypotensive effect of bisoprolol.

β-sympathomimetics (for example, orpripenalin, isoprenaline, dobutamine): administration in combination with bisoprolol may decrease the therapeutic effect of both agents. To treat allergic reactions, you may need higher doses of adrenaline.

Sympathomimetics that activate α- and β-adrenergic receptors (e.g., adrenaline, norepinephrine): the vasodilating effect mediated via α-adrenergic receptors is possible, leading to an increase in arterial pressure and an increase in intermittent luminosity. Such interaction is most likely with the use of nonselective β-blockers.

When used jointly with antihypertensive drugs and drugs that exert a hypotensive effect (eg, tricyclic antidepressants, barbiturates, phenothiazine), an increased risk of arterial hypotension may occur.

Possible combinations

Meflokhin: may increase the risk of developing bradycardia.

MAO inhibitors (with the exception of MAO inhibitors of type B) increase the hypotensive effect of β-blockers, but there is a risk of hypertensive crisis.

Application features

The treatment of stable chronic heart failure using bisoprolol should begin with the titration phase.

Patients with coronary heart disease should not be stopped suddenly without urgent need, as this may result in a transient deterioration of the condition. Initiation and discontinuation of bisoprolol treatment requires regular monitoring.

To date, there is not enough therapeutic experience in the treatment of heart failure in patients with the following diseases and pathological conditions: type I diabetes mellitus (insulin dependent), severe renal or hepatic impairment, restrictive cardiomyopathy, congenital heart defects, hemodynamically significant acquired valve heart defects, myocardial infarction within the last 3 months.

The drug should be used with caution in patients with the following conditions:

• bronchospasm (with bronchial asthma, obstructive diseases of the respiratory tract);
• diabetes mellitus with significant fluctuations in blood glucose levels, with symptoms of hypoglycemia (tachycardia, palpitations, increased sweating) may be concealed;
• strict diet;
• carrying out desensitizing therapy. Like other β-blockers, bisoprolol can increase sensitivity to allergens and increase the severity of anaphylactic reactions. In such cases adrenaline treatment does not always have a positive therapeutic effect;
• atrioventricular block of the I degree;
• angina pectoris;
• obliterating diseases of the peripheral arteries (at the beginning of therapy it is possible to increase the complaints);
• general anesthesia

In patients who are planning a general anesthetic, the use of β-blockers reduces cases of arrhythmia and myocardial ischemia during the introduction into anesthesia, intubation and postoperative period. It is recommended to continue the use of β-blockers during the perioperative period. It is imperative to warn the anesthesiologist about the use of β-adrenoceptor blockers as the physician should take into account the potential interaction with other drugs, which can lead to bradyarrhythmia, reflex tachycardia, and reduced possibilities for the reflex mechanism of blood loss compensation. In the event of bisoprolol cancellation before surgery, the dose should be gradually reduced and stopped taking the medication 48 hours prior to general anesthesia.

Combinations of bisoprolol with calcium antagonists of the verapamil group or diltiazem, with class I antiarrhythmic drugs and centrally acting hypotensive agents are not recommended (see section "Interaction with other drugs and other types of interactions").

Although cardioselective β-blockers (β1) have less effect on the lung function than non-selective β-blockers, they should be avoided, as with all β-blockers, in obstructive airways diseases, if there are no compelling reasons for conducting therapy. If necessary, Bisoprolol-Astrapharm should be used with caution. In patients with obstructive airway disease, bisoprolol treatment should be initiated at the lowest possible dose and patients should be monitored for new symptoms (such as shortness of breath, intolerance to physical activity, cough).

With bronchial asthma or other chronic obstructive pulmonary diseases that can cause symptoms, accompanying therapy with bronchodilators is indicated. In some cases, patients receiving bronchial asthma may require higher doses of β2-sympathomimetics due to increased respiratory tract resistance.

Patients with psoriasis (including history), β-blockers (for example, bisoprolol) are prescribed after careful use / risk ratios.

Patients with pheochromocytoma prescribe Bisoprolol-Astrafarm only after the appointment of α-blockers. Symptoms of thyrotoxicosis may be hidden on the background of the drug. When using the drug, a positive result may be observed during doping control.

Use during pregnancy or breastfeeding

Pregnancy Bisoprolol has pharmacological properties that can cause adverse effects on the course of pregnancy and / or the development of the fetus / newborn. As a rule, β-blockers reduce placental blood flow, which may cause intrauterine growth retardation, intrauterine death, involuntary abortion or premature birth. Side effects of the fetus and the newborn (such as hypoglycemia, bradycardia) may develop. If treatment with β-blockers is necessary, it is desirable that this be a β1-selective adrenergic blocker.

During pregnancy, the drug is only used when the expected benefit to the mother outweighs the potential risk to the fetus. It is necessary to control the utero-placental blood flow and increase the fetus. In the case of adverse effects on the course of pregnancy or the fetus should consider the possibility of alternative treatment.

After birth, the newborn should be under close observation. Symptoms of hypoglycemia and bradycardia can be expected during the first 3 days.

Breast feeding period. There is no data on the excretion of bisoprolol in breast milk, so it is not recommended to use the drug during breastfeeding.

Ability to influence the speed of reaction when driving motor vehicles or other mechanisms

In the course of studies involving patients with ischemic heart disease, the drug did not affect the ability to drive vehicles or other mechanisms. However, in individual cases, the drug may affect the ability to drive vehicles or work with complex mechanisms. Particular attention should be paid at the start of treatment, when changing the dose of the drug or when interacting with alcohol.

Method of administration and dose

Bisoprolol-Astrapharm should be taken without chewing, in the morning, on an empty stomach or during breakfast, with a small amount of liquid.

Arterial hypertension; ischemic heart disease (angina pectoris).

The recommended dose is 5 mg (1 tablet 5 mg) per day. In the case of moderate arterial hypertension (diastolic pressure up to 105 mm Hg), a dose of 2.5 mg is acceptable.

If necessary, the daily dose may be increased to 10 mg (1 tablet per 10 mg) per day. The maximum recommended dose is 20 mg per day.

Adjustment of the dose is done by the doctor individually, depending on the patient's condition.

Bisoprolol-Astrapharmum should be used with caution in patients with arterial hypertension or coronary heart disease accompanied by heart failure.

Chronic heart failure with systolic dysfunction of the left ventricle, in combination with ACE inhibitors, diuretics, and, if necessary, cardiac glycosides.

Standard therapy for chronic heart failure: ACE inhibitors (or angiotensin receptor blockers in the case of ACE inhibitors intolerance), β-adrenergic receptor blockers, diuretics and, if necessary, cardiac glycosides.

Bisoprolol-Astrapharm is prescribed for the treatment of patients with chronic heart failure without signs of exacerbation.

Therapy should be performed by a doctor with experience in the treatment of chronic heart failure.

Treatment of chronic heart failure with bisoprolol begins in accordance with the chart below of the titration and can be adjusted depending on the individual reactions of the body.

1.25 mg * bisoprolol fumarate 1 time per day for 1 week, increasing to
2.5 mg * bisoprolol fumarate 1 time per day for the next 1 week, increasing to
3.75 mg * bisoprolol fumarate 1 time per day for the next 1 week, increasing to
5 mg bisoprolol fumarate 1 time in a knock for the next 4 weeks, raising to
7.5 mg bisoprolol fumarate 1 time per day for the next 4 weeks, increasing to
10 mg bisoprolol fumarate once daily, as maintenance therapy.
* Apply in appropriate dosage. At the beginning of therapy for chronic heart failure, it is recommended that bisoprolol be administered in tablets of 2.5 mg.

The maximum recommended dose of bisoprolol fumarate is 10 mg once a day.

At the beginning of treatment for chronic chronic failure, regular monitoring is required. During the titration phase, monitoring is required for indicators of vital activity (blood pressure, heart rate) and symptoms of progression of heart failure. Symptoms may develop from the first day after starting treatment.

Modification of treatment.

If during the titration phase or after it there is a deterioration in heart failure, arterial hypotension or bradycardia develops, dose adjustment is recommended, which may require a temporary decrease in the dose of bisoprolol or possibly a cessation of treatment. After stabilizing the patient's condition, treatment continues.

The course of treatment with Bisoprolol-Astrapharm is prolonged.

You should not stop treatment suddenly and change the recommended dose without consulting your doctor, as this can lead to a deterioration in the patient's condition. If necessary, treatment with the drug should be completed slowly, gradually reducing the dose (for example, by reducing the dose twice every week).

Patients with hepatic and renal insufficiency.

Arterial hypertension; ischemic heart disease. For patients with impaired hepatic or renal function, mild to moderate doses are usually not necessary. For patsyentov with severe renal insufficiency formoy (ride height creatinine <20 ml / min) and patsyentov with severe hepatic insufficiency formoy dose not dolzhna prevыshat sutochnuyu dose of 10 mg bisoprolol. Ymeyutsya ohranychennыe about A Application Data bisoprolol patients, nahodyaschymsya on dyalyze.

Hronycheskaya serdechnaya nedostatochnostNet data about A pharmacokinetics of bisoprolol patsyentov hronycheskoy with cardiac insufficiency function simultaneously with abuse liver and / or kidneys, the dose uvelychyvat Therefore neobhodimo with caution.

Patsyentы pozhyloho age not trebuyut dozы correction.

Where are you

Clinical Data about A of the effectiveness and safety of treatment for bisoprolol Application absent children, sleduet Therefore no drug Apply this category patients.

Overdose

Most chastыmy signs peredozyrovky javljajutsja bisoprolol bradycardia, hypotension, Acute serdechnaya failure, bronchospasm and hypoglycemia. There shyrokaya variability yndyvydualnoy chuvstvytelnosty for odnokratnoy Peak dose of bisoprolol, patsyentы with cardiac insufficiency mogut bыt more than chuvstvytelnы for the drug.

In cases peredozyrovky neobhodimo nemedlenno obratytsya for the doctor.

In dependence from degree peredozyrovky prekraschayut Treatment and drug provodjat podderzhyvayuschuyu and symptomatic therapy. There ohranychennыe Data on volume of heavy bisoprolol something poddaetsya dyalyzu.

If bradycardia: Introduction of intravenous atropine. If the reaction is absent, with caution or vvodyat yzoprenalyn Another drug with polozhytelnыm hronotropnыm effect. In cases ysklyuchytelnыh vvodyat Artificial vodytel rhythm.

If hypotension arteryalnoy: Application vasoconstrictive drugs, intravenous glucagon Introduction.

In atryoventrykulyarnoy block II and III degree: Introduction yzoprenalyna infusion; Need at - kardyostymulyatsyya.

When exacerbations hronycheskoy cardiac failure: Introduction of intravenous diuretic funds and vazodylatatorov.

When bronchospasm, bronholytycheskye Preparations (for example yzoprenalyn), β2-adrenomymetyky and / or aminophylline.

When hypoglycemia: Introduction of intravenous glucose.

Adverse reactions

Co storony cardiovascular system: bradycardia (in patsyentov with hronycheskoy cardiac insufficiency), signs uhudshenyya cardiac failure (in patsyentov with hronycheskoy cardiac insufficiency), violation atryoventrykulyarnoy conduction, bradycardia (in patsyentov with arteryalnoy hypertension or yshemycheskoy illness of the heart), signs uhudshenyya cardiac failure (in patsyentov arteryalnoy with hypertension or heart illness yshemycheskoy) oschuschenye Kholod or onemenyya in the extremities, hypotension (especially in at patsyentov with cardiac insufficiency).

Co storony nervous system: dizziness, Headache pain (kasaetsya Only patsyentov arteryalnoy with hypertension or heart illness yshemycheskoy. These symptoms voznykayut Usually early in therapy, low vыrazhenы and disappear within 1-2 weeks techenye First), syncope.

Co storony bodies of view: Reduction slezovыdelenyya (It should uchytыvat at noshenyy contact-lens), conjunctivitis.

Co storony organs of hearing, hearing uhudshenye.

Co storony dыhatelnoy system: bronchospasm in asthma patsyentov with bronhyalnoy in anamneze and with chronic obstructive disease dыhatelnыh tracks, allerhycheskyy rynyt.

Co storony pyschevarytelnoho tract: nausea, vomiting, diarrhea, constipation.

Co storony kozhy and fabrics soedynytelnыh: hypersensitivity reactions, itching vkljuchaja, pokrasnenye, vыsыpanyya; alopetsyya. In Treatment β-blockers uhudshenye Can be observed in psoriasis patients STATUS video psoriatic sыpy.

Co storony osteo-mыshechnoy system: mыshechnaya weakness, cramps.

Co storony liver: hepatitis.

Co storony Reproductive system: violation potentsyy.

Psyhycheskye disorders: depression, sleep violation, nochnыe koshmarы, galljucinacii.

Laboratory indicators: Increase urovnja triglycerides in the blood Increase pechenochnыh activity of enzymes in the blood plasma (AST, ALT).

Sharing disorders: weakness (in patsyentov hronycheskoy with cardiac insufficiency), Fatigue (kasaetsya Only patsyentov arteryalnoy with hypertension or heart illness yshemycheskoy. These symptoms voznykayut Usually early in therapy, low vыrazhenы and disappear within 1-2 weeks techenye First), weakness (in patsyentov arteryalnoy with hypertension or heart illness yshemycheskoy).

In cases of occurrence or phenomena pobochnыh nezhelatelnыh reactions neobhodimo nemedlenno proynformyrovat doctor.

Shelf life

3 years.

Storage conditions

Store in original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Packaging

10 tablets in a blister; 2 or 3 blister in a box.

Vacation category

By recipe