bisoprolol | Bisogamma tablets are covered.pl.ob. 10 mg 30 pcs.

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SKU
BID463143
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Release form

Film-coated tablets.
Release form

Film-coated tablets.

Packing

30 pcs. 10 mg each.

Pharmacological action

Selective beta1-blocker without internal sympathomimetic activity, does not have a membrane-stabilizing effect. Reduces blood plasma renin activity, reduces myocardial oxygen demand, reduces heart rate (at rest and during exercise).

It has hypotensive, antiarrhythmic and antianginal effects. Blocking in low doses the 1-adrenergic receptors of the heart, it reduces the formation of cAMP stimulated by catecholamines from ATP, reduces the intracellular current of calcium ions, and has a negative chrono-, dromo-, batmo- and inotropic effect.

With an increase in the dose above the therapeutic, it has a beta2-blocking effect.

At the beginning of the use of the drug, in the first 24 hours, OPSS increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of stimulation of 2-adrenergic receptors) and after 1-3 days it returns to the original, 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 renin-angiotensin system (of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure and effects on the central nervous system.

With arterial hypertension, the effect occurs after 2-5 days, a stable effect - after 1-2 months.

The antianginal effect is due to a decrease in myocardial oxygen demand as a result of decreased heart rate and reduced contractility, lengthening of diastole, and improved myocardial perfusion. By increasing the final diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, it can increase the need for oxygen, especially in patients with chronic heart failure.

Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and a slowdown in AV conduction (mainly in antegrade and, to a lesser extent, in retrograde directions through the AV node) and along additional paths.

When used in medium therapeutic doses, unlike non-selective beta-blockers, Bisogamma® has a less pronounced effect on organs, containing 2-adrenergic receptors (pancreas, skeletal muscle, smooth muscles of the peripheral arteries, bronchi and uterus) and carbohydrate metabolism, does not cause a delay of sodium ions in the body according to the severity of the atherogenic effect does not differ from propranolol.

Contraindications

Shock (including cardiogenic).

Collapse.

Pulmonary edema.

Acute heart failure.

Chronic heart failure in the decompensation stage.

AV block II and III degree.

Sinoatrial blockade.

SSSU.

Severe bradycardia.

Angina pectoris.

Cardiomegaly (without signs of heart failure).

Arterial hypotension (systolic pressure <100 mmHg, especially with myocardial infarction).

Severe forms of bronchial asthma and other obstructive airways diseases.

Late stages of peripheral circulation disturbance, Raynaud's disease.

Pheochromocytoma (without the simultaneous use of alpha-blockers).

metabolic acidosis.

Depression.

Concurrent administration of MAO inhibitors (except for type B MAO inhibitors).

Children and adolescents under 18 years of age.

Hypersensitivity to the drug and other beta-blockers.

Precautions: the drug should be prescribed to patients with liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes mellitus, grade I AV blockade, psoriasis with a history of depression, allergic reactions to elderly patients.

Use during pregnancy and lactation

Prescribing during pregnancy and lactation is possible only if the intended benefits to the mother outweigh the potential risk to the fetus or infant.

Special instructions

Monitoring patients taking BisogammaВ® includes measuring heart rate and blood pressure (daily at the beginning of treatment, then 1 time in 3-4 months), an ECG, determination of blood glucose level with concomitant 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 on the need for medical consultation with a heart rate of less than 50 beats / min.

Before starting treatment, it is recommended to study the function of external respiration in patients with a history of bronchopulmonary burden.

In approximately 20% of patients with angina pectoris, beta-blockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats / min) and an increased final diastolic volume of the left ventricle, which disrupts subendocardial blood flow.

When using the drug in patients with pheochromocytoma, there is a risk of developing paradoxical hypertension (if an effective -adrenoreceptor blockade has not been previously achieved).

With thyrotoxicosis, bisoprolol may mask certain clinical symptoms of thyrotoxicosis (eg, tachycardia).

Abrupt withdrawal of the drug BisogammaВ® in patients with thyrotoxicosis is contraindicated, since it can aggravate the symptoms.

In diabetes, BisogammaВ® 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.

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

If it is necessary to carry out planned surgical treatment, BisogammaВ® 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 vagus nerve activation can be eliminated iv by administration of atropine (1-2 mg).

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

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

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

It is recommended that therapy be discontinued if depression develops.

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

When used in combination with clonidine, its administration can be stopped only a few days after the withdrawal of bisoprolol.

In smokers, beta-blockers are less effective.

Patients using contact lenses should take into account that tear fluid production may decrease with Bisogamma treatment.

The drug should be discontinued before examining the blood and urine levels of catecholamines, normetanephrine and vanillinindic acid, and antinuclear antibody titers.

Influence on the ability to drive vehicles and control mechanisms

During the treatment period, patients should be careful when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Composition

1 tablet contains:

Active ingredient:

bisoprolol hemifumarate - 10 mg.

Excipients:

crospovidone,

pregelatinized starch,

microcrystalline cellulose,

silicon dioxide colloidal,

magnesium stearate,

macrogol 6000,

polysorbate

titanium dioxide (E171),

calcium carbonate (E170),

talc,

dye iron (III) oxide yellow (E172),

hypromellose (HPMC 5),

hypromellose (HPMC 50).

Dosage and administration of

The drug is administered orally at a dose of 5 mg 1 time / day, in the morning, on an empty stomach. If necessary, increase the dose to 10 mg 1 time / day. The maximum dose is 20 mg / day.

For elderly patients: dose adjustment not required.

In patients with impaired renal function with CC <20 ml / min or with severe impaired liver function: the maximum daily dose is 10 mg.

Tablets are taken without chewing.

Side effects of

From the central nervous system and peripheral nervous system: fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion, or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesia in the extremities (in patients with intermittent claudication and Raynaud's syndrome), tremors, convulsions.

From the sensory organs: impaired vision, decreased secretion of lacrimal fluid, dry and sore eyes, conjunctivitis.

From the cardiovascular system: sinus bradycardia, palpitations, impaired myocardial conduction, AV block (up to the development of complete transverse blockade and cardiac arrest), weakening of myocardial contractility, development (worsening) of chronic heart failure (swelling of the ankles, feet shortness of breath) , decreased blood pressure, orthostatic hypotension, the manifestation of angiospasm (increased impairment of peripheral circulation, cooling of the lower extremities, Raynaud's syndrome), chest pain.

From the digestive system: dry oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, impaired liver function (dark urine, yellowness of the sclera or skin, cholestasis), a change in the activity of liver enzymes (increased ALT, ACT) and bilirubin levels, taste changes.

From the respiratory system: nasal congestion, difficulty breathing when prescribed in high doses (loss of selectivity) and / or in predisposed patients - laryngo- and bronchospasm.

From the endocrine system: hyperglycemia (in patients with non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid state.

From the hemopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.

From the musculoskeletal system: back pain, arthralgia, cramps in the calf muscles.

From the reproductive system: weakening libido, decreased potency. Allergic reactions: skin itch, rash, urticaria.

Dermatological reactions: increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms, alopecia.

Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

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

Drug Interactions

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 drugs for iv administration increase the risk of anaphylactic reactions in patients receiving bisoprolol.

Phenytoin with iv administration, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive action and the likelihood of a decrease in blood pressure in patients receiving bisoprolol.

Bisoprolol alters the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Bisoprolol reduces the clearance of lidocaine and xanthines (except diphillin) and increases their concentration in plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

The antihypertensive effect of bisoprolol is reduced by NSAIDs (sodium ion retention and prostaglandin synthesis blockade by the kidneys), corticosteroids and estrogens (sodium ion retention).

Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), amiodarone, and other antiarrhythmics when used simultaneously with bisoprolol increase the risk of developing or worsening bradycardia, AV blockade, cardiac arrest and heart failure.

With simultaneous use with nifedipine, a significant decrease in blood pressure is possible.

When used simultaneously with bisoprolol, diuretics, clonidine, sympatholytics, hydralazine, and other antihypertensive drugs can lead to an excessive decrease in blood pressure.

Bisoprolol prolongs the action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotic drugs (antipsychotics), ethanol, sedatives and hypnotics increase the inhibitory effect of bisoprolol on the central nervous system.

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

Non-hydrogenated ergot alkaloids (including ergotamine) with simultaneous use with bisoprolol increase the risk of peripheral circulation disorders.

Sulfasalazine increases the concentration of bisoprolol in blood plasma.

Rifampicin reduces T1 / 2 of bisoprolol.

overdose

Symptoms:

ventricular extrasystole, severe bradycardia, AV blockade, severe BP, chronic heart failure, nail cyanosisth fingers or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment:

gastric lavage and the appointment of adsorbing drugs. Carrying out symptomatic therapy: at the developed AV blockade - in / in introduction of 1-2 mg of atropine, epinephrine or staging of a temporary pacemaker with ventricular extrasystole - lidocaine (class IA drugs are not used). At decrease in blood pressure the patient should be in the position of Trendelenburg if there are no signs of pulmonary edema - in / in plasma replacement solutions, with inefficiency - the introduction of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate pronounced decrease in blood pressure), diuretics, glucagon in convulsions - in / in diazepam with bronchospasm - beta2-adreno-stimulators inhalation.

Storage conditions

Keep out of the reach and sight of children at temperatures not exceeding 25 РC.

Shelf life

3 years.

Active substance

bisoprolol

Terms and conditions otpuska from

pharmacies Prescription

dosage form

tablets

Prescribing

Prescribing

For adults as prescribed by a doctor

S.K. Master K and K S.R.L., Germany

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