Bisogamma pills 5mg, 30pcs

Composition

1 tablet contains:

Active ingredient:

bisoprolol hemifumarate – 5 mg.

Auxiliary substances:

crospovidone,

pregelatinized starch,

microcrystalline cellulose,

colloidal silicon dioxide,

magnesium stearate,

macrogol 6000,

polysorbate 20,

titanium dioxide (E 171),

calcium carbonate (E170),

talc,

iron (III) oxide yellow dye (E172),

hypromellose (HPMC 5),

hypromellose (HPMC 50).

Pharmacological action

Selective beta_-1-adrenoblocker without internal sympathomimetic activity, does not have a membrane-stabilizing effect. Reduces the activity of blood plasma renin, reduces the need for myocardial oxygen, reduces heart rate (at rest and during exercise).

It has antihypertensive, antiarrhythmic and antianginal effects. 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, and has a negative chrono -, dromo -, batmo-and inotropic effect.

When the dose is increased above the therapeutic dose, it has a beta_-2-adrenoblocking effect.

At the beginning of the drug use, in the first 24 hours, OPSS increases (as a result of a reciprocal increase in alpha-adrenergic activity and elimination of beta_-2-adrenergic stimulation) and returns to the initial value after 1-3 days, and decreases with prolonged use.

The hypotensive 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 (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 occurs in 2-5 days, stable effect – in 1-2 months.

The antianginal effect is due to a decrease in the myocardial oxygen demand as a result of a decrease in heart rate and contractility, an elongation of the diastole, and an improvement in 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.

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

When used in the medium therapeutic doses, unlike nonselective beta-blockers, Bisogamma® has a less pronounced effect on the organs containing the β₂-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause the delay of sodium ions in the body; according to the severity of atherogenic action is not different from that of propranolol.

Indications

• Arterial hypertension.
• IHD: prevention of angina attacks.

Use during pregnancy and lactation

Prescribing the drug during pregnancy and lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus or infant.

Contraindications

• Shock (including cardiogenic).
• Collapse.
• Pulmonary edema.
• Acute heart failure.
• Chronic heart failure in the stage of decompensation.
• AV blockage of II and III degrees.
• Sinoatrial blockade.
• SSSU.
• Severe bradycardia.
• Prinzmetal angina pectoris.
• Cardiomegaly (no signs of heart failure).
• Arterial hypotension (systolic pressure
• Severe forms of bronchial asthma and other obstructive airway diseases.
• Late-stage peripheral circulatory disorders, Raynaud’s disease.
• Pheochromocytoma (without simultaneous use of alpha-blockers).
• Metabolic acidosis.
• Depression.
• Concomitant use of MAO inhibitors (with the exception of MAO type B inhibitors).
• Children and adolescents under 18 years of age.
• Hypersensitivity to the components of the drug and other beta-blockers.

With caution:  the drug should be prescribed to patients with hepatic insufficiency, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes mellitus, AV block I degree, psoriasis; if indicated in the anamnesis for depression, allergic reactions; elderly patients.

Side effects

From the central nervous system and peripheral nervous system:  increased 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), tremor, convulsions.

From the side of the senses:  visual impairment, decreased lacrimal fluid secretion, dry and painful eyes, conjunctivitis.

From the cardiovascular system:  sinus bradycardia, palpitation, impaired myocardial conduction, AV block (up to the development of complete transverse block and cardiac arrest), weakening of myocardial contractility, development (aggravation) of chronic heart failure (swelling of the ankles, feet, shortness of breath), decreased blood pressure, orthostatic hypotension, angiospasm manifestation (increased peripheral circulatory disorders, cold of the lower extremities, Raynaud’s syndrome), chest pain.

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

Respiratory system disorders:  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), hypothyroidism.

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

Musculoskeletal disorders:  back pain, arthralgia, cramps in the calf muscles.

From the side of the reproductive system:  decreased libido, decreased potency. Allergic reactions: pruritus, rash, urticaria.

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

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

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

Interaction

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 intravenous use increase the risk of anaphylactic reactions in patients receiving bisoprolol.

Phenytoin with intravenous use, drugs for inhaled general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive effects and the likelihood of lowering blood pressure in patients receiving bisoprolol.

Bisoprolol changes 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 diphylline)and increases their plasma concentrations, especially in patients with initially elevated theophylline clearance due to smoking.

The hypotensive effect of bisoprolol is reduced by NSAIDs (sodium ion retention and blockade of prostaglandin synthesis 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 concomitantly with bisoprolol increase the risk of developing or worsening bradycardia, AV block, cardiac arrest and heart failure.

When used concomitantly with nifedipine, a significant decrease in blood pressure is possible.

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

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

Tri-and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and sleeping pills increase the depressing effect of bisoprolol on the central nervous system.

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

Non-hydrogenated ergot alkaloids (including ergotamine) when used concomitantly with bisoprolol, the risk of developing peripheral circulatory disorders increases.

Sulfasalazine increases the concentration of bisoprolol in the blood plasma.

Rifampicin reduces T_1/2 bisoprolol.

How to take, course of use and dosage

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

For elderly patients: no dose adjustment is required.

In patients with impaired renal function with creatinine clearance: the maximum daily dose is 10 mg.

Tablets are taken without chewing.

Overdose

Symptoms: ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, chronic heart failure, cyanosis of the fingernails or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: gastric lavage and use of adsorbent drugs. Symptomatic therapy: if AV block develops, intravenous use of 1-2 mg of atropine, epinephrine or a temporary pacemaker is performed; for ventricular extrasystole, lidocaine (class IA drugs are not used). With a decrease in blood pressure, the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema – intravenous plasma – substituting solutions, if ineffective – use of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic effects and eliminate a pronounced decrease in blood pressure); with heart failure – cardiac glycosides, diuretics, glucagon; with convulsions – intravenous diazepam; with bronchospasm-beta-2-adrenostimulants by inhalation.

Special instructions

Monitoring of patients taking Bisogamma® includes measurement of heart rate and blood pressure (at the beginning of treatment – daily, then once every 3-4 months), ECG, determination of blood glucose levels in patients with concomitant diabetes mellitus (once every 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.

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

Beta-blockers are ineffective in approximately 20% of patients with angina pectoris. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats / min) and increased end 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 arterial hypertension (if an effective blockade of alpha-adrenergic receptors is not achieved beforehand).

In thyrotoxicosis, bisoprolol can mask certain clinical symptoms of thyrotoxicosis (for example, tachycardia).

Abrupt withdrawal of Bisogamma® in patients with thyrotoxicosis is contraindicated, as it can increase symptoms.

In diabetic patients, Bisogamma may 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 levels.

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, Bisogamma should be discontinued 48 hours before the start of general anesthesia. If the patient has taken the drug before surgery, they should choose a general anesthesia medication with minimal negative inotropic effects.

Reciprocal activation of the vagus nerve can be eliminated by intravenous use of atropine (1-2 mg).

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

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

If elderly patients are found to have increasing bradycardia (less than 50 beats / min), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV-blockade, the dose should be reduced or treatment should be discontinued.

It is recommended to stop therapy if depression develops.

Do not abruptly interrupt treatment due to the risk of developing severe arrhythmia and myocardial infarction. Withdrawal 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, it can be discontinued only a few days after the withdrawal of bisoprolol.

In smoking patients, the effectiveness of beta-blockers is lower.

Patients who use contact lenses should consider that during treatment with Bisogamma, the production of tear fluid may decrease.

The drug should be discontinued before testing the blood and urine levels of catecholamines, normetanephrine and vanillinmindalic acid, and titers of antinuclear antibodies.

Influence on the ability to drive motor vehicles and manage mechanisms

During treatment, patients should exercise caution when driving vehicles and engaging in 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

3 years

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Arrhythmia, Heart Failure, Hypertension