Bisoprolol pills 2.5mg, 30pcs

Composition

1 film-coated tablet contains:

Active ingredient:

bisoprolol fumarate 2.5 mg

. excipients:

lactose monohydrate,

microcrystalline cellulose,

colloidal silicon dioxide,

crospovidone,

magnesium stearate.

Pharmacological action

Pharmacodynamics

Bisoprolol is a selective beta-1-adrenoblocker without its own sympathomimetic activity; it has antihypertensive, antiarrhythmic and antianginal effects. Blocking the beta-1-adrenergic receptors of the heart in low doses, it reduces the formation of cyclic adenosine monophosphate (cAMP) stimulated by catecholamines from adenosine triphosphate (ATP), reduces the intracellular flow of calcium ions (Ca2+), has a negative chrono -, dromo -, batmo – and inotropic effect (reduces heart rate, inhibits conduction and excitability, reduces myocardial contractility).

When the dose is increased, it has a beta-2-adrenoblocking effect. Total peripheral vascular resistance at the beginning of beta-blockers use, in the first 24 hours, increases (as a result of a reciprocal increase in alpha-adrenergic activity and elimination of beta-2-adrenergic stimulation), which returns to its original value after 1-3 days, 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-aldosterone system (it is more important for patients with initial hypersecretion of renin), restoration of sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure (BP)) 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 myocardial oxygen demand as a result of a decrease in heart rate and contractility, prolongation of diastole, and improvement of 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 myocardial oxygen, especially in patients with chronic heart failure (CHF).

Unlike non-selective beta-blockers, when administered in medium therapeutic doses, it has a less pronounced effect on the organs containing beta-2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, and does not cause sodium (Na+) ion retention in the body. When used in large doses, it has a blocking effect on both subtypes of beta-adrenergic receptors.

Pharmacokinetics.

Bisoprolol is almost completely absorbed from the gastrointestinal tract (80-90%). Food intake does not affect the absorption of the drug. The maximum concentration in the blood plasma is reached in 2-3 hours. Binding to plasma proteins is approximately 35%. Permeability through the blood-brain barrier and placental barrier is low, and secretion with breast milk is low.

It is metabolized in the liver. The half-life (T 1/2) is 9-12 hours, it is prolonged in cases of impaired renal function (with creatinine clearance less than 40 ml / min-3 times), in the elderly, in liver diseases (with cirrhosis increases to 21.7 hours). It is excreted by the kidneys-50% unchanged, less than 2% through the intestines.

Indications

• Arterial hypertension,
• prevention of angina attacks,
• chronic heart failure.

Use during pregnancy and lactation

Use during pregnancy and lactation is not recommended and is possible if the expected benefit to the mother exceeds the potential risk of side effects in the fetus and child.

In exceptional cases of use during pregnancy, bisoprolol should be discontinued 72 hours before the expected date of delivery due to the possibility of bradycardia, hypotension, hypoglycemia and respiratory depression in the newborn. If cancellation is not possible, then the newborn’s condition should be carefully monitored within 72 hours after delivery.

If it is necessary to use bisoprolol during lactation, breastfeeding should be discontinued.

Contraindications

• Acute heart failure,
• chronic heart failure in the stage of decompensation,
• cardiogenic shock,
• collapse,
• AV-block II and III degree (without pacemaker),
• SSSU;
• sinoatrial block,
• bradycardia (heart rate
• Prinzmetal’s angina,
• marked reduction in blood pressure (systolic blood pressure
• , a severe form of bronchial asthma and COPD, a history of
• the later stages of peripheral circulatory disorders,
• Raynaud’s disease,
• pheochromocytoma (without the simultaneous use of alpha-blockers),
• metabolic acidosis,
• simultaneous reception of MAO inhibitors (except MAO inhibitors of type B),
• childhood and adolescence to 18 years,
• increased sensitivity to bisoprolol and to other beta-blockers.

Side effects

 Nervous system disorders: weakness, fatigue, dizziness, headache, sleep disorders, mental disorders (depression, rarely hallucinations), feeling of cold and paresthesia in the extremities.

From the cardiovascular system: orthostatic hypotension, bradycardia, impaired AV conduction, the appearance of symptoms of heart failure, exacerbation of intermittent claudication and the main clinical symptoms in Raynaud’s syndrome.

From the side of the organ of vision: decreased secretion of lacrimal fluid, conjunctivitis.

From the digestive system: diarrhea, constipation, nausea, abdominal pain.

Musculoskeletal disorders: muscle weakness, muscle cramps.

From the skin and subcutaneous tissues: itching of the skin; in some cases – increased manifestations of psoriasis, the appearance of psoriasis-like rashes.

From the respiratory system: in predisposed patients, symptoms of bronchial obstruction may occur.

Other: sweating, hot flashes, impaired potency, decreased glucose tolerance in patients with diabetes mellitus, allergic reactions.

Interaction

With simultaneous use of antacids and antidiarrheal agents, it is possible to reduce the absorption of beta-blockers.

With simultaneous use of antiarrhythmic drugs, a sharp decrease in blood pressure, a decrease in heart rate, the development of arrhythmia and/or heart failure may occur.

With the simultaneous use of antihypertensive agents, the antihypertensive effect may increase.

With simultaneous use of cardiac glycosides, conduction disturbances may occur.

With the simultaneous use of sympathomimetics (including those included in cough remedies, nasal drops, eye drops), the effectiveness of bisoprolol decreases.

With the simultaneous use of verapamil, diltiazem, a sharp decrease in blood pressure, a decrease in heart rate, the development of arrhythmia and/or heart failure is possible.

With the simultaneous use of guanfacine, severe bradycardia and conduction disturbances are possible.

With simultaneous use of insulin, hypogligemic agents for oral use, the effect of insulin or other hypogligemic agents increases (regular monitoring of blood glucose levels is necessary).

With the simultaneous use of clonidine, severe bradycardia, arterial hypotension, and conduction disorders are possible.

In case of sudden withdrawal of clonidine in patients receiving bisoprolol, a sharp increase in blood pressure may occur.

With the simultaneous use of nifedipine, other calcium channel blockers, dihydropyridine derivatives, the antihypertensive effect of bisoprolol is enhanced.

With the simultaneous use of reserpine, alpha-methyldopa, severe bradycardia is possible.

With simultaneous use of rifampicin, a slight decrease in T1/2 bisoprolol is possible.

Concomitant use of ergotamine derivatives (including drugs for the treatment of migraines containing ergotamine) increases the symptoms of peripheral circulatory disorders.

How to take it, course of use and dosage

Inside, in the morning on an empty stomach, without chewing,5 mg once.

If necessary, the dose is increased to 10 mg once a day. The maximum daily dose is 20 mg / day.

In patients with impaired renal function with creatine clearance less than 20 ml/min or with severe hepatic impairment, the maximum daily dose is 10 mg.

No dose adjustment is required in elderly patients.

Overdose

Symptoms: arrhythmia, 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 recommended; 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-the introduction of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic effects and eliminate a pronounced decrease in blood pressure);

In case of heart failure-cardiac glycosides, diuretics, glucagon;

For convulsions-intravenous diazepam; for bronchospasm-beta-2-adrenostimulants by inhalation

Special instructions

Monitoring of patients taking Bisoprolol should include measurement of heart rate and blood pressure (at the beginning of treatment – daily, then once every 3-4 months), ECG, determination of blood glucose in patients with 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.

In “smokers”, the effectiveness of beta-blockers is lower. Patients who use contact lenses should take into account that during treatment, there may be a decrease in the production of tear fluid. When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if an effective alpha-adrenoblockade is not previously achieved).

In thyrotoxicosis, Bisoprolol can mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase symptoms. In diabetes mellitus, it can 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.

When taking clonidine at the same time, it can be stopped only a few days after the withdrawal of Bisoprolol.

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, the drug is withdrawn 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 activation of the vagus nerve can be eliminated by intravenous use of atropine (1-2 mg).

Drugs that reduce the supply of catecholamines (including reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be constantly monitored by a doctor for 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 pronounced 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 arrhythmias 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). It should be canceled before testing the content of catecholamines, normetanephrine and vanillinmindalic acid in the blood and urine, and titers of antinuclear antibodies.

During the treatment period, care should be taken 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

Store in a dry place protected from light, out of reach of children, at a temperature not exceeding 20 °C.

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Heart Failure, Arrhythmia, Hypertension