Bisoprolol pills 10mg, 60pcs

Composition

1 tablet contains:

Active ingredient:

bisoprolol fumarate 10 mg.

Auxiliary substances:

lactose monohydrate,

microcrystalline cellulose,

colloidal silicon dioxide,

crospovidone,

magnesium stearate.

Pharmacological action

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.

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), a 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 visual organ:  decreased lacrimal fluid secretion, conjunctivitis.

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

Musculoskeletal disorders: muscle weakness, muscle cramps.

Skin and subcutaneous tissue disorders:  skin pruritus; in some cases – increased manifestations of psoriasis, the appearance of psoriasis-like rashes.

Respiratory system disorders:  predisposed patients may develop symptoms of bronchial obstruction.

Other services:  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, 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:

with advanced AV blockade – intravenous injection of 1-2 mg of atropine, epinephrine or staging temporary pacemaker; ventricular premature beats – lidocaine (IA drugs of a class not applicable ); the decrease in blood pressure – the patient must be in the Trendelenburg position; if there are no signs of pulmonary edema, intravenous plasma-substituting solutions, the ineffectiveness of the epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic actions and elimination of severely impaired BP); heart failure – cardiac glycosides, diuretics, glucagon; in convulsions – diazepam intravenously; with bronchospasm – beta 2-agonists inhaled

Special instructions

Nervous system disorders:  weakness, fatigue, dizziness, headache, sleep disorders, mental disorders (depression, rarely hallucinations), a 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 visual organ:  decreased lacrimal fluid secretion, conjunctivitis.

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

Musculoskeletal disorders:  muscle weakness, muscle cramps.

Skin and subcutaneous tissue disorders: skin pruritus; in some cases – increased manifestations of psoriasis, the appearance of psoriasis-like rashes.

Respiratory system disorders: predisposed patients may develop symptoms of bronchial obstruction.

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

Form of production

Pills.

Active ingredient

Bisoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Arrhythmia, Heart Failure