Biprol, 10 mg 30 pcs

A selective beta1-adrenoblocker with no sympathomimetic activity of its own, has no membrane stabilizing effect.

It has antihypertensive, antiarrhythmic and antianginal action.

By blocking in low doses beta1-adrenoreceptors of the heart it decreases stimulated by catecholamines formation of cyclic adenosine monophosphate from adenosine triphosphate, decreases intracellular ions flux.br>
calcium, has negative chrono-, dromo-, batmo- and inotropic effects, reduces atrioventricular (AV) conduction and excitability.

In case of therapeutic dose it has beta2-adrenoblocking action.

The total peripheral vascular resistance at the beginning of the drug administration (during the first 24 hours) increases (as a result of reciprocal increase of activity of alpha-adrenoreceptors and elimination of

stimulation of beta2-adrenoreceptors) that after 1-3 days returns to the initial level, and decreases after the long-term administration.

Antihypertensive effect is associated with a decrease in the minute blood volume, sympathetic stimulation of peripheral vessels, reduction of the activity of the renin-angiotensin-aldosterone system (has great

important for patients with initial renin hypersecretion), restoration of aortic arch baroreceptors sensitivity (there is no increase of their activity in response to a decrease in blood pressure) and the effect on the central nervous system.

In case of arterial hypertension the effect is developed in 2-5 days, its stable effect – in 1-2 months.

Antianginal action is determined by the decrease of myocardial oxygen demand due to slow heart rate and decreased myocardial contractility, prolongation of diastole, improvement of myocardial perfusion.

By increasing end diastolic pressure in the left ventricle and increasing ventricular muscle fiber stretch may increase myocardial oxygen demand, especially in patients with chronic heart failure (CHF).

Antiarrhythmic action is due to the elimination of arrhythmogenic factors (tachycardia, increased sympathetic nervous system activity, increased cyclic adenosine monophosphate,

arterial hypertension), decreased rate of spontaneous excitation of sinus and ectopic pacemakers, and deceleration of AV conduction (predominantly antegrade and, to a lesser extent, retrograde) through the atrioventricular node and along accessory pathways.

In contrast to non-selective beta-adrenoblockers, when administered in medium therapeutic doses it has less pronounced effect on organs containing beta2-adrenoreceptors (pancreas, skeletalbr>
muscles, smooth muscles of peripheral arteries, bronchi and uterus) and carbohydrate metabolism; does not cause sodium ion retention in the body.

Pharmacokinetics

Absorption. Absorption is 80-90%, food intake does not affect absorption of the drug. Maximal concentration in blood plasma is observed after 1-3 hours. Bioavailability is about 90%. Binding with blood plasma proteins is about 30%.

Distribution. Volume of distribution is 3.5 l/kg. Permeability through the blood-brain barrier and the placental barrier is low.

Metabolism. Metabolized in liver with participation of CYP3A4 (up to 95%) and CYP2D6 isoenzymes. The effect of “primary passage” through the liver is insignificant (about 10%). Biotransformation of bisoprolol is not accelerated in patients with thyroid hyperfunction.

Excretion. Total clearance is 15.6±3.2 l/hour, renal clearance is 9.6±1.6 l/hour. Balanced clearance of bisoprolol is determined by the balance between its excretion through the kidneys in unchanged form (about

50%) and oxidation in the liver (about 50%) to inactive metabolites, which are then also excreted by the kidneys; less than 2% is excreted through the intestine (with bile).

It does not accumulate in the body. Half-life period is 9-12 hours.

Dependence of bisoprolol pharmacokinetics on dose is linear.

Pharmacokinetics of bisoprolol is stable, independent of patient age and sex.

Pharmacokinetics in special clinical cases

Renal insufficiency. In case of marked renal function impairment (creatinine clearance less than 20 ml/min) and in patients with anuria half-life period may increase more than 2 times.

Hepatic insufficiency. In case of severe hepatic insufficiency half-life period is increased up to 13-15 hours.

Chronic heart failure. In patients with chronic heart failure (functional class III according to the NYHA classification), plasma concentration of bisoprolol is higher than in healthy volunteers, and the half-life is increased up to 17 hours.

Indications

Active ingredient

Composition

Active ingredient:

Bisoprolol fumarate 5,000 mg/10,000 mg;

Supplements:

Microcrystalline cellulose 44,500 mg/ 62,400 mg;

Ludipress LCE (lactose monohydrate 94.7-98.3%, povidone 3-4%) 40,000 mg/ 38,500 mg;

Corn starch 8,000 mg/ 11,000 mg;

Colloidal silica 0.500 mg/ 0.600 mg;

Crospovidone (collidon CL) 1,000 mg/ 1,250 mg;

Magnesium stearate 1,000 mg/ 1,250 mg;

Shell:

Titanium dioxide 0.287 mg/ 0.430 mg;

Macrogol (polyethylene glycol 4000) 0.287 mg/ 0.430 mg;

Hypromellose 1.320 mg/ 1.968 mg;

Talc 0.106 mg/ 0.172 mg.

How to take, the dosage

Biprol is taken orally, in the morning, once a day with some fluid, before, during or after breakfast. The tablets should not be chewed or crushed into a powder.

In all cases, the dosage and the regimen are determined by the physician for each patient individually, especially taking into account the heart rate and the patient’s condition.

In case of arterial hypertension and coronary heart disease, the drug is prescribed 5 mg once a day. If necessary, the dose is increased to 10 mg once daily. In treatment of arterial hypertension and angina pectoris the maximum daily dose is 20 mg once daily.

In patients with significant renal impairment (creatinine clearance less than 20 ml/min) or with significant hepatic impairment, the maximum daily dose is 10 mg once daily. Increasing the dose in such patients should be carried out with extreme caution.

In elderly patients no dose adjustment is required.

Interaction

Special Instructions

Contraindications

Side effects

Overdose

Pregnancy use

The use of Biprol during pregnancy and lactation is possible if the benefit to the mother exceeds the risk of side effects in the fetus and child.

Similarities