Biprol, 5 mg 50 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 ion 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 reduction of the minute blood volume, sympathetic stimulation of peripheral vessels, reduction of renin-angiotensin-aldosterone system activity (of great importance for patients with

initial renin hypersecretion), restoration of sensitivity of aortic arch baroreceptors (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 – about 30%.

Distribution.

Distribution volume is 3.5 l/kg. Permeability through the blood-brain and placental barriers is low.

Metabolism. Metabolized in the liver with the participation of CYP3A4 (up to 95%) and CYP2D6 isoenzymes. The e

ffekt “primary passage” through the liver is insignificant (about 10%). Bisoprolol biotransformation 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), the plasma concentration of bisoprolol is higher than in healthy volunteers, and the half-life is increased to 17 hours.

Indications

Active ingredient

Composition

How to take, the dosage

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