Biprol, 5 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 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 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 unchanged (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 up to 17 hours.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

The use of allergens used for immunotherapy or allergen extracts for skin tests during therapy with Bisoprolol increases the risk of severe systemic allergic reactions or anaphylaxis.

The simultaneous use with bisoprolol of iodine-containing X-ray contrasting drugs for IV administration increases the risk of anaphylactic reactions.

Concomitant use of bisoprolol with IV phenytoin, drugs for inhalation general anesthesia (hydrocarbon derivatives) increases the severity of cardiodepressive effects and the likelihood of BP decrease.

In concomitant use, bisoprololol alters the effectiveness of insulin and oral hypoglycemic drugs and masks the symptoms of developing hypoglycemia (tachycardia, increased BP).

Concomitant use of bisoprolol decreases clearance of lidocaine and xanthines (except diphylline) and increases their plasma concentrations, especially in patients with initially increased clearance of theophylline due to smoking.

The hypotensive effect of bisoprolol is reduced by NSAIDs (Na+ retention and blockade of prostaglandin synthesis by the kidneys), GCS and estrogens (retention of Na+ ions).

When used concomitantly, cardiac glycosides, methyldopa, reserpine and guanfacine, calcium channel blockers (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV blockade, heart failure and heart failure.

When used concomitantly with bisoprolol, nifedipine may cause a significant decrease in BP.

When used concomitantly with bisoprololol, diuretics, clonidine, sympatholytics, hydralazine and other hypotensive drugs may lead to excessive BP reduction.

Bisoprolol prolongs the effects of nondepolarizing myorelaxants and the anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics increase the CNS depressant effect of bisoprolol.

The concomitant use of bisoprolol with MAO inhibitors is not recommended due to the significant increase in hypotensive effect (interval between intake of MAO inhibitors and bisoprolol should be at least 14 days).

When used concomitantly with bisoprololol, nonhydrogenated ergot alkaloids, ergotamine increase the risk of peripheral circulatory disorders.

Concomitant use of sulfasalazine increases the plasma concentration of bisoprolol.

Concomitant use of rifampicin decreases T 1/2 of bisoprolol.

Special Instructions

Synopsis

Features

Contraindications

Side effects

Overdose

Symptoms:

Arrhythmias, ventricular extrasystoles, marked bradycardia, AV blockade, marked BP decrease, chronic heart failure, cyanosis of finger and palm nails, difficulty breathing, bronchospasm, dizziness, fainting, seizures.

Treatment:

Gastric lavage, administration of adsorbents. If necessary, symptomatic therapy: in developed AV-blockade intravenous injection of atropine (1-2 mg), epinephrine, or placement of a temporary pacemaker; in ventricular extrasystole – lidocaine (Class I A drugs are not used).

In case of BP decrease, the patient should be in Trendelenburg position; if there are no signs of pulmonary edema, IV plasma exchange solutions are administered; if ineffective, epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and to eliminate marked BP decrease).

In case of heart failure, cardiac glycosides, diuretics, glucagon are prescribed; in convulsions – intravenous diazepam; in bronchospasm – beta 2 -adreno stimulants by inhalation.

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