Bisoprolol Alkaloid, 5 mg 30 pcs

Pharmacotherapeutic group:

Beta1-adrenoblocker selective
ATC:
C.07.A.B Selective beta1-adrenoblockers
C.07.A.B.07 Bisoprolol

Pharmacodynamics:

Bisoprolol is a selective beta1-adrenoblocker without intrinsic sympathomimetic activity and has no membrane-stabilizing effect. Bisoprolol reduces plasma renin activity, reduces myocardial oxygen demand, and decreases heart rate (HR). It has antihypertensive, antiarrhythmic and anti-angina action.

By blocking in low doses beta1-adrenoceptors of heart, decreases catecholamine-stimulated cyclic adenosine monophosphate (cAMP) formation from adenosine triphosphate (ATP), decreases intracellular calcium ions flow, inhibits all heart functions, decreases atrioventricular (AV) conduction and excitability. If the therapeutic dose is exceeded, it has a beta2-adrenoblocking effect. Overall peripheral vascular resistance increases at the beginning of the drug administration, during the first 24 hours (as a result of reciprocal increase of activity of alpha-adrenoreceptors and elimination of stimulation of beta2-adrenoreceptors), after 1-3 days it returns to its baseline value, and during prolonged use it decreases.

Antihypertensive effect is related to the reduction of the blood minute volume, sympathetic stimulation of peripheral vessels, decrease of the sympathoadrenal system (SAS) activity (of great importance for patients with initial renin hypersecretion), restoration of sensitivity in response to blood pressure (BP) reduction and influence on the central nervous system. In arterial hypertension the effect is developed in 2-5 days, stable effect is observed after 1-2 months.

Antianginal effect is caused by decrease of myocardial oxygen demand due to decrease of contractility and other myocardial functions, prolongation of diastole, improvement of myocardial perfusion. Due to increased end diastolic pressure in the left ventricle and increased stretching of ventricular muscle fibers may increase oxygen demand, especially in patients with chronic heart failure (CHF).

When used in medium therapeutic doses, unlike non-selective beta-adrenoblockers, it has less pronounced effect on the organs containing beta2-adrenoreceptors (pancreas, skeletal muscles, smooth muscle of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism; Does not cause retention of sodium ions in the body; intensity of atherogenic action does not differ from that of propranolol.

Pharmacokinetics:

Bisoprolol is almost completely (over 90%) absorbed in the gastrointestinal tract, food intake does not affect absorption. The effect of “primary passage” through the liver is insignificant (at 10-15%), resulting in high bioavailability (90%). Food intake has no effect on the bioavailability of bisoprolol.

Bisoprolol is metabolized by the oxidative pathway without subsequent conjugation. All metabolites are strongly polar and are excreted by the kidneys. The major metabolites detected in plasma and urine have no pharmacological activity. Experiments with human liver microsomes in vitro show that bisoprolol is metabolized primarily by CYP3A4 isoenzyme (about 95%), and CYP2D6 isoenzyme plays only a minor role.

Binding with blood plasma proteins is about 30%. Volume of distribution is 3.5 l/kg. Total clearance is approximately 15 l/h. Maximal concentration in blood plasma is determined after 2-3 hours. The blood plasma half-life (10-12 hours) provides efficacy for 24 hours after a single daily dose.
Bisoprololol is eliminated from the body in two ways, 50% of the dose is metabolized in the liver to form inactive metabolites. About 98% is excreted by the kidneys, of which 50% is excreted unchanged; less than 2% – through the intestine (with bile).

Since excretion takes place in the kidneys and the liver equally, patients with impaired liver function or with renal failure do not require dose adjustment. The pharmacokinetics of bisoprolol are linear and independent of age.

In patients with CHF, the plasma concentrations of bisoprolol are higher and the elimination half-life is longer compared to healthy volunteers.

There is no information on the pharmacokinetics of bisoprolol in patients with CHF and concurrent hepatic or renal impairment.

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