Cordinorm, 5 mg 90 pcs.

A selective beta₁-adrenoblocker without intrinsic sympathomimetic activity and membrane stabilizing properties. By blocking in low doses β₁-adrenoreceptors of the heart, bisoprolol reduces catecholamine-stimulated formation of cAMP from ATP, reduces intracellular flow of calcium ions. It has negative chrono-, dromo-, batmo- and inotropic effects, inhibits conduction and excitability, slows AV conduction, reduces myocardial oxygen demand. Reduces HR at rest and during exercise. Reduces plasma renin activity. It has hypotensive, antiarrhythmic and antianginal action.

When increasing the dose, bisoprolol has beta₂-adrenoblocking effect.

In the beginning of drug administration (in the first 24 h) as a result of reciprocal increase of α-adrenoreceptor activity and elimination of β₂-adrenoreceptor stimulation, ROS increases slightly. After 1-3 days, OPPS returns to the initial level, and with prolonged use it decreases.

The hypotensive effect of bisoprololol is due to reduction of IOC, sympathetic stimulation of peripheral vessels, decrease of renin-angiotensin system activity (important for patients with initial renin hypersecretion), restoration of sensitivity in response to BP reduction and influence on CNS. For arterial hypertension the effect occurs in 2-5 days, stable effect – in 1-2 months.

The antianginal effect is caused by decrease of myocardial oxygen demand as a result of HR shortening and decrease of contractility, prolongation of diastole, improvement of myocardial perfusion. By increasing left ventricular end-diastolic pressure and increasing ventricular muscle fiber stretch can increase oxygen demand, especially in patients with chronic heart failure.

The antiarrhythmic effect is caused by the removal of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased content of CAMF, arterial hypertension) and also by a decrease of the rate of spontaneous excitation of sinus and ectopic pacemakers and delay of AV conduction (mainly in the antegrade and, to a lesser degree, in the retrograde direction through the AV node) and through additional pathways.

In contrast to non-selective beta-adrenoblockers, bisoprolol has less pronounced effect on the organs containing β₂-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and carbohydrate metabolism, does not cause sodium retention in the body. The severity of atherogenic action does not differ from that of propranolol.

When used in high doses it has a blocking effect on both β-adrenoreceptor subtypes.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Nervous system disorders: increased fatigue, weakness, dizziness, headache, drowsiness or insomnia, “nightmares” dreams, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesias in extremities (in patients with “intermittent” claudication and Raynaud’s syndrome), tremor.

Sense organs: visual impairment, decreased tear fluid secretion, dry and painful eyes, conjunctivitis.

Cardiovascular system disorders: sinus bradycardia, palpitations, myocardial conduction disorders, AV blockade (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakened myocardial contractility, development (worsening) of chronic heart failure, BP reduction, orthostatic hypotension, manifestation of angiospasm (worsening of peripheral circulation disorders, coldness of the lower extremities, Raynaud’s syndrome), chest pain.

Gastrointestinal disorders: dry mouth, nausea, vomiting, abdominal pain, constipation or diarrhea, liver disorders (dark urine, jaundice of sclerae or skin, cholestasis), changes in taste.

Respiratory system: nasal congestion, difficulty in breathing when prescribed in high doses (loss of selectivity) and/or in susceptible patients – laryngo- and bronchospasm.

Endocrine system: hyperglycemia (in patients with insulin-independent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroidism.

Allergic reactions: itching, rash, urticaria.

Skin disorders: increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms, alopecia.

Laboratory parameters: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in enzyme activity, bilirubin and triglyceride levels.

Fetal effects: intrauterine growth retardation, hypoglycemia, bradycardia.

Muscular system: muscle weakness, cramps in the calf muscles.

Others: back pain, arthralgia, decreased libido; rarely – decreased potency, withdrawal syndrome (increased angina attacks, increased BP).

Overdose

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