Binelol, pills 5mg, 28pcs

Composition

1 tablet contains:

Active ingredient:

nebivolol (in the form of nebivolol hydrochloride) 5 mg,

excipients:

lactose monohydrate;

crospovidone (type A);

poloxamer 188;

povidone K 30;

MCC;

magnesium stearate

Pharmacological action

Binelol has antiarrhythmic, antihypertensive, and antianginal effects.

Pharmacodynamics

Nebivolol is a third-generation lipophilic, cardioselective beta-1 blocker with vasodilating properties. It has antihypertensive, antianginal and antiarrhythmic effects. Reduces elevated blood pressure at rest, during physical exertion and stress. Competitively and selectively blocks synaptic and postsynaptic β1-adrenergic receptors, making them inaccessible to catecholamines, modulates the release of endothelial vasodilating factor-nitric oxide (NO).

Nebivolol is a racemate consisting of two enantiomers: SRRR-nebivolol (D-nebivolol) and RSSS-nebivolol (L-nebivolol), combining two pharmacological actions:

– D-nebivolol is a competitive and highly selective blocker of β1-adrenergic receptors (affinity for β1-adrenergic receptors is 293 times higher than for β2-adrenergic receptors);

– L-nebivolol has a mild vasodilating effect by modulating the release of relaxing factor (NO) from the vascular endothelium.

Hypotensive effect develops on the 2nd-5th day of treatment, stable effect is noted after 1 month. The antihypertensive effect persists with long-term treatment.

The hypotensive effect is also due to a decrease in the activity of the renin-angiotensin system (it does not directly correlate with changes in the activity of renin in blood plasma).

Nebivolol improves the parameters of systemic and intracardiac hemodynamics. Nebivolol reduces heart rate and blood pressure at rest and during exercise, reduces the final diastolic pressure of the left ventricle, reduces OPSS, improves diastolic function of the heart (reduces filling pressure), increases the ejection fraction.

Reducing the need for myocardial oxygen (reducing heart rate, reducing preload and afterload), reduces the number and severity of angina attacks and increases exercise tolerance.

The antiarrhythmic effect is due to the suppression of pathological automatism of the heart (including in the pathological focus) and a slowdown in AV conduction.

Pharmacokinetics

Suction. After oral use, nebivolol is rapidly absorbed from the gastrointestinal tract. Food intake does not affect absorption, so nebivolol can be taken regardless of food intake. Bioavailability is on average 12% in patients with fast metabolism and is almost complete in patients with slow metabolism. The effectiveness of nebivolol does not depend on the metabolic rate.

Distribution. Plasma clearance in most patients (with rapid metabolism) is achieved within 24 hours, and for hydroxymetabolites – after a few days. The concentration in blood plasma (1-30 mcg/l) is proportional to the dose.

The relationship with plasma proteins (mainly albumin) for D-nebivolol is 98.1%, and for L-nebivolol — 97.9%.

Metabolism. Nebivolol is extensively metabolized, partly to form active hydroxymetabolites. The rate of metabolism of nebivolol by aromatic hydroxylation is genetically determined by an oxidative polymorphism and depends on the CYP2D6 isoenzyme.

Output. One week after use,38% (the amount of unchanged Active ingredient is less than 0.5%) of the dose is excreted by the kidneys and 48% – through the intestines.

In patients with rapid metabolism, the T1/2 values of nebivolol enantiomers from blood plasma are on average 10 hours. In patients with “slow” metabolism, these values increase 3-5 times.

In patients with fast metabolism, the values of T1 / 2 hydroxymetabolites of both enantiomers from blood plasma are on average 24 hours, in patients with slow metabolism, these values increase approximately 2 times.

The pharmacokinetics of nebivolol are not affected by the age and gender of patients.

Indications

• arterial hypertension;
• ischemic heart disease (prevention of angina attacks of tension);
• chronic heart failure (as part of combination therapy).

Use during pregnancy and lactation

During pregnancy, the drug Binelol is prescribed only for strict indications, when the benefit to the mother exceeds the risk to the fetus (due to the possible development of bradycardia, arterial hypotension, hypoglycemia and respiratory paralysis in the newborn). Treatment should be interrupted 48-72 hours before delivery.

In cases where this is not possible, it is necessary to ensure strict monitoring of the newborn within 48-72 hours after delivery.

Animal studies have shown that nebivolol is excreted in breast milk. If the use of the drug during lactation is necessary, then breastfeeding should be discontinued.

Contraindications

• hypersensitivity to nebivolol or one of the components of the drug Linalol;
• severe disturbances of liver function;
• acute heart failure;
• chronic heart failure in the stage of decompensation (requiring intravenous drugs with inotropic effect);
• cardiogenic shock;
• the syndrome of weakness of the sinus node, including sinoauricular blockade;
• AV blockade II and III degree (without an artificial pacemaker);
• bronchospasm and bronchial asthma;
• untreated pheochromocytoma;
• depression;
• metabolic acidosis;
• bradycardia (heart rate
• severe hypotension (SBP
• severe occlusive peripheral vascular disease (intermittent claudication, Raynaud’s syndrome);
• myasthenia gravis;
• the age of 18;
• lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

With caution: renal failure; diabetes mellitus; hyperthyroidism; a history of allergic diseases; psoriasis; AV block I degree; Prinzmetal angina pectoris; chronic obstructive pulmonary disease; patients over 65 years of age.

Side effects

From the central nervous system and peripheral nervous system: headache, dizziness, fatigue, weakness, paresthesia (from 1 to 10%); in very rare cases — depression, decreased ability to concentrate, drowsiness, insomnia, nightmares, hallucinations, psychosis, convulsions.

From the gastrointestinal tract: nausea, constipation, flatulence, diarrhea, dry mouth (more than 1%).

From the cardiovascular system: bradycardia, acute heart failure, AV block, orthostatic hypotension, exacerbation of intermittent claudication, shortness of breath; in very rare cases — cardiac arrhythmias, Raynaud’s syndrome, peripheral edema, cardialgia.

Allergic reactions: pruritus of the skin, erythematous rash.

Others: bronchospasm (including in the absence of obstructive pulmonary diseases in the anamnesis), photodermatosis, hyperhidrosis, rhinitis, exacerbation of psoriasis, visual impairment, dry eyes.

Interaction

Concomitant use of beta-blockers with BMCC (verapamil and diltiazem) increases the negative effect on myocardial contractility and AV conduction. Intravenous use of verapamil with nebivolol is contraindicated. When combined with antihypertensive agents, nitroglycerin or BMCC, severe arterial hypotension may develop (special caution is necessary when combined with prazosin).

When used concomitantly with Class I antiarrhythmic drugs and amiodarone, it is possible to increase the negative inotropic effect and prolong the time of atrial excitation.

When nebivolol was co-administered with cardiac glycosides, there was no increase in the effect on slowing AV conduction.

Concomitant use of nebivolol and general anaesthetic agents may cause suppression of reflex tachycardia and increase the risk of hypotension.

There is no clinically significant interaction between nebivolol and NSAIDs. Acetylsalicylic acid as an antiplatelet agent can be used simultaneously with nebivolol.

Concomitant use of tricyclic antidepressants, barbiturates and phenothiazine derivatives may increase the hypotensive effect of nebivolol.

Pharmacokinetic interaction

When used concomitantly with drugs that inhibit serotonin reuptake, or other agents that biotransform with the participation of the CYP2D6 isoenzyme, nebivolol metabolism slows down.

Concomitant use of nebivolol did not affect the pharmacokinetic parameters of digoxin.

When used concomitantly with cimetidine, the concentration of nebivolol in blood plasma increases (there are no data on the effect on the pharmacological effects of the drug). Concomitant use of ranitidine did not affect the pharmacokinetic parameters of nebivolol.

When nebivolol is co-administered with nicardipine, the concentration of active substances in the blood plasma increases slightly, but this is not of clinical significance.

Concomitant use of ethanol, furosemide or hydrochlorothiazide does not affect the pharmacokinetics of nebivolol.

There was no clinically significant interaction between nebivolol and warfarin.

When used concomitantly, sympathomimetic agents inhibit the activity of nebivolol.

How to take it, course of use and dosage

Inside, at the same time of day, regardless of food intake, without chewing and with a sufficient amount of liquid.

Arterial hypertension and coronary heart disease.The average daily dose for the treatment of arterial hypertension and CHD is 2.5-5 mg (1/2-1 tablet) once a day. It is possible to use the drug in monotherapy or as part of a combination therapy.

In patients with renal insufficiency, as well as in patients over the age of 65 years, the initial dose is 2.5 mg / day (1/2 tablet of 5 mg).

If necessary, the daily dose can be increased to 10 mg (2 tablets of 5 mg) in one dose.

Chronic heart failure. Treatment of chronic heart failure should begin with a gradual increase in the dose until the individual optimal maintenance dose is reached.

The dose selection at the beginning of treatment should be carried out according to the following scheme, maintaining weekly intervals and based on the patient’s tolerance to this dose: the dose of 1.25 mg of the drug (1/4 tablet) 1 time per day can be increased first to 2.5–5 mg (1/2–1 tablet), and then to 10 mg (2 tablets) 1 time per day.

Overdose

Symptoms: decreased blood pressure, nausea, vomiting, cyanosis, sinus bradycardia, AV block, bronchospasm, cardiogenic shock, loss of consciousness, coma, cardiac arrest.

Treatment: gastric lavage, use of activated charcoal. In case of a marked decrease in blood pressure, it is necessary to give the patient a horizontal position with raised legs, if necessary, intravenous fluid and vasopressors; as a follow-up,1-10 mg of glucagon may be prescribed. With bradycardia,0.5–2 mg of atropine is administered intravenously; in the absence of a positive effect, a transvenous or intracardiac electrostimulator is possible. In case of grade II–III AV block, intravenous use of beta-adrenostimulants is recommended; if they are ineffective, an artificial pacemaker should be considered. In case of heart failure, treatment begins with the introduction of cardiac glycosides and diuretics, if there is no effect, it is advisable to introduce dopamine, dobutamine or vasodilators. When bronchospasm is prescribed intravenously beta-adrenomimetics. For ventricular extrasystole — lidocaine (class IA antiarrhythmics should not be administered). For convulsions-intravenous diazepam.

Special instructions

Beta-blockers should be discontinued gradually over 10 days (up to 2 weeks in patients with CHD).

Monitoring of blood pressure and heart rate at the beginning of taking the drug should be daily.

In elderly patients, monitoring of renal function is necessary (1 time in 4-5 months).

With angina pectoris, the dose of the drug should provide a resting heart rate of 55-60 beats / minute, with a load of no more than 110 beats / minute.

beta-blockers can cause bradycardia: the dose should be reduced if the heart rate is less than 50-55 beats / minute.

When deciding whether to prescribe Binelol to patients with psoriasis, the expected benefit of the drug and the possible risk of exacerbation of psoriasis should be carefully weighed.

Patients using contact lenses should take into account that the use of beta-blockers may reduce the production of tear fluid.

When performing surgical interventions, the anesthesiologist should be warned that the patient is taking beta-blockers.

Nebivolol does not affect glucose levels in patients with diabetes mellitus. However, caution should be exercised when treating these patients, as Binelol may mask certain symptoms of hypoglycemia (e. g. tachycardia) caused by the use of hypoglycemic agents.

Blood glucose monitoring should be performed once every 4-5 months (in patients with diabetes mellitus).

beta-blockers should be used with caution in patients with COPD, as bronchospasm may increase.

beta-blockers may increase sensitivity to allergens and the severity of anaphylactic reactions.

The effectiveness of beta-blockers in smokers is lower than in non-smokers.

Influence on the ability to drive a car or perform work that requires an increased rate of physical and mental reactions. Research studies have shown that nebivolol has no effect on the speed of psychomotor reactions. Pilots of flight personnel with mild arterial hypertension, admitted to flight work, the drug is prescribed in an initial dose of 2.5 mg. In the future (no earlier than 2 weeks), if the treatment is well tolerated and blood pressure is not sufficiently controlled, the dose may be increased by 2.5 mg. The recommended dose is 5 mg / day. Some patients may experience side effects, most often dizziness, due to low blood pressure. If such effects occur, the patient should not drive vehicles or engage in potentially dangerous activities that require special attention and speed of psychomotor reactions. These effects occur most often immediately after starting treatment or when the dose is increased.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 30 °C. Keep out of reach of children.

Shelf

life is 3 years.

Active ingredient

Nebivolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Nursing mothers as prescribed by a doctor, Pregnant women as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Heart Failure, Angina, Arrhythmia, Hypertension