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active ingredient: Nebivolol;

1 tablet contains: Nebivolol — in the form of Nebivolol hydrochloride) - 5 mg;

excipients: colloidal anhydrous silicon dioxide (colloidal anhydrous silica gel); magnesium stearate; sodium croscarmellose; polyethylene glycol (PEG 6000); lactose, monohydrate.

Dosage form. Pills.

Basic physical and chemical properties: tablets of white color, round shape, with a biconvex surface, 9 mm in diameter, with a cross-shaped risk on one side of the tablet and the "N5" logo on the other.

Pharmacotherapeutic group. Selective beta-adrenergic blockers.

ATX code C07A B12.

Pharmacological properties.


Nebivolol is a racemate that consists of two enantiomers: SRRR-Nebivolol (D‑Nebivolol ) and RSSS-Nebivolol (L-Nebivolol). It combines two pharmacological properties:

-due to the D-enantiomer, Nebivolol is a competitive and selective blocker of β1-adrenergic receptors;

– due to its L-enantiomer, it has mild vasodilatory properties due to its metabolic interaction with L-arginine/ nitric oxide (no).

With a single and repeated use of Nebivolol, the heart rate decreases at rest and during exercise, both in people with normal blood pressure and in people with arterial hypertension. The antihypertensive effect persists with long-term treatment. At therapeutic doses, alpha-adrenergic antagonism is not observed. During short-term and long-term treatment with Nebivolol in patients with arterial hypertension, systemic vascular resistance decreases. Despite the decrease in heart rate, the decrease in cardiac output at rest and during exercise is limited due to an increase in stroke volume. The clinical significance of this hemodynamic difference compared to other beta-adrenergic Blockers is still poorly understood. In patients with arterial hypertension, Nebivolol increases the vascular response to acetylcholine mediated by nitric oxide; in patients with endothelial dysfunction, this response is reduced. The use of Nebivolol as an adjunct to standard therapy for chronic heart failure with or without a decrease in the left ventricular ejection fraction significantly extended the time to death or hospitalization associated with cardiovascular pathology. The effect of Nebivolol does not depend on age, gender, or left ventricular ejection fraction. In patients treated with Nebivolol, a decrease in the frequency of cases of sudden death was found.

In vitro and in vivo animal experiments have shown that Nebivolol does not have sympathomimetic activity.

In vitro and in vivo animal experiments have shown that Nebivolol has no membrane-stabilizing activity at pharmacological doses.

In healthy volunteers, Nebivolol does not significantly affect the ability to tolerate maximum physical activity or endurance.

Available preclinical and clinical data for hypertensive patients do not indicate a negative effect of Nebivolol on erectile function.


After oral administration, both Nebivolol enantiomers are rapidly absorbed. The absorption of Nebivolol is not affected by food, so it can be taken with or without food. Nebivolol is completely metabolized, partially to form active hydroxymetabolites. Nebivolol is metabolized by acyclic or aromatic hydroxylation, N-dealkylation, and glucuronidation; in addition, hydroxymetabolite glucuronides are formed. Nebivolol metabolism by hydroxylation undergoes a CYP2D6-dependent genetic oxidative polymorphism. The oral bioavailability of Nebivolol is 12% in individuals with a fast metabolism and is almost complete in individuals with a slow metabolism. When a steady-state is achieved and at the same dose, the maximum plasma concentration of unchanged Nebivolol in individuals with a slow metabolism is approximately 23 times higher than in individuals with a fast metabolism. If we take into account the sum of the unchanged drug and its active metabolites, the difference in the maximum concentration in plasma is from 1.3 to 1.4 times. Given the differences in the degree of metabolism, the dose of Nebiar® should always be adjusted depending on the individual needs of the patient: therefore, people with a slow metabolism may need lower doses.

In individuals with rapid metabolism, the elimination Half-Life of Nebivolol enantiomers is on average 10 hours. In people with a slow metabolism, this value is 3-5 times higher. In individuals with rapid metabolism, the concentration of the RSSS enantiomer is slightly higher than that of the SRRR enantiomer. In people with a slow metabolism, this difference is greater.

In individuals with a fast metabolism, the Half-Life of hydroxymetabolites of both enantiomers is on average 24 hours, and in individuals with a slow metabolism, these values are approximately 2 times higher.

A stable plasma level in most patients with rapid metabolism is reached within 24 hours, for hydroxymetabolites – within a few days.

The plasma concentration, which is from 1 to 30 mg of Nebivolol, is proportional to the dose. Human age does not affect the pharmacokinetics of Nebivolol.

In plasma, both enantiomers are predominantly bound to albumin. Plasma protein binding for SRRR-Nebivolol is 98.1%, and for RSSS-Nebivolol – 97.9%.

A week after administration, 38% of the dose is excreted in the urine and 48% in the faeces. Excretion of unchanged Nebivolol by the kidneys is less than 0.5% of the dose.

Preclinical safety data.

Preclinical data based on generally accepted studies of genotoxicity and carcinogenicity did not reveal any danger to humans.

Clinical characteristics.


Essential arterial hypertension. Chronic heart failure of mild or moderate severity, as an adjunct to standard treatment methods for patients over 70 years of age.


- Hypersensitivity to the active substance or to other components of the drug;

- liver failure or limited liver function;

- acute heart failure, cardiogenic shock or episodes of decompensation of heart failure that require intravenous administration of active substances with a positive inotropic effect;

- sinus node weakness syndrome, including sinoauricular block, Grade II-III AV block (without artificial pacemaker);

- a history of bronchospasm and bronchial asthma;

- untreated pheochromocytoma;

- metabolic acidosis;

- bradycardia (before starting treatment, the heart rate is less than 60 beats/min);

- arterial hypotension (systolic blood pressure less than 90 mm Hg). art.);

- severe peripheral circulatory disorders.

Interactions with other drugs and other types of interactions.

Simultaneous use is not recommended:

A) with Class I antiarrhythmic drugs (quinidine, hydroquinidine, cybenzoline, flecainide, disopyramide, lidocaine, mexiletine, propafenone) – the effect on AV conduction may increase and the negative inotropic effect may increase;

B) with calcium antagonists such as verapamil/diltiazem – negative effect on AV conduction and myocardial contractility. Intravenous administration of verapamil to patients taking beta‑blockers may lead to significant hypotension and AV block;

C) with antihypertensive drugs of Central action (clonidine, guanfacine, moxonidine, methyldofa, rilmenidine) – may lead to increased heart failure due to a decrease in heart rate, stroke volume and vasodilation. With sudden withdrawal, in particular before the end of the use of beta-blockers, the probability of an increase in blood pressure (withdrawal syndrome) may increase.

Caution should be exercised when using it at the same time:

A) with Class III antiarrhythmic drugs (amiodarone) – the effect on AV conduction may increase;

B) with halogenated volatile anesthetics – may inhibit reflex tachycardia and increase the risk of hypotension. If the patient is using Nebiar®, the anesthesiologist should be informed about this;

C) with insulin and oral antidiabetic agents - although Nebiar® does not affect blood glucose levels, it can still mask hypoglycemic symptoms such as tachycardia and increased heart rate;

D) with baclofen (antispasmodic agent), amifostin (additional antitumor agent) – their simultaneous use with antihypertensive agents can lead to a significant decrease in blood pressure, so the dose of antihypertensive agents should be adjusted accordingly.

When using it simultaneously, you should consider:

a) digitalis glycosides – AV conduction slows down, but clinical studies have not given instructions on this interaction. Nebivolol does not affect the kinetics of digoxin;

B) calcium antagonists such as dihydropyridine (amlodipine, felodipine, lacidipine, nifedipine, nicardipine, nimodipine, nitrendipine) – increases the risk of hypotension, and in patients with heart failure, ventricular pumping function may worsen;

C) antipsychotics, antidepressants (tricyclic antidepressants, barbiturates, phenothiazine derivatives) - the antihypertensive effect may increase (the principle of adding effects);

d) nonsteroidal anti – inflammatory drugs-do not affect the antihypertensive effect of Nebiar;

e) sympathomimetics – can counteract the antihypertensive effect of beta-blockers. Active substances with beta-adrenergic action can lead to unhindered α-adrenergic activity of sympathomimetics with the presence of both α-and β-adrenergic effects (risk of arterial hypertension, severe bradycardia and cardiac blockade).

Interactions due to the pharmacokinetics of the drug:

– since the CYP2D6 isoenzyme is involved in the metabolism of Nebivolol, the combined use of drugs that inhibit this enzyme (paroxetine, fluoxetine, thioridazine, quinidine) increases the level of Nebivolol in blood plasma and thus increases the risk of excessive bradycardia and other adverse reactions;

- cimetidine increases the level of Nebivolol in blood plasma, but without changing the clinical efficacy. Ranitidine does not affect the pharmacokinetics of Nebivolol;

– provided that Nebiar® is used during meals and an antacid is used between meals, these drugs can be prescribed together;

- with the simultaneous use of Nebivolol and nicardipine, the concentrations of both substances in blood plasma slightly increased without changing the clinical efficacy;

- concomitant use of alcohol, furosemide or hydrochlorothiazide does not affect the pharmacokinetics of Nebivolol;

- Nebivolol does not affect the pharmacodynamics and pharmacokinetics of warfarin.

Application features.

Common to b-adrenergic blockers are the following warnings and precautions.

Maintaining beta-adrenergic blockade reduces the risk of cardiac arrhythmias during anesthesia and intubation. When preparing for surgery, the use of beta-adrenergic blockers should be discontinued at least 24 hours in advance. Caution should be exercised when using certain anesthetics that cause myocardial depression, such as cyclopropane, ether, or trichloroethylene. The appearance of vagal reactions in the patient can be prevented by intravenous administration of atropine.

As a general rule, Patients with untreated chronic heart failure should not be prescribed beta‑adrenergic blockers until their condition becomes stable. Discontinue therapy with a beta-adrenergic blocker in patients with coronary heart disease should be gradual, i.e. within 1-2 weeks. If necessary, to prevent an exacerbation of the disease, it is recommended to start treatment with a substitute drug at the same time. Beta‑adrenergic blockers can cause bradycardia. If the resting heart rate decreases to 50-55 beats per minute and/or the patient develops symptoms that indicate bradycardia, then it is recommended to reduce the dose. Beta‑adrenergic blockers should be used with caution in the treatment of: a) patients with peripheral circulatory disorders (Raynaud's disease or syndrome, intermittent claudication), since an exacerbation of these diseases may develop; B) patients with Grade I atrioventricular block due to the negative effect of beta‑adrenergic blockers on conduction; C) patients with Prinzmetal angina due to unhindered vasoconstriction of the coronary arteries mediated through a‑adrenergic receptors: beta-adrenergic blockers may increase the frequency and duration of angina attacks.

The combination of Nebivolol with calcium antagonists such as verampamil and diltiazem, with antiarrhythmic agents of Group I, as well as with antihypertensive agents of Central action is not recommended at all.

Nebiar® does not affect the blood glucose level in patients with diabetes mellitus. However, caution should be exercised when using it for the treatment of patients in this category, as Nebivolol may mask some signs of hypoglycemia, such as tachycardia and increased heart rate. B-adrenergic blockers can mask the symptoms of tachycardia in hyperthyroidism. If therapy is suddenly discontinued, these symptoms may worsen.

In patients with obstructive airway diseases, beta‑adrenergic blockers should be used with caution, as airway constriction may increase.

At the beginning of treatment of chronic heart failure with Nebivolol, regular monitoring of the patient is necessary. Treatment should not be abruptly discontinued unless absolutely necessary.

Patients with a history of psoriasis should be prescribed beta-blockers only after the situation is carefully considered. Beta-adrenergic blockers may increase sensitivity to allergens and the severity of anaphylactic reactions.

The drug contains lactose monohydrate, so it should not be taken in patients with hereditary galactose intolerance, lactase deficiency in the body, or glucose-galactose malabsorption syndrome.

Use during pregnancy or lactation.

Pregnancy. The pharmacological effects of Nebivolol can negatively affect the course of pregnancy, the fetus and the infant, so it should only be used when the benefits of using it outweigh the potential risk to the fetus. If Nebivolol treatment is necessary, uteroplacental circulation and fetal growth should be monitored. If a negative effect is confirmed, treatment with alternative medications should be considered. The baby should be carefully monitored and keep in mind that symptoms such as hypoglycemia and bradycardia can be expected within the first 3 days.

Lactation period. It is not known whether Nebivolol is excreted in human breast milk. Animal studies have shown that Nebivolol is excreted in breast milk. Most beta-blockers, especially lipophilic compounds such as Nebivolol, enter breast milk, although to varying degrees. Therefore, breast-feeding is not recommended during treatment with Nebivolol.

Dosage and administration.

Essential arterial hypertension.

Adult patients should take 1 tablet of Nebiar® (5 mg Nebivolol) per day, if possible at the same time. The drug can be taken with a meal. The hypotensive effect becomes apparent after 1-2 weeks of treatment, but sometimes the optimal effect is observed only after 4 weeks.

Combination with other antihypertensive agents. Nebiar® can be used both for monotherapy and in combination with other antihypertensive agents. By this time, an additional hypotensive effect was observed only when it was combined with 12.5–25 mg of hydrochlorothiazide.

Patients with renal insufficiency. The recommended starting dose is 2.5 mg per day. If necessary, the daily dose can be increased to 5 mg.

Patients with hepatic insufficiency. The experience of using the drug in such patients is limited, so Nebivolol is contraindicated.

Elderly patients (over 65 years of age). For this group of patients, the recommended starting dose is 2.5 mg per day, and if necessary, it can be increased to 5 mg. Due to insufficient experience in using the drug in patients over 75 years of age, its use requires caution and careful monitoring.

Chronic heart failure.

Treatment of chronic heart failure should begin with slow titration of the dose until the individual optimal maintenance dose is reached. Such patients should be prescribed the drug if there is chronic heart failure without episodes of its acute decompensation within the last 6 weeks. The doctor must have experience in treating heart failure. Patients using other cardiovascular medications (diuretics, digoxin, angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor antagonists) should already have a dose of these medications selected within the last 2 weeks before starting treatment with Nebiar. Initial titration of the dose should be carried out according to the following scheme, while maintaining intervals from 1 to 2 weeks and focusing on the patient's dose tolerance: 1.25 mg of Nebivolol per day can be increased to 5 mg per day, and then – to 10 mg 1 time per day. The maximum recommended dose is 10 mg per day. At the beginning of treatment and with each dose increase, the patient should be under the supervision of an experienced doctor for at least 2 hours to make sure that the clinical condition remains stable (especially for blood pressure, heart rate, myocardial conduction disorders, as well as increased symptoms of heart failure). The occurrence of adverse reactions may lead to the fact that not all patients can be treated with the highest recommended doses. If necessary, the already achieved dose can be gradually reduced again or returned to it again. If the symptoms of heart failure increase or if the drug is intolerant during its titration phase, it is recommended to first reduce the dose of Nebivolol or, if necessary, immediately cancel the drug (if severe hypotension occurs, if the symptoms of heart failure increase with acute pulmonary edema, if cardiogenic shock, symptomatic bradycardia or AV block occur). Treatment with Nebivolol should not be stopped suddenly, as this may lead to increased symptoms of heart failure. If discontinuation of the drug is necessary, then the dose should be gradually reduced to twice a week. As a rule, treatment of chronic heart failure with Nebivolol is long-term.

Patients with renal insufficiency. Since titration of the dose to the maximum tolerated dose occurs individually, its correction in mild to moderate renal failure is not necessary. There is no experience of using the drug in patients with severe renal insufficiency (serum creatinine ≥ 250 mmol/L), so the use of Nebivolol in such patients is not recommended.

Patients with hepatic insufficiency. In patients with hepatic insufficiency, the use of Nebivolol is contraindicated due to limited experience of use.

Elderly patients (over 65 years of age). Since titration of the dose to the maximum tolerated dose occurs individually, its correction in the elderly is not necessary.


Studies on the use of the drug in children and adolescents have not been conducted, so the drug is not recommended for this age group.

Tags: Nebivolol