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"Nebivolol": analogues, instructions for use. Method of administration and dosage in humans

Instructions for use. Contraindications and release form.

Release form

Tablets white or almost white, round, flat-cylindrical in shape, with a chamfer and a cross-shaped mark on one side.

Package

Pack of 28 pcs.

pharmachologic effect

Nebivolol is a cardioselective beta1-blocker III generation with vasodilating properties. Active substance is a racemate consisting of two enantiomers: D-nebivolol and L-nebivolol. D-nebivolol is a competitive and highly selective β1-adrenergic receptor blocker; L-nebivolol has a mild vasodilatory effect by modulating the release of vasodilating factor (NO) from the vascular endothelium.
Nebivolol reduces heart rate and blood pressure at rest and during exercise, reduces final diastolic pressure left ventricle, reduces peripheral vascular resistance, improves diastolic heart function (reduces filling pressure), increases ejection fraction; causes an antianginal effect in patients with coronary artery disease.
The hypotensive effect is also due to a decrease in the activity of the renin-angiotensin system (does not directly correlate with changes in renin activity in the blood plasma).
The antiarrhythmic effect is due to the suppression of pathological automatism of the heart (including in the pathological focus) and slowdown of AV conduction.
Sustainable hypotensive effect develops after 1-2 weeks of regular use of the drug, and in some cases - after 4 weeks, a stable effect is observed after 1-2 months.

Indications

Arterial hypertension.
IHD: prevention of angina attacks.
Chronic heart failure (as part of combination therapy).

Contraindications

Acute heart failure; chronic heart failure in the stage of decompensation (requiring intravenous administration of drugs with a positive inotropic effect); severe arterial hypotension (systolic blood pressure less than 90 mm Hg); SSSU, including sinoatrial block; AV block II and III degree(without artificial pacemaker); bradycardia (heart rate less than 60 beats/min); cardiogenic shock; pheochromocytoma (without simultaneous use of alpha-blockers); metabolic acidosis; severe liver dysfunction; bronchospasm and bronchial asthma in the anamnesis; heavy obliterating diseases peripheral vessels (intermittent claudication, Raynaud's syndrome); myasthenia gravis; depression; children and adolescents up to 18 years of age; increased sensitivity to nebivolol.

Use during pregnancy and breastfeeding

Use during pregnancy is only possible if strict indications(due to possible development in newborns, bradycardia, arterial hypotension, hypoglycemia and respiratory paralysis). Nebivolol should be stopped 48-72 hours before delivery. In cases where this is not possible, newborns should be closely monitored for 48-72 hours after birth.

special instructions

Nebivolol should be used with caution in patients with renal failure, diabetes mellitus, hyperfunction thyroid gland, allergic diseases history of psoriasis, COPD, 1st degree AV block, Prinzmetal's angina, as well as in patients over 75 years of age.
The withdrawal of beta-blockers should be carried out gradually over 10 days (up to 2 weeks in patients with coronary artery disease).
At the beginning of treatment, blood pressure and heart rate should be monitored daily.
The effectiveness of beta-blockers in smokers is lower than in non-smokers.
Nebivolol has no effect on glucose levels in patients with diabetes, however, under the influence of nebivolol, certain signs of hypoglycemia (tachycardia, rapid heartbeat) caused by the use of hypoglycemic drugs may be masked.
If it is necessary to use nebivolol in patients with psoriasis, the expected benefit of therapy should be carefully assessed and possible risk exacerbation of psoriasis.
Beta blockers should be used with caution when increased function thyroid gland due to the fact that under the influence of beta-blockers, tachycardia can be leveled.
Nebivolol may increase symptoms of peripheral circulatory disorders.
Patients wearing contact lenses, should take into account that the use of beta-blockers may reduce the production of tear fluid.
When conducting surgical interventions The anesthesiologist should be warned that the patient is taking beta-blockers.
Monitoring of glucose levels in blood plasma should be carried out once every 4-5 months (in patients with diabetes mellitus).
Laboratory tests of renal function should be monitored once every 4-5 months (in elderly patients).
Use in children is not recommended.

Compound

Excipients: lactose monohydrate - 139.91 g, corn starch - 46 mg, microcrystalline cellulose - 16.1 mg, croscarmellose sodium - 13.8 mg, hyprolose (hydroxypropylcellulose) - 4.6 mg, polysorbate 80 - 2.3 mg, magnesium stearate - 1.15 mg, colloidal silicon dioxide - 0.69 mg.

Directions for use and doses

Adults for oral administration - 2.5-5 mg/day in the morning. The optimal effect develops after 1-2 weeks of treatment, and in some cases - after 4 weeks. If necessary, the daily dose is increased to 10 mg/day.
For patients over 65 years of age, the initial dose is 2.5 mg/day. If necessary, the daily dose can be increased to 5 mg.

Side effects

The frequency of adverse reactions listed below was determined according to the following (classification World Organization healthcare): very often - at least 10%; often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including individual messages.
From the outside of cardio-vascular system(CVS): infrequently - bradycardia, worsening of CHF, slowing of atrioventricular conduction, atrioventricular block, marked decrease in blood pressure, orthostatic hypotension, cardiac arrhythmias, cardialgia, progression of concomitant intermittent claudication, peripheral edema.
From the outside nervous system: often - increased fatigue, headache, dizziness, paresthesia; infrequently - “nightmare dreams”, decreased ability to concentrate, drowsiness, insomnia, depression; very rarely - hallucinations, fainting.
From the senses: infrequently - blurred vision.
From the outside respiratory system: often - shortness of breath; infrequently - bronchospasm, rhinitis.
From the outside digestive system: often - dryness of the oral mucosa, constipation, nausea, diarrhea; infrequently - vomiting, flatulence.
From the outside skin: very rarely - exacerbation of psoriasis, photodermatosis, hyperhidrosis.
Allergic reactions: uncommon - itchy skin, erythematous rash; very rarely - angioedema.
From the outside reproductive system: infrequently - impotence.

Drug interactions

At simultaneous use With antiarrhythmic drugs Class I, amiodarone may enhance the negative inotropic effect and inhibit AV conduction.
When used simultaneously with blockers calcium channels(verapamil and diltiazem) the negative inotropic effect and inhibition of AV conduction are enhanced.
With intravenous administration of verapamil while taking nebivolol, there is a risk of cardiac arrest (simultaneous use is contraindicated).
When used concomitantly with nebivolol antihypertensive drugs, nitroglycerin or slow calcium channel blockers, severe arterial hypotension may develop (special caution is required when combined with prazosin).
When used simultaneously with sympathomimetics, it is suppressed pharmacological activity nebivolol.
When used simultaneously with anesthesia, it is possible to suppress reflex tachycardia and increase the risk of developing arterial hypotension.
When used simultaneously with tricyclic antidepressants, barbiturates, phenothiazine derivatives, the antihypertensive effect of nebivolol may be enhanced.
When used simultaneously with cimetidine, it is possible to increase the concentration of nebivolol in the blood plasma.
With simultaneous use of nebivolol with drugs that inhibit serotonin reuptake, or other drugs that are biotransformed with the participation of the CYP2D6 isoenzyme, the concentration of nebivolol in the blood plasma increases, the metabolism of nebivolol slows down, which may increase the risk of developing bradycardia.
When nebivolol is used concomitantly with insulin and oral hypoglycemic agents, the symptoms of hypoglycemia (tachycardia) may be masked.

Overdose

There are no data on cases of overdose with nebivolol.
Symptoms: bradycardia, marked decrease in blood pressure, severe bradycardia, AV block, cardiogenic shock, cardiac arrest, loss of consciousness, coma, nausea, vomiting, cyanosis, bronchospasm, acute heart failure.
Treatment: the patient is hospitalized and placed in a ward intensive care. It is immediately necessary to determine the concentration of glucose in the blood. Perform gastric lavage, take activated carbon, maintaining the function of the cardiovascular system, monitoring heart and lung performance, monitoring circulating blood volume and diuresis.
If necessary, a complex is carried out resuscitation measures.
The effect of beta blockers can be counteracted by slow intravenous (IV) administration of isoprenaline at an initial dose of about 5 mcg/min or dobutamine at an initial dose of approximately 2.5 mcg/min. In case of severe bradycardia, 0.5-2 mg of atropine is administered intravenously; in the absence of positive effect placement of a transvenous pacemaker is possible. In case of heart failure, treatment begins with the administration of cardiac glycosides and diuretics; if there is no effect, it is advisable to administer dopamine, dobutamine or vasodilators. For bronchospasm, β2-acrenergic receptor stimulators are used intravenously. For ventricular estracystole - lidocaine (cannot be administered antiarrhythmic drugs IA class).

The basis of this medicine is nebivolol hydrochloride. Each tablet contains 5 mg of this substance.

The drug is available in packages of 14, 20, 28, 30, 42, 56 or 60 tablets. Depending on the quantity, they are placed in contour cells or jars.

pharmachologic effect

The active substance of the drug "Nebivolol" is a third-generation cardioselective beta1-blocker with vasodilating properties. The active element of the drug, which is a racemate, includes two enantiomers - D-nebivolol (a competitive and highly selective β1-adrenergic receptor blocker) and L-nebivolol, the mild vasodilatory effect of which is due to the modulation of the release of vasodilating factor (NO) from the vascular endothelium.

The therapeutic effect of Nebivolol is to lower heart rate and blood pressure (both at rest and during exercise), reduce left ventricular end-diastolic pressure, reduce the level of total peripheral vascular resistance (TPVR) and improve diastolic function of the heart, as well as increasing ejection fraction.

When prescribing the drug to patients with coronary heart disease, an antianginal effect is observed.

The hypotensive effect of Nebivolol is due to the ability to reduce the activity of the renin-angiotensin system.

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

In standard cases, a stable hypotensive effect is formed within one or two weeks from the start of regular use of Nebivolol, but sometimes this process takes longer.

Pharmacokinetics

After oral administration, Nebivolol is quickly absorbed from gastrointestinal tract, regardless of food intake. The level of bioavailability of the drug ranges from 12% to almost 100% (determined by the rate of metabolic processes).

The drug leaves the body through the kidneys (38%) and intestines (48%).

Indications

The drug "Nebivolol" is used:

in the treatment of arterial hypertension;
for coronary heart disease (in order to prevent attacks of angina pectoris);
as part of complex therapy- for chronic heart failure.

Dosage and duration of treatment

Typically, adult patients are prescribed Nebivolol in daily dose 2.5-5 mg. If necessary, the dosage can be increased by 10 mg per day.

For patients over 65 years of age, it is recommended to prescribe 2.5 mg/day as an initial dose. Taking into account individual reaction The dosage of the drug can subsequently be increased to 5 mg.

Side effect

When using Nebivolol, the patient may experience such unwanted manifestations, How:

from the central nervous system and peripheral nervous system: headache, dizziness, sleep disturbances, nightmares, drowsiness, anxiety and fatigue, depression, paresthesia, inability to concentrate, etc.; extremely rarely - hallucinations, fainting;
from the digestive system: feeling of dry mouth, nausea, vomiting, flatulence, stool disorders;
from the cardiovascular system: bradycardia, cardialgia, acute heart failure, swelling, the formation of Raynaud's syndrome;
on the part of the skin and subcutaneous tissues: skin itching, erythematous rash; extremely rarely - aggravation of psoriasis.

In addition, it is not excluded allergic reactions, in some cases - angioedema.

Contraindications

The drug "Nebivolol" is not used for:

acute heart failure;
chronic heart failure in the stage of decompensation, when intravenous administration of drugs that have a positive inotropic effect is necessary;
severe arterial hypotension (with systolic blood pressure less than 90 mmHg);
weakness syndrome sinus node(SSSU), including sinoatrial block;
AV blockade II and III degrees, without artificial pacemaker);
bradycardia, in which the heart rate is less than 60 beats per minute);
cardiogenic shock;
pheochromocytoma (without simultaneous use of alpha-blockers);
metabolic acidosis;
severe liver dysfunction;
bronchospasm and bronchial asthma;
severe occlusive peripheral vascular disease, including intermittent claudication and Raynaud's syndrome);
myasthenia gravis;
depression.

Contraindications to the use of Nebivolol include age under 18 years and hypersensitivity to the substances that make up the drug.

special instructions

The use of the drug "Nebivolol" during pregnancy is recommended only under strict indications, as it can lead to the development of arterial hypertension, bradycardia, hypoglycemia and respiratory paralysis in newborns. The medication should be completely stopped 48-72 hours before delivery. In cases where this is not possible, newborns require strict medical supervision in the first few days.

Nebivolol is used with caution to treat patients who have previously been diagnosed with:

renal failure;
diabetes;
hyperfunction of the thyroid gland;
allergic diseases;
psoriasis;
chronic obstructive pulmonary disease (COPD);
AV block of the first degree;
Prinzmetal's angina.

Special observation is necessary when prescribing Nebivolol to patients over 75 years of age.

In the first days of using the drug, daily monitoring of blood pressure and heart rate is necessary.

When treating, it is necessary to take into account that in smoking patients the level of effectiveness of beta-blockers is lower than in non-smokers.

The drug "Nebivolol" does not have a noticeable effect on the speed of psychomotor reactions and the ability to concentrate. However, while taking the drug, dizziness and increased drowsiness, fatigue and feeling tired. Taking this into account, patients are advised to refrain from driving and other potentially dangerous activities during the period of treatment.

Interaction with other drugs

The negative inotropic effect and inhibition of AV conduction may be enhanced by the simultaneous administration of Nebivolol and class I antiarrhythmic drugs, amiodarone, as well as calcium channel blockers (verapamil, diltiazem).

Nebivolol is not prescribed simultaneously with intravenous administration verapamil, since drugs in combination can cause cardiac arrest.

When prescribing Nebivolol, it is necessary to take into account that under the influence of the drug, more intense manifestations impaired peripheral circulation.

Patients who use contact lenses should remember that the volume of tear fluid produced may be reduced due to the use of beta-blockers.

Before performing surgical interventions, anesthesiologists must be warned that the patient is receiving treatment with beta-blockers.

Patients with diabetes need to monitor plasma glucose every 4-5 months.

Elderly patients need to monitor laboratory parameters of renal function every 4-5 months.

Analogues

Among the drugs similar to Nebivolol in pharmacological composition and therapeutic effects, we can highlight “Bivotens”, “Binelol”, “Nebivator”, “Nebilan Lannacher”, “Nebilet”, “Nebilong” and other drugs in which the active substance is nebivolol.

In Russian pharmacies, in addition to domestically produced Nebivolol, you can find similar drugs, released foreign companies, in particular, Nebivolol Sandoz (Slovenia) and Nebivolol-teva (Israel).

pharmachologic effect

Cardioselective beta 1-blocker of the third generation with vasodilating properties. The active substance is a racemate consisting of two enantiomers: D-nebivolol and L-nebivolol. D-nebivolol is a competitive and highly selective β 1 -adrenergic receptor blocker; L-nebivolol has a mild vasodilatory effect by modulating the release of vasodilating factor (NO) from the vascular endothelium.

Nebivolol reduces heart rate and blood pressure at rest and during exercise, reduces left ventricular end-diastolic pressure, reduces peripheral vascular resistance, improves diastolic heart function (reduces filling pressure), increases ejection fraction; causes an antianginal effect in patients with coronary artery disease.

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

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

A stable hypotensive effect develops after 1-2 weeks of regular use of the drug, and in some cases - after 4 weeks; a stable effect is observed after 1-2 months.

Pharmacokinetics

After oral administration, nebivolol is rapidly absorbed from the gastrointestinal tract. Eating does not affect absorption. Bioavailability averages 12% in rapid metabolizers (hepatic first-pass effect) and is almost complete in slow metabolizers.

In blood plasma, both enantiomers bind preferentially to albumin. Plasma protein binding of D-nebivolol is 98.1%, L-nebivolol - 97.9%.

Metabolized by acyclic and aromatic hydroxylation and partial N-dealkylation. The resulting hydroxy and amino derivatives are conjugated with glucuronic acid and are excreted in the form of O- and N-glucuronides.

Excreted by the kidneys (38%) and through the intestines (48%).

In persons with rapid metabolism T1/2 of hydroxymetabolites - 24 hours, enantiomers of nebivolol - 10 hours; in persons with slow metabolism: hydroxymetabolites - 48 hours, enantiomers of nebivolol - 30-50 hours.

Excretion of unchanged nebivolol in urine is less than 0.5%.

Indications

Arterial hypertension.

IHD: prevention of angina attacks.

Chronic heart failure (as part of combination therapy).

Dosage regimen

For patients over 65 years of age, the initial dose is 2.5 mg/day. If necessary, the daily dose can be increased to 5 mg.

Side effect

From the central nervous system and peripheral nervous system: headache, dizziness, feeling of fatigue, paresthesia, depression, decreased ability to concentrate, drowsiness, insomnia, nightmares; very rarely - fainting, hallucinations.

From the digestive system: nausea, constipation, diarrhea, dry mouth, flatulence, vomiting.

From the cardiovascular system: bradycardia, orthostatic hypotension, shortness of breath, edema, acute heart failure, AV block, Raynaud's syndrome, cardialgia.

For the skin and subcutaneous tissues:skin rash erythematous, itching; very rarely - aggravation of psoriasis.

Allergic reactions: in some cases - angioedema.

Others: bronchospasm, dry eyes.

Contraindications for use

Acute heart failure; chronic heart failure in the stage of decompensation (requiring intravenous administration of drugs with a positive inotropic effect); severe arterial hypotension (systolic blood pressure less than 90 mm Hg); SSSU, including sinoatrial block; AV block II and III degrees (without artificial pacemaker); bradycardia (heart rate less than 60 beats/min); cardiogenic shock; pheochromocytoma (without simultaneous use of alpha-blockers); metabolic acidosis; severe liver dysfunction; history of bronchospasm and bronchial asthma; severe obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); myasthenia gravis; depression; children and adolescents up to 18 years of age; hypersensitivity to nebivolol.

Use during pregnancy and breastfeeding

Use during pregnancy is possible only under strict indications (due to the possible development of bradycardia, arterial hypotension, hypoglycemia and respiratory paralysis in newborns). Nebivolol should be stopped 48-72 hours before delivery. In cases where this is not possible, newborns should be closely monitored for 48-72 hours after birth.

Use in children

Contraindicated in children and adolescence up to 18 years old.

Drug interactions

When used simultaneously with class I antiarrhythmic drugs, amiodarone, the negative inotropic effect and inhibition of AV conduction may be enhanced.

When used simultaneously with calcium channel blockers (verapamil and diltiazem), the negative inotropic effect and inhibition of AV conduction are enhanced.

With intravenous administration of verapamil while taking nebivolol, there is a risk of cardiac arrest (simultaneous use is contraindicated).

When nebivolol is used simultaneously with antihypertensive drugs, nitroglycerin or slow calcium channel blockers, severe arterial hypotension may develop (special caution is required when combined with prazosin).

When used simultaneously with sympathomimetics, the pharmacological activity of nebivolol is suppressed.

When used simultaneously with anesthesia, it is possible to suppress reflex tachycardia and increase the risk of developing arterial hypotension.

When used simultaneously with tricyclic antidepressants, barbiturates, phenothiazine derivatives, the antihypertensive effect of nebivolol may be enhanced.

When used simultaneously with cimetidine, it is possible to increase the concentration of nebivolol in the blood plasma.

With simultaneous use of nebivolol with drugs that inhibit serotonin reuptake, or other drugs that are biotransformed with the participation of the CYP2D6 isoenzyme, the concentration of nebivolol in the blood plasma increases, the metabolism of nebivolol slows down, which may increase the risk of developing bradycardia.

When nebivolol is used concomitantly with insulin and oral hypoglycemic agents, the symptoms of hypoglycemia (tachycardia) may be masked.

Use for liver dysfunction

Contraindicated in severe violations liver functions.

Use for renal impairment

Use with caution in patients with renal failure.

Use in elderly patients

Use with caution in patients over 65 years of age. Laboratory tests of renal function in elderly patients should be monitored once every 4-5 months.

special instructions

Nebivolol should be used with caution in patients with renal failure, diabetes mellitus, hyperthyroidism, a history of allergic diseases, psoriasis, COPD, first degree AV block, Prinzmetal's angina, as well as in patients over 75 years of age.

The withdrawal of beta-blockers should be carried out gradually over 10 days (up to 2 weeks in patients with coronary artery disease).

At the beginning of treatment, blood pressure and heart rate should be monitored daily.

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

Nebivolol has no effect on glucose levels in patients with diabetes, however, under the influence of nebivolol, certain signs of hypoglycemia (tachycardia, rapid heartbeat) caused by the use of hypoglycemic drugs may be masked.

If it is necessary to use nebivolol in patients with psoriasis, the expected benefits of therapy and the possible risk of exacerbation of psoriasis should be carefully assessed.

Beta-blockers should be used with caution in case of increased thyroid function due to the fact that under the influence of beta-blockers, tachycardia can be leveled.

Nebivolol may increase symptoms of peripheral circulatory disorders.

Patients wearing 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.

Laboratory tests of renal function should be monitored once every 4-5 months (in elderly patients).

Impact on the ability to drive vehicles and operate machinery

Nebivolol does not affect the speed of psychomotor reactions. Dizziness and a feeling of fatigue are sometimes possible while taking nebivolol, so patients taking nebivolol should avoid potential activities dangerous species activities.

Drugs from the group of adrenergic blockers received wide use in the treatment of many cardiac diseases. Among the drugs in this group, Nebivolol stands out significantly. Analogues of this medicine have also gained great popularity due to their effectiveness. What kind of medicine is this, how does it work and in what cases can it be used?

What kind of drug is this?

"Nebivolol" belongs to the group of beta-blockers. The main effect of this drug is antihypertensive (the drug lowers blood pressure). The effect is observed due to the selective blocking of beta receptors located in the vessels (affects beta-1 adrenergic receptors).

Nebivolol Sandoz is currently used.

This drug is a combination drug, consisting of several isomers (D- and L-rotating). This combination of substances has a beneficial effect on the development of the clinical effect. One of the isomers is responsible for the development of antihypertensive effects, while the second has a greater effect on heart rate.

The drug appeared relatively recently, in the middle of the last century. Since then it has become widespread in the cardiology community. Nebivolol Sandoz is the drug of choice in the treatment of arterial hypertension, as well as some heart rhythm disorders.

How does the drug work and which organs are responsible for its absorption?

Pharmacokinetics

Nebivolol Sandoz is best absorbed. The drug is well absorbed from the gastrointestinal tract. Can be taken with food (absorption is not impaired). Bioavailability is relatively low - about 12 percent. If possible, you should avoid taking the medicine together with alcohol, as it may develop side effects.

Once in the blood plasma, the drug binds to albumin and forms insoluble complexes. In this bound form, the availability of the drug is about 98 percent, i.e., almost all of Nebivolol Sandoz is absorbed. Its analogues go through the same path before they enter the blood plasma and bind to protein.

The unabsorbed drug is excreted through the gastrointestinal tract and kidneys. It is processed in the liver, where it binds to glucuronic acid.

The half-life of the drug in individuals with an accelerated metabolite is about a day. In case of slow metabolism, Nebivolol can accumulate and remain in the blood plasma for about 48 hours.

The drug does not accumulate in tissues, which makes it possible to avoid its overdose (this is only possible if it is used in patients with kidney or liver pathologies).

Indications for use

In what cases is Nebivolol, analogues prescribed? this tool or drugs with similar pharmacological effects?

The first indication for prescribing the drug is the use of beta blockers is resorted to when use is ineffective ACE inhibitors(“Enalapril”, “Captopril”). In addition, Nebivolol is also used for endocrine hypertension.

To others, no less important indication to the use of "Nebivolol", is coronary heart disease. For frequent exacerbations of exertional angina, as well as for the prevention of such attacks, Nebivolol is indicated. In this case, its analogues may be even more effective than the pure drug itself.

Nebivolol is also included in combination therapy for the treatment of chronic heart failure. In this case, the drug helps improve heart function, reduce pre- and afterload on the chambers of the organ, as well as reduce pressure.

This medicine can also be used to prevent the development of hypertensive crises, as well as in persons prone to atherosclerotic lesions of cerebral vessels.

Contraindications

When should you not use Nebivolol? Instructions for use usually include all those cases that were identified clinically, when the development of certain complications was observed during the use of the product. Due to the strong antihypertensive effect, the drug should not be prescribed for severe

First of all, it is prohibited to use the drug in acute heart failure. This is due to the fact that he has inotropic effect, which can adversely affect the body due to insufficient heart function.

If pheochromocytoma develops, it is also prohibited to use Nebivolol. Instructions for use indicate that for this endocrine tumor The drug can only be used in conjunction with

The drug should not be prescribed to children, as well as to persons with existing mental health disorders.

"Nebivolol" is contraindicated in persons with individual intolerance medicines. When the first signs appear (tearing, difficulty breathing), you should immediately stop using the drug and switch to a safer option.

Side effects

Like any medicine, Nebivolol has its side effects. The main ones are:

From the nervous system - headache, depression, drowsiness, insomnia, hallucinations, fainting, dizziness.

Side effects from the digestive system are nausea, constipation, dry mouth, vomiting. Dyspeptic disorders may appear, and joint reception with antibiotics - dysbacteriosis.

The cardiovascular system reacts to the administration of Nebivolol with bradycardia, shortness of breath, edema, the development of acute heart failure, atrioventricular block, and Raynaud's syndrome. Overdose can lead to uncontrolled arterial hypotension, which can be complicated by collapse and fainting. In severe cases, shock develops.

Side effects of Nebivolol can manifest themselves in the form of an erythematous rash and psoriasis.

In severe cases, angioedema develops. In milder cases, uncontrollable sneezing or coughing develops.

Features of using the drug

The drug is used with caution in patients with renal failure, diabetes mellitus or overproduction of thyroid hormones. The drug is withdrawn gradually over 10-14 days. At the beginning of the course of treatment, blood pressure and heart rate should be monitored. If possible, you should stop smoking while using the drug. Before the upcoming operation, you should definitely warn the anesthesiologist that the patient is using beta-blockers.

During the entire period of use of the drug, it is necessary to monitor blood sugar levels, especially in diabetics. In addition, renal filtration capacity (especially creatinine and urea levels) should be assessed if long time Nebivolol is prescribed. Instructions for use (analogues have a similar effect) warn that the development of renal failure is possible if this drug is irrationally prescribed.

It is prohibited to use the drug in children under 18 years of age, as well as in elderly patients with decompensated heart failure. This ban is primarily due to the possibility of developing metabolic disorders and the appearance of problems with blood pressure.

Since dizziness may develop when using the drug, it should not be prescribed to drivers and doctors.

Use of the drug by pregnant women

Purpose of this medicine for a pregnant woman is possible only after consultation with a gynecologist and therapist. The drug is used quite rarely due to negative influence on the body of mother and child.

The drug is prescribed only in case of emergency, as bradycardia, arterial hypotension, hypoglycemia, paralysis may develop respiratory center, seizures.

Three days before the expected birth, you must stop using this medication. If this is not possible, early postpartum period Careful monitoring of the health status of mother and child is necessary. Required when using spinal anesthesia, warn the anesthesiologist about the ongoing treatment with adrenergic blockers.

It should be remembered that while using the drug, fetal hypoxia may develop. The teratogenic effect of the drug has not been proven, but there are known cases of such an effect on the fetus.

If, nevertheless, a pregnant woman is prescribed Nebivolol, the instructions for use warn that distortion is possible therapeutic action the drug when prescribed with intravenous administration of magnesia.

Interaction with drugs of other medicinal groups

The combined use of Nebivolol and class 1 antiarrhythmics can lead to an increased negative inotropic effect. AV block may develop. A similar effect is observed if calcium channel blockers and Nebivolol Sandoz are used simultaneously.

The prescribing instructions for the drug warn that when it is administered intravenously, cardiac arrest is possible (provided that the drug is administered together with Verapamil). In this case, emergency cardioversion using electrical impulse therapy will be required.

There is a significant risk of developing severe arterial hypotension when prescribing the drug with Nitroglycerin.

The simultaneous administration of sympathomimetics and Nebivolol helps to inhibit the effect of the latter.

Concomitant use with anesthetic drugs may lead to sharp fall blood pressure, which will serve as an indication for mechanical ventilation and the use of hypertensive drugs.

When prescribing the drug with insulin, it is possible to develop an overdose of the hormone and conceal the clinical signs of hypoglycemia.

Dosage of the drug

So in what doses should the drug be used in order for the necessary clinical effect? If Nebivolol Sandoz is used, the instructions for use suggest next view dosing.

The most optimal dose for an adult is 20 milligrams per day. The drug is taken orally in the morning on an empty stomach. Maximum effect from the dose used, it develops within one to two weeks from the start of treatment. If necessary, the daily amount of the drug can be increased to 10 milligrams. For elderly patients, the maximum daily dose is 5 milligrams, and the optimal dose for treatment is 2.5 milligrams per day. For pregnant women, the amount of the drug is selected according to clinical signs and body weight. It is best to use Nebivolol Sandoz (5 mg) in tablets.

If you have kidney problems, it is better to stop using Nebivolol or prescribe it in minimal dosages.

With the simultaneous administration of sympathomimetics and Nebivolol, the effect may be potentiated, due to which the prescribed dose of the drug can be slightly reduced.

Prescribing the drug in smaller doses has no effect on the body. It is possible to develop receptor tolerance to the drug with long-term administration of small doses of the drug.

Analogues of the drug

It is not always possible to find it in pharmacies necessary drug, so we have to resort to using analogues. Thanks to the expansion of the medicine market, find similar drugs is not difficult. What medications can replace Nebivolol?

Analogues (synonyms) of this drug are as follows:

"Binelol";
"Nebivator";
"Nebivolol canon";
"Nebivolol stada";
"Nebivolol teva;
"Nebikar";
"Nebilet";
"Nebilong";
"Od-heaven."

Each of these drugs has its own positive and negative traits. Some of them are enhanced better than the classic Nebivolol. The instructions for use of each of them, however, also warn about more negative effects. Therefore, only a qualified and competent doctor can help you decide which drug is better.

You should not use these remedies yourself without first consulting a doctor, as this can only significantly worsen your condition and harm both your health and the health of your friends and loved ones.

Name of the drug - Nebivolol
Latin name Nebivololum ( Genitive- Nebivololi)
Chemical name drug: alpha, alpha"-[Iminobis(methylene)bis-2H-1-benzopyran-2-methanol
Racemic form, which consists of L- and D-enantiomers
Gross formula of nebivolol: C22H25F2NO4
Pharmacological group: Beta blockers
Object of application: humans, cats and dogs
Application: therapy of arterial hypertension, coronary heart disease, chronic heart failure, arrhythmia
Where to buy: medical pharmacies
Synonyms (analogues, generics): Binelol, Bivotenz, Nebivolol, Nebivator, Nebivolol Shtada, Nebivolol Sandoz, NEBIVOLOL-NANOLEK, OD-Neb, Nebivolol hydrochloride, Nebivolol-Teva, Nebilet, Nebilan Lannacher, Nebilong
Release form: 5 mg tablets

Physico-chemical characteristics

Nebivolol hydrochloride is an off-white or off-white powder. Soluble in dimethyl sulfoxide, methanol, and dimethylformamide; poorly soluble in propylene glycol, ethanol and polyethylene glycol; practically insoluble in dichloromethane, hexane and methylbenzene.

Pharmacological characteristics of the drug "Nebivolol"

Pharmacological effects of the drug:

antianginal
hypotensive
antiarrhythmic

Nebivolol specifically blocks β1-adrenergic receptors, and also stimulates the production of endothelial relaxing factor (NO). A decrease in blood pressure occurs due to a decrease in cardiac output, circulating blood volume, relative peripheral vascular resistance, inhibition of renin synthesis, decreased sensitivity of vascular baroreceptors. Expressed hypotensive effect is formed within 7-14 days from the start of use, its stabilization occurs within a month from the start of use. Nebivolol reduces heart rate both during exercise and at rest, diastolic arterial pressure in the cavity of the left ventricle, improves filling of the left ventricle in diastole, significantly reduces myocardial oxygen demand, antianginal effect, with long-term use significantly reduces the mass of the left ventricular myocardium and the mass index of the left ventricular myocardium. The drug has positive influence on circadian rhythm arterial blood pressure in patients with both disturbed rhythm and normal rhythm. The drug does not have any effect when used for a long time negative impact on lipid metabolism.

When conducting experimental preclinical studies on mice, it was established that nebivolol at a dose of 40 mg/kg significantly increases the risk of developing benign testicular neoplasia caused by the proliferation of interstitial cells of the testis.

When administered orally, nebivolol is quickly absorbed from the gastrointestinal tract. The bioavailability of the drug is 12% with a “fast” type of metabolism (the “first pass” phenomenon through the liver). With a “slow” type of metabolism, the bioavailability of the drug is almost complete. The binding of the drug to plasma proteins is 98%. The equilibrium concentration in the blood serum in individuals with a “fast” type of metabolism develops within 24 hours, the half-life is approximately 10 hours. In individuals with a “slow” type of metabolism, these indicators are 3–5 times higher. Metabolized in the liver mainly by aromatic and alicyclic hydroxylation, partly by N-dealkylation. The resulting amino and hydroxy derivatives combine with glucuronic acid and are excreted by the kidneys in the form of glucuronides. The half-life of hydroxymetabolites for persons with a “fast” metabolism lasts approximately within a day, with a “slow” one - on average 2-2.5 times longer. Nebivolol in humans, dogs and cats is excreted by the intestines by 60% and by the kidneys by 40%. The drug penetrates well through the blood-brain barrier and into breast milk.

The effect of nebivolol on reproductive function. In a 24-month preclinical study of the drug in mice (using the drug at a dose of 40 mg/kg per day (5 times higher than the maximum therapeutic dose) a significant increase in the risk of testicular tissue hyperplasia and the development of testicular adenoma was established.

Use of the drug

Nebivolol is used for the following pathologies :

Arterial hypertension, both in monotherapy and in combination with others antihypertensive drugs)
Angina pectoris
Ischemic disease hearts
Tachycardia
Chronic heart failure

Method of administration and dosage in humans

In humane medicine, nebivolol is prescribed orally, at the same time of day. Do not chew the drug and wash it down with a sufficient amount of water. Use the drug during or after meals - 5 mg 1 time per 24 hours. Persons with chronic renal failure, as well as patients over 65 years of age - 2.5 mg per day. The maximum daily dose of the drug is 10 mg.

Directions for use and dosage in dogs and cats

Evidence base There is no evidence of the effectiveness of nebivolol for chronic heart failure in dogs and cats. There are separate clinical studies that show good tolerability of nebivolol in dogs with chronic heart failure caused by dilated cardiomyopathy or endocardiosis of the atrioventricular heart valves, as well as in cats with arterial hypertension and hypertrophic cardiomyopathy.

In veterinary medicine nebivolol is given orally to dogs and cats, at the same time of day, simultaneously with food at a daily target dose of 0.1-0.2 mg/kg. It is advisable to titrate from 1/4 of the target dose every 7 days, increasing the dose by 2 times to the target dose. In case of chronic renal failure, the dose is reduced by 2-4 times.

Precautionary measures

Treatment with nebivolol should be discontinued gradually over 14 days. The development of bradycardia requires a dose reduction. Against the background of diabetes mellitus, the drug can mask the symptoms of hypoglycemia, and in case of thyroid pathologies - tachycardia. Nebivolol may increase allergic reactions to pollen and other substances. Before surgical intervention When using anesthesia, the drug should be discontinued one day before, and an anesthetic agent with minimal negative inotropic effect should be selected. At joint use antacids, the specified beta blocker is used during meals, and antacids - in the intervals between meals. Use nebivolol with caution when working with severe, dangerous mechanisms, while driving Vehicle, as well as specialists whose profession is based on increasing concentration and attention. It is not recommended to drink alcohol while taking nebivolol.

Contraindications

Contraindications to the use of nebivolol are:

sinus bradycardia
hypersensitivity and allergic reactions
cardiogenic shock
arterial hypotension
atrioventricular block II–III degree
sick sinus syndrome
circulatory disorders in peripheral vessels
forms of heart failure refractory to treatment
liver dysfunction
sinoatrial block
bronchospasm
bronchial asthma
childhood
lactation
pregnancy
Special instructions for use

According to the instructions for the use of nebivolol in humans, special caution is required in following situations:

diabetes
history of bradycardia
hyperthyroidism
psoriasis
history of allergies
elderly age

Features of the use of the drug during breastfeeding and pregnancy

During pregnancy, the use of nebivolol is possible only under strict indications. The benefit/risk ratio of side effects and complications should be assessed. When taking the drug, breastfeeding should be avoided.

Experimental preclinical studies on rats have proven that nebivolol and its metabolites penetrate well through the hematoplacental barrier. When nebivolol was administered to female rats in doses of 1.25 - 2.5 mg/kg per day in the last trimester of pregnancy, during childbirth and the lactation period, a significant decrease in body weight was observed in newborn rat pups. When daily doses of 5 mg/kg and higher were used in rats, post-term pregnancy, birth pathologies, and a decrease in the reflex of caring for the offspring were detected. In another study, rats were treated with nebivolol in the first trimester of pregnancy in daily doses of 20-40 mg/kg; the development of malnutrition, persistent disturbance of ossification of the ribs and sternum, and increased bone resorption were established in the pups. When nebivolol was administered to pregnant rabbits at a daily dose of 20 mg/kg, no negative side effects were detected in the offspring.

Experimental preclinical studies in rats showed that nebivolol and its metabolites are well excreted from breast milk. However, it is still unknown whether it is excreted this drug and its metabolites in human breast milk.

Side effects when using nebivolol

In humans, dogs, and cats in rare cases It is possible to develop side effects when using this beta blocker:

From the gastrointestinal tract:

vomit
nausea
diarrhea
flatulence
constipation

From the outside hematopoietic organs, hemostasis and cardiovascular system:

hypotension
atrioventricular block
heart failure
symptomatic bradycardia

From the nervous system and sense organs:

dizziness
headache
paresthesia
fatigue (weakness)
nightmares
depression
transient disturbance vision

Others adverse reactions:

skin rash
bronchospasm

Effect of oral administration of nebivolol on laboratory blood parameters

IN laboratory research In people with arterial hypertension taking nebivolol, a number of deviations in serum laboratory parameters relative to the norm have been established. A correlation has been established between the use of nebivolol and an increase in serum triglyceride concentrations, uric acid. In the blood serum of sick people using this drug, the concentration of cholesterol and lipoproteins significantly decreased high density, and in peripheral blood- platelet count decreased.

Drug interactions

Calcium channel blockers (verapamil, diltiazem, amlodipine) potentiate the likelihood of developing atrioventricular block; class I antiarrhythmic drugs, as well as amiodarone, significantly lengthen the time of conduction of a cardiac impulse through the atria. Anesthesia - diethyl ether, trichloroethylene, cyclopropane, as well as barbiturates, tricyclic antidepressants, phenothiazine derivatives increase arterial hypotension. Nicardipine and cimetidine increase the plasma concentration of nebivolol, sympathomimetics eliminate pharmacological effects drug.

Nebivolol overdose

In humans, dogs and cats, the following symptoms develop when overdosing on the drug:

arterial hypotension
bradycardia
acute heart failure
bronchospasm

Tactics for providing assistance in case of overdose and poisoning with nebivolol:

gastric probing
gastric lavage
taking activated carbon or other sorbents (Aerosil, Polyphepan, Smecta)
use of laxatives
in severe cases artificial ventilation lungs
for bradycardia and increased vagotonia, atropine sulfate is used
if necessary, use solutions of electolites, colloids, plasma or plasma substitutes
it is possible to use catecholamines for pharmacological correction

In order to eliminate the β-blocking effect on adrenergic receptors, isoprenaline hydrochloride is used, which is administered intravenously slowly at a starting dose of 5 mcg/minute until the desired clinical effect is achieved, dobutamine at a starting dose of 2.5 mcg/minute, in the absence of a therapeutic effect - glucagon (intravenous). at a dose of 50–100 mcg/kg, repeat after 1 hour, and then, if necessary, carry out a continuous infusion at a dose of 70 mcg/kg/hour.For severe atrioventricular block, transvenous cardiac pacing is used.

Synonyms (analogs, generics) Nebivolol

Synonyms: Bivotenz, Binelol, Nebivator, Nebivolol, Nebivolol Sandoz, Nebivolol Stada, NEBIVOLOL-NANOLEK, Nebivolol-Teva, Nebivolol hydrochloride, Nebilan Lannacher, Nebilet, Nebilong, OD-Neb

Release form of the medicinal product

The drug is released in following form: 5 mg tablets in blisters of 10-14 pieces.