Binelol tablets 5mg, # 28

Arterial hypertension.

IHD: prevention of exertional angina attacks.

Chronic heart failure (as part of combination therapy).

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

Arterial hypertension and ischemic heart disease. The average daily dose for the treatment of arterial hypertension and ischemic heart disease is 2.5-5 mg (1 / 2-1 table.) 1 time per 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, the initial dose is 2.5 mg / day (1/2 table, 5 mg each).

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

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

The selection of the dose 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: a dose of 1.25 mg of the drug (1/4 table) 1 time per day can be increased first to 2.5 Ц5 mg (1 / 2Ц1 tab.), And then - up to 10 mg (2 tab.) 1 time per day.

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 blockade; AV block II and III degree (without an artificial pacemaker); bradycardia (heart rate less than 60 beats / min); cardiogenic shock; pheochromocytoma (without the simultaneous use of alpha-blockers); metabolic acidosis; severe liver dysfunction; history of bronchospasm and bronchial asthma; severe obliterating peripheral vascular disease (intermittent claudication, Raynaud's syndrome); myasthenia gravis; depression; children and adolescents up to 18 years old; hypersensitivity to nebivolol.

Clinical and pharmacological group: Beta1-blocker of the III generation with vasodilating properties

Pharmaco-therapeutic group: Selective beta1-blocker

pharmachologic effect

III generation cardioselective beta1-blocker 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 ?1-adrenergic receptor blocker; L-nebivolol has a mild vasodilator effect by modulating the release of vasodilating factor (NO) from the vascular endothelium.

Nebivolol lowers heart rate and blood pressure at rest and during exertion, reduces left ventricular end-diastolic pressure, decreases systemic vascular resistance, improves diastolic heart function (decreases 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 (it does not directly correlate with a change in renin activity in the blood plasma).

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

A stable hypotensive effect develops after 1-2 weeks of regular administration 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. Food intake does not affect absorption. Bioavailability averages 12% in those with a fast metabolism (the 'first pass' effect through the liver) and is almost complete in those with a slow metabolism.

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

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

It is excreted by the kidneys (38%) and through the intestines (48%).

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

Urinary excretion of unchanged nebivolol is less than 0.5%.

Indications of active

Arterial hypertension.

IHD: prevention of exertional angina attacks.

Chronic heart failure (as part of combination therapy).

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

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

Side effect

From the side of the central nervous system and peripheral nervous system: headache, dizziness, 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 side of the cardiovascular system: bradycardia, orthostatic hypotension, shortness of breath, edema, acute heart failure, AV block, Raynaud's syndrome, cardialgia.

Skin and subcutaneous tissue disorders: erythematous skin rash, itching; very rarely - worsening of the course 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 blockade; AV block II and III degree (without an artificial pacemaker); bradycardia (heart rate less than 60 beats / min); cardiogenic shock; pheochromocytoma (without the simultaneous use of alpha-blockers); metabolic acidosis; severe liver dysfunction; history of bronchospasm and bronchial asthma; severe obliterating peripheral vascular disease (intermittent claudication, Raynaud's syndrome); myasthenia gravis; depression; children and adolescents up to 18 years old; hypersensitivity to nebivolol.

Application during pregnancy and lactation

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

Application for violations of liver function

Contraindicated in severe liver dysfunction.

Application for impaired renal function

Use with caution in patients with renal insufficiency.

Application in children

Contraindicated in children and adolescents under 18 years of age.

Use in elderly patients

Use with caution in patients over the age of 65 years. Monitoring of laboratory parameters of renal function in elderly patients should be carried out 1 time in 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, 1st degree AV block, Prinzmetal's angina, as well as in patients over the age of 75 years.

Cancellation 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 does not affect glucose levels in patients with diabetes, but nebivolol may mask certain signs of hypoglycemia (tachycardia, heart palpitations) caused by the use of hypoglycemic drugs.

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

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 exacerbate symptoms of peripheral circulatory disorders.

Patients wearing contact lenses should take into account that with the use of beta-blockers, a decrease in the production of tear fluid is possible.

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

Plasma glucose control should be carried out 1 time in 4-5 months (in patients with diabetes mellitus).

Monitoring of laboratory parameters of renal function should be carried out 1 time in 4-5 months (in elderly patients).

The use in children is not recommended.

Influence on the ability to drive vehicles and use mechanisms

Nebivolol does not affect the speed of psychomotor reactions. Dizziness and fatigue can sometimes occur while taking nebivolol, so patients taking nebivolol should refrain from potentially hazardous activities.

Drug interactions

With simultaneous use with class I antiarrhythmic drugs, amiodarone, an increase in the negative inotropic effect and inhibition of AV conduction is possible.

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 threat of cardiac arrest (simultaneous use is contraindicated).

With the simultaneous use of nebivolol with antihypertensive drugs, nitroglycerin or slow calcium channel blockers, severe arterial hypotension may develop (special care is needed when combined with prazosin).

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

With simultaneous use with drugs for anesthesia, it is possible to suppress reflex tachycardia and increase the risk of developing arterial hypotension.

With simultaneous use with tricyclic antidepressants, barbiturates, phenothiazine derivatives, the antihypertensive effect of nebivolol may be enhanced.

With simultaneous use with cimetidine, an increase in the concentration of nebivolol in blood plasma is possible.

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

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