Universal reference book for medicines
Name of the drug: NEBIVATOR (NEBIVATOR)

Active substance: nebivolol

Type: Beta 1 -adrenoblock III generation with vasodilating properties

Manufacturer: TORRENT PHARMACEUTICALS (India)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
Cardioselective beta- 1- adrenoblocker III 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 blocker? 1- adrenoreceptors; L-nebivolol has a mild vasodilating effect due to the modulation of the release of the vasodilating factor (NO) from the vascular endothelium.
Nebivolol reduces heart rate and blood pressure at rest and under load, reduces the end-diastolic pressure of the left ventricle, reduces OPSS, improves diastolic function of the heart (reduces filling pressure), increases the ejection fraction;
causes antianginal effect in patients with IHD.
The hypotensive effect is also due to a decrease in the activity of the renin-angiotensin system (does not directly correlate with a change in renin activity in the blood plasma).

Antiarrhythmic effect due to suppression of pathological automatism of the heart (including in the pathological focus) and slowing AV-conduction.

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

PHARMACOKINETICS
After ingestion, nebivolol is rapidly absorbed from the digestive tract.
Eating does not affect absorption. Bioavailability averages 12% in persons with fast metabolism (the effect of "first passage" through the liver) and is almost complete in individuals with slow metabolism.
In blood plasma, both enantiomers predominantly bind to albumin.
Binding to plasma proteins 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 as O- and N-glucuronides.
It is excreted by the kidneys (38%) and through the intestines (48%).

In individuals with a fast metabolism of T 1/2 hydroxymetabolites - 24 h, enantiomers of nebivolol - 10 h;
in persons with a slow metabolism: hydroxymetabolites - 48 h, enantiomers nebivolol - 30-50 h.
The excretion of unchanged nebivolol with urine is less than 0.5%.

INDICATIONS
Arterial hypertension.

IHD: prevention of angina pectoris attacks.

Chronic heart failure (as part of combination therapy).

DOSING MODE
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 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 cardiovascular system: bradycardia, orthostatic hypotension, dyspnea, edema, acute heart failure, AV blockade, Raynaud's syndrome, cardialgia.

From the skin and subcutaneous tissues: skin rash erythematous nature, itching;
very rarely - aggravation of the course of psoriasis.
Allergic reactions: in some cases - angioedema.

Other: bronchospasm, dry eyes.

CONTRAINDICATIONS
Acute congestive 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 the sinoatrial blockade; AV-blockade II and III degree (without an artificial rhythm driver); bradycardia (heart rate less than 60 beats per minute); cardiogenic shock; pheochromocytoma (without simultaneous use of alpha-blockers); metabolic acidosis; severe liver dysfunction; bronchospasm and bronchial asthma in history; severe obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); myasthenia gravis; depression; children and adolescents under 18; increased sensitivity to nebivolol.
PREGNANCY AND LACTATION
Application in pregnancy is possible only on strict indications (in connection with the possible development in newborns of bradycardia, arterial hypotension, hypoglycemia and respiratory paralysis).
Nebivolol should be discontinued 48-72 hours before delivery. In cases where this is not possible, strict supervision of newborns should be made within 48-72 hours after delivery.
APPLICATION FOR FUNCTIONS OF THE LIVER
Use with caution in patients with renal insufficiency.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.

APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.

APPLICATION IN ELDERLY PATIENTS
Use with caution in patients older than 65 years.
Control of laboratory indicators of kidney function in elderly patients should be performed once every 4-5 months.
SPECIAL INSTRUCTIONS
Caution should be used nebivolol in patients with renal insufficiency, diabetes, thyroid hyperthyroidism, history of allergies, psoriasis, COPD, grade I AV blockade, prinzmetal angina, and patients older than 75 years.

The abolition of beta-blockers should be carried out gradually, within 10 days (up to 2 weeks in patients with ischemic heart 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 that of non-smokers.

Nebivolol has no effect on 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 nebivolol is necessary in patients with psoriasis, the expected benefit of therapy and the possible risk of exacerbation of psoriasis should be carefully evaluated.

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

Nebivolol can enhance the 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 an anesthetist should be warned that the patient is taking beta-blockers.

Control of glucose in the blood plasma should be done 1 time in 4-5 months (in patients with diabetes mellitus).

Control of laboratory indicators of kidney function should be performed once every 4-5 months (in elderly patients).

Use in children is not recommended.

Impact on the ability to drive vehicles and manage mechanisms

Nebivolol does not affect the rate of psychomotor reactions.
With nebivolol, sometimes dizziness and fatigue are possible, so patients taking nebivolol should refrain from engaging in potentially hazardous activities.
DRUG INTERACTION
With simultaneous use with antiarrhythmic drugs of the first class, amiodarone, an increase in the negative inotropic effect and inhibition of AV conduction are possible.

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

With IV administration of verapamil against the background of nebivolol, there is a threat of cardiac arrest (concomitant use is contraindicated).

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

With simultaneous use with sympathomimetics, the pharmacological activity of nebivolol is suppressed.

With simultaneous use with funds 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 is possible.

With simultaneous application with cimetidine, nebivolol concentration in the blood plasma can be increased.

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

When joint use of nebivolol with insulin and hypoglycemic agents for oral administration may mask symptoms of hypoglycemia (tachycardia).

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