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

Active substance: nebivolol

Type: Beta 1 -adrenoblock III generation with vasodilating properties

Manufacturer: ACTAVIS GROUP PTC ehf.
(Iceland) manufactured by ACTAVIS (Malta)
Composition, form of production and packaging
Tablets are
white in color, round, convex on one side marked "N5", on the other - with a cross-shaped risk with a prominent face on each of the divided sectors.

1 tab.

nebivolol hydrochloride 5.45 mg,

which corresponds to the content of nebivolol 5 mg

Excipients: silicon dioxide colloid - 0.65 mg, magnesium stearate - 2 mg, croscarmellose sodium - 11.5 mg, macrogol 6000 - 20 mg, lactose monohydrate - 192.4 mg.

7 pcs.
- blisters (1) - packs of cardboard.
7 pcs.
- blisters (2) - packs of cardboard.
7 pcs.
- blisters (4) - packs of cardboard.
7 pcs.
- blisters (8) - packs of cardboard.
10 pieces.
- blisters (1) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (5) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2013.

PHARMACHOLOGIC EFFECT

Cardioselective lipophilic beta- 1- adrenoblocker III generation with vasodilating properties.
Has antihypertensive, anti-anginal and antiarrhythmic effect. Reduces elevated blood pressure at rest, with physical stress and stress. Competently and selectively blocks synaptic and postsynaptic? 1- adrenoreceptors, 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 types of pharmacological action:

- D-nebivolol is a competitive and highly selective blocker?
1- adrenoreceptors (affinity for? 1- adrenoreceptors is 293 times higher than for β2-adrenoreceptors).
L-nebivolol has a mild vasodilating effect by modulating the release of the relaxing factor (NO) from the vascular endothelium.

The hypotensive effect develops on the 2nd-5th day of treatment, stable effect is observed after 1 month.
Antihypertensive effect persists with long-term treatment.
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).

The use of nebivolol improves the indices of systemic and intracardiac hemodynamics.
Nebivolol reduces heart rate and blood pressure at rest and with physical activity, reduces the end-diastolic pressure of the left ventricle, lowers the OPSS, improves diastolic function of the heart (reduces filling pressure), increases the ejection fraction.
Reducing the need for myocardium in oxygen (decreasing heart rate, reducing preload and afterload), reduces the number and severity of angina attacks and increases the tolerance of exercise.

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

PHARMACOKINETICS

Suction

After oral administration, nebivolol is rapidly absorbed from the digestive tract.
Eating does not affect absorption, so nebivolol can be taken regardless of food intake.Bioavailability averages 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

Clearance in the blood plasma in most patients (with a "fast" metabolism) is achieved within 24 hours, and for hydroxy metabolites - in a few days.
Concentrations in blood plasma of 1-30 mcg / l are proportional to the dose.
Binding to blood plasma proteins (mainly with albumin) for D-nebivolol is 98.1%, and for L-nebivolol - 97.9%.

Metabolism

Nebivolol is actively metabolized, in part with the formation of active hydroxymetabolites.
The metabolic rate of nebivolol by aromatic hydroxylation is genetically determined by oxidative polymorphism and depends on the isoenzyme CYP2D6.
Excretion

One week after the introduction of 38% (the amount of unchanged active substance is less than 0.5%), the dose is excreted by the kidneys and 48% by the intestine.
In patients with "fast" metabolism, the values ​​of T 1/2 enantiomers of nebivolol from the plasma are an average of 10 hours. In patients with "slow" metabolism, these values ​​increase 3-5 times.
In patients with "fast" metabolism, the T 1/2 values ​​of the hydroxy metabolites of both enantiomers from the plasma are on average 24 hours, in patients with a "slow" metabolism these values ​​are approximately 2-fold increased.

The pharmacokinetics of nebivolol is not affected by age and sex of patients.

INDICATIONS

- arterial hypertension;

- IHD: prevention of attacks of stable angina pectoris;

- chronic heart failure (as part of combination therapy).

DOSING MODE

Nevotenz should be taken inside at the same time of the day, regardless of food intake, without chewing and drinking with a sufficient amount of liquid.

Hypertension and coronary artery disease

The average daily dose is 5 mg 1 time / day.
The optimal effect becomes pronounced after 1-2 weeks of treatment, and in some cases - after 4 weeks. It is possible to use the drug in the form of monotherapy or as part of a combination therapy.
If necessary, the daily dose can be increased to 10 mg (2 tablespoons of 5 mg per 1 dose).
The maximum daily dose is 10 mg.
In patients with renal insufficiency , as well as in patients of elderly patients (over 65 years of age), the initial dose is 2.5 mg / day (1/2 tablets of 5 mg).
If necessary, increase the dose to 5 mg.
At the expressed infringements of function of kidneys (KK <20 ml / mines) and at patients with serious diseases of a liver the maximum daily dose makes 10 mg.
Increase in the dose in such patients should be done with extreme caution.
Chronic heart failure

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

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 tolerance of this dose to the patient: Nevotenz is prescribed in a dose of 1.25 mg (1/4 tab.) 1 time / day, then this dose can be increased first to 2.5-5 mg (1 / 2-1 tab.), and then - up to 10 mg (2 tab.) 1 time / day.
The patient should be under the supervision of a doctor within 2 hours after taking the first dose of the drug, and also after each subsequent increase in the dose. Each dose increase should be carried out not later than 2 weeks. The maximum recommended dose of Nevotenz in the treatment of chronic heart failure is 10 mg 1 time / day. During titration, regular monitoring of blood pressure, heart rate and symptoms of chronic heart failure is recommended.
During the titration phase, in case of worsening of the course of chronic heart failure or intolerance of the drug, it is recommended to reduce the dose of Nevotenz or, if necessary, to stop it immediately (in case of pronounced arterial hypotension, worsening of chronic heart failure with acute pulmonary edema, in case of cardiogenic shock , symptomatic bradycardia, or with AV blockade).

SIDE EFFECT

On the part of the nervous system: headache, dizziness, fatigue, paresthesia, depression, decreased ability to concentrate, drowsiness, insomnia, nightmares, hallucinations, loss of consciousness.

On the part of the digestive system: nausea, constipation, flatulence, diarrhea, dryness of the oral mucosa.

From the cardiovascular system: bradycardia, heart failure, AV blockade, orthostatic hypotension, peripheral circulation disorders (cold sensation in the extremities, cyanosis), shortness of breath, heart rhythm disturbances, Raynaud's syndrome, peripheral edema, cardialgia, worsening of the chronic course heart failure 1 , a marked decrease in blood pressure.

On the part of the respiratory system: bronchospasm (including in the absence of obstructive pulmonary disease in the anamnesis), bronchospasm in patients with bronchial asthma or airway obstruction in anamnesis, rhinitis.

Dermatological reactions: alopecia, photodermatosis, hyperhidrosis, exacerbation of psoriasis.

Allergic reactions: skin itching, erythematous rash, angioedema, skin flushing.

Other: visual impairment (dry eyes), a violation of potency.

1 - This side effect predominantly occurs during the titration of the dose of the drug



CONTRAINDICATIONS

- pronounced violations of the liver function;

- acute heart failure;

- Chronic heart failure in the stage of decompensation (requiring the use of drugs that have an inotropic effect);

- cardiogenic shock;

- SSSU, including sinoatrial blockade;

- AV blockade II and III degree (without artificial pacemaker);

- bronchospasm and bronchial asthma;

- pheochromocytoma (without simultaneous use of alpha-blockers);

- Depression;

metabolic acidosis;

- pronounced bradycardia (heart rate less than 50 beats per minute);

- severe arterial hypotension;

- severe severe disturbances of peripheral circulation (intermittent claudication, Raynaud's syndrome);

- age up to 18 years;

- lactose intolerance, lactase deficiency or glucose malabsorption / galactose syndrome;

- simultaneous administration with floktaphenin, sultopride;

- Hypersensitivity to nebivalol and other components of the drug.

Caution should be applied to the drug with severe renal failure (CC <20 ml / min), liver function disorders, diabetes mellitus, hyperthyroidism, desensitizing therapy, psoriasis, grade I AV block, Prinzmetal angina, COPD, elderly patients 65 years old).

PREGNANCY AND LACTATION

In pregnancy, the drug is prescribed only on strict indications, when the potential benefit to the mother exceeds the risk for the fetus (due to the possible development of a newborn bradycardia, arterial hypotension, hypoglycemia and respiratory paralysis).
Treatment should be interrupted for 48-72 hours before childbirth. In cases where this is not possible, it is necessary to ensure strict observation of the newborn within 48-72 hours after delivery.
In experimental animal studies, it has been shown that nebivolol excreted in breast milk.
There is no data on excretion of nebivalol with breast milk. Therefore, the drug Nevotenz is not recommended for women during lactation. If the drug is used during lactation, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be applied to the drug with severe renal failure (CC <20 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should apply the drug for violations of liver function.

Contraindicated in severe violations of liver function.

APPLICATION FOR CHILDREN

Contraindicated in children and adolescents under 18 years.

APPLICATION IN ELDERLY PATIENTS

With caution should be used in elderly patients (over 65 years).

SPECIAL INSTRUCTIONS

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

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

Older patients need control of kidney function (1 time in 4-5 months).

With angina pectoris, it is necessary that the dose of the drug provide the heart rate at rest within 55-60 beats / min, with a load - no more than 110 beats per minute.

Beta-adrenoblockers can cause bradycardia, so the dose should be reduced if the heart rate is less than 50-55 bpm.

When deciding on the appointment of the drug Nevotenz, patients with psoriasis should carefully correlate the estimated benefits of using the drug and the possible risk of exacerbation of psoriasis.

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

Nebivolol does not affect the level of glucose in patients with diabetes mellitus.
Nevertheless, caution should be exercised in the treatment of these patients, since Nevotenz may mask certain symptoms of hypoglycemia (eg, tachycardia) caused by the use of hypoglycemic agents.
In patients with diabetes mellitus, the control of glucose in the blood plasma should be carried out 1 time in 4-5 months.

Beta-adrenoblockers should be used with caution in patients with COPD, since it is possible to strengthen bronchospasm.

With hyperfunction of the thyroid gland, the drug levels tachycardia.

Beta-adrenoblockers can increase sensitivity to allergens and the severity of anaphylactic reactions.

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

The effectiveness of beta-adrenoblockers in smokers is lower than in non-smoking patients.

Impact on the ability to drive vehicles and manage mechanisms

Research has shown that nebivolol has no effect on the rate of psychomotor reactions.
Pilots flying crew with hypertension I degree (admitted to flight work), the drug is prescribed in an initial dose of 2.5 mg. In the future (no earlier than 2 weeks) with good tolerability of treatment and insufficient control of blood pressure, a 2.5 mg dose increase is possible. The recommended dose is 5 mg / day. Some patients may develop side effects, most often - dizziness, due to low blood pressure. If such effects occur, the patient should not drive vehicles or engage in potentially hazardous activities requiring special attention and speed of psychomotor reactions. These effects occur most often immediately after the start of treatment or with increasing doses.
OVERDOSE

Symptoms: marked decrease in blood pressure, severe bradycardia, AV blockade, cardiogenic shock, acute heart failure, cardiac arrest, bronchospasm, unconsciousness, coma, nausea, vomiting, cyanosis.

Treatment: gastric lavage, reception of activated charcoal.
In the case of a marked decrease in blood pressure, it is necessary to give the patient a horizontal position with raised legs, if necessary, in / in the administration of liquid and vasopressors; as a follow-up, it is possible to administer 1-10 mg of glucagon.
When bradycardia is expressed, intravenous injection of 0.5-2 mg of atropine is administered, in the absence of a positive effect, a transvenous artificial pacemaker is available.

With AV block II and III degree, the introduction of beta-adrenomimetics is recommended, if they are ineffective, consider setting up an artificial pacemaker.
With heart failure treatment begins with the introduction of cardiac glycosides and diuretics, in the absence of effect, it is advisable to administer dopamine, dobutamine or vasodilators.
When bronhospazme enter in / in beta 2 -adrenomimetiki.

When ventricular extrasystole is lidocaine (do not administer antiarrhythmic drugs of class IA).

With convulsions - in / in diazepam.

DRUG INTERACTION

In the case of shock or arterial hypotension caused by the use of floktaphenina, beta-adrenoblockers weaken the compensatory mechanisms of the cardiovascular system.

When used simultaneously with sultopride, the risk of ventricular arrhythmia increases, especially of the pirouette type.

With the simultaneous use of beta-blockers with slow calcium channel blockers (BCCA) (verapamil and diltiazem), the effect on contractility of the myocardium and AV-conduction increases.
Contraindicated in / in the administration of verapamil on the background of nebivolol.
When combined with antihypertensive drugs, nitroglycerin or BCCC, severe arterial hypotension may develop (special caution is necessary when combined with prazosin).

With simultaneous use with antiarrhythmic agents of the first class and with amiodarone, an increase in the negative inotropic effect and an extension of the time of excitation to the atria are possible.

With the simultaneous use of nebivolol with cardiac glycosides, there was no evidence of an increase in the effect on AV conduction slowing.

Simultaneous use of nebivolol and preparations for general anesthesia can cause suppression of reflex tachycardia and increase the risk of developing arterial hypotension.

Clinically significant interaction of nebivolol and NSAIDs is not established.
Acetylsalicylic acid as antiplatelet agent can be used concomitantly with nebivolol.
The simultaneous use of tricyclic antidepressants, barbiturates and phenothiazine derivatives can enhance the antihypertensive effect of nebivolol.

Pharmacokinetic interaction

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

With simultaneous use nebivolol had no effect on the pharmacokinetic parameters of digoxin.

With simultaneous use with cimetidine, the concentration of nebivolol in the blood plasma increases (there is no evidence of an effect on the pharmacological effects of the drug).

The simultaneous use of ranitidine did not affect the pharmacokinetic parameters of nebivolol.

With the simultaneous use of nebivolol with nicardipine, concentrations of active substances in the blood plasma increased slightly, but this has no clinical significance.

Simultaneous administration of ethanol, furosemide or hydrochlorothiazide did not affect the pharmacokinetics of nebivolol.

Clinically significant interactions of nebivolol and warfarin have not been established.

With the simultaneous use of sympathomimetic drugs suppress the activity of nebivolol.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of the reach of children at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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