Universal reference book for medicines
Product name: NEBILET ® (NEBILET ® )

Active substance: nebivolol

Type: Beta 1 -adrenoblock III generation with vasodilating properties

Manufacturer: BERLIN-CHEMIE / MENARINI PHARMA (Germany) manufactured by BERLIN-CHEMIE (Germany)
Composition, form of production and packaging
Tablets are
almost white, round, biconvex, with a cross-shaped notch for division.

1 tab.

nebivolol hydrochloride micronized 5.45 mg,

which corresponds to the content of nebivolol 5 mg

Auxiliary substances: lactose monohydrate - 141.75 mg, corn starch - 46 mg, croscarmellose sodium - 13.8 mg, hypromellose 15 mPa? S - 4.6 mg, polysorbate 80 - 0.46 mg, microcrystalline cellulose 16.1 mg, silicon colloidal dioxide 0.69 mg, magnesium stearate 1.15 mg.

7 pcs.
- blisters (1) - packs of cardboard.
7 pcs.
- blisters (2) - packs of cardboard.
7 pcs.
- blisters (4) - packs of cardboard.
14 pcs.
- blisters (1) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
14 pcs.
- blisters (4) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Cardioselective beta 1- adrenoblocker.
Has antihypertensive, anti-anginal and antiarrhythmic effect. Reduces elevated blood pressure at rest, with physical stress and stress. Competently and selectively block postsynaptic? 1- adrenoreceptors, making them inaccessible to catecholamines, modulates the release of endothelial vasodilating factor nitric oxide (NO).
Nebivolol is a racemate of two enantiomers: SRRR-nebivolol (D-nebivolol) and RSSS-nebivolol (L-nebivolol), which combines two pharmacological actions:

- D-nebivolol is a competitive and highly selective blocker?
1- adrenoreceptors;
- L-nebivolol has a mild vasodilating effect due to modulation of the release of the vasodilating factor (NO) from the endothelium
vessels.
The hypotensive effect is also due to a decrease in the activity of the renin-angiotensin-aldosterone system (RAAS) (does not directly correlate with a change in renin activity in the blood plasma).

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.

Reducing the need for myocardium in oxygen (decreasing heart rate and 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, both enantiomers are rapidly absorbed.
Eating does not affect absorption, so nebivolol can be taken regardless of food intake. Bioavailability of nebivolol after ingestion is an average of 12% in individuals with "fast" metabolism (the effect of the first passage through the liver) and is almost complete in individuals with a "slow" metabolism.
Distribution

In plasma, both enantiomers are predominantly associated with albumin.
The binding to plasma proteins for D-nebivolol is 98.1%, and for L-nebivolol, 97.9%.
Metabolism

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.
Excretion

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.
Elimination of unchanged nebivolol with urine is less than 0.5% of the amount taken internally.

INDICATIONS

- arterial hypertension;

- Coronary heart disease: prevention of angina pectoris attacks;

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

DOSING MODE

Tablets are taken orally, 1 time / day, preferably always at the same time of the day, regardless of food intake, with a sufficient amount of liquid.

The average daily dose for the treatment of hypertension and arterial hypertension is 2.5-5 mg (1 / 2-1 tab.).
Nebilet ® can be used in monotherapy or in combination with other means that reduce blood pressure.
In patients with renal insufficiency, as well as in patients older than 65 years, the recommended initial dose is 2.5 mg (1/2 tab.) / Day.
If necessary, daily dose can be increased to the maximum 10 mg (2 tablets of 5 mg per 1 dose).
Treatment of chronic heart failure should begin with a slow increase in the dose until an individual optimal maintenance dose is reached.
Selection of the dose at the beginning of treatment should be carried out according to the following scheme, while maintaining intervals of 1 to 2 weeks and based on the tolerance of this dose to the patient: a dose of 1.25 mg of nebivolol (1/4 tablets of 5 mg) 1 time / day may be was first increased to 2.5-5 mg (1/2 tablets of 5 mg or 1 table, 5 mg), and then to 10 mg (2 tablets of 5 mg) 1 time / day.
The maximum daily dose is 10 mg 1 time / day.

At the beginning of treatment and at each dose increase, the patient should be under the supervision of a doctor for at least 2 hours to ensure that the clinical condition remains stable (especially, blood pressure, heart rate, conduction disorders, and symptoms of worsening of chronic heart failure).

Rules for the division of tablets

For division, place the tablet on a firm, level surface with a cross-shaped notch up, press the tablet with both index fingers.
To obtain 1/4 tablets, repeat the same actions with 1/2 tablet.
SIDE EFFECT

Frequency of side effects: very often
(> 10%), often (> 1% and <10%), infrequently (> 0.1% and <1%), rarely (> 0.01% and <0.1%), very rarely (<0.01%, including individual messages).
From the central nervous system and peripheral nervous system: often - headache, dizziness, fatigue, weakness, paresthesia;
infrequently - depression, nightmares, confusion; very rarely - fainting, hallucinations.
From the digestive system: often - nausea, constipation, diarrhea;
infrequently - dyspepsia, flatulence, vomiting.
From the side of the cardiovascular system: infrequently - bradycardia, acute
heart failure, AV-blockade, orthostatic hypotension, Raynaud's syndrome.
From the skin and subcutaneous tissues: infrequently - skin rash of erythematous nature, itching;
very rarely - exacerbation of psoriasis; in some cases - angioedema edema.
Other: infrequent bronchospasm;
rarely - dry eyes.
CONTRAINDICATIONS

- acute heart failure;

- Chronic heart failure in the stage of decompensation (requiring in / in the administration of drugs with inotropic effect);

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

- SSSU, including 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;

- pronounced violations of the liver function;

- bronchospasm and bronchial asthma in history;

- severe obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome);

- Myasthenia gravis;

- Depression;

lactose intolerance, deficiency
lactase and glucose / galactose malabsorption syndrome;
- children and adolescents under 18 years of age (efficacy and safety not studied);

- Hypersensitivity to nebivolol or one of the components of the drug.

Caution should be used for renal failure, diabetes, thyroid gland hyperthyroidism, history of allergies, psoriasis, chronic obstructive pulmonary disease, grade I AV block, Prinzmetal angina, and patients over the age of 75 years.

PREGNANCY AND LACTATION

In pregnancy, the drug Nebilet ® is prescribed only for vital indications, when the benefit to the mother exceeds the possible risk to the fetus or newborn (due to possible development
in fetus and newborn bradycardia, arterial hypotension, hypoglycemia). If treatment with Nebilet ® is necessary, then it is necessary to observe utero-placental blood flow and fetal growth. Treatment should be interrupted for 48-72 hours before childbirth. In cases where this is not possible, it is necessary to establish strict observation of newborns within 48-72 hours after delivery.
Nebivolol is excreted in breast milk.
If you need to take Nebilet ® during lactation, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER

In patients with renal insufficiency, the initial dose is 2.5 mg / day.

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

Caution should be applied to patients aged over 75 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, the dose of the drug should provide a heart rate at rest within 55-60 beats / min, with a load - no more than 110 beats per minute.

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

When deciding whether to use Nebilet ® in patients with psoriasis, the expected benefits of using the drug and the possible risk of exacerbation of psoriasis should be carefully correlated.

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

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

Nebivolol
does not affect the concentration of glucose in blood plasma in patients with diabetes mellitus. Nevertheless, caution should be exercised in the treatment of these patients, since Nebelet ® can mask certain symptoms of hypoglycemia (eg, tachycardia) caused by the use of hypoglycemic agents for ingestion and insulin.Controlling the concentration of glucose in the blood plasma should be to spend 1 time in 4-5 months (in patients with diabetes mellitus).
With hyperthyroidism, beta-adrenoblockers can mask tachycardia.

Beta-adrenoblockers should be used with caution in patients with chronic obstructive pulmonary disease, as bronchospasm may increase.

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

Impact on the ability to drive vehicles and manage mechanisms

The effect of Nebilet ® on the ability to drive vehicles and control mechanisms has not been specifically studied.
Studies of the pharmacodynamics of nebivolol have shown that the drug Nebilet ® has no effect on the psychomotor function. During the period of treatment with Nebilet ® (if side effects occur), care must be taken when driving vehicles and potentially potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
OVERDOSE

Symptoms: marked decrease in blood pressure, nausea, vomiting, cyanosis, sinus bradycardia, AV blockade, bronchospasm, loss of consciousness, cardiogenic shock, coma, cardiac arrest.

Treatment: gastric lavage, reception of activated charcoal.
In the case of a marked decrease in blood pressure, give the patient a horizontal position with raised legs, if necessary, in / in the introduction of liquid and vasopressors. When bradycardia should be administered to / in 0.5-2 mg of atropine in the absence of a positive effect, a transvenous or intracardiac electrostimulator can be staged. With AV-blockade (II-III st.) It is recommended to / in the introduction of beta-adrenostimulyatorov, if their inefficiency should be considered the question of 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 apply IV stimulants? 2-adrenoreceptors. When ventricular estrasystole - lidocaine (you can not inject antiarrhythmic drugs IA class).
DRUG INTERACTION

Pharmacodynamic interaction

With the simultaneous use of beta-blockers with slow calcium channel blockers (verapamil and diltiazem), the effect on contractility of the myocardium and AV-conduction increases.

Contraindicated in / in the administration of verapamil against the background of nebivolol.

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 the simultaneous use of nebivolol with antiarrhythmic drugs I class and with
Amiodarone may increase the negative inotropic effect and prolong the time of excitation in the atria.
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 interactions of nebivolol and
NSAIDs not installed.
Simultaneous
the use of nebivolol with tricyclic antidepressants, barbiturates and phenothiazine derivatives can enhance the antihypertensive effect of nebivolol.
Pharmacokinetic interaction

With the simultaneous use of nebivolol with drugs that inhibit serotonin reuptake, or other agents biotransforming with the participation of the isoenzyme CYP2D6, the concentration of nebivolol in the blood plasma increases, the metabolism of nebivolol slows down,
what can lead to risk of bradycardia.
When used simultaneously with digoxin, nebivolol has no effect on the pharmacokinetic parameters of digoxin.

With the simultaneous use of nebivolol with cimetidine, the concentration of nebivolol in the blood plasma increases.

Simultaneous use of nebivolol and ranitidine does not affect the pharmacokinetic parameters of nebivolol.

With the simultaneous use of nebivolol with nicardipine, the concentrations of active substances in the blood plasma increase slightly, but this does not have a clinical
values.
Simultaneous administration of nebivolol and ethanol, furosemide or hydrochlorothiazide does not affect the pharmacokinetics of nebivolol.

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

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