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

Active substance: nebivolol

Type: Beta 1 -adrenoblock III generation with vasodilating properties

Manufacturer: LANNACHER HEILMITTEL (Austria)
Composition, form of production and packaging
Tablets are
white or almost white, round, biconvex, with a cross-shaped notch.

1 tab.

nebivolol (in the form of hydrochloride) 5 mg

Excipients: lactose monohydrate 143.475 mg, corn starch 34.50 mg, croscarmellose sodium 13.8 mg, hypromellose (6 cps) 3.45 mg, microcrystalline cellulose 26.45 mg, silicon dioxide colloid 0.575 mg, magnesium stearate 2.30 mg.

10 pieces.
- blisters (2) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Cardioselective beta- 1- adrenoblocker of the third generation with vasodilating properties;
has antihypertensive, antianginal and antiarrhythmic effect. Selectively and competitively blocks synaptic and postsynaptic beta 1 -adrenoceptors; making them inaccessible to catecholamines, modulates the release of the endothelial vasodilating factor (NO). Nebivolol reduces heart rate and reduces blood pressure at rest and with physical activity, improves diastolic function of the heart (reduces the final diastolic filling pressure of the left ventricle). Nebivolol is a racemate consisting of a mixture of two enantiomers, D and L-nebivolol, which have different pharmacodynamic properties. D-nebivolol is a competitive and highly selective beta 1 -adrenoceptor blocker. L-nebivolol has a mild vasodilating effect by modulating the release of the relaxing factor (NO) from the vascular endothelium.
Reduces elevated blood pressure at rest, with physical activity and stress.
Decrease in blood pressure is due to a decrease in cardiac output, a decrease in the volume of circulating blood (BCC) and the overall peripheral vascular resistance, a decrease in the activity of the renin-angiotensin-aldosterone system. Antihypertensive effect occurs within 2-5 days, stable effect is observed after 1-2 months. Antihypertensive effect persists with long-term treatment.
Reducing the need for myocardium in oxygen (decreasing heart rate, reducing pre- and postnagruzki), reduces the number and severity of angina attacks and increases the tolerance of exercise.

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

PHARMACOKINETICS

Suction

After administration, nebivolol is rapidly absorbed from the digestive tract.
Eating does not affect the absorption of the drug, so nebivolol can be taken regardless of food intake. Bioavailability after ingestion is about 12% in persons with "fast" metabolism and is almost complete in individuals with "slow" metabolism. Efficiency
Nebivolol does not depend on the metabolic rate.

Distribution

Communication with plasma proteins for D-nebivolol - 98.1%, for L-nebivolol - 97.9%.

Metabolism

Nebivolol is metabolized by acyclic or aromatic hydroxylation, N-dealkylation and glucuronation, in addition, glucuronides of hydroxy metabolites are formed.
On the metabolism of nebivolol
pathways of aromatic hydroxylation is affected by genetic polymorphism of the enzyme system CYP2D6.
In patients with "fast" metabolism, the T 1/2 values ​​of enantiomers of nebivolol averagely average 10 hours, in patients with a "slow" metabolism, these values ​​increase by 3-5 times. T 1/2 hydroxymetabolites is 24 h in individuals with "fast" metabolism, in those with "slow" - approximately 2 times longer. The equilibrium concentration of nebivolol in plasma in most patients with "fast" metabolism "is reached within 24 hours, for hydroxymetabolite, this period increases to several days.
Excretion

The drug is excreted by the intestine (48%) and kidneys (38%).
Excretion of unchanged nebivolol by the kidney does not exceed 0.5% of the dose.
INDICATIONS

- arterial hypertension (monotherapy or in combination with other antihypertensive drugs);

- Coronary heart disease: prevention of attacks of stable angina pectoris;

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

DOSING MODE

Nebylan Lannacher should be taken orally, regardless of food intake, with a sufficient amount of fluid, preferably at the same time of day.

With arterial hypertension and ischemic heart disease , 2.5-5 mg (1/2 tablets of 5 mg - 1 tablet of 5 mg) 1 time / day.
If necessary, the daily dose can be increased to 10 mg (2 tablets of 5 mg at a time).
The maximum daily dose is 10 mg.
In patients with renal insufficiency (CC greater than 20 ml / min), as well as in patients older than 65 years, the initial dose is 25 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 less than 20 ml / mines) themaximum 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 (CHF) should begin with a gradual increase in the dose to achieve an individual optimal maintenance dose.Selection of doses 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: a dose of 1.25 mg of Nebilan Lannacher (1/4 tablets of 5 mg) once a day can be increased first to 2.5 -5 mg of Nebilan Lannacher (1/2 tablets of 5 mg - 1 tablet), and then to 10 mg (2 tablets of 5 mg) 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 in at least 2 weeks. The maximum recommended dose for the treatment of CHF is 10 mg of the drug 1 time / day. During titration, regular monitoring of blood pressure, heart rate and symptoms of CHF 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 or, if necessary, immediately stop taking it (in case of pronounced arterial hypotension, worsening of the course of CHF with acute pulmonary edema, in case of cardiogenic shock, symptomatic bradycardia or AV blockade).
SIDE EFFECT

From the side of the nervous system: headache, dizziness, fatigue, paresthesia;
depression, drowsiness, "nightmarish dreams", hallucinations, confusion, psychosis, convulsions, insomnia, amnesia.
From the digestive system: nausea, constipation, diarrhea, dryness of the oral mucosa, flatulence.

From the cardiovascular system: bradycardia, orthostatic hypotension, dyspnea, edema, AV blockade, worsening of the course of chronic heart failure, aggravation of "intermittent" lameness;
heart rhythm disturbances, Raynaud's syndrome, cardialgia, a marked decrease in blood pressure.
From the side of the organ of vision: visual impairment (dry eyes).

Allergic reactions: skin itching, erythematous rash, angioedema, hyperemia of the skin, alopecia.

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.

Other: photodermatosis, hyperhidrosis, exacerbation of psoriasis, violation of potency.

CONTRAINDICATIONS

severe hepatic impairment;

- acute heart failure, cardiogenic shock, chronic heart failure in the stage of decompensation (requiring inotropic therapy);

- AV blockade of II-III degree;

- syndrome of weakness of the sinus node, sino-atrial block;

- pronounced bradycardia (heart rate less than 50 / min);

- severe arterial hypotension;

- severe violations of peripheral circulation ("intermittent" lameness, Raynaud's syndrome);

- a severe form of bronchial asthma and bronchospasm in the anamnesis;

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

metabolic acidosis;

- Myasthenia gravis, muscle weakness;

- Depression;

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

- simultaneous administration with floktaphenin, sultopride;

- age up to 18 years;

- lactation period;

- Hypersensitivity to nebivolol or other components of the drug.

Caution should be applied to the drug with severe renal failure (creatinine clearance less than 20 ml / min), liver function disorders, diabetes mellitus, hyperthyroidism, conduction, desensitizing therapy, psoriasis, grade I atrioventricular block, prinzmetal angina, chronic obstructive pulmonary disease (COPD), in elderly patients (over 65 years of age).

PREGNANCY AND LACTATION

In pregnancy, the drug is prescribed when the 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 delivery. Studies in animals have shown that nebivolol excreted in breast milk. If the use of the drug during lactation is necessary, then breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER

With caution apply the drug with severe renal failure (creatinine clearance (CC) less than 20 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

The drug is contraindicated in severe violations of liver function.

Use with caution in case of violations of the liver.

APPLICATION FOR CHILDREN

Contraindicated in children under 18 years.

APPLICATION IN ELDERLY PATIENTS

Use with caution elderly persons (over 65 years of age).
In elderly patients it is recommended to monitor kidney function (1 time in 4-5 months).
SPECIAL INSTRUCTIONS

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 / minute.

It is necessary to monitor heart rate and blood pressure, at the beginning of the procedure - daily;
for, concentration of glucose level in blood of patients with diabetes mellitus (1 time in 4-5 months). In elderly patients it is recommended to monitor kidney function (1 time in 4-5 months).
Beta-adrenergic block should be used with caution in patients with chronic obstructive pulmonary disease, as bronchospasm may increase.
The effectiveness of beta-blockers in smokers is lower than in non-smoking patients.
For surgical interventions, the anesthetist should be informed of the patient's admission to nebivolol.

The drug can enhance the manifestation of violations of peripheral arterial blood circulation.
With diabetes, the drug can mask hypoglycemia. With hyperthyroidism, the drug can level tachycardia. Beta-adrenoblockers can increase sensitivity to allergens and the severity of anaphylactic reactions.
Patients using contact and lenses should take into account that against a background of treatment with beta-blockers.
it is possible to reduce the production of tear fluid. The use of the drug in athletes can lead to positive results of doping tests. The abolition of beta-adrenoblockers should be carried out gradually, within 10 days (up to 2 weeks in patients with coronary heart disease).
Impact on the ability to drive vehicles and manage mechanisms

No negative impact on the ability to drive vehicles or other complex mechanisms against the background of Nebilan Lannacher was observed, however, care should be taken when driving vehicles and mechanisms.

OVERDOSE

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

Treatment: gastric lavage, activated charcoal;
in the case of a pronounced decrease in blood pressure, give the patient a horizontal position with raised legs, if necessary, / in the introduction of liquids and vasopressors, if necessary - glucagon; with bradycardia - intravenous injection of 0.5-2 mg of atropine, in the absence of a positive effect, a transvenous or intracardiac electrostimulator can be inserted; with AV blockade of II-III degree, the administration of beta-adrenostimulators is recommended, if they are ineffective, consider setting up an artificial pacemaker; when 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; at bronhospazme - in / in the introduction of beta-2-adrenomimetik. When ventricular extrasystole is lidocaine (preparations of Class Ia are not used). With convulsions - in / in diazepam.
DRUG INTERACTION

Floktaphenin: in the case of shock or arterial hypertension caused by the use of floktaphenina, beta-adrenoblockers weaken the compensatory mechanisms of the cardiovascular system.

Sultopride: increased risk of ventricular arrhythmia, especially in the form of "pirouette" (torsade des pointes).

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

Contraindicated in / in the introduction of verapamil against nebivolol.
When combined with antihypertensive drugs, nitroglycerin or BCCC, severe arterial hypotension may develop (special caution is necessary when
combination with prazosin).

When used simultaneously with antiarrhythmic drugs of the first class and with amiodarone, an increase in the negative inotropic effect and prolongation of the excitation time at the atria are possible.

With the simultaneous use of nebivolol with cardiac glycosides, no effect on AV conduction slowing is detected.
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 non-steroidal anti-inflammatory drugs (NSAIDs) have not been 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.

Baclofen, amifostine: their simultaneous use with antihypertensive drugs can cause a significant drop in blood pressure, therefore, a correction of the dose of antihypertensive drugs is required.

Mefloquine: theoretically, the co-administration of mefloquine with nebivolol may lead to an elongation of the QT interval.

Insulin and other hypoglycemic drugs: although nebivolol does not affect the level of glucose, its use simultaneously with insulin and other hypoglycemic drugs can mask symptoms of hypoglycemia

(palpitation and tachycardia).

When used simultaneously with eye drops containing beta-blockers, the effect of nebivolol may be enhanced.

Pharmacokinetic interaction

When used simultaneously with drugs inhibiting the reuptake of serotonin, or with other agents biotransforming with the participation of the isoenzyme CYP2D6, the metabolism of nebivolol slows down.
With the simultaneous use of nebivolol does not affect 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 does not affect the pharmacological parameters of nebivolol.
With the simultaneous use of nebivolol with nicardipine, concentrations of active substances in the blood plasma increase slightly, but this has no clinical significance.

The simultaneous administration of ethanol, furosemide or hydrochlorothiazide does not affect the pharmacokinetics of nebivolol.

There is no clinically relevant interaction, nebivolol and warfarin.
With the simultaneous use of sympathomimetic drugs suppress the activity of nebivolol.
TERMS OF RELEASE FROM PHARMACY

On prescription.

TERMS AND CONDITIONS OF STORAGE

Does not require special storage conditions.
Keep out of the reach of children. Shelf life - 3 years.
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