Universal reference book for medicines
Name of the drug: NEBIKOR ADIFHARM (NEBICOR ADIPHARM)

Active substance: nebivolol

Type: Beta 1 -adrenoblock III generation with vasodilating properties

Manufacturer: ADIPHARM (Bulgaria)
Composition, form of production and packaging
Tablets are
round, biconvex, white with a cross-shaped risk.

1 tab.

nebivolol (in the form of hydrochloride) 5 mg

Excipients: lactose monohydrate, crospovidone, poloxamer, povidone, microcrystalline cellulose, magnesium stearate.

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

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

PHARMACHOLOGIC EFFECT

Nebivolol is a lipophilic, cardioselective beta-adrenoblocker of the third generation with vasodilating properties.
Has antihypertensive, anti-anginal and antiarrhythmic effect. Reduces elevated blood pressure at rest, with physical stress and stress. Competitively and selectively blocks synaptic and postsynaptic beta-1 adrenergic receptors, making them inaccessible to catecholamines, modulating the release of the endothelial vasodilating factor of nitric oxide (NO). Nebivolol is a racemate consisting 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 of beta1-adrenergic receptors (affinity for beta 1-adrenergic receptors is 293 times higher than for beta2-adrenergic receptors).

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. This effect persists with long-term treatment. The hypotensive effect is also due to a decrease in the activity of the renin-angiotensin-aldosterone system (does not directly correlate with changes in renin activity in the blood plasma).
The use of nebivolol improves the indices of systemic and intracardiac hemodynamics.
Nebivolol reduces the heart rate and blood pressure at rest and during exercise, reduces the end-diastolic pressure of the left ventricle, reduces the overall peripheral vascular resistance, improves the 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 improves the tolerance of exercise.
Antiarrhythmic effect is due to the suppression of the heart's automaticity (including in the pathological focus) and the slowing of atrioventricular (AV) conduction.
PHARMACOKINETICS

After oral administration, nebivolol is rapidly absorbed from the gastrointestinal tract.
Eating does not affect the absorption of the drug, 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. The clearance in the blood plasma in most patients (with "fast" metabolism) is reached 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.
The association with blood plasma proteins (mainly with albumin) for D-nebivolol is 98.1%, and for L-nebivolol - 97.9%.

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.
After the administration 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 T 1/2 values ​​of the enantiomers of Nebivolol from blood plasma are an average of 10 hours. In patients with a "slow" metabolism, these values ​​increase 3-5-fold. In patients with "fast" metabolism, the T 1/2 values ​​of the hydroxy metabolites of both enantiomers from the blood 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; chronic heart failure (as an adjunct to standard therapy with diuretics, cardiac glycosides, angiotensin converting enzyme (ACE) inhibitors, angiotensin II receptor antagonists).
DOSING MODE

Tablets are taken inside at the same time of the day, regardless of food intake, tablets can be divided in half and into four identical parts (but not chewed) and washed down with liquid.

Arterial hypertension.
The average daily dose is 5 mg (1 tablet) at one time. 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 monotherapy or as part of a combination therapy.
If necessary, the daily dose can be increased to 10 mg (2 tablets) at one time.
The maximum daily dose is 10 mg.
In patients with renal insufficiency, as well as in patients older than 65 years, the initial dose is 2.5 mg (1/2 tablet) at one time.
If necessary, increase the dose to 5 mg.
At the expressed infringements of function of kidneys (KK less than 20 ml / mines) and at patients with serious diseases of a liver the maximum daily dose makes 10 mg.

Increasing the dose in these patients should be done with extreme caution.

Chronic heart failure.
Treatment should begin with a gradual increase in the dose until an individual optimal maintenance dose is reached. The dose selection 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 (1/4 tablet) 1 time per day can be increased first to 2.5 mg to 5 mg 1/2 tablets - 1 tablet) per day in a single dose, and then - up to 10 mg (2 tablets) per day. in one step. 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 for the therapy of chronic heart failure is 10 mg of the drug per day. in one step. 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 the drug or, if necessary, immediately stop it (in case of pronounced arterial hypotension, worsening of the course of chronic heart failure with acute pulmonary edema, in case of cardiogenic shock, symptomatic bradycardia or AV blockade).

SIDE EFFECT

From the side of the central nervous system: headache, dizziness, fatigue, paresthesia, depression, decreased ability to concentrate, drowsiness, insomnia, nightmarish dreams, 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 course of chronic cardiac insufficiency (occurs mainly during the titration of the dose of the drug), marked decrease in blood pressure.

Allergic reactions from the skin: skin itching, erythematous rash, angioedema, skin flushing, 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, visual impairment (dry eyes), impaired potency.

CONTRAINDICATIONS

- Hypersensitivity to nebivolol or excipients;

- pronounced violations of the liver function;

- acute heart failure;

- cardiogenic shock;

- Chronic heart failure in the stage of decompensation (requiring inotropic therapy);

- syndrome of weakness of the sinus node, including sinoatrial block;

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

- bronchospasm and bronchial asthma;

- Depression;

metabolic acidosis;

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

- arterial hypotension;

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

- lactose intolerance, lactase deficiency or glucose-galactose malosorption (the preparation contains lactose);

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

- age up to 18 years;

- lactation period;

- simultaneous administration with floktaphenin, sultopride.

Carefully.
Severe renal insufficiency (creatinine clearance less than 20 ml / min), impaired liver function, diabetes mellitus, hyperthyroidism, desensitizing therapy, psoriasis, first degree I blockade, Prinzmetal angina, chronic obstructive pulmonary disease (COPD), elderly patients (over 65 years of age).
PREGNANCY AND LACTATION

In pregnancy, the drug is prescribed only on strict indications if the intended benefit for the mother exceeds the potential risk to the fetus (due to possible development in 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.
Studies in animals have shown that nebivolol excreted in breast milk.
There is no data on the isolation of nebivolol in breast milk. Therefore, the use of the drug is not recommended for women during lactation. If taking the drug during lactation is necessary, then breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER

With caution: severe renal failure (creatinine clearance (CK) less than 20 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in severe violations of liver function.

With caution: a violation of the liver.

APPLICATION FOR CHILDREN

Contraindicated at the age of 18 years.

APPLICATION IN ELDERLY PATIENTS

With caution: patients of advanced age (over 65 years).

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

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 on the use of Nebicor, patients with psoriasis should carefully correlate the intended benefit and possible risk of exacerbation of psoriasis.
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, the anesthetist should be warned that the patient is taking nebivolol.

Nebivolol does not affect the concentration of glucose in the blood plasma in patients with diabetes mellitus.
Nevertheless, care should be taken in the treatment of these patients, since nebivolol can mask certain symptoms of hypoglycemia (eg, tachycardia) caused by the use of hypoglycemic agents.
Control of the concentration of glucose in the blood plasma should be done 1 time in 4-5 months (in patients with diabetes mellitus).

Beta-adrenoblockers should be used with caution in patients with COPD, as bronchospasm may increase.

With hyperthyroidism, the drug masks tachycardia.
Beta-adrenoblockers can increase sensitivity to allergens and the severity of anaphylactic reactions.
The effectiveness of beta-blockers in smokers is lower than in non-smoking patients.

Impact on the ability to drive and other complex mechanisms

Research has shown that nebivolol has no effect on the rate of psychomotor reactions.
Pilots flying crew with arterial 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 experience side effects, most often dizziness, due to lowered 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

Data on overdose are absent.

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

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, with / in the administration of liquid and vasopressors.
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 blockade (II-III st.) It is recommended iv administration of beta-adrenomimetics, 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 beta2-adrenomimetiki. With ventricular extrasystole - lidocaine (do not administer antiarrhythmic drugs IA class).
DRUG INTERACTION

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

Sul- topride: 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 and diltiazem), the effect on contractility of the myocardium and AV conduction is increased.
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).
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, there is 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 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.

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 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 pharmacokinetic 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.

Simultaneous administration of ethanol, furosemide or hydrochlorothiazide does 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 preparation should be stored at a temperature not exceeding 30 ° C.
Keep out of the reach of children.
Shelf life - 3 years.
Do not use after the expiry date printed on the package.
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