Nebilong, pills 5mg, 50pcs

Composition

Active ingredient:

Nebivolol hydrochloride 5.56 mg.

Equivalent Nebivolol 5.0 mg.

Auxiliary substances:

Lactose monohydrate – 60,44 mg,

microcrystalline cellulose – 57,00 MI;

betadex – 30,00 mg,

docusate sodium – 2,00 mg,

croscarmellose sodium – 24,00 mg,

povidone -5,00 mg,

silicon dioxide colloid – 2,00 mg,

talc – 2,00 mg,

magnesium stearate – 2,00 mg.

Pharmacological action

of NEBILONG is highly competitive blocker -adrenergic receptors. Due to the metabolic interaction with L-arginine / nitric oxide, it shows a moderate vasodilator effect. In therapeutic doses, it does not show membrane-stabilizing and drainage-blocking activity. Reduces heart rate and blood pressure at rest, as well as during exercise, both in patients with normal blood pressure and with arterial hypertension. The antihypertensive effect persists with prolonged treatment. Food intake does not affect the absorption of Nebilong. Nebivolol is metabolized by alicyclic and aromatic hydroxylation, N-dealkylation, and glucuronidation; in addition, hydroxymetabolite glucuronides are formed. Pharmacokinetics. The oral bioavailability of nebivolol is on average 12% in patients whose body metabolizes it rapidly; full bioavailability is noted in patients whose body metabolizes nebivolol slowly. In individuals with fast metabolism, the half-life of nebivolol enantiomers is 10 hours, in individuals with slow metabolism — 3-5 times longer. The state of equilibrium concentration in blood plasma for nebivolol in most patients is reached within 24 hours, and for hydroxymetabolites – after several days. Binding to plasma proteins for SRRR-nebivolol is 98.1%, and for RSSS-nebivolol-97.9%. One week after use, approximately 38% of the nebivolol dose is excreted in the urine and 48% in the faeces. No more than 0.5% of nebivolol is excreted unchanged in the urine.

Indications

• Arterial hypertension.
• Prevention of stable angina attacks in patients with ischemic heart
• disease and chronic heart failure (as part of combination therapy).

Contraindications

• Hypersensitivity to the Active ingredient or one of the components of the drug and to other beta-blockers.
• Severe liver function disorders.
• Acute heart failure.
• Cardiogenic shock.
• Chronic heart failure in the stage of decompensation (requiring inotropic therapy).
• Sinus node weakness syndrome, including sinoatrial block.
• Grade II and III atrioventricular block (without artificial pacemaker).
• Bronchial obstructive syndrome in chronic obstructive pulmonary disease and bronchial asthma; severe forms of bronchial asthma and chronic obstructive pulmonary disease in the anamnesis.
• Pheochromocytoma (without simultaneous use of alpha-blockers).
• Depression
• Metabolic acidosis.
• Bradycardia (Heart rate less than 60 beats / min).
• Severe arterial hypotension (systolic blood pressure less than 90 mmri).
• Severe peripheral atherosclerosis.
• Age up to 18 years (efficacy and safety have not been established).
• Lactose intolerance, lactase deficiency, or glucose-galactose malsorption (the drug contains lactose).
• Simultaneous use with floctafenin, sultoprid.

With caution:

• Kidney failure.
• Liver function disorders.
• Diabetes mellitus.
• Hyperthyroidism.
• History of bronchospasm episodes.
• A history of allergic diseases (possibly increased sensitivity to allergens, increased severity of allergic reactions, and decreased response to epinephrine).
• Psoriasis.
• Grade I atrioventricular block.
• Prinzmetal angina pectoris.
• Chronic obstructive pulmonary disease (COPD).
• Age (over 65 years).
• Peripheral atherosclerosis.

Side effects

The frequency of side effects is presented in the following gradation:

Very often (more than 10%).

Often (more than 1% and less than 10%).

Infrequently (more than 0.1% and less than 1%).

Rarely (more than 0.01% and less than 0.1%).

Very rare (less than 0.01%), including individual messages.

Nervous system disorders:

Often – headache, Dizziness, fatigue, weakness, Paresthesia.

Infrequently – Depression, vivid dreams, confusion, insomnia.

Very rarely – Fainting hallucinations, Amnesia.

Disorders of the gastrointestinal tract:

Often – nausea, constipation, diarrhea.

Infrequently-dyspepsia, flatulence, vomiting.

Disorders of the cardiovascular system:

Infrequently – bradycardia, acute heart failure, atrioventricular block, Orthostatic hypotension peripheral circulatory disorders (feeling” cold ” in the extremities, cyanosis), shortness of breath, cardiac arrhythmias, Raynaud’s syndrome, peripheral edema, cardialgia, worsening of the course of CHF 1, a pronounced decrease in blood pressure.

Skin and subcutaneous tissue disorders:

Infrequently – erythematous skin rash, pruritus, hyperemia of the skin.

Very rarely-aggravation of the course of psoriasis, alopecia.

In some cases – angioedema.

Respiratory system disorders:

Infrequently-bronchospasm (including in the absence of obstructive pulmonary diseases in the anamnesis), bronchospasm in patients with bronchial asthma or a history of airway obstruction.

Other services: Photodermatosis, hyperhidrosis, visual disturbances (dry eyes), sexual dysfunction.

Interaction

When used concomitantly with drugs that inhibit serotonin reuptake or other agents that biotransform with the participation of the CYP2D6 isoenzyme, nebivolol metabolism slows down, which may lead to the risk of developing bradycardia.

Concomitant use of nebivolol did not affect the pharmacokinetic parameters of digoxin.

When used concomitantly with cimetidine, the concentration of nebivolol in blood plasma increases (there are no data on the effect on the pharmacological effects of the drug).

Concomitant use of ranitidine did not affect the pharmacokinetic parameters of nebivolol.

Rifampicin increases the metabolism of nebivolol.

Concomitant use of nebivolol and nicardipine resulted in a slight increase in plasma concentrations of active substances, but this is not clinically relevant.

Concomitant use of ethanol, furosemide, or hydrochlorothiazide did not affect the pharmacokinetics of nebivolol.

There was no clinically significant interaction between nebivolol and warfarin.

When used concomitantly, sympathomimetic agents inhibit the activity of nebivolol.

When nebivolol is co-administered with insulin and hypoglycemic agents for oral use, symptoms of hypoglycemia (tachycardia, tremor) may be masked.

How to take, course of use and dosage

Nebilong should be taken orally, once a day, preferably at the same time, regardless of food intake, without chewing and with a sufficient amount of liquid.

With arterial hypertension:

The average daily dose for the treatment of arterial hypertension is 5 mg (1 tablet) once a 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 monotherapy or as part of a combination therapy.

If necessary, the daily dose can be increased to 10 mg. The maximum daily dose is 10 mg.

In patients with renal insufficiency, as well as in patients over the age of 65 years

The initial dose is 2.5 mg / day. If necessary, the dose is increased to 5 mg.

In severe renal impairment (creatinine clearance less than 20 ml / min) and in patients with liver disease, the maximum daily dose is 10 mg.

Increasing the dose in such patients should be carried out with extreme caution.

In patients with chronic heart failure (CHF):

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

Dose selection at the beginning of treatment should be carried out according to the following scheme, maintaining intervals of up to two weeks and based on the patient’s tolerance to this dose: the dose of 1.25 mg (1/2 tablet of 2.5 mg) once a day can be increased first to 2.5-5 mg once a day of Nebilong, and then to 10 mg once a day. The patient should be monitored by a doctor for 2 hours after taking the first dose of the drug, as well as after each subsequent increase in the dose. Each dose increase should be carried out at least 2 weeks later. {The maximum recommended dose for CHF therapy is 10 mg of Nebilong 1 time per day. During titration, regular monitoring of blood pressure, heart rate, and CHF symptoms is recommended.

During the titration phase, if the course of chronic heart failure or drug intolerance worsens, it is recommended to reduce the dose of Nebilong or, if necessary, immediately stop taking it (in case of pronounced arterial hypotension, worsening of CHF with acute pulmonary edema, in case of cardiogenic shock, symptomatic bradycardia or AV block).

Overdose

Symptoms: marked decrease in blood pressure, bradycardia, severe intracardiac conduction disorders, shock, asystole, respiratory arrest, bronchospasm, loss of consciousness, coma, convulsions, nausea, vomiting, cyanosis, hypoglycemia, hyperkalemia.

Treatment: gastric lavage, taking activated charcoal. In case of a marked decrease in blood pressure, it is necessary to give the patient a horizontal position with raised legs, if necessary, intravenous use of fluid and vasopressors.

With bradycardia,0.5-2 mg of atropine is administered intravenously; in the absence of a positive effect, a transvenous or intracardiac artificial pacemaker is possible.

In case of AV block (I-III st. ), intravenous use of beta-adrenomimetics is recommended; if they are ineffective, an artificial pacemaker should be considered. In case of heart failure, treatment begins with the introduction of cardiac glycosides and diuretics, if there is no effect, it is advisable to introduce dopamine, dobutamine or vasodilators. With bronchospasm, beta-2-adrenomimetics are administered intravenously. For convulsions-intravenous use of diazepam.

For ventricular extrasystole, lidocaine (class IA antiarrhythmics should not be administered).

Special instructions

Withdrawal of beta-blockers should be carried out gradually, over 10 days (up to 2 weeks in patients with coronary heart disease.

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

In elderly patients, monitoring of renal function is necessary (1 time in 4-5 months).

With angina pectoris, the selected dose of the drug should provide a resting heart rate in the range of 55-60 beats / min., with a load of no more than 110 beats / min.

When deciding whether to use Nebilong in patients with psoriasis, the expected benefit of the drug should be carefully correlated with the possible risk of exacerbation of psoriasis.

When performing surgical procedures, the surgeon/anesthesiologist should be warned that the patient is taking Nebilong.

Nebivolol does not affect the plasma glucose concentration in patients with diabetes mellitus. However, caution should be exercised when treating these patients, as Nebilong may mask certain symptoms of hypoglycemia (such as tachycardia) caused by the use of hypoglycemic agents.

Monitoring of glucose concentration in blood plasma should be carried out once every 4-5 months (in patients with diabetes mellitus).

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

With hyperthyroidism, the drug levels tachycardia.

Beta-blockers may increase sensitivity to allergens and the severity of anaphylactic reactions.

The effectiveness of beta-blockers in smokers is lower than in non-smokers.

Influence on the ability to drive motor vehicles and manage mechanisms:

During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25°C.

Shelf life

3 years

Active ingredient

Nebivolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For pregnant women as prescribed by a doctor, for Nursing mothers as prescribed by a doctor, For adults as prescribed by a doctor

Indications

Angina, Hypertension, Arrhythmia, Heart Failure