Nebilan Lannacher - instructions for use, dose, side effects, contraindications

Excipientslactose monohydrate 143.475 mg, corn starch 34.50 mg, croscarmellose sodium 13.80 mg, hypromellose (6cps) 3.45 mg, microcrystalline cellulose 26.45 mg, silicon dioxide colloid 0.575 mg, magnesium stearate 2.30 mg.

Description:Round biconvex tablets white or almost white with a cross-shaped notch.

Pharmacotherapeutic group:Beta-1-blocker selective

ATX: & nbsp

C.07.A.B.12 Nebivolol

Pharmacodynamics:

Cardioselective beta-1-adrenoblocker of the third generation with vasodilating properties; has antihypertensive, anti-anginal and antiarrhythmic effect. It selectively and competitively blocks synaptic and postsynaptic beta-1-adrenergic receptors, making them unavailable for catecholamines, modulates the release of the endothelial vasodilating factor (NO). Nebivolol reduces the heart rate (heart rate) and lowers blood pressure (BP) at rest and at physical exertion, improves the 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 LNebivolol, which have different pharmacodynamic properties. D-nebivolol is a competitive and highly selective beta-1-adrenergic 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 caused by a decrease in cardiac output, a decrease in the volume of circulating blood (BCC) and the overall peripheral vascular resistance, and 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 suppression of pathological automatism of the heart (including in the pathological focus);and slowing of atrioventricular (AV) conductivity.

Pharmacokinetics:

Suction

After application inside nebivolol quickly absorbed from the gastrointestinal tract. The intake of food does not affect the absorption of the drug, therefore nebivolol can be taken regardless of food intake. Bioavailability - after ingestion is about 12% in individuals with "fast" metabolism and is almost complete in individuals with "slow" metabolism. The effectiveness of nebivolol does not depend on the metabolic rate.

Distribution

Connection with plasma proteins for DNebivolol - 98.1%, for L- nebivolol - 97.9%.

Metabolism

Nebivolol is metabolized by acyclic or aromatic, hydroxylation, N-decalcification and glucuronation, in addition, glucuronides of hydroxy metabolites are formed. The metabolism of nebivolol along the path of aromatic hydroxylation is affected by the genetic polymorphism of the enzyme system CYP2D6. In patients with "fast" metabolism, the values of the half-life (T1 / 2) of enantiomers of nebivolol averagely average 10 hours, in patients with a "slow" metabolism, these values increase 3-5 times.T1 / 2 hydroxymetabolites are 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 achieved 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 kidneys does not exceed 0.5% of the accepted dose.

Indications:

Arterial hypertension (monotherapy or in combination with other anti-hypertensive drugs);

Ischemic heart disease: prevention of attacks of stable angina pectoris;

Chronic heart failure (as part of combination therapy).

Contraindications:

Hypersensitivity to nebivolol or other components of the drug;

Severe liver dysfunction;

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

AV blockade II-III degree;

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

Pronounced bradycardia (heart rate less than 50 / min);

Pronounced arterial hypotension;

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

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 to 18 years;

Lactation period.

Carefully:

Carefully the drug should be used in case of severe renal failure (creatinine clearance less than 20 ml / min), liver function disorders, diabetes mellitus, hyperthyroidism, desensitizing therapy, psoriasis, atrioventricular blockade I, grade, Prinzmetal angina, chronic obstructive pulmonary disease (COPD) ), in elderly patients (over 65 years).

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 use of the drug during lactation - it is necessary, then breastfeeding should be stopped.

Dosing and Administration:

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

When Arterial hypertension and ischemic heart diseasea 2.5 - 5 mg (1/2 tablets of 5 mg - 1 tablet of 5 mg) once a 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 of the initial dose, is 2.5 mg / day (1/2 tablet of 5 mg). If necessary, increase the dose to 5 mg. At expressed, infringements kidney function (QC less than 20 ml / min), the maximum daily dose is 10 mg. Increasing 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, it is necessary to carry out the following scheme, maintaining weekly intervals and based on the patient's per-tolerance of this dose: a dose of 1.25 mg Nebilan® Lannacher (1/4 tablets 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) once a 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 for CHF therapy is 10 mg once a day. During titration, regular monitoring of PD, 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 development, cardiogenic shock, symptomatic bradycardia or AV blockade).

Side effects:

From the nervous system: headache, dizziness, fatigue, paresthesia; depression, drowsiness, nightmares, hallucinations, confusion, psychosis, convulsions, insomnia, amnesia.

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

From the side of the cardiovascular system: bradycardia, orthostatic hypotension, dyspnea, swelling, AV blockade, aggravation of the course of chronic heart failure, aggravation of "intermittent" lameness-heart rhythm disturbances, Raynaud's syndrome, cardialgia, marked decrease in blood pressure.

From the side of the organ of vision: impaired vision (dry eyes).

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

From 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 history, rhinitis.

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

Overdose:

Symptoms: a 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 carbon; 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 electrostimulation is possible; 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. With ventricular extrasystole - lidocaine (preparations of class 1a are not applied). With convulsions - in / in diazepam.

Interaction:

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

Sultopride: increased risk of developing, ventricular arrhythmia, especially by the type of "pirouette" (torsade des pointes).

With simultaneous use of beta-blockers with blockers of "slow" calcium channels (BCC) (verapamil, diltiazem) the negative effect on myocardial contractility increases, and AV conductivity. 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 combined with prazosin).

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

With the simultaneous use of nebivolol with cardiac glycosides, no effect on slowing AV conductivity.

The simultaneous use of nebivolol to 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 an 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, so correction of the dose of antihypertensive drugs is required.

Mefloquine: theoretically, the joint administration of mefloquine with nebivolol can lead to lengthening of the interval QT.

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

When used concomitantly with eye drops containing beta-adrenoblockers, the effect of nebivolol can be enhanced.

Fermacokinetic interaction

With simultaneous use with drugs that inhibit the inverseseizure of serotonin, or with other agents biotransforming with the participation of isoenzyme CYP2D6, the metabolism of nebivolol slows down.

With simultaneous application nebivolol no impact on the pharmacokinetic parameters of digoxin.

With simultaneous application, with cimetidine, the concentration of nebivolol in the plasma increases (data on the effect on the pharmacological effects of the drug are absent). The simultaneous use of ranitidine does not affect the pharmacological 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 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, inhibit the activity of nebivolol.

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 the heart rate and blood pressure, at the beginning of the procedure - daily for the concentration of glucose in the blood of diabetic patients (1 time in 4- 5 months). In elderly patients it is recommended to monitor kidney function (1 time in 4-5 months).

Beta-blockers 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, 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 who use contact lenses should take into account that against the background of treatment with beta-adrenoblockers. 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).

Effect on the ability to drive transp. cf. and fur:Any negative impact on the ability to drive vehicles or other complex mechanisms against the background of Nebilan® Lannacher was not observed, but caution should be exercised when driving vehicles and mechanisms.

Form release / dosage:

Tablets 5 mg.

Packaging:

For 10 tablets in PVC / Al blister.

For 2 or 3 blisters together with instructions for use in a cardboard box.

Storage conditions:

Does not require special storage conditions.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000647

Date of registration:28.09.2011 / 12.11.2013

Expiration Date:28.09.2016

The owner of the registration certificate:VALEANT, LLC VALEANT, LLC Russia

Manufacturer: & nbsp

G. L. Pharma GmbH

Representation: & nbspVALEANT LLC VALEANT LLC Russia

Information update date: & nbsp18.06.2018

Illustrated instructions

Instructions

Nebilan® Lannacher (Nebilan Lannacher)