Nebilong, tablets 5 mg 50 pcs

NEBILONG is a highly selective competitive -adrenoreceptor blocker. Due to metabolic interaction with L-arginine/nitric oxide it shows moderate vasodilator effect. In therapeutic doses it does not exhibit membrane stabilizing and draining activity. It decreases HR and BP at rest and during exercise both in patients with normal BP and in those with arterial hypertension.

Indications

Active ingredient

Composition

Active ingredient:

Nebivololol hydrochloride 5.56 mg.

The equivalent of Nebivololol 5.0 mg.

Auxiliary Ingredients:

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,

colloidal silica – 2.00 mg,

talk – 2.00 mg,

magnesium stearate – 2.00 mg.

How to take, the dosage

Nebilong should be taken orally, once daily, preferably at the same time, regardless of meals, without chewing and with plenty of fluid.

In arterial hypertension:

The average daily dose to treat arterial hypertension is 5 mg (1 tablet) once daily. 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 combined therapy.

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

In patients with renal insufficiency and in patients over 65 years of age

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

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

Dose escalation in such patients should be carried out with extreme caution.

In chronic heart failure (CHF):

The treatment of chronic heart failure should begin with a gradual increase in dose until an individual optimal maintenance dose is reached.

The dose selection at the beginning of treatment should follow the following pattern, at intervals of up to two weeks and based on patient tolerance of this dose: a dose of 1.25 mg (1/2 tablet of 2.5 mg) once daily may be increased first to 2.5 5 mg once daily with Nebilong and then to 10 mg once daily. The patient should be monitored by a physician for 2 hours after the first dose of the drug and after each subsequent dose increase. Each dose increase should be at least 2 weeks later. {Maximal recommended dose in therapy of CHF is 10 mg of Nebilong once daily. During titration, regular monitoring of BP, HR and symptoms of CHF severity is recommended.

When titration phase occurs with worsening chronic heart failure or intolerance of the drug it is recommended to decrease Nebilong dosage or if necessary discontinue it immediately (in case of marked arterial hypothermia, worsening CHF course with acute pulmonary edema, if cardiogenic shock, symptomatic bradycardia or AV blockade develop).

Interaction

In concomitant use with drugs that inhibit serotonin reuptake or other agents biotransformed with the participation of CYP2D6 isoenzyme, nebivololol metabolism is delayed, which may lead to a risk of bradycardia.

When used concomitantly, nebivololol had no effect on the pharmacokinetic parameters of digoxin.

Concomitant use with cimetidine increases plasma concentrations of nebivololol (data on the effect on the pharmacological effects of the drug are not available).

The concomitant use of ranitidine had no effect on the pharmacokinetic parameters of nebivololol.

Rifampicin increases the metabolism of nebivololol.

Concomitant use of nebivololol with nicardipine slightly increased plasma concentrations of the active substances, but this has no clinical significance.

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

No clinically significant interaction between nebivololol and warfarin has been established.

In concomitant use, sympathomimetic agents inhibit the activity of nebivololol.

When nebivololol is coadministered with insulin and hypoglycemic agents for oral administration, symptoms of hypoglycemia (tachycardia, tremor) may be masked.

Special Instructions

The withdrawal of beta-adrenoblockers should be done gradually, over 10 days (up to 2 weeks in patients with coronary heart disease.

The monitoring of BP and heart rate at the start of therapy should be daily.

In elderly patients, monitoring of renal function is necessary (once every 4-5 months).

In tension angina, the selected dose of the drug should provide a resting heart rate of 55-60 beats/min, on exertion no more than 110 beats/min.

When considering the use of Nebilong in patients with psoriasis, the anticipated benefit of the drug must be carefully weighed against the possible risk of exacerbation of the psoriasis.

The surgeon/anesthesiologist should be advised when performing surgical procedures that the patient is taking Nebilong.

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

Plasma glucose concentrations should be monitored once every 4-5 months (in diabetic patients).

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

The drug levels out tachycardia if thyroid hyperfunction occurs.

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

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

Impact on ability to drive and operate machinery:

During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and rapid psychomotor reactions.

Contraindications

With caution:

Side effects

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

Very common (more than 10%).

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

Infrequent (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 reports.

Nervous system disorders:

Often – Headache, Dizziness increased fatigue, weakness, Paresthesias.

Infrequent – Depression, vivid dreams, confusion, insomnia.

Very rare – Fainting hallucinations, Amnesia.

Gastrointestinal tract disorders:

Often – nausea, constipation, diarrhea.

Infrequent – dyspepsia, flatulence, vomiting.

Cardiovascular system disorders:

Infrequent – bradycardia, acute heart failure, atrioventricular block, Orthostatic hypotension peripheral circulatory disorders (feeling of “cold” in extremities, cyanosis), shortness of breath, heart rhythm disorders, Raynaud syndrome, peripheral edema, cardialgia, worsening the course of CHF 1 , marked BP reduction.

Skin and subcutaneous tissue disorders:

Infrequent – erythematous skin rash, pruritus, cutaneous hyperemia.

Very rarely – worsening of the course of psoriasis, alopecia.

In isolated cases – angioedema.

Respiratory system disorders:

Infrequent – bronchospasm (including in the absence of obstructive lung disease in the history), bronchospasm in patients with bronchial asthma or airway obstruction in the history.

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

Overdose

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

Treatment: gastric lavage, administration of activated charcoal. In case of marked BP decrease the patient should be placed in a horizontal position with elevated legs, if necessary, IV administration of fluids and vasopressors.

In case of bradycardia, 0.5-2 mg of atropine is administered by IV, in the absence of a positive effect, transvenous or intracardiac artificial pacemaker can be placed.

In AV blockade (stage I-III), intravenous administration of beta-adrenomimetics is recommended, and if they are ineffective, the placement of an artificial pacemaker should be considered. In case of cardiac insufficiency, treatment begins with administration of cardiac glycosides and diuretics; if there is no effect, administration of dopamine, dobutamine or vasodilators is reasonable. In bronchospasm, intravenous beta 2 -adrenomimetics are administered. For seizures, intravenous diazepam.

In case of ventricular extrasystole, lidocaine (Class IA antiarrhythmic agents should not be administered).

Similarities