Nebivolol-Teva, pills 5mg 28pcs

Composition

1 tablet contains: Active ingredient: nebivolol hydrochloride – 5.45 mg, which corresponds to nebivolol in the amount of 5 mg; additional components: corn starch, lactose monohydrate, colloidal silicon dioxide, microcrystalline cellulose, magnesium stearate, hypromellose-E 15, croscarmellose sodium.

Pharmacological action

Beta-1-adrenoblocker SELECTIVETX: C. 07. A. B. 12 Nebivolol Pharmacodynamics : Cardioselective β1-adrenoblocker. Nebivolol has antihypertensive, antianginal and antiarrhythmic effects. Reduces high blood pressure (BP) at rest, during physical exertion and stress. Competitively and selectively blocks postsynaptic β1-adrenergic receptors, making them inaccessible to catecholamines, modulates the release of endothelial vasodilating factor nitric oxide (NO). Nebivolol is a racemate of two enantiomers:  SRRR-nebivolol (D-nebivolol) and RSSS-nebivolol (L-nebivolol), combining two pharmacological actions:

D-nebivolol is a competitive and highly selective blocker of β1-doporeceptors;

L-nebivolol has a mild vasodilator effect by modulating the release of vasodilating factor (NO) from the vascular endothelium.

The antihypertensive effect is also due to a decrease in the activity of the renin – angiotensin-aldosterone system (RAAS) (it does not directly correlate with changes in the activity of renin in blood plasma).

A stable antihypertensive effect develops after 1-2 weeks of regular use of the drug, and in some cases-after 4 weeks, a stable effect is noted after 1-2 months.

Nebivolol reduces the number and severity of angina attacks and increases exercise tolerance by reducing the need for oxygen in the myocardium (reduction of heart rate, reduction of preload and afterload). The antiarrhythmic effect is due to the suppression of pathological automatism of the heart (including in the pathological focus) and slowing of atrioventricular conduction. Pharmacokinetics:

Suction

After oral use, both enantiomers are rapidly absorbed. Food intake does not affect absorption, so nebivolol can be taken regardless of food intake. The bioavailability of orally administered nebivolol is on average 12% in patients with a “fast” metabolism (the “first pass” effect) and is almost complete in patients with a” slow ” metabolism.

Distribution

In blood plasma, both enantiomers are predominantly bound to albumin. Binding to plasma proteins is 98.1% for D-nebivolol and 97.9% for L-nebivolol. Deduction

Nebivolol is metabolized by alicyclic and aromatic hydroxylation, partial N-dealkylation. The metabolism of nebivolol by aromatic hydroxylation is CYP2D6 dependent and is characterized by a genetically determined polymorphism. The resulting hydroxy and amino derivatives are conjugated with glucuronic acid and are excreted as O – and N-glucuronides by the kidneys (38%) and through the intestines (48%).

Half-life (T 1/2) in patients with “fast” metabolism: hydroxymetabolites-24 hours, nebivolol enantiomers-10 hours; in patients with “slow” metabolism: hydroxymetabolites-48 hours, nebivolol enantiomers-30-50 hours. Excretion of unchanged nebivolol through the kidneys is less than 0.5% of the dose of the drug taken orally.

Indications

Arterial hypertension;

Ischemic heart disease: prevention of tension-type angina attacks; chronic heart failure (as part of combination therapy).

Contraindications

– Hypersensitivity to the Active ingredient or to any component of the drug;

acute heart failure;

– chronic heart failure in the stage of decompensation (requiring intravenous drugs with inotropic action); severe hypotension (systolic BP less than 90 mm Hg. St. ) the syndrome of weakness of the sinus node, including sinoauricular blockade; atrioventricular block II and III degree (without an artificial pacemaker); bradycardia (heart rate less than 60 beats/min);

– cardiogenic shock; pheochromocytoma (without the simultaneous use of alpha-blockers); metabolic acidosis;

severe disturbances of liver function;

– bronchospasm and bronchial asthma in history;

– severe violations of peripheral blood circulation (intermittent claudication, Raynaud’s syndrome);

– lactose intolerance, lactase deficiency syndrome glucose-galactose malabsorption;

– simultaneous reception with floctafenine, sultopride the age of 18 years (efficacy and safety in this age group have not been studied).

With caution:

– Renal failure;

– diabetes mellitus;

– hyperthyroidism;

– burdened allergic history;

– psoriasis;

– chronic obstructive pulmonary disease; atrioventricular block I degree;

– Prinzmetal angina pectoris;

– peripheral circulatory disorders;

– liver function disorders;

– age over 75 years.

Side effects

the Frequency of adverse reactions listed below were determined according to the following (classification of the world health organization): very often – at least 10%; often – not less than 1% but < 10%; infrequently – no more than 0.1% but < 1%; rarely – not less than 0.01%, but less than 0.1%; very rarely – less than 0.01%, including individual messages.

Mental disorders:

Infrequently:  depression, “nightmarish” dreams, confusion.

Nervous system disorders:

Often:  headache, dizziness, fatigue, weakness, paresthesia. Very rare:  fainting, hallucinations.

Gastrointestinal disorders:

Often:  nausea, constipation, diarrhea.

Infrequently:  dyspepsia, flatulence, vomiting.

Cardiac disorders:

Infrequently:  bradycardia, acute heart failure, atrioventricular block.

Vascular disorders:

Infrequently:  intermittent or worse claudication, orthostatic hypotension, Raynaud’s syndrome.

Respiratory, thoracic and mediastinal disorders:

Common: dyspnoea

Infrequently:  bronchospasm.

Track and subcutaneous tissue disorders:

Infrequently:  erythematous skin rash, pruritus.

Very rare:  aggravation of psoriasis.

Immune system disorders:

Frequency unknown:  hypersensitivity reactions, angioedema.

Visual disturbances:

Infrequently:  reduced vision

Rarely:  dry eyes.

Disorders of the reproductive system and mammary glands:

Infrequently:  erectile dysfunction.

General disorders and reactions at the injection site:

Often:  increased fatigue, peripheral edema.

Interaction

When used concomitantly with Class I antiarrhythmic drugs, amiodarone may increase the negative inotropic effect and inhibit AV conduction.

When used concomitantly with calcium channel blockers (verapamil and diltiazem), the negative inotropic effect and inhibition of AV conduction are enhanced.

With intravenous use of verapamil while taking nebivolol, there is a risk of cardiac arrest (simultaneous use is contraindicated). Concomitant use of nebivolol with antihypertensive agents, nitroglycerin or slow calcium channel blockers may result in severe hypotension (special caution is necessary when combined with prazosin).

When used concomitantly with sympathomimetics, the pharmacological activity of nebivolol is suppressed.

When used concomitantly with anaesthetic agents, reflex tachycardia may be suppressed and the risk of hypotension may increase.

Concomitant use with tricyclic antidepressants, barbiturates, and phenothiazine derivatives may increase the antihypertensive effect of nebivolol.

Concomitant use with cimetidine may increase the concentration of nebivolol in blood plasma.

Concomitant use of nebivolol with drugs that inhibit serotonin reuptake or other agents that biotransform with the participation of the CYP2D6 isoenzyme increases the concentration of nebivolol in blood plasma, the metabolism of nebivolol slows down, which may increase the risk of bradycardia.

Concomitant use of nebivolol with insulin and oral hypoglycemic agents may mask the symptoms of hypoglycemia (tachycardia).

How to take it, course of use and dosage

Nebivolol-Teva tablets are taken orally, once a day, preferably at the same time, regardless of the meal time, with a sufficient amount of liquid.

Treatment of arterial hypertension and coronary heart disease

The average daily dose for the treatment of arterial hypertension and coronary heart disease is 2.5-5 mg (1/2 tablet – 1 tablet).

Nebivolol-Teva can be used alone or in combination with other blood pressure-lowering agents.

If necessary, the daily dose can be increased to a maximum of 10 mg (2 tablets 1 time a day).

Discontinuation of the drug should be carried out gradually, over 10-14 days, gradually reducing the dose.

Patients with impaired renal function

In patients with impaired renal function, the recommended starting dose is 2.5 mg (1/2 tablet 1 time per day). If necessary, the daily dose can be increased to a maximum of 5 mg (1 tablet once a day).

Patients with impaired liver function

Nebivolol should be administered with caution in patients with moderate hepatic impairment; the recommended starting dose is 2.5 mg (1/2 tablet once daily). The use of the drug in patients with severe hepatic impairment is contraindicated.

Elderly patients

In the treatment of arterial hypertension and coronary heart disease, the recommended starting dose for patients over 65 years of age is 2.5 mg (1/2 tablet 1 time per day). The maximum daily dose of the drug is 5 mg (1 tablet once a day).

Caution should be exercised in patients over 75 years of age due to the limited experience of using the drug in this category of patients. Patients over 75 years of age should be under close medical supervision while taking the drug.

Treatment of chronic heart failure

Treatment should be initiated if the patient has been stable for the last 6 weeks, with a slow increase in the dose until the individual optimal maintenance dose is reached.

Patients taking diuretics and/or digoxin and/or angiotensin-converting enzyme inhibitors and / or angiotensin II receptor blockers should take stable doses of these drugs for 2 weeks before starting nebivolol treatment.

Dose selection at the beginning of treatment should be carried out according to the following scheme: maintaining intervals from one to two weeks and focusing on the patient’s tolerance to this dose: the dose of 1.25 mg of Nebivolol-Teva (1/4 tablet of 5 mg) 1 time per day can be increased first to 2.5 – 5 mg 1 time per day of Nebivolol-Teva (1/2 tablet of 5 mg or 1 tablet), and then to 10 mg (2 tablets of 5 mg) 1 time per day.

The maximum daily dose is 10 mg once a day. At the beginning of treatment and with each dose increase, the patient should be under medical supervision for at least 2 hours to make sure that the clinical condition remains stable (especially: blood pressure, heart rate, conduction disorders, as well as symptoms of exacerbation of the course of chronic heart failure). To divide, place the tablet on a hard, flat surface with a cross-shaped notch facing up, and press the tablet with both index fingers. For a quarter (1/4) tablet, repeat the same steps with half (1/2) tablet.

During the selection of the dose of the drug, if the course of chronic insufficiency worsens or there is no therapeutic effect, the dose of the drug should be reduced or stopped if necessary (pronounced decrease in blood pressure, pulmonary edema, cardiogenic shock, symptomatic bradycardia, AV block).

Patients with impaired renal function

In patients with mild to moderate renal impairment, no dose adjustment is required. Nebivolol is not recommended for use in patients with chronic heart failure and severe renal impairment, as there is no experience of using the drug in this category of patients.

Overdose

There are no data on nebivolol overdose cases. Symptoms: bradycardia, marked decrease in blood pressure, severe bradycardia, AV block, cardiogenic shock, cardiac arrest, loss of consciousness, coma, nausea, vomiting, cyanosis, bronchospasm, acute heart failure.

Treatment: the patient is hospitalized and placed in the intensive care unit. Immediately it is necessary to determine the concentration of glucose in the blood. Gastric lavage, taking activated charcoal, maintaining the function of the cardiovascular system, monitoring the performance of the heart and lungs, monitoring the volume of circulating blood and diuresis are carried out.

If necessary, a complex of resuscitation measures is carried out.

The effect of beta-blockers can be neutralized by slow intravenous (iv) use of isoprenaline at an initial dose of about 5 mcg / min or dobutamine at an initial dose of about 2.5 mcg / min. With severe bradycardia,0.5-2 mg of atropine is administered intravenously; in the absence of a positive effect, a transvenous pacemaker can be installed. 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.

In bronchospasm, intravenous beta-2-acrenoreceptor stimulators are used. For ventricular estrasystole – lidocaine (class IA antiarrhythmics cannot be administered).

Special instructions

Nebivolol should be used with caution in patients with renal insufficiency, diabetes mellitus, hyperthyroidism, a history of allergic diseases, psoriasis, COPD, AV block I degree, Prinzmetal angina, as well as in patients over the age of 75 years.

Beta-blockers should be discontinued gradually over 10 days (up to 2 weeks in patients with CHD). At the beginning of treatment, blood pressure and heart rate should be monitored daily.

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

Nebivolol has no effect on glucose levels in patients with diabetes mellitus, but nebivolol may mask certain signs of hypoglycemia (tachycardia, rapid heartbeat) caused by the use of hypoglycemic drugs.

If nebivolol is needed in patients with psoriasis, the expected benefit of therapy and the possible risk of psoriasis exacerbation should be carefully evaluated. Beta-blockers should be used with caution with increased thyroid function due to the fact that under the influence of beta-blockers, tachycardia can be leveled.

Nebivolol may increase the symptoms of peripheral circulatory disorders. Patients who wear contact lenses should take into account that the use of beta-blockers may reduce the production of tear fluid.

When performing surgical procedures, the anesthesiologist should be warned that the patient is taking beta-blockers. Blood glucose monitoring should be performed once every 4-5 months (in patients with diabetes mellitus).

Monitoring of laboratory parameters of renal function should be carried out once every 4-5 months (in elderly patients).

Form of production

Pills.

Storage conditions

Store at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Nebivolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, Pregnant women as prescribed by a doctor, Nursing mothers as prescribed by a doctor

Indications

Heart Failure, Hypertension, Angina, Arrhythmia