Nebivolol tabs 5mg #60

Nebivolol instruction

You can buy Nebivolol here

Nebivolol is a third generation selective β1-blocker with vasodilating properties.

Release form and composition

Dosage form of Nebivolol - tablets: from white to almost white, round, flat-cylindrical, with a chamfer and a straight / cross-shaped line on one side (14, 15, 20 or 30 pcs. In blisters made of PVC film and Al foil, either 14, 28 or 60 pcs. in polyethylene cans; in a cardboard box 1, 2 or 4 packs of 14 pcs. or 1, 2 or 4 packs of 15 pcs., or 3 packs of 20 pcs., or 1-2 packages of 30 pcs., or 1 can).
Composition for 1 tablet:
    active substance: Nebivolol - 5 mg (corresponds to the content of Nebivolol hydrochloride - 5.45 mg);
    auxiliary components: magnesium stearate, corn starch, lactose monohydrate, microcrystalline cellulose, hyprolose (hydroxypropyl cellulose), croscarmellose sodium, polysorbate 80, colloidal silicon dioxide.
Due to the presence of a large number of manufacturers, the existence of other types of packaging and a change in the composition of auxiliary components is possible.

Pharmacodynamics

The active component of the drug - Nebivolol - has antihypertensive, antianginal and antiarrhythmic efficacy, reduces heart rate (heart rate) and lowers blood pressure (blood pressure) at rest and during exercise; reduces the end diastolic pressure in the left ventricular cavity, normalizing the diastolic function of the heart; reduces the total peripheral vascular resistance, increasing the ejection fraction. Competitively and selectively blocking synaptic and postsynaptic β1-adrenergic receptors, makes them inaccessible to catecholamines, modulates the release of endothelial vasodilating factor NO (nitric oxide). Nebivolol is a racemate - an equimolar mixture of two enantiomers: D-Nebivolol (SRRR-Nebivolol), a competitive and highly selective β1-adrenergic receptor blocker, and L-Nebivolol (RSSS-Nebivolol), which has a vasodilating effect due to the modulation of vasodilatory NO-releasing factor vasodilator ...
Antihypertensive efficacy is also due to inhibition of the activity of the RAAS (renin-angiotensin-aldosterone system), but there is no direct correlation with changes in the plasma activity of renin.
The antihypertensive effect occurs after 2–5 days from the start of treatment, and a stable effect is established after 1–2 months, with prolonged therapy this effect persists.
Due to a decrease in heart rate and a decrease in pre- and afterload under the influence of Nebivolol, myocardial oxygen demand decreases, which leads to a decrease in the number and severity of angina attacks and an improvement in exercise tolerance. The antiarrhythmic efficacy of the drug is due to the suppression of the automatism of the heart (including in the pathological zone) and a decrease in the rate of atrioventricular conduction.

Pharmacokinetics

    absorption: after oral administration, both enantiomers of Nebivolol are rapidly absorbed; the diet and the qualitative composition of food do not affect their absorption, and therefore the drug can be taken at any convenient time, regardless of the meal. In patients with a fast metabolism, bioavailability is ~ 12% with a first pass metabolism (the effect of the first passage through the liver), in patients with a slow metabolism, the bioavailability of Nebivolol is almost complete;
    distribution: the substance enters the systemic circulation, where both enantiomers bind to blood plasma proteins, mainly albumin: D-Nebivolol - by 98.1%, L-Nebivolol - by 97.9%;
    metabolism: by alicyclic and aromatic hydroxylation, as well as partial N-dealkylation, active metabolites are formed - hydroxy and amino derivatives, which are conjugated with glucuronic acid, after which they are excreted in the form of N- and O-glucuronides. The rate of metabolic processes of Nebivolol by aromatic hydroxylation is genetically determined by oxidative polymorphism, depends on the cytochrome isoenzyme CYP2D6;
    excretion: up to 38% of oral Nebivolol is eliminated by the kidneys (unchanged <0.5%) and 48% is excreted with feces through the intestines. In patients with a fast metabolism, T1 / 2 (half-life) of hydroxymetabolites is 24 hours, and of Nebivolol enantiomers - 10 hours; with a slow metabolism, T1 / 2 of hydroxymetabolites is 48 hours, of Nebivolol enantiomers - from 30 to 50 hours.

Indications for use

Nebivolol is recommended for the treatment of arterial hypertension, prevention of exertional angina attacks in patients with coronary artery disease (ischemic heart disease), as well as as part of the complex therapy of CHF (chronic heart failure).

Contraindications

Absolute:
    CHF in the stage of decompensation, in which intravenous administration of drugs with inotropic action is necessary;
    acute heart failure;
    severe arterial hypotension, systolic blood pressure <90 mm Hg. Art .;
    SSSU (sick sinus syndrome), including sinoauricular block;
    atrioventricular (AV) block II and III degree without an artificial pacemaker;
    cardiogenic shock;
    severe bradycardia, heart rate <50 beats / min;
    metabolic acidosis;
    pheochromocytoma (except for use in combination with α-blockers);
    history of bronchospasm / bronchial asthma;
    severe liver failure;
    severe renal failure, CC (creatinine clearance) <20 ml / min;
    severe peripheral circulatory disorders (Raynaud's syndrome, intermittent claudication);
    depression;
    muscle weakness, myasthenia gravis;
    lack of lactase, glucose-galactose malabsorption syndrome, lactose intolerance;
    children and adolescents under 18 years of age;
    period of breastfeeding (lactation);
    combined reception with floktaphenin and sultopride;
    simultaneous administration of verapamil intravenously;
    hypersensitivity to Nebivolol and / or any other components of the drug.
Nebivolol is recommended to be used with caution in diabetes mellitus, thyroid hyperfunction, COPD (chronic obstructive pulmonary disease), aggravated allergic history, desensitizing therapy, psoriasis, 1st degree AV block, Prinzmetal angina pectoris, during pregnancy and in old age (over 65 years).

Instructions for the use of Nebivolol: method and dosage

Nebivolol is taken by mouth, regardless of the diet, preferably at the same time. The tablets should not be chewed; they must be washed down with a sufficient amount of liquid.

Arterial hypertension and ischemic heart disease

In the treatment of arterial hypertension and ischemic heart disease, an average daily dose of 2.5–5 mg (½ – 1 tablet) 1 time per day is recommended. Achievement of the optimal therapeutic effect occurs after 1-2 weeks of taking the drug, but in some cases it is possible to increase the period to 4 weeks. If necessary, the dose can be increased to a maximum daily dose of 10 mg (2 tablets per dose).
Nebivolol can be taken as monotherapy or in combination with other antihypertensive drugs.
The use of Nebivolol for the treatment of arterial hypertension and coronary artery disease in special groups of patients:
    patients with renal insufficiency: initial dose - 2.5 mg (½ tablet) once a day; if necessary, the dose can be increased to a maximum daily dose of 5 mg (1 tablet); the efficacy of Nebivolol in severe renal failure (CC <20 ml / min) has not been studied, therefore, the appointment of the drug in such patients is contraindicated;
    patients with hepatic impairment: data on the use of Nebivolol are limited, the drug is used with caution; with mild to moderate hepatic impairment, the initial dose is 2.5 mg (½ tablet) once a day; if necessary, the dose can be increased to a maximum daily dose of 5 mg (1 tablet); the efficacy of Nebivolol in severe hepatic impairment has not been studied, therefore the drug is contraindicated in such patients;
    elderly patients: patients over 65 years of age take the drug at an initial dose of 2.5 mg (½ tablet) once a day; if necessary, the dose can be increased to a maximum daily dose of 5 mg (1 tablet). Given the limited experience with Nebivolol in elderly patients, it must be administered with caution after careful evaluation.

CHF

With a stable course of CHF, treatment should begin with gradual titration of the dose until the optimal individual maintenance dose is achieved. During the last 6 weeks, patients should not have attacks of acute heart failure. Treatment must be carried out under close medical supervision.
Patients taking diuretics, cardiac glycosides, ACE (angiotensin converting enzyme) inhibitors, and angiotensin II receptor antagonists should take stable doses of these drugs for at least 2 weeks before starting Nebivolol.
It is necessary to start therapy for CHF with β-adrenergic receptor blockers when the patient is clinically stable for the last 2 weeks. The selection of the dose in the initial period is carried out according to the scheme (maintaining 2-week intervals between dose increases): the initial dose is 1.25 mg per day (¼ tablet), then it can be increased to 2.5 mg per day (½ tablet), then up to 5-10 mg per day (1-2 tablets). The maximum daily dose should not exceed 10 mg (2 tablets). Each stage between increasing doses should last 2 weeks or more, its duration for each patient is individual and depends on the tolerance of the drug.
It is necessary to start treatment and gradually increase the dose of the drug under strict medical supervision, especially during the first two hours. When titrating the dose, blood pressure, heart rate and symptoms of CHF are regularly monitored.
Therapy for stable CHF is usually a long-term process. It is not recommended to stop taking Nebivolol sharply, since this can lead to a temporary exacerbation of the course of the underlying disease (CHF). If there is a need for a break in treatment, the cancellation is carried out by gradually reducing the dose of the drug by 2 times for 1 week.
The use of Nebivolol for the treatment of CHF in special groups of patients:
    patients with renal failure: mild and moderate renal failure (CC> 20 ml per minute) - dose adjustment is not required, the dose is selected individually with a gradual increase to the maximum tolerable. Experience with the use of the drug in severe renal dysfunction (CC <20 ml per minute) is absent, the use of the drug is contraindicated;
    patients with hepatic insufficiency: due to the limited experience of using the drug in case of liver dysfunction, it should be prescribed with caution in mild to moderate hepatic insufficiency, the dose must be selected individually, with a gradual increase to the maximum tolerable, if necessary, it can be increased to the maximum daily - 5 mg (1 tablet). There is no experience with Nebivolol in severe hepatic dysfunction, the drug is contraindicated;
    elderly patients: dose adjustment is not required, it should be selected individually, gradually increasing to the maximum tolerated.

Side effects

The frequency of negative side effects according to the WHO (World Health Organization) classification: very often -> 10%, often -> 1% and <10%, infrequently -> 0.1% and <1%, rarely -> 0.01% and <0.1%, extremely rarely - <0.01%, including isolated cases.
    nervous system: often - dizziness, headache, weakness, fatigue, paresthesia; infrequently - nightmares, insomnia, depression, confusion; extremely rare - hallucinations, fainting;
    gastrointestinal tract: often - nausea, diarrhea, constipation; infrequently - flatulence, dyspepsia, vomiting;
    cardiovascular system: often - peripheral edema; infrequently - heart failure, bradycardia, AV blockade, orthostatic hypotension, cardiac arrhythmias, Raynaud's syndrome, cardialgia, worsening of CHF, marked decrease in blood pressure;
    skin and subcutaneous tissue: infrequently - erythematous rash, pruritus; extremely rare - worsening of the course of psoriasis; in some cases - alopecia, angioedema;
    respiratory system: often - shortness of breath; infrequently - bronchospasm (including in the absence of anamnestic data on obstructive pulmonary disease);
    other reactions: infrequently - photosensitivity reactions, visual impairment, impotence, hyperhidrosis; rarely - dryness of the mucous membrane of the eye.

Overdose

Symptoms of Nebivolol overdose are nausea / vomiting, hypoglycemia, cyanosis, severe bradycardia, marked decrease in blood pressure, AV block, acute heart failure, cardiogenic shock, bronchospasm, loss of consciousness, convulsions, coma, cardiac arrest.
In case of an overdose, first of all, you should rinse the stomach and take activated charcoal. Further therapy is carried out depending on the symptoms:
    marked decrease in blood pressure: the patient should be laid in a horizontal position and his legs raised above the level of the head; if required, administer intravenous fluids and vasopressors;
    bradycardia: 0.5–2 mg of atropine is injected intravenously; in the absence of a positive effect, it is possible to install an intracardiac or transvenous electrostimulator;
    AV-blockade of II – III degree: β-adrenostimulants are administered intravenously; in the absence of a positive effect, it is possible to install an artificial pacemaker;
    heart failure: cardiac glycosides and diuretics are administered, in the absence of a positive effect, it is advisable to administer dobutamine, dopamine or vasodilators;
    bronchospasm: β-adrenomimetics are administered intravenously;
    ventricular premature beats: lidocaine is administered (class IA antiarrhythmics cannot be administered);
    convulsions: diazepam is administered intravenously;
    hypoglycemia: intravenous glucose (dextrose) may be needed.

Special instructions

Abrupt cessation of β-blockers, including Nebivolol, is unacceptable, therapy should be completed gradually, over 10 days (for patients with coronary artery disease - up to 14 days).
Controlling blood pressure and heart rate at the beginning of treatment is required daily.
Elderly patients need to monitor renal function once every 4–5 months.
The selection of the dose of Nebivolol in patients with exertional angina should provide a heart rate at rest - 55–60 beats / min, with a load - ≤ 110 beats / min.
Β-blockers can cause bradycardia; the dose of Nebivolol should be reduced when the heart rate is <50–55 bpm.
For patients with psoriasis, the drug is prescribed with caution, after a careful assessment of the ratio of the expected benefits of therapy with the possible risk of exacerbation of the course of psoriasis.
When using contact lenses, it must be borne in mind that due to the use of β-blockers, the production of tear fluid may decrease.
Before surgical interventions, it is required to warn the anesthesiologist about the intake of β-blockers.
Nebivolol does not affect plasma glucose levels in diabetic patients. But when treating such patients, care should be taken, since a β-blocker can mask some symptoms of hypoglycemia (tachycardia, heart palpitations) caused by oral administration of hypoglycemic agents and the use of insulin. In diabetes mellitus, the concentration of glucose in the blood plasma should be monitored at least once every 4–5 months.
In patients with hyperfunction of the thyroid gland, β-blockers are able to mask tachycardia.
Β-blockers are recommended to be used with caution in patients with COPD (chronic obstructive pulmonary disease), since they can increase bronchospasm.
If you are prone to allergies, it is important to take into account that β-blockers can increase sensitivity to allergens, as well as the severity of anaphylaxis.
In smoking patients, the effectiveness of β-blockers is lower than in nonsmokers.

Influence on the ability to drive vehicles and complex mechanisms

During treatment with Nebivolol (due to possible adverse reactions), care should be taken when driving vehicles and complex mechanisms, as well as performing potentially dangerous types of work that require increased concentration of attention and rapid psychomotor reactions.

Application during pregnancy and lactation

According to the instructions, Nebivolol during pregnancy is prescribed only according to strict indications, provided that the benefits for the mother exceed the risk for the fetus, since drug therapy can contribute to delayed growth and development of the fetus, premature labor, the development of a decrease in blood pressure in a newborn, bradycardia, hypoglycemia, paralysis respiration, as well as intrauterine fetal death. Taking pills should be discontinued 48–72 hours before the onset of labor, and if this is not possible, monitor uteroplacental blood flow, as well as strict observation of the newborn during the first 3 days after birth.
In the course of experiments on animals, it was revealed that Nebivolol passes into breast milk. If it is necessary to take the drug during lactation, breastfeeding must be interrupted.

Childhood use

The use of Nebivolol in children and adolescents under the age of 18 is contraindicated due to insufficient safety and efficacy data.

With impaired renal function

In the treatment of arterial hypertension and coronary artery disease in patients with impaired renal function of any severity, as well as the treatment of CHF with mild to moderate renal failure, caution should be exercised.
Due to the lack of experience with the use of Nebivolol for the treatment of CHF in severe renal dysfunction with CC <20 ml per minute, its use is not recommended.

For violations of liver function

Due to the limited experience of using Nebivolol for mild to moderate liver dysfunction, it should be prescribed with caution, the dose should be selected individually, with a gradual increase to the maximum tolerable. There is no experience with Nebivolol therapy in severe hepatic impairment, and the use of the drug is contraindicated.

Use in the elderly

Caution should be exercised in the treatment of hypertension and coronary artery disease in elderly patients.
There is no need for dose adjustment in the treatment of CHF in elderly patients; it should be selected individually, gradually increasing to the maximum tolerable.

Drug interactions

Pharmacodynamic interaction:
    verapamil and diltiazem - BMCC (slow calcium channel blockers): β-blockers increase their negative effect on myocardial contractility and AV conduction; IV verapamil is contraindicated when taking Nebivolol;
    antihypertensive drugs, nitroglycerin: development of severe arterial hypotension is possible (special care should be taken when combined with prazosin);
    BMCC dihydropyridine series (amlodipine, nitrendipine, nifedipine, lacidipine, nicardipine, nimodipine, felodipine): the likelihood of arterial hypotension may increase; in patients with CHF, the possibility of a further decrease in the contractility of the heart muscle cannot be ruled out;
    antihypertensive drugs of central action (methyldopa, clonidine, moxonidine, guanfacine, rilmenidine): the course of heart failure may be aggravated due to a decrease in sympathetic tone (decrease in heart rate and decrease in cardiac output, symptoms of vasodilation); with a sharp withdrawal of these drugs, especially before the withdrawal of Nebivolol, the development of rebound arterial hypertension is possible;
    amiodarone, class I antiarrhythmics (hydroquinidine, quinidine, propafenone, flecainide, cybenzoline, lidocaine, disopyramide, mexiletine): it is possible to increase their negative inotropic effect and lengthen the time of atrial excitation;
    cardiac glycosides: suppression of atrioventricular conduction is possible;
    means for general anesthesia: probably suppression of reflex tachycardia and an increase in the risk of developing arterial hypotension;
    NSAIDs (non-steroidal anti-inflammatory drugs): no clinically significant drug interactions with Nebivolol have been established;
    acetylsalicylic acid: can be used with Nebivolol as an antiplatelet drug;
    tricyclic antidepressants, barbiturates and phenothiazine derivatives, anxiolytics, hypnotics, ethanol: may enhance the hypotensive effect of Nebivolol;
    insulin and oral hypoglycemic agents: Nebivolol can mask symptoms of hypoglycemia (palpitations, tachycardia);
    floctafenin: Nebivolol may inhibit the compensatory reactions of the cardiovascular system associated with arterial hypotension or shock, which floctafenin can cause (concomitant use is contraindicated);
    baclofen, amifostine: possible increased arterial hypotension;
    sultopride: the risk of pirouette-type ventricular arrhythmias increases (concomitant use with Nebivolol is contraindicated).
Pharmacokinetic interaction:
    serotonin reuptake inhibitors, other drugs biotransformed with the participation of the CYP2D6 isoenzyme: increase the plasma concentration of Nebivolol, slow down its metabolism, as a result of which bradycardia may develop;
    digoxin: Nebivolol has no effect on its pharmacokinetic parameters;
    cimetidine: increases the plasma concentration of Nebivolol (no data on the effect on pharmacological efficacy);
    rifampicin: enhances the metabolism of Nebivolol;
    ranitidine: does not affect the pharmacokinetics of Nebivolol;
    nicardipine: plasma concentrations of active substances increase slightly, which does not have a clinically significant effect;
    ethanol, furosemide, hydrochlorothiazide: do not alter the pharmacokinetic parameters of Nebivolol;
    warfarin: no clinically significant interaction with Nebivolol has been established;
    sympathomimetic agents: inhibit the pharmacological activity of Nebivolol.

Terms and conditions of storage

Store at temperatures up to 25 ° C in a dark place. Keep out of the reach of children.
Shelf life is 2 years.

Reviews

According to reviews, Nebivolol is a fairly effective drug that allows you to eliminate pressure problems, and also normalizes the pulse, but at the same time it can cause many and often manifested side reactions.

Terms of sell

You don't need a prescription to buy Nebivolol.