Binelol tabs 5mg #56

Instruction for Binelol

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Binelol is a third generation lipophilic cardioselective beta1-blocker with vasodilating properties. It has antianginal, hypotensive and antiarrhythmic effects.

Release form and composition

Binelol dosage form - tablets: round, convex on both sides, white, with a cross-shaped notch on one side (14 pcs. In a blister, in a cardboard box 1, 2 or 4 blisters).
Active ingredient: nebivolol (in the form of hydrochloride), 1 tablet - 5 mg.
Additional components: povidone K-30, magnesium stearate, microcrystalline cellulose, crospovidone (type A), lactose monohydrate, poloxamer188.

Pharmacodynamics

The active component of Binelol, nebivolol, is a lipophilic, cardioselective β1-adrenergic blocker of the third generation with vasodilating efficacy. It has antianginal, hypotensive and antiarrhythmic effects on the body, reducing high blood pressure (blood pressure) at rest, during physical exertion and stress. Blocks synaptic / postsynaptic β1-adrenergic receptors competitively and selectively, ensuring their inaccessibility for catecholamines and modulating the release of endothelial vasodilating factor NO (nitric oxide).
Nebivolol is a racemate composed of two enantiomers and has a pharmacological effect that combines their actions:
    D-nebivolol (SRRR-nebivolol): a competitive and highly selective β1-adrenergic receptor blocker (showing an affinity for β1-adrenergic receptors is 293 times higher than for β2-adrenergic receptors).
    L-nebivolol (RSSS-nebivolol): by modulating the release of the relaxing factor - NO from the vascular endothelium - has a mild vasodilatory effect.
The hypotensive effect of Binelol develops on days 2–5 of therapy, a stable effect is recorded after 1 month. The antihypertensive effect of the drug persists with prolonged use, it is also due to inhibition of the activity of the renin-angiotensin system (but does not directly correlate with the change in the blood plasma of renin activity).
Nebivolol improves not only systemic but also intracardiac hemodynamics. It reduces heart rate (heart rate) and blood pressure at rest and during physical exertion, helps to reduce the end-diastolic pressure of the left ventricle, reduces OPSS (total peripheral vascular resistance), normalizes the diastolic function of the heart (reducing filling pressure), and increases the ejection fraction.
Due to a decrease in myocardial oxygen demand due to a decrease in heart rate, a decrease in pre- and afterload, the duration, severity and frequency of angina attacks decrease; increased exercise tolerance.
The antiarrhythmic effect is due to the inhibition of the pathological automatism of the heart (including in the lesion focus) and the slowing down of AV (atrioventricular) conduction.

Pharmacokinetics

    absorption: after oral administration, nebivolol is rapidly absorbed from the gastrointestinal tract (gastrointestinal tract). The absorption of the substance is not affected by simultaneous food intake, therefore Binelol can be taken regardless of the diet. The average bioavailability in patients with a fast metabolic phenotype is approximately 12% and is almost complete in patients with a slow metabolic type, but the effectiveness of nebivolol does not depend on this indicator;
    distribution to tissues and organs: plasma clearance of nebivolol in most fast metabolizers is ~ 24 hours, and its hydroxy metabolites - several days. Plasma concentration is proportional to the dose and varies from 1 to 30 μg / l. With plasma proteins, mainly albumin, D-nebivolol binds by 98.1%, and L-nebivolol - by 97.9%;
    metabolism: the process takes place in the liver with partial formation of active hydroxymetabolites; the rate of aromatic hydroxylation depends on genetically determined oxidative polymorphism and is determined by the isoenzyme CYP2D6;
    excretion: within a week after taking Binelol, 38% of the dose, of which less than 0.5% unchanged, is excreted in the urine and 48% with feces. In fast metabolizers, T1 / 2 (half-life) for nebivolol enantiomers from plasma averages 10 hours; for slow metabolizers, the indicator increases by 3–5 times. The values ​​of T1 / 2 of hydroxymetabolites of both enantiomers from blood plasma with fast metabolism are on average 24 hours, with slow metabolism they increase approximately 2 times.
The age and gender of patients do not affect the pharmacokinetics of nebivolol.

Indications for use

    arterial hypertension therapy;
    prevention of strokes of exertional angina in ischemic heart disease;
    treatment of chronic heart failure (as part of complex therapy).

Contraindications

Absolute:
    chronic heart failure in the stage of decompensation, requiring intravenous administration of drugs with an inotropic effect;
    acute heart failure;
    atrioventricular (AV) blockade of the II and III degrees (without an artificial pacemaker);
    sick sinus syndrome, including sinoauricular block;
    cardiogenic shock;
    severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
    severe bradycardia (heart rate less than 50 beats / minute);
    untreated pheochromocytoma;
    bronchospasm and bronchial asthma;
    severe liver dysfunction;
    metabolic acidosis;
    depression;
    myasthenia gravis;
    severe obliterating peripheral vascular disease such as intermittent claudication and Raynaud's syndrome;
    lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
    age up to 18 years;
    lactation (or you should stop breastfeeding);
    hypersensitivity to the individual components of Binelol.
Relative:
    renal failure;
    diabetes;
    hyperfunction of the thyroid gland;
    a history of allergic diseases;
    psoriasis;
    AV block I degree;
    Prinzmetal's angina;
    chronic obstructive pulmonary disease;
    pregnancy;
    age over 65.

Instructions for use: method and dosage

Binelol tablets should be taken orally 1 time a day at the same time: swallow whole and drink them with a sufficient amount of liquid. Food does not affect the absorption of the drug.
With arterial hypertension and ischemic heart disease, adult patients are prescribed 2.5–5 mg (½ – 1 tab.) 1 time per day, depending on the severity of the therapeutic effect. Binelol can be used both as a single drug and as part of a combination therapy.
Patients with renal insufficiency and the elderly (over 65 years of age) are not recommended to exceed the daily dose of 2.5 mg.
In chronic heart failure, the dose is determined individually by titration: the initial dose is 1.25 mg (¼ tab.) 1 time per day, after a week, if necessary, it is increased to 2.5 mg. If the therapeutic effect is not enough, the dose continues to be increased once a week: first up to 5 mg, then up to 10 mg (2 tab.). It is necessary to take Binelol, regardless of the dose, once a day.

Side effects

    allergic reactions: erythematous rash, pruritus;
    from the gastrointestinal tract: nausea, flatulence, dry mouth, constipation or diarrhea;
    on the part of the cardiovascular system: AV block, orthostatic hypotension, bradycardia, shortness of breath, acute heart failure, exacerbation of intermittent claudication; very rarely - peripheral edema, cardiac arrhythmias, cardialgia, Raynaud's syndrome;
    from the central and peripheral nervous system: weakness, fatigue, headache, paresthesia, dizziness; very rarely - drowsiness or insomnia, nightmares, decreased ability to concentrate, psychosis, hallucinations, depression, convulsions;
    others: exacerbation of the course of psoriasis, hyperhidrosis, dry eyes, photodermatosis, visual impairment, rhinitis, bronchospasm (including in the absence of a history of obstructive pulmonary disease).

Overdose

Symptoms of nebivolol overdose are nausea / vomiting, decreased blood pressure, cyanosis, AV blockade, sinus bradycardia, bronchospasm, loss of consciousness, cardiogenic shock, coma, cardiac arrest.
The first stage of therapy is gastric lavage and absorption of absorbents, such as activated carbon.
Further, treatment is carried out depending on the symptoms:
    a pronounced decrease in blood pressure: the patient is given a horizontal position, the legs are raised above the level of the pelvis, if necessary, intravenous fluid and vasopressors are injected, after which glucagon may be prescribed at a dose of 1–10 mg;
    bradycardia: 0.5–2 mg of atropine is injected intravenously, and if there is no positive effect, a transvenous or intracardiac pacemaker may be required;
    AV-blockade of II – III degree: β-adrenostimulants are injected intravenously, in the absence of an effect, the issue of setting an artificial pacemaker is considered;
    heart failure: at the beginning of treatment, cardiac glycosides and diuretics are administered, if there is no effect, dopamine, dobutamine or vasodilators are prescribed;
    bronchospasm: drugs that stimulate β2-adrenergic receptors are administered intravenously;
    ventricular premature beats: lidocaine is prescribed. Class IA antiarrhythmics should not be administered;
    convulsions: diazepam is administered intravenously.

Special instructions

At the beginning of therapy, it is necessary to monitor blood pressure (BP) and heart rate (HR) indicators daily.
Elderly people should have their kidney function checked at least once every 4–5 months.
With angina pectoris, the dose of Binelol should provide a resting heart rate of 55-60 beats per minute, with a load - no more than 110 beats per minute.
In case of development of bradycardia (heart rate less than 50–55 beats per minute), the dose of Binelol should be reduced.
If surgical intervention is necessary, the patient must warn the doctor that he is receiving a beta-blocker.
In diabetic patients, Binelol can mask some of the symptoms of hypoglycemia (tachycardia, for example). Plasma glucose control is indicated at least once every 4–5 months.
The drug can reduce the production of tear fluid, which should be considered by patients who use contact lenses.
Nebivolol can increase the sensitivity to allergens and the severity of anaphylactic reactions, in patients with chronic obstructive pulmonary disease - increase bronchospasm.
In smokers, the effectiveness of beta-blockers is reduced.
You can not abruptly cancel Binelol, treatment should be completed gradually, reducing the dose within 10-14 days.

Influence on the ability to drive vehicles and complex mechanisms

Basically, Binelol does not affect the speed of reactions and the ability to concentrate. However, in some cases, especially at the beginning of treatment and when the dose is increased, the drug causes dizziness. Such patients should be careful when driving vehicles and performing potentially hazardous activities.

Application during pregnancy and lactation

During pregnancy, it is permissible to prescribe Binelol only according to strict indications, if the benefits to the mother significantly outweigh the risks to the fetus, since as a result of therapy, newborns may develop bradycardia, arterial hypotension, hypoglycemia and respiratory paralysis. The course must be interrupted 48–72 hours before the expected delivery. If this is not possible, the newborn should be monitored closely for 48–72 hours after delivery.
Animal studies have shown that nebivolol is excreted in breast milk. Therefore, if it is necessary to use Binelol during lactation, breastfeeding should be stopped.

Childhood use

According to the instructions, Binelol should not be used to treat children and adolescents under 18 years of age.

With impaired renal function

Recommended dosage of Binelol for patients with renal insufficiency:
    CC (creatinine clearance) more than 20 ml / min: the initial dose is 1/2 tablet of 5 mg (2.5 mg / day); if necessary, the dose can be increased to 1 tablet (5 mg / day);
    CC less than 20 ml / min: there is no experience with nebivolol, therefore its appointment in patients with severe renal impairment is not recommended.
Increasing the dose in case of impaired renal function should be carried out with extreme caution.

For violations of liver function

It is contraindicated to prescribe Binelol for severe liver dysfunction.

Use in the elderly

For elderly patients over 65 years of age, the initial dose of Binelol is 1/2 tablet of 5 mg (2.5 mg / day), if necessary, the dose can be increased to 1 tablet (5 mg / day). Given the limited experience with nebivolol in elderly patients, care must be taken during therapy and careful monitoring of patients is required.

Drug interactions

    class I antiarrhythmics and amiodarone: the negative inotropic effect is enhanced, it is possible to lengthen the time of excitation through the atria;
    blockers of slow calcium channels: AV conduction increases and a negative effect on myocardial contractility, there is a risk of severe arterial hypotension (intravenous verapamil is contraindicated during nebivolol treatment);
    drugs for general anesthesia: it is possible to suppress reflex tachycardia and increase the risk of developing arterial hypotension;
    tricyclic antidepressants, barbiturates, phenothiazine derivatives: the hypotensive effect of nebivolol may increase;
    drugs that inhibit the reuptake of serotonin, and other drugs that biotransform with the participation of the CYP2D6 isoenzyme: the metabolism of nebivolol slows down;
    cimetidine: increases the concentration of nebivolol in blood plasma;
    nicardipine: the concentration of both active substances increases slightly;
    sympathomimetic agents: the activity of nebivolol is suppressed.

Terms and conditions of storage

Store at temperatures up to 30 ºС out of reach of children.
The shelf life is 3 years.

Reviews about the drug

Patients suffering from high blood pressure and who started taking Binelol, reviews of the drug are extremely positive. They characterize it as a very good tool that quickly stabilizes and reliably maintains normal pressure, without strong side effects.
The disadvantages most often indicate the need for lifelong pills and their high cost.

Terms of sell

You don't need a prescription to buy Binelol.