Binelol Valium 5mg 56 pc

Description

Composition
Active substance:
1 tablet contains: nebivolol (in the form of nebivolol hydrochloride) – 5.00 mg ;.
Excipients:
Lactose monohydrate, crospovidone (type A), Poloxamer 188, Povidone K-30, microcrystalline cellulose, magnesium stearate.
Description:
Round, biconvex tablets of white color, with the cruciform notch on one side.
Product form:
Tablets of 5 mg.
14 tablets in PVC / PE / PVDC // Al blister. 1,2 or 4 blisters with instructions for use placed in a cardboard box.
Contraindications
Hypersensitivity to Nebivolol or one component of the drug. expressed human liver, acute heart failure, chronic heart failure decompensation (requiring intravenous administration of drugs with inotropic effect), cardiogenic shock, sick sinus syndrome, including sinus block, atrioventricular (AV) block II and III degree (without artificial pacemaker), bronchospasm and asthma, untreated pheochromocytoma, depression, metabolic acidosis, bradycardia (heart rate less than 50 bpm. / min.), expressed Arter cial hypotension (systolic blood pressure less than 90 mm Hg. Art.), heavy obliterating peripheral vascular disease ( “intermittent” claudication, Raynaud’s syndrome), male, age 18, lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
With care in renal failure, diabetes, while hyperthyroidism, in allergic diseases in history, in psoriasis. with atrioventricular block I degree, Prinzmetal angina, chronic obstructive pulmonary disease (COPD), in patients older than 65 years.
Dosage
5 mg
Indications
Arterial hypertension;
Coronary heart disease (CHD) prevention of attacks of angina.
Chronic heart failure (in a combination therapy).
Interaction with other drugs
With simultaneous use of beta-blockers with blockers “slow” calcium channel (BCCI) (verapamil and diltiazem) amplifies a negative effect on the myocardial contractility and AV conduction. Protivopokazano / introduction of verapamil in patients receiving nebivolol. When combined with antihypertensives, nitroglycerin or BCCI may develop severe hypotension (special caution is required in combination with prazosin).
While the use of class I antiarrhythmics amiodarone and may increase the negative inotropic action and an elongation time of the excitation of the atria.
When applied simultaneously with cardiac glycosides nebivolol revealed no amplification effect on slowing AV conduction.
Concomitant use of nebivolol and drugs for general anesthesia can cause suppression of the reflex tachycardia and increase the risk of hypotension.
Clinically significant interaction nebivolol and non-steroidal anti-inflammatory drugs (NSAIDs) has been established. Acetylsalicylic acid as an antiplatelet agent may be applied simultaneously with nebivolol.
The simultaneous use of tricyclic antidepressants, barbiturates and phenothiazine derivatives may potentiate the hypotensive effect of nebivolol.
pharmacokinetic interactions
While the use of drugs that inhibit the reuptake of serotonin, or by other means involving biotransformed isoenzyme CYP2D6, it slows the metabolism of nebivolol.
With simultaneous use of nebivolol had no effect on the pharmacokinetic parameters of digoxin.
While the use of cimetidine plasma concentrations of nebivolol in the blood increases (data on the influence on the pharmacological effects of the drug available). Concurrent administration of ranitidine had no effect on the pharmacokinetic parameters of nebivolol.
When applied simultaneously with nebivolol nicardipine concentration of active substances in the blood plasma increased somewhat, but it has no clinical significance.
Simultaneous reception of ethanol, furosemide or hydrochlorothiazide did not affect the pharmacokinetics of nebivolol.
No clinically significant interaction established nebivolol and warfarin. With simultaneous application of sympathomimetic agents inhibit the activity of nebivolol.
Overdose
Symptoms: reduced blood pressure, nausea, vomiting, cyanosis, sinus bradycardia, AV block, bronchospasm, cardiogenic shock, loss of consciousness, coma, cardiac arrest.
Treatment: gastric lavage, administration of activated charcoal. In the case of pronounced reduction in blood pressure is necessary to give a patient a horizontal position with legs raised, optionally in / in a liquid and vasopressors; as a follow-up appointment may 1-10 mg glucagon. If bradycardia is introduced into / from 0.5-2 mg atropine, with no positive effect can be posing transvenous or intracardiac pacemaker. When AV blockade (II-1II v.) Is recommended in / in a beta-agonists. at their ineffectiveness should consider setting an artificial pacemaker. In heart failure, treatment is initiated with introduction of cardiac glycosides and diuretics, with no effect expedient administering dopamine, dobutamine or vasodilators. When bronchospasm assign I / beta2-adrenergic receptors. When ventricular extrasystole – lidocaine (antiarrhythmic can not enter the class IA agents). In convulsions – in / diazepam.
pharmachologic effect
Pharmacological group:
Beta1-selective blocker.
Pharmacodynamics:
Nebivolol is a lipophilic, cardioselective beta-blockers third generation with vasodilating properties. It has antihypertensive, antianginal and antiarrhythmic action. Reduces high blood pressure (BP) at rest, physical exertion and stress. Competitive and selectively blocks synaptic and postsynaptic adrenoreceptors beta1-, making them inaccessible to catecholamines modulate release factor endothelial vasodilator nitrogen oxide (N0).
Nebivolol is a racemate consisting of two enantiomers: SRRR-nebivolol (D-nebivolol) and the RSSS-nebivolol (L-nebivolol), which combines two pharmacological activities: D-nebivolol is a competitive and highly selective blocker of the beta1-adrenergic receptors (affinity for beta1-adrenoceptors 293 times higher than for beta2 adrenoceptors).
L-nebivolol has a mild vasodilator effect by modulation of release of relaxing factor (N0) of the vascular endothelium.
Hypotensive effect develops in 2-5 days of treatment, stable effect observed after 1 month. The antihypertensive effect is maintained with prolonged treatment.
Hypotensive effect is also due to a decrease in activity of the renin system -angiotenzinovoy (not directly correlate with changes in the activity of renin in blood plasma).
The use of Nebivolol improves system and intracardiac hemodynamics. Nebivolol slows the heart rate (HR) and blood pressure at rest and during exercise, reducing left ventricular end-diastolic pressure, reducing the total peripheral vascular resistance, improves diastolic cardiac function (filling pressure decreases) and increases the ejection fraction.
Reducing myocardial oxygen demand (slowing the heart rate, decrease in preload and afterload), reduces the number and severity of attacks of angina and exercise tolerance increases.
Antiarrhythmic effect due to suppression of abnormal automaticity of the heart (including in the pathological focus) and slowing AV conduction.
Pharmacokinetics:
Suction
After oral administration of nebivolol is rapidly absorbed from the gastrointestinal tract. Food intake does not affect absorption, so nebivolol can be taken regardless of meals. Bioavailability is an average of 12% in patients with ‘fast’ metabolism and is almost complete in patients with a “slow” metabolism. Efficacy nebivolol does not depend on the rate of metabolism.
Distribution
Clearance in blood plasma in the majority of patients (with “fast” metabolism) is reached within 24 hours and for gidroksimetabolitov -. A few days. plasma concentration 1-30 g / L proportional to dose.
Communication with plasma proteins (mainly albumin) for D-nebivolol is 98.1% and L-nebivolol – 97.9%.
Metabolism
Nebivolol is extensively metabolised, partly to form active gidroksimetabolitov. The rate of metabolism of nebivolol by aromatic hydroxylation polymorphism genetically determined oxidative and depends on isozyme CYP2D6.
breeding
One week after the administration of 38% (the amount of the unchanged active substance is less than 0.5%) of the dose excreted by the kidneys and 48% – in the intestine. Patients with “fast” metabolism half-life values ​​(T1 / 2) enantiomers of nebivolol plasma averages 10 hours. Patients with “slow” metabolism of these values ​​are increased by 3-5 times.
Patients with “fast” metabolism values ​​T1 / 2 gidroksimetabolitov both enantiomers from plasma averages 24 hours, in patients with “slow” metabolism of these values ​​are approximately 2-fold increase.
On the pharmacokinetics of nebivolol is not affected by the age and sex of patients.
Pregnancy and breast-feeding
In pregnancy, the drug is prescribed only under strict indications, where the benefits to the mother outweighs the risk to the fetus (in connection with the possible development of a newborn bradycardia, hypotension, hypoglycemia and respiratory paralysis). Treatment should be interrupted for 48-72 hours before delivery. In cases where this is not possible, it is necessary to ensure strict monitoring of the newborn within 48-72 hours after delivery.
Animal studies have shown that nebivolol is excreted in breast milk. If application during lactation is necessary, breast-feeding should be discontinued.
Conditions of supply of pharmacies
On prescription.
side effects
Part of the central and peripheral nervous system: headache, dizziness, fatigue, weakness, paresthesias (from 1% to 10%); In very rare cases, depression, decreased ability to concentrate, drowsiness, insomnia, “nightmarish” dream, hallucinations, psychosis, convulsions.
On the part of the gastrointestinal tract: nausea, constipation, flatulence, diarrhea, dry mouth (more than 1%).
With the cardiovascular system: bradycardia, congestive heart failure, AV block, orthostatic hypotension, worsening of “intermittent” claudication, shortness of breath; in very rare cases: cardiac rhythm disturbances, Raynaud’s syndrome, peripheral edema, cardialgia.
Allergic reactions: itching, rash erythematous character.
Other: bronchospasm (including the absence of obstructive lung disease history), photodermatosis, hyperhidrosis, rhinitis, exacerbation of psoriasis flow, blurred vision, dry eyes.
special instructions
Abolition of beta-blockers should be carried out gradually, within 10 days (up to 2 weeks in patients with coronary heart disease).
Blood pressure and heart rate control at the start of drug administration should be daily.
In elderly patients, renal function should be monitored (1 every 4-5 months).
Angina dose voltage should provide resting heart rate in the range of 55-60 bpm. . / Min, with a load – not more than 110 beats. / Min.
Beta-blockers may cause bradycardia: the dose should be reduced if the heart rate less than 50-55 bpm. / Min. (Cm. Partition CONTRA).
In deciding on the appointment of the drug BINELOL® patients with psoriasis should carefully correlate the expected benefits of the drug and the potential risk of exacerbation of psoriasis.
Patients who use contact lenses should bear in mind that during treatment with beta-blockers may reduce the production of tear fluid.
During surgery should alert the anesthetist that the patient is taking beta-blockers.
Nebivolol does not affect glucose levels in diabetic patients. However, caution should be exercised in the treatment of these patients because BINELOL® may mask certain symptoms of hypoglycemia (e.g., tachycardia) caused by the use of hypoglycemic agents.
Control of glucose in the blood plasma should be 1 every 4-5 months. (In patients with diabetes).
Beta-blockers should be used with caution in patients with chronic obstructive pulmonary disease, as it may worsen bronchospasm.
Beta-blockers may increase the sensitivity to allergens and the severity of anaphylactic reactions.
The effectiveness of beta-blockers in smokers is lower than that of non-smokers.
Research studies have shown that nebivolol does not affect the speed of psychomotor reactions. Pilots aircrew with mild degrees of arterial hypertension (admitted to the flight operations) the drug administered in an initial dose of 2.5 mg. Subsequently (no sooner than 2 weeks) with good tolerability and insufficient control of blood pressure may increase the dose to 2.5 mg. The recommended dose -5 mg / day. Some patients may experience side effects, most commonly dizziness due to low blood pressure. If you experience such effects, the patient should not drive vehicles or to engage in potentially hazardous activities that require special attention and speed and quickness of psychomotor reactions. These effects occur most frequently immediately after the start of treatment, or at higher doses.
Storage conditions
At a temperature of not higher than 30 ° C.
Keep out of the reach of children!.
Dosing and Administration
BINELOL® taken orally in the same time of the day independently of food intake, liquid squeezed a sufficient amount of liquid.
Hypertension and coronary heart disease
The average daily dose for the treatment of hypertension and coronary heart disease of 2.5 – 5 mg (1/2 tablet 5 mg – 1 tablet) 1 time per day. Perhaps the use of the drug in monotherapy or in combination therapy.
In patients with renal insufficiency and in patients older than 65 years of the initial dose is 2.5 mg / day. (1/2 5 mg tablets).
When necessary, the daily dose can be increased to 10 mg (2 tablets of 5 mg per one dose).
Chronic heart failure
Treatment of chronic heart failure should begin with a gradual increase in the dose until the optimal individual maintenance dose.
Selection of doses in the beginning of treatment necessary to carry out the following scheme, keeping weekly intervals, and based on the tolerability of that dose by the patient: the dose is 1.25 mg BINELOL® drug (1/4 5 mg tablets) 1 times a day, can be increased at first and 2.5 – 5 mg BINELOL® drug (2.1 to 5 mg tablets – 1 tablet) and then – 10 mg (2 tablets of 5 mg), 1 time per day.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist