Nebivolol 5mg tab cs-28 pcs


Nebivolol 5mg tab cs-28 pcs



Active substance:
nebivolol hydrochloride in terms of nebivolol – 5.0 mg;
monohydrate lactose (milk sugar) – 89.87 mg pregelatinized starch (Starch 1500) – 22.5 mg, CROS-carmellose sodium (primelloza) – 9.0 mg, povidone (polyvinylpyrrolidone of middle) – 4.5 mg Microcrystalline cellulose – 17,25 mg colloidal silicon dioxide (aerosil) – 0.38 mg calcium stearate – 1.5 mg.
Tablets white or almost white, round, Valium, chamfered and cruciform mark.
Product form:
Packaging 28 tablets
– increased sensitivity to the active agent or one component of the drug;
– acute heart failure;
– chronic heart failure decompensation (requiring intravenous administration of drugs with inotropic effect);
– severe hypotension (systolic blood pressure less than 90 mmHg);
– sick sinus syndrome, including sinus block;
– atrioventricular block II and III degree (without pacemaker);
– severe bradycardia (heart rate less than 50 beats / min.);
– cardiogenic shock;
– pheochromocytoma (without simultaneous application of alpha-adrenoblo Katori);
– metabolic acidosis;
– severe hepatic dysfunction;
– severe bronchial asthma (BA) and chronic obstructive pulmonary disease (COPD);
– heavy obliterating peripheral vascular disease ( “intermittent” claudication, Raynaud’s syndrome);
– myasthenia gravis;
– depression;
– lactose intolerance, lactase deficiency and syndrome of glucose-galactose malabsorption;
– the age of 18 years (effectiveness and safety have not been studied in this age group);
– simultaneous reception floctafenine, sultopride (see “Interaction with other drugs.”).
Be wary – renal failure;
– diabetes;
– hyperthyroidism;
– allergic history; holding desensibilizi-al treatment of psoriasis;
– asthma and COPD;
– I degree atrioventricular block;
– Prinzmetal angina;
– age over 65 years.
5 mg
– arterial hypertension;
– Ischemic heart disease: prevention of attacks of angina pectoris;
– Chronic heart failure (in a combination therapy).
Interaction with other drugs
pharmacodynamic interactions
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. Contraindicated in / with the introduction of verapamil during treatment with nebivolol.
When applied simultaneously with nebivolol antihypertensives, nitroglycerin or BCCI may develop severe hypotension (special caution is required in combination with prazosin).
The simultaneous use of baclofen and amifostine with antihypertensive drugs can cause a significant drop in blood pressure, and therefore the correction required dose of antihypertensive drugs.
When applied simultaneously with nebivolol centrally acting antihypertensive agents (clonidine, guanfacine, moxonidine, methyldopa, rilmenidine) possibly worsening of heart failure due to decrease sympathetic tone (decrease heart rate and cardiac output, vasodilation symptoms). This abrupt withdrawal of these drugs, especially to cancel nebivolol possible the development of “rebound” hypertension.
When applied simultaneously with nebivolol class I antiarrhythmic drugs and amiodarone 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 (HPBP) is not established.
The simultaneous use of nebivolol tricyclic antidepressants, barbiturates and phenothiazine derivatives may potentiate the hypotensive effect of nebivolol.
Concomitant use of nebivolol and floctafenine, since there is a risk of significant decrease in blood pressure or shock.
Concomitant use of nebivolol and sultopride as an increased risk of ventricular arrhythmias, especially type “pirouette”.
When applied simultaneously with nebivolol insulin and hypoglycemic agents for oral administration may be masked symptoms of hypoglycemia (tachycardia). With simultaneous application of sympathomimetic agents inhibit the activity of nebivolol.
pharmacokinetic interactions
With simultaneous application of nebivolol with drugs that inhibit the reuptake of serotonin, or by other means involving biotransformed isoenzyme CYP2D6, nebivolol increases the concentration in plasma, nebivolol metabolism slows down, which can lead to the risk of bradycardia.
While the use of digoxin, nebivolol has no effect on the pharmacokinetic parameters of digoxin.
When applied simultaneously with nebivolol cimetidine, nebivolol plasma concentration increases.
The simultaneous use of nebivolol and ranitidine did not affect 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 treatment with nebivolol and ethanol, furosemide or hydrochlorothiazide did not affect the pharmacokinetics of nebivolol.
No clinically significant interaction established nebivolol and warfarin.
Symptoms: marked reduction of blood pressure, nausea, vomiting, cyanosis, sinus bradycardia, atrioventricular (AV) block, bronchospasm, loss of consciousness, cardiogenic shock, coma, cardiac arrest, hypoglycemia, seizures.
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. Bradycardia, be administered in / in 0.5 – 2 mg atropine with no positive effect can be posing transvenous or intracardiac pacemaker. When AV blockade (II- III cent.) Is recommended in / with the introduction of beta-agonists, while their inefficiency 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 used intravenously bronchospasm stimulants beta2-adrenergic receptors. When ventricular extrasystole – lidocaine (antiarrhythmic drugs can not be administered IA class). When hypoglycemia – intravenous solution of dextrose (glucose), and convulsions – diazepam.
pharmachologic effect
Pharmacological group:
Beta1-selective blocker
Cardioselective beta1-blocker. Nebivolol has antihypertensive, antianginal and antiarrhythmic action. Reduces high blood pressure (BP) at rest, physical exertion and stress. Selectively and competitively blocks postsynaptic beta1-adrenergic receptors, making them inaccessible to catecholamines release simulates endothelial vasodilating factor nitric oxide (NO).
Nebivolol is a racemate of the two enantiomers: SRRR-nebivolol (D- nebivolol) and the RSSS-nebivolol (L-nebivolol), which combines two pharmacological activities:
– D-nebivolol is a highly selective and competitive beta1- adrenoceptor blocker;
– L-nebivolol has a mild vasodilator effect by modulation of release of vasodilating factor (NO) from the vascular endothelium.
Hypotensive effect is also due to a decrease in activity of the renin-angiotensin-aldosterone system (RAAS) (not directly correlate with changes in the activity of renin in blood plasma).
Stable hypotensive effect develops after 1-2 weeks of regular drug administration, and in some cases – after 4 weeks, stable operation is noted after 1-2 months.
Reducing myocardial oxygen demand (slowing the heart rate (HR), the reduction of preload and afterload), nebivolol reduces the number and severity of angina attacks and increases exercise tolerance.
Antiarrhythmic effect due to suppression of abnormal automaticity of the heart (including in the pathological focus) and slowing of atrioventricular conduction.
Suction. After oral administration is rapid absorption of both enantiomers. Eating does not affect the absorption, so nebivolol can be administered independently from the meal. The bioavailability of ingested nebivolol averages 12% in patients with a “fast” metabolism (the effect of “first pass”) and is almost complete – in patients with a “slow” metabolism.
Distribution. In plasma, both enantiomers are predominantly associated with albumin. Binding to plasma proteins is for D-nebivolol – 98.1%, for L- nebivolol – 97.9%.
It metabolized by nebivolol alicyclic and aromatic gidroskilirovaniya and partial N-dealkylation. The resulting hydroxy- and amino derivatives conjugated with glucuronic acid and excreted in the form of O- and N-glucuronides, kidneys (38%) through the intestines (48%). T1 / 2 in patients with “fast” metabolism: gidroskimetabolitov – 24 hours, enantiomers nebivolol – 10 hours; patients with “slow” metabolism:. gidroskimetabolitov – 48 hours, enantiomers nebivolol – 30 – 50 hour excretion through the kidney unchanged nebivolol is less than 0.5% of the dose ingested.
Given the differences in metabolic rate, dose must always be individualized: patients with “slow” metabolism requires a smaller dose.
Pregnancy and breast-feeding
When pregnancy Nebivolol drug is prescribed only for vital indications, where the benefits to the mother outweighs the potential risk to the fetus or newborn (in connection with the possible development of the fetus and newborn bradycardia, hypotension, hypoglycemia). If treatment with nebivolol is necessary, it is necessary to carry out monitoring of the utero-placental blood flow and fetal growth and development. Treatment should be interrupted for 48 – 72 hours before delivery. In cases where this is not possible, it is necessary to establish a strict monitoring of the newborn for 48 – 72 hours after delivery.
Nebivolol is excreted in breast milk. If necessary, the drug Nebivolol lactation, breastfeeding must stop.
Conditions of supply of pharmacies
side effects
The frequency of side effects: very often (10%), frequent (more than 1% and less than 10%), rare (more than 0.1% and less than 1%), rare (0.01% and less than 0.1%) very rare (less than 0.01%) including individual messages.
Disorders of the nervous system:
Common: headache, dizziness, fatigue, weakness, paresthesias; Uncommon: depression, “nightmarish” dream, confusion, decreased ability to concentrate, drowsiness, insomnia;
Very rare: syncope, hallucinations.
Disorders of the gastrointestinal tract:
Frequently: dryness of the oral mucosa, nausea, constipation, diarrhea; Uncommon: dyspepsia, flatulence, vomiting.
Violations of the cardiovascular system:
Uncommon: bradycardia, exacerbation flow CHF, congestive heart failure, retardation of atrioventricular conduction, atrioventricular block, marked decrease in blood pressure, orthostatic hypotension, cardiac arrhythmias, cardialgia, exacerbation “Intermittent” claudication, peripheral edema, Raynaud’s syndrome.
Violations of the skin and subcutaneous tissue disorders:
Uncommon: rash erythematous character, itching;
Very rarely flow worsening of psoriasis, photodermatosis, increased sweating; In some cases: angioedema.
Violations by the organ of vision:
Uncommon: blurred vision.
Violations of the respiratory system:
Common: shortness of breath;
Uncommon: bronchospasm, rhinitis.
Violations of the reproductive system:
Uncommon: erectile dysfunction. Other disorders: alopecia.
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 beats / min, with a load -.. Not more than 110 beats / min..
Beta blockers can cause bradycardia: the dose should be reduced if the heart rate less than 50 to 55 beats / min.. (See. Section “Contraindications”).
When deciding on the use of the drug nebivolol in patients with psoriasis should carefully correlate the expected benefits of the drug and the possible 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 the concentration of plasma glucose in patients with diabetes mellitus. However, caution should be exercised in the treatment of these patients because Nebivolol preparation can mask certain symptoms of hypoglycaemia (e.g., tachycardia) caused by the use of hypoglycemic agents for oral and insulin. Controlling the glucose concentration in the blood plasma should be 1 every 4-5 months. (In patients with diabetes).
When hyperthyroidism beta-blockers may mask tachycardia. 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.
Smokers efficacy of beta-blockers lower compared to non-smokers patients.
During treatment with nebivolol (in case of side effects), should be careful when driving vehicles and classes of potentially hazardous activities that require high concentration and psychomotor speed reactions.
Storage conditions
In a dry, dark place at a temperature not higher than 25 ° C. Keep out of the reach of children.
Dosing and Administration
Nebivolol tablet taken orally, once daily, preferably in one and the same time,
regardless of food intake, drinking plenty of fluids.
The average daily dose for the treatment of hypertension and coronary heart disease of 2.5 mg – 5 mg nebivolol preparation (1.2 mg tablet 5 – 1 5 mg tablet). Nebivolol may be used alone or in combination with other agents that reduce blood pressure.
In patients with renal failure and patients over 65 years, the recommended initial dose of 1/2 tablet (2.1 mg tablet 5) Nebivolol drug per day. When necessary, the daily dose can be increased to a maximum of 10 mg (2 tablets of 5 mg per one dose).
Treatment of chronic heart failure should begin with a slow increase in the dose until the optimal individual maintenance dose. Selection of doses in the beginning of treatment must be carried out as follows: maintaining at the same intervals from one to two weeks, and focusing on the tolerance of the patient dose: initial dose – 1.25 mg (1/4 tablet 5 mg Phillips Valium) 1 time per day It can be increased first to 2.5 – 5 mg nebivolol preparation (2.1 mg tablet 5 – 1 5 mg tablet) and then – 10 mg (2 tablets of 5 mg), 1 time per day.
The maximum daily dose is 10 mg (2 tablets of 5 mg), 1 time per day.
At the beginning of treatment and at each increasing dose the patient should be at least 2 hours to be under medical supervision to ensure that the clinical condition is stable (especially: blood pressure, heart rate, conduction abnormalities, as well as symptoms of worsening of chronic heart failure).
We do not recommend the use of nebivolol in patients with severe renal and / or hepatic insufficiency, due to the lack of application experience.
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg


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