Nebilet tablets 5mg №14×2

Name:
Nebilet tabl 5mg in bl. in pack. No. 14х2
Description:
Tablets of white color, round, biconvex, with a cross-shaped notch for division. The main active ingredient Nebivolol Release form Tablets are white, round, biconvex, with a cross notch for dividing. 1 tab. nebivolol hydrochloride micronized 5.45 mg, which corresponds to the content of nebivolol 5 mg – 16.1 mg, colloidal silicon dioxide – 0.69 mg, magnesium stearate – 1.15 mg. 7 pcs. – blisters (1) – packs of cardboard. 7 pcs. – blisters (2) – packs of cardboard. 7 pcs. – blisters (4) – packs of cardboard. 14 pcs. – blisters (1) – packs of cardboard. 14 pcs. – blisters (2) – packs of cardboard. 14 pcs. – blisters (4) – packs of cardboard. Special instructions Cancellation of beta-blockers should be carried out gradually over 10 days (up to 2 weeks in patients with coronary artery disease). Control of blood pressure and heart rate at the beginning of the drug should be daily. In elderly patients, monitoring of kidney function is necessary (1 time in 4-5 months). With exertional angina, the dose of the drug should provide heart rate at rest in the range of 55-60 beats / min, with exercise – no more than 110 beats / min. Beta-blockers can cause bradycardia: the dose should be reduced if the heart rate is less than 50-55 bpm. When deciding whether to use the drug Nebilet in patients with psoriasis, the expected benefits of using the drug and the possible risk of exacerbation of the course of psoriasis should be carefully correlated. Patients using contact lenses should take into account that against the background of the use of beta-blockers, a decrease in the production of lacrimal fluid is possible. When performing surgical interventions, the anesthesiologist should be warned that the patient is taking beta-blockers. Nebivolol does not affect the concentration of glucose in blood plasma in patients with diabetes mellitus. However, caution should be exercised in the treatment of these patients, since Nebilet® may mask certain symptoms of hypoglycemia (eg, tachycardia) caused by the use of oral hypoglycemic agents and insulin. Control of the concentration of glucose in the blood plasma should be carried out 1 time in 4-5 months (in patients with diabetes mellitus). With hyperthyroidism, beta-blockers can mask tachycardia. Beta-blockers should be used with caution in patients with chronic obstructive pulmonary disease, as bronchospasm may increase. Beta-blockers may increase sensitivity to allergens and the severity of anaphylactic reactions. Influence on the ability to drive vehicles and control mechanisms The effect of the drug Nebilet® on the ability to drive vehicles and control mechanisms has not been specifically studied. Studies of the pharmacodynamics of nebivolol have shown that Nebilet® does not affect psychomotor function. During the period of treatment with Nebilet® (if side effects occur), care should be taken when driving vehicles and when engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Pharmacological action Cardioselective beta1-blocker. It has antihypertensive, antianginal and antiarrhythmic effects. Reduces high blood pressure at rest, during physical exertion and stress. Competitively and selectively blocks postsynaptic ?1-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 ?1-adrenergic receptors; — L-nebivolol has a mild vasodilating effect by modulating the release of vasodilator factor (NO) from the vascular endothelium. The hypotensive effect is also due to a decrease in the activity of the renin-angiotensin-aldosterone system (RAAS) (does not directly correlate with changes in plasma renin activity). A stable hypotensive effect develops after 1-2 weeks of regular use of the drug, and in some cases – after 4 weeks, a stable effect is observed after 1-2 months. By reducing myocardial oxygen demand (decreased heart rate and reduced preload and afterload), it reduces the number and severity of angina attacks and increases exercise tolerance. The antiarrhythmic effect is due to the suppression of the pathological automatism of the heart (including in the pathological focus) and the slowing of AV conduction. Pharmacokinetics Absorption After oral administration, both enantiomers are rapidly absorbed. Food does not affect absorption, so nebivolol can be taken with or without food. The bioavailability of nebivolol after oral administration averages 12% in individuals with a “fast” metabolism (effect of the first pass through the liver) and is almost complete in individuals with a “slow” metabolism. Distribution In plasma, both enantiomers are predominantly bound to albumin. Plasma protein binding for D-nebivolol is 98.1%, and for L-nebivolol it is 97.9%. Metabolism Metabolized by acyclic and aromatic hydroxylation and partial N-dealkylation. The resulting hydroxy- and amino derivatives are conjugated with glucuronic acid and excreted as O- and N-glucuronides. Excretion Excreted by the kidneys (38%) and through the intestines (48%). In persons with a “fast” metabolism T1 / 2 of hydroxymetabolites – 24 hours, enantiomers of nebivolol – 10 hours; in persons with a “slow” metabolism: hydroxymetabolites – 48 hours, enantiomers of nebivolol – 30-50 hours. The excretion of unchanged nebivolol in the urine is less than 0.5% of the amount of the drug taken orally. Indications for use – arterial hypertension; – ischemic heart disease: prevention of angina attacks; – chronic heart failure (as part of combination therapy). Dosage and administration Tablets are taken orally, 1 time / day, preferably always at the same time of day, regardless of food intake, with a sufficient amount of liquid. The average daily dose for the treatment of arterial hypertension and coronary artery disease is 2.5-5 mg (1/2-1 tab.). Nebilet® can be used as monotherapy or in combination with other blood pressure lowering agents. In patients with renal insufficiency, as well as in patients over the age of 65, the recommended initial dose is 2.5 mg (1/2 tab.) / day. If necessary, the daily dose can be increased to a maximum of 10 mg (2 tablets of 5 mg in 1 dose). Treatment of chronic heart failure should begin with a slow dose increase until the individual optimal maintenance dose is reached. Dose selection at the beginning of treatment should be carried out according to the following scheme, while maintaining intervals of 1 to 2 weeks and based on the tolerance of this dose by the patient: a dose of 1.25 mg of nebivolol (1/4 tab. 5 mg) 1 time / day can be increased first to 2.5-5 mg (1/2 tab. 5 mg or 1 tab. 5 mg), and then to 10 mg (2 tab. 5 mg) 1 time / day. The maximum daily dose is 10 mg 1 time / day. At the beginning of treatment and with each increase in dose, the patient should be under the supervision of a physician for at least 2 hours to ensure that the clinical condition remains stable (especially blood pressure, heart rate, conduction disturbances, as well as symptoms of exacerbation of chronic heart failure). Rules for dividing tablets To divide, place the tablet on a hard, flat surface with a cross-shaped notch up, press the tablet with both index fingers. For 1/4 tablet, repeat the same steps for 1/2 tablet. Use during pregnancy and lactation During pregnancy, Nebilet® is prescribed only for vital indications, when the benefit to the mother outweighs the possible risk to the fetus or newborn (due to the possible development of bradycardia, arterial hypotension, hypoglycemia in the fetus and newborn). If treatment with Nebilet® is necessary, then uteroplacental blood flow and fetal growth should be monitored. Treatment must be interrupted 48-72 hours before delivery. In cases where this is not possible, it is necessary to establish strict observation of newborns within 48-72 hours after delivery. Nebivolol is excreted in breast milk. If you need to take the drug Nebilet® during lactation, breastfeeding should be stopped. Precautions Contraindicated in severe liver dysfunction. In patients with renal insufficiency, the initial dose is 2.5 mg / day. Contraindicated in children and adolescents under 18 years of age. The drug should be used with caution in patients over the age of 75 years. Interaction with other drugs Pharmacodynamic interaction With the simultaneous use of beta-blockers with blockers of slow calcium channels (verapamil and diltiazem), the negative effect on myocardial contractility and AV conduction is enhanced. Contraindicated in / in the introduction of verapamil against the background of the use of nebivolol. With the simultaneous use of nebivolol with antihypertensive drugs, nitroglycerin or slow calcium channel blockers, severe arterial hypotension may develop (special caution is necessary when combined with prazosin). With the simultaneous use of nebivolol with class I antiarrhythmic drugs and with amiodarone, it is possible to increase the negative inotropic effect and lengthen the time of excitation through the atria. With the simultaneous use of nebivolol with cardiac glycosides, there was no increase in the effect on slowing down AV conduction. The simultaneous use of nebivolol and drugs for general anesthesia can cause suppression of reflex tachycardia and increase the risk of arterial hypotension. A clinically significant interaction of nebivolol and NSAIDs has not been established. The simultaneous use of nebivolol with tricyclic antidepressants, barbiturates and phenothiazine derivatives may enhance the hypotensive effect of nebivolol. Pharmacokinetic interaction With the simultaneous use of nebivolol with drugs that inhibit the reuptake of serotonin, or other agents that biotransform with the participation of the CYP2D6 isoenzyme, the concentration of nebivolol in the blood plasma increases, the metabolism of nebivolol slows down, which can lead to the risk of bradycardia. When used simultaneously with digoxin, nebivolol does not affect the pharmacokinetic parameters of digoxin. With the simultaneous use of nebivolol with cimetidine, the concentration of nebivolol in the blood plasma increases. The simultaneous use of nebivolol and ranitidine does not affect the pharmacokinetic parameters of nebivolol. With the simultaneous use of nebivolol with nicardipine, the concentration of active substances in the blood plasma increases slightly, but this has no clinical significance. Co-administration of nebivolol and ethanol, furosemide or hydrochlorothiazide does not affect the pharmacokinetics of nebivolol. No clinically significant interaction between nebivolol and warfarin has been established. With the combined use of nebivolol with insulin and oral hypoglycemic agents, symptoms of hypoglycemia (tachycardia) may be masked. Contraindications – acute heart failure; – chronic heart failure in the stage of decompensation (requiring intravenous administration of drugs with an inotropic effect); – severe arterial hypotension (systolic blood pressure less than 90 mm Hg); – SSSU, including sinoatrial blockade; – AV block II and III degree (without artificial pacemaker); – bradycardia (heart rate less than 60 bpm); – cardiogenic shock; – pheochromocytoma (without the simultaneous use of alpha-blockers); – metabolic acidosis; – severe violations of liver function; – bronchospasm and bronchial asthma in history; – severe obliterating diseases of peripheral vessels (intermittent claudication, Raynaud’s syndrome); – myasthenia gravis; – depression; – lactose intolerance, lactase deficiency and glucose / galactose malabsorption syndrome; – children and adolescents under 18 years of age (efficacy and safety have not been studied); – hypersensitivity to nebivolol or one of the components of the drug. With caution, the drug should be used for renal failure, diabetes mellitus, hyperthyroidism, a history of allergic diseases, psoriasis, chronic obstructive pulmonary disease, AV block I degree, Prinzmetal’s angina, as well as patients over the age of 75 years. CompositionNebivolol hydrochloride micronized 5.45 mg, which corresponds to the content of nebivolol 5 mg – 16.1 mg, colloidal silicon dioxide – 0.69 mg, magnesium stearate – 1.15 mg. Overdose Symptoms: marked decrease in blood pressure, nausea, vomiting, cyanosis, sinus bradycardia, AV blockade, bronchospasm, loss of consciousness, cardiogenic shock, coma, cardiac arrest. Treatment: gastric lavage, activated charcoal. In the case of a pronounced decrease in blood pressure, it is necessary to give the patient a horizontal position with raised legs, if necessary, in / in the introduction of fluid and vasopressors. In case of bradycardia, 0.5-2 mg of atropine should be administered intravenously; in the absence of a positive effect, a transvenous or intracardiac pacemaker can be placed. With AV blockade (II-III stage), it is recommended to / in the introduction of beta-adrenergic stimulants, if they are ineffective, the question of setting an artificial pacemaker should be considered. In heart failure, treatment begins with the introduction of cardiac glycosides and diuretics, in the absence of an effect, it is advisable to administer dopamine, dobutamine or vasodilators. With bronchospasm, intravenous α2-adrenergic stimulants are used. With ventricular estrasystole – lidocaine (antiarrhythmic drugs of class IA cannot be administered). Side effects Frequency of side effects: very often (> 10%), often (> 1% and <10%), infrequently (> 0.1% and <1%), rarely (> 0.01% and <0.1%), very rarely (< 0.01% including individual messages). From the side of the central nervous system and peripheral nervous system: often - headache, dizziness, fatigue, weakness, paresthesia; infrequently - depression, nightmares, confusion; very rarely - fainting, hallucinations. From the digestive system: often - nausea, constipation, diarrhea; infrequently - dyspepsia, flatulence, vomiting. From the side of the cardiovascular system: infrequently - bradycardia, acute heart failure, AV blockade, orthostatic hypotension, Raynaud's syndrome. On the part of the skin and subcutaneous tissues: infrequently - skin rash of an erythematous nature, itching; very rarely - aggravation of the course of psoriasis; in some cases - angioedema. Other: infrequently - bronchospasm; rarely - dry eyes. Storage conditions The drug should be stored out of the reach of children at a temperature not exceeding 25 ° C. Buy Nebilet tablets 5mg No. 14x2