Nebilet 5mg tabs 14 pcs

Description

Composition
Active substance:
1 tablet contains: micronized nebivolol hydrochloride – 5.45 mg (equivalent nebivolol – 5.00 mg).
Excipients:
Lactose monohydrate – 141, 75 mg; Corn starch – 46.0 mg; Croscarmellose sodium – 13.80 mg; Hypromellose (viscosity 15 mPas.) – 4.60 mg; Polysorbate 80 – 0.46 mg; microcrystalline cellulose – 16.10 mg; colloidal silicon dioxide – 0.69 mg; magnesium stearate – 1.15 mg.
Description:
Round biconvex tablets almost white with cruciform notch for division.
Product form:
Tablets of 5 mg.
At 7 or 14 tablets in blisters (blister) [PVC / aluminum foil].
1, 2 or 4 blister together with instructions for use in a cardboard box.
Contraindications
Hypersensitivity to the active agent or one component of the drug; congestive heart failure; chronic heart failure decompensation (requiring intravenous administration of drugs with inotropic effect); marked hypotension (systolic blood pressure less than 90 mmHg..); sick sinus syndrome, including sinus block; atrioventricular block II and III degree (without pacemaker); bradycardia (heart rate less than 60 beats / min.); cardiogenic shock; pheochromocytoma (without simultaneous application of alpha-blockers); metabolic acidosis; severe liver function; bronchospasm and bronchial asthma in history; heavy obliterating peripheral vascular disease ( “intermittent” claudication, Raynaud’s syndrome); myasthenia gravis; depression; lactose intolerance, lactase deficiency and syndrome of glucose-galactose malabsorption; age 18 years (effectiveness and safety have not been studied in this age group).
Precautions renal failure; diabetes; hyperthyroidism; allergic diseases, psoriasis; chronic obstructive pulmonary disease; I degree atrioventricular block; Prinzmetal angina; age over 75 years.
Dosage
5 mg
Indications
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).
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.
pharmacokinetic interactions
With simultaneous application of nebivolol with drugs that inhibit the reuptake of serotonin, or by other means involving biotransformed isozyme CYP2D6. nebivolol increases the concentration in blood 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.
When nebivolol joint application with insulin and hypoglycemic agents for oral administration may be masked symptoms of hypoglycemia (tachycardia).
Overdose
Symptoms: marked reduction of blood pressure, nausea, vomiting, cyanosis, sinus bradycardia, atrioventricular (AV) block, bronchospasm, loss of consciousness, cardiogenic shock, 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. 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 bronchospasm used in / beta2-adrenergic receptors. When ventricular extrasystole – lidocaine (antiarrhythmic drugs can not be administered IA class).
pharmachologic effect
Pharmacodynamics:
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 modulate release factor endothelial vasodilator 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 competitive and highly selective blocker of the beta1-adrenergic receptors; L-nebivolol has a mild vasodilator action for 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.
Pharmacokinetics:
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 orally administered 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%.
Withdrawal. It metabolized by nebivolol alicyclic and aromatic hydroxylation, N-dealkylation partial. 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” metabolic-hydroxy-metabolites – 24 hours, enantiomers nebivolol – 10 hours; patients with “slow” metabolism:. gidroksimetabolitov – 48 hours, enantiomers nebivolol – 30 – 50 hour excretion through the kidney unchanged nebivolol is less than 0.5% of the dose ingested.
Pregnancy and breast-feeding
When pregnancy Nebilet® 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 Nebilet® necessary, should be carried out monitoring of the utero-placental blood flow and fetal growth. 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 within 48-72 hours after delivery.
Nebivolol is excreted in breast milk. If necessary, the drug Nebilet® lactation, breastfeeding must stop.
Conditions of supply of pharmacies
On prescription.
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;
Very rare: syncope, hallucinations.
Disorders of the gastrointestinal tract:
Common: nausea, constipation, diarrhea;
Uncommon: dyspepsia, flatulence, vomiting.
Violations of the cardiovascular system:
Infrequently: aetiology, acute heart failure, heart block, orthostatic hypotension, Raynaud’s syndrome.
Violations of the skin and subcutaneous tissue disorders:
Uncommon: rash erythematous character, itching;
Very rare: aggravation of current psoriasis;
In some cases: angioedema.
Other:
Uncommon: bronchospasm;
Rare: 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. (See. Section “Contraindications”).
When deciding on the use of the drug Nebilet® 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 Nebilet® 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.
Effects on ability to drive vehicles and management mechanisms
Nebilet® influence of the drug on the ability to drive vehicles and management mechanisms have not been studied specifically. Study the pharmacodynamics of nebivolol showed that Nebilet® drug has no effect on psychomotor performance. During drug treatment Nebilet® (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
Store at a temperature not higher than 25 C.
Keep out of the reach of children!.
Dosing and Administration
Nebilet® 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 is 2.5-5 mg Nebilet® preparation (1 / 2-1 tab).
Nebilet® may be used alone or in combination with other agents that reduce blood pressure.
In patients with renal failure and patients over 65 years recommended starting dose of 1/2 tablet (2.5 mg) of the drug per day Nebilet®. 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: dose of 1.25 mg Nebilet® drug (1/4 5 mg tablets) once in 1 per day may be increased first to 2.5 – 5 mg once a day Nebilet® drug (2.1 to 5 mg tablets or one tablet), and then – 10 mg (2 tablets of 5 mg), 1 time per day .
The maximum daily dose is 10 mg 1 time per day.
At the beginning of treatment and at each increasing dose the patient should be at least 2 hours 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).
To divide the tablet put on a hard, flat surface cruciform notch upward push the pill two forefingers. For a quarter (1/4) tablets repeat the same action and a half (1/2) tablets.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist