Arterial hypertension. Mild and moderate stable chronic heart failure as adjuvant therapy for standard therapy in elderly patients (> 70 years of age).
Composition:
1 tabl contains 5 mg of nebivolol in the form of a hydrochloride.
Action:
Nebivolol is the racemate of two enantiomers: SRRR nebivolol (d-nebivolol) and RSSS nebivolol (1-nebivolol) with dual pharmacological activity. It is a competitive and selective antagonist of β-adrenergic receptors (the SRRR enantiomer), has a mild vasodilatory effect related to the influence on the metabolic pathway L-arginine / nitric oxide. It does not show α-adrenergic antagonism. Following oral administration, both enantiomers of nebivolol are rapidly absorbed from the gastrointestinal tract (food does not affect the absorption of the drug). Nebivolol is almost completely metabolised, partly to active hydroxyl derivatives. Bioavailability is about 12% in people with rapid metabolism and is almost complete in people with low metabolism. After using the same doses, the maximum concentration of unchanged nebivolol in blood is about 23 times higher in slow metabolisers compared to people with rapid metabolism. T0,5 enantiomers are in people with rapid metabolism of about 10 h; in patients with a slow metabolism is 3-5 times longer. In patients with rapid metabolism T0,5 The hydroxyl metabolites of both enantiomers are about 24 h, it is twice as long in people with low metabolism. In most patients (rapidly metabolizing) steady-state blood levels of nebivolol are achieved within 24 h and hydroxylated metabolites within a few days. Both enantiomers mainly bind to serum albumin. 38% of the administered dose is excreted in the urine and 48% in the faeces.
Contraindications:
Hypersensitivity to the components of the preparation. Liver failure or liver dysfunction. acute heart failure, cardiogenic shock or episodes of decompensated heart failure requiring intravenous administration of positive inotropic drugs. The sick bay syndrome, including the sinoatrial block. Atrio-ventricular block IIst. or III degree (without starter). Bronchial asthma or chronic obstructive lung disease. Untreated phaeochromocytoma. Metabolic acidosis. Bradycardia (heart rate <60 beats per minute before starting treatment). Hypotension (systolic blood pressure <90 mmHg). Severe peripheral circulation disorders.
Precautions:
Do not use in patients with severe renal impairment (creatinine blood ≥250 μmol / l) and in patients with untreated congestive heart failure until their condition has stabilized. Use caution in patients with peripheral circulation disorders (Raynaud's disease or syndrome, intermittent claudication - possible exacerbation of the disease), heart block Ist. (prolonged conduction time), Prinzmetal angina (risk of coronary artery spasm, increased number and prolonged angina) and patients over 75 years. In patients with ischemic disease, nebivolol should be discontinued gradually, ie for more than 1-2 weeks. if necessary, institute appropriate treatment to prevent exacerbation of angina. Beta-blockers may cause bradycardia: if the pulse rate is below 50-55 beats per minute and (or) the patient feels symptoms suggesting bradycardia, the dose should be reduced. Nebivolol may mask the symptoms of tachycardia in hyperthyroidism and hypoglycaemia (be cautious in patients with diabetes). Caution should be exercised when administering the preparation in patients with chronic obstructive respiratory diseases (risk of worsening of narrowing of the airways) and psoriasis. The drug may increase sensitivity to allergens and exacerbate anaphylactic reactions. Due to the lactose content, the preparation should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.Due to the lack of data on the use of nebivolol in children and adolescents under 18 years of age, use is not recommended.
Pregnancy and lactation:
Nebivolol may interfere with the normal course of pregnancy and / or cause disorder in the fetus or newborn. Β-blockers reduce the flow of blood through the placenta, which is associated with growth retardation, intrauterine fetal death, miscarriage or premature delivery. In the fetus and newborn nebivolol can cause, among others hypoglycaemia and bradycardia. If treatment with β-blockers is necessary, drugs that selectively block β receptors are recommended1-Adrenergic. The drug should not be used during pregnancy unless it is absolutely necessary. If it is considered that nebivolol treatment is necessary, uterine placental blood flow and fetal development should be monitored. The newborn should be under strict control. Symptoms of hypoglycaemia and bradycardia may occur within the first 3 days. It is not recommended to use the product during breastfeeding.
Side effects:
Common: pain and dizziness, paresthesia, shortness of breath, constipation, nausea, diarrhea, fatigue, edema. Uncommon: nightmares, depression, blurred vision, bradycardia, heart failure, atrioventricular conduction / atrioventricular block, arterial hypotension, intermittent claudication, bronchospasm, indigestion, bloating, vomiting, pruritus, erythematous rash, impotence. Very rare: fainting, worsening of psoriasis. In addition, there were: angioneurotic edema, hallucinations, psychosis, confusion, cold / bruising of limbs, Raynaud's, dry eye and oculi-muco-cutaneous syndrome, decreased tear secretion. In patients with chronic heart failure, bradycardia, dizziness, worsening of heart failure, orthostatic hypotension, hypersensitivity reactions, and atrioventricular block Ist were observed. and swollen limbs.
Dosage:
Orally. Adults.Hypertension: 5 mg a day at a fixed time (the effect occurs after 1-2 weeks of treatment, in some cases - after 4 weeks). It is possible to use β-blockers alone or in combination with other antihypertensive agents, so far, the additive antihypertensive effect has only been observed when co-administered with hydrochlorothiazide 12.5-25 mg. In renal failure and patients> 65 years, the recommended starting dose is 2.5 mg per day, which can be increased to 5 mg if necessary.Chronic heart failure. The condition of patients should be stable (without acute failure for 6 weeks before starting treatment). In patients receiving cardiovascular medications, including diuretics, Digoxin, ACE inhibitors, angiotensin II receptor antagonists, the doses of these drugs should be determined during the 2 weeks before treatment with nebivolol. Starting treatment and increasing the dose should be done under the supervision of a physician experienced in the treatment of chronic heart failure, the patient should be observed for at least 2 hours. The starting dose is 1.25 mg once a day, it should be increased gradually (doubling the dose) every 1 hour. -2 weeks to obtain an effective maintenance dose. The maximum daily dose is 10 mg. The tablet should be taken with a glass of water and taken with or without food. The tablet can be divided into half.
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