Index of drugs

Treatment of essential hypertension. Treatment of mild to moderate stable chronic heart failure as adjunctive therapy to standard therapy in elderly patients (≥70 years).

1 tabl contains 5 mg of nebivolol (as hydrochloride); drug contains lactose.

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 associated with the interaction of the L-arginine / nitric oxide metabolic pathway. It causes relief of heart activity and lowering of blood pressure at rest and during physical activity, both in people with normal pressure and with hypertension. It does not show α-adrenergic antagonism. After oral administration, both enantiomers of nebivolol are rapidly absorbed from the gastrointestinal tract (food does not affect the absorption of nebivolol). It is extensively metabolised, in part to active hydroscimetabolites. The bioavailability of nebivolol is about 12% in people with rapid metabolism and is almost complete in people with low metabolism. After applying the same doses of C_max unchanged nebivolol in blood is about 23 times higher in people with slow metabolism compared to people with rapid metabolism. T_0,5 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 T_0,5 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 (98.1% for nebivolol SRRR and 97.9% for nebivolol RSSS). Within one week of administration, 38% of the dose is excreted in the urine and 48% in the faeces.

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. Heart block IIst. and III. (without starter). Bronchospasm in the interview and bronchial asthma. Untreated phaeochromocytoma. Metabolic acidosis. Bradycardia (heart rate <60 beats / min before starting treatment). Hypotension (systolic blood pressure <90 mmHg). Severe peripheral circulation disorders. Co-administration of floctafenine or sultopride.

Persistent blockade of β-adrenergic receptors reduces the risk of arrhythmia during the introduction of anesthesia and intubation. If blockade of β-adrenergic receptors is interrupted in order to prepare the patient for surgery, the β-blockers should be discontinued at least 24 hours before the procedure. Caution should be exercised when using some anesthetic agents depressing the myocardium. The vagus nerve can be prevented by intravenous administration of atropine. Do not use β-blockers in patients with untreated congestive heart failure until their condition has stabilized. If the pulse rate is <50-55 beats per minute at rest and (or) the patient experiences symptoms indicating bradycardia, the dose should be reduced. Caution in patients with: peripheral circulation disorders (Raynaud's disease or symptom, intermittent claudication) - risk of exacerbation of these disorders; heart block Ist. - prolonged conduction time; Prinzmetal angina - the risk of increasing the number and duration of angina attacks; diabetes - risk of masking the symptoms of hypoglycaemia (tachycardia, palpitations); chronic obstructive pulmonary diseases - the risk of worsening of narrowing of the airways.Β-blockers can mask the symptoms of tachycardia in hyperthyroidism; sudden withdrawal of the preparation may exacerbate symptoms. Patients with a history of psoriasis should only take β-blockers after careful consideration. The initiation of treatment for chronic heart failure with nebivolol requires regular observation. In patients with ischemic heart disease, treatment with beta-blockers should be discontinued gradually, ie for more than 1-2 weeks; if necessary, replacement therapy should be initiated at the same time to prevent exacerbation of angina. It is not usually recommended to co-administer nebivolol with Verapamil and diltiazem Calcium antagonists, class I antiarrhythmics, and centrally-acting antihypertensives. Β-blockers can increase the sensitivity to allergens and the severity of anaphylactic reactions. There are no data on the use of nebivolol in children and adolescents - use is not recommended. Due to the lactose content, do not use the preparation in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

Nebivolol can have a harmful effect on pregnancy and / or on the fetus / newborn baby. Β-adrenergic blocking drugs reduce the blood flow through the placenta, which is associated with growth retardation, intrauterine fetal death, miscarriage or preterm 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. Nebivolol should not be used during pregnancy unless clearly necessary, then the utero-placental blood flow and fetal development should be monitored. The newborn should be closely watched. Symptoms of hypoglycaemia and bradycardia may occur within the first 3 days. It is not known whether the drug is excreted in breast milk, therefore breast-feeding is not recommended when taking nebivolol.

Hypertension. 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, occurrence or worsening of intermittent claudication, bronchospasm, indigestion, bloating, vomiting, pruritus, erythematous rash, impotence. Very rare: angioneurotic edema, fainting, worsening of psoriasis. Not known: hypersensitivity. Some hallucinations, psychoses, confusion, cold / bruising of limbs, Raynaud's, dry eyes, and oculo-mucocutaneous syndrome typical for practicalolol have also been observed with the use of certain β-adrenergic blocking agents.Chronic heart failure. The most common were: bradycardia and dizziness. In addition, the following may occur: severity of heart failure, orthostatic hypotension, drug intolerance, atrioventricular block Ist, lower limb edema.

Orally. Adults.Hypertension: 5 mg daily at the same time of the day (the effect occurs after 1-2 weeks of treatment, in some cases - after 4 weeks). Β-blockers can be used as monotherapy or in combination with other antihypertensive agents; so far, the antihypertensive effect was observed only after administration of nebivolol and 12.5-25 mg of hydrochlorothiazide. In renal insufficiency and in patients> 65 years, the recommended starting dose is 2.5 mg daily, which can be increased to 5 mg if necessary. Patients> 75 years should be cautious and closely watched.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 stabilized during the 2 weeks before treatment with nebivolol. The starting dose of nebivolol is 1.25 mg once a day, it should be gradually increased (doubling the dose) every 1-2 weeks to obtain an effective maintenance dose. The maximum dose is 10 mg once a day.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 h to ensure that the clinical condition remains stable (especially blood pressure, heart rate, conduction abnormalities, symptoms of worsening heart failure). During a gradual dose escalation, if your heart failure or intolerance is worsening, it is recommended to reduce the dose of nebivolol first or, if necessary, stop treatment immediately (in severe hypotension, worsening heart failure with acute pulmonary edema, cardiogenic shock, symptomatic bradycardia or atrial block) -komorowego). Sudden discontinuation of treatment with nebivolol is not recommended, as it may lead to transient worsening of heart failure. If treatment discontinuation is necessary, the dose should be reduced gradually, by half every week. No dose adjustment is required for mild to moderate renal impairment. No experience in patients with severe renal impairment (serum creatinine ≥250 μmol / l), therefore the use of nebivolol in these patients is not recommended.
The tablet should be taken with a glass of water and taken with or without food. The tablet can be divided into 4 equal parts.