Nebilong, tablets 10 mg 30 pcs

Nebilong is a III generation cardioselective beta-adrenoblocker with vasodilatory properties.

The active substance is a racemate consisting of two enantiomers: D-nebivololol and L-nebivolol.

Nebivololol is a competitive and selective blocker of β1-adrenoreceptors (affinity to β1-adrenoreceptors is 288 times higher than to β2-adrenoreceptors). In addition it has mild vasodilatory action due to modulation of release of relaxing factor (NO) from vascular endothelium.

Nebivololol decreases HR and BP at rest and at load, decreases left ventricular end-diastolic pressure, decreases PEEP, improves diastolic heart function (decreases filling pressure), increases ejection fraction; causes antianginal effect in CHD patients.

The optimal hypotensive effect is seen after 1-2 weeks of treatment. In some cases maximal effect is reached after 4 weeks.

Indications

Essential (primary) arterial hypertension, IHD.

Active ingredient

Composition

1 tablet contains nebivolol 10 mg.

How to take, the dosage

Adults for oral administration – 2.5-5 mg/day in the morning.

The optimal effect develops after 1-2 weeks of treatment, and in some cases – after 4 weeks.

If necessary the daily dose is increased up to 10 mg/day.

For patients over 65 years of age the starting dose is 2.5 mg/day. If necessary, the daily dose can be increased to 5 mg.

Interaction

Concomitant use with antiarrhythmic drugs of class I, amiodarone may increase negative inotropic effect and inhibition of AV conduction.

In concomitant use with calcium channel blockers (verapamil and diltiazem) the negative inotropic effect and suppression of AV conduction are increased.

Concomitant use with sympathomimetics suppresses pharmacological activity of nebivololol.

Concomitant use with anesthetic agents may suppress reflex tachycardia and increase the risk of arterial hypotension.

Concomitant use with tricyclic antidepressants, barbiturates, phenothiazine derivatives may increase the antihypertensive effect of nebivolol.

Concomitant use with cimetidine may increase plasma concentrations of nebivololol.

Special Instructions

Nebilong should be used with caution in patients with renal insufficiency, thyroid hyperfunction, allergic diseases, psoriasis, persons aged over 65 years and diabetics. Beta-adrenoblockers should be withdrawn gradually over 10 days (up to 2 weeks in patients with CHD). At the beginning of treatment, BP and HR should be monitored daily.

The efficacy of beta-adrenoblockers in smokers is lower than in non-smokers. Nebivolol has no effect on glucose levels in patients with diabetes, however certain signs of hypoglycemia (tachycardia, palpitations) caused by the use of hypoglycemic agents may be masked by nebivolol. If it is necessary to use nebivolol in patients with psoriasis, the expected benefit of therapy and the possible risk of psoriasis exacerbation should be carefully evaluated.

Beta-adrenoblockers should be used with caution in patients with elevated thyroid function due to the fact that tachycardia may be alleviated under the influence of beta-adrenoblockers. Nebivolol may increase the symptoms of peripheral circulatory disorders.

Patients who wear contact lenses should consider that against the background of the use of beta-adrenoblockers there may be a decrease in lacrimal fluid production. If surgery is performed, the anesthesiologist should be advised that the patient is taking beta-adrenoblockers.

Plasma glucose control should be performed once every 4-5 months (in diabetic patients). Control of laboratory indexes of renal function should be carried out once every 4-5 months (in elderly patients). It is not recommended to use in children.

Contraindications

Bronchial asthma, decompensated chronic heart failure, untreated pheochromocytoma, severe liver dysfunction, depression, angiospastic angina pectoris (Prinzmetal angina), obliterating peripheral vascular disease (intermittent claudication), hypotension, cardiogenic shock, bradycardia (HR

Side effects

CNS and peripheral nervous system disorders: headache, dizziness, fatigue, paresthesia, depression, decreased ability to concentrate, drowsiness, insomnia, nightmares, hallucinations.

Digestive system disorders: nausea, constipation, diarrhea, dry mouth.

Cardiovascular system disorders: bradycardia, orthostatic hypotension, dyspnea, edema, heart failure, AV-blockade, heart rhythm disorders, Raynaud’s syndrome, cardialgia.

Allergic reactions: skin rash.

Other: bronchospasm (including in the absence of obstructive lung disease in the anamnesis), photodermatosis, hyperhidrosis, rhinitis.

Overdose

Symptoms: bradycardia, arterial hypotension, bronchospasm and acute heart failure.

Treatment: in case of overdose or hypersensitivity reaction the patient should be under medical supervision and treated in the intensive care unit. Blood glucose concentration should be determined. Gastric lavage, prescription of laxatives and enterosorbents will prevent absorption of drug residues in the gastrointestinal tract.

In treatment of bradycardia, atropine or methylatropine are prescribed. In case of hypotension, replacement plasma transfusion and administration of catecholamines are performed. The effect of β-adrenoreceptor blockade can be reversed by slow IV administration of isoprenaline hydrochloride, starting at a dose of 5 µg/min, or dobutamine, starting at a dose of 2.5 µg/min, until the desired effect is achieved.

If there is no effect, consideration should be given to an intravenous injection of glucagon 50-100 µg/kg. If necessary, the injection can be repeated after one hour, followed by glucagon infusion at a dose of 70 µg/kg/h.

Pregnancy use

The use in pregnancy is possible only under strict indications (due to the possible development of bradycardia, arterial hypotension, hypoglycemia and respiratory paralysis in newborns).

The use of nebivololol should be stopped 48-72 hours before delivery. Where this is not possible, close monitoring of the newborn should be ensured for 48-72 h after delivery.

Similarities