Nebilong, tablets 5 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-nebivolol 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 DFS, 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, coronary artery disease.

Pharmacological effect

Nebilong is a third-generation cardioselective beta-blocker with vasodilating properties. The active substance is a racemate consisting of two enantiomers: D-nebivolol and L-nebivolol.

Nebivolol is a competitive and selective blocker of β1-adrenergic receptors (the affinity for β1-adrenergic receptors is 288 times higher than for β2-adrenergic receptors), in addition, it has a mild vasodilating effect by modulating the release of relaxing factor (NO) from the vascular endothelium.

Nebivolol reduces heart rate and blood pressure at rest and during exercise, reduces left ventricular end-diastolic pressure, reduces peripheral vascular resistance, improves diastolic heart function (reduces filling pressure), increases ejection fraction; causes an antianginal effect in patients with coronary artery disease.

The optimal hypotensive effect appears after 1-2 weeks of treatment. In some cases, the maximum effect is achieved after 4 weeks.

Special instructions

Use Nebilong with caution in patients with renal failure, hyperfunction of the thyroid gland, allergic diseases, psoriasis, people over 65 years of age and patients with diabetes mellitus. The withdrawal of beta-blockers should be carried out gradually over 10 days (up to 2 weeks in patients with coronary artery disease).

At the beginning of treatment, blood pressure and heart rate should be monitored daily. The effectiveness of beta-blockers in smokers is lower than in non-smokers. Nebivolol has no effect on glucose levels in patients with diabetes, however, under the influence of nebivolol, certain signs of hypoglycemia (tachycardia, rapid heartbeat) caused by the use of hypoglycemic drugs may be masked.

If it is necessary to use nebivolol in patients with psoriasis, the expected benefits of therapy and the possible risk of exacerbation of psoriasis should be carefully assessed. Beta-blockers should be used with caution in case of increased thyroid function due to the fact that under the influence of beta-blockers, tachycardia can be leveled. Nebivolol may increase symptoms of peripheral circulatory disorders.

Patients wearing contact lenses should take into account that the use of beta-blockers may reduce the production of tear fluid. When performing surgical interventions, the anesthesiologist should be warned that the patient is taking beta-blockers.

Monitoring of glucose levels in blood plasma should be carried out once every 4-5 months (in patients with diabetes mellitus). Laboratory tests of renal function should be monitored once every 4-5 months (in elderly patients). Use in children is not recommended.

Active ingredient

Nebivolol

Composition

1 tablet contains nebivolol 5 mg.

Pregnancy

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

Nebivolol should be stopped 48-72 hours before delivery.

In cases where this is not possible, newborns should be closely monitored for 48 to 72 hours after birth.

Contraindications

Bronchial asthma, chronic heart failure in the decompensation stage, untreated pheochromocytoma, severe liver dysfunction, depression, angiospastic angina (Prinzmetal’s angina), obliterating peripheral vascular diseases (intermittent claudication syndrome), arterial hypotension, cardiogenic shock, bradycardia (heart rate less than 50 beats/min), SSSU, AV block II and III degrees, myasthenia gravis, muscle weakness, children and adolescents up to 18 years of age, hypersensitivity to nebivolol.

Side Effects

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

From the digestive system: nausea, constipation, diarrhea, dry mouth.

From the cardiovascular system: bradycardia, orthostatic hypotension, shortness of breath, edema, heart failure, AV block, cardiac arrhythmias, Raynaud’s syndrome, cardialgia.

Allergic reactions: skin rash.

Other: bronchospasm (including in the absence of a history of obstructive pulmonary diseases), photodermatosis, hyperhidrosis, rhinitis.

Interaction

When used simultaneously with class I antiarrhythmic drugs, amiodarone, the negative inotropic effect and inhibition of AV conduction may be enhanced.

When used simultaneously with calcium channel blockers (verapamil and diltiazem), the negative inotropic effect and inhibition of AV conduction are enhanced.

When used simultaneously with sympathomimetics, the pharmacological activity of nebivolol is suppressed.

When used simultaneously with anesthesia, it is possible to suppress reflex tachycardia and increase the risk of developing arterial hypotension.

When used simultaneously with tricyclic antidepressants, barbiturates, phenothiazine derivatives, the antihypertensive effect of nebivolol may be enhanced.

When used simultaneously with cimetidine, it is possible to increase the concentration of nebivolol in the blood plasma.

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 an intensive care unit.

It is necessary to determine the blood glucose concentration. Gastric lavage, prescribing a laxative and enterosorbents will prevent the absorption of drug residues into the gastrointestinal tract.

When treating bradycardia, atropine or methylatropine is prescribed. For hypotension, plasma exchange transfusion and catecholamine administration are performed.

The effect of β-adrenergic receptor blockade can be eliminated by slow intravenous administration of isoprenaline hydrochloride, starting at a dose of 5 mcg/min, or dobutamine, starting at a dose of 2.5 mcg/min, until the desired effect is achieved.

If there is no effect, the possibility of intravenous administration of glucagon 50–100 mcg/kg should be considered. If necessary, the injection can be repeated after an hour, followed by an infusion of glucagon at a dose of 70 mcg/kg/hour.

Storage conditions

At 15–30 °C

Shelf life

3 years

Manufacturer

Micro Labs Ltd, India