Nebivolol pills 5mg №28

Packaging

In packing of 28 pieces.

Mechanism of action

Nebivolol is a III generation cardioselective beta1-blocker with vasodilating properties. The active substance is a racemate consisting of two enantiomers: D-nebivolol and L-nebivolol. D-nebivolol is a competitive and highly selective blocker of β1-adrenoreceptors; L-nebivolol has a mild vasodilator effect by modulating the release of vasodilating factor (NO) from the vascular endothelium.
Nebivolol reduces heart rate and blood pressure at rest and under load, reduces the end diastolic pressure of the left ventricle, lowers the round neck, improves the diastolic function of the heart (lowers the filling pressure), increases the ejection fraction; causes an antianginal effect in patients with IHD.
The hypotensive effect is also due to a decrease in the activity of the renin-angiotensin system (it does not directly correlate with changes in the activity of renin in the blood plasma).
The antiarrhythmic effect is due to the suppression of the pathological automatism of the heart (including in the pathological focus) and the slowing down of AV conduction.
A sustained hypotensive effect develops after 1-2 weeks of regular use of the drug, and in some cases after 4 weeks, a stable effect is noted after 1-2 months.

• Arterial hypertension.
• CHD: prevention of strokes of angina.
• Chronic heart failure (as part of combination therapy).

Contraindications

Acute heart failure; chronic heart failure in the stage of decompensation (requiring iv injection of drugs with a positive inotropic effect); severe arterial hypotension (systolic blood pressure less than 90 mm Hg); SSSU, including sinoatrial blockade; AV-blockade II and III degree (without an artificial pacemaker); bradycardia (heart rate less than 60 beats / min); cardiogenic shock; pheochromocytoma (without simultaneous use of alpha-blockers); metabolic acidosis; severe liver dysfunction; a history of bronchospasm and bronchial asthma; severe obliterating diseases of peripheral vessels (intermittent claudication,Raynaud's syndrome); myasthenia gravis; depression; children and adolescents up to 18 years; Hypersensitivity to nebivolol.

Pregnancy and Breastfeeding

Use during pregnancy is possible only under strict indications (due to the possible development of newborn bradycardia, arterial hypotension, hypoglycemia and respiratory paralysis). Reception of nebivolol must be stopped 48-72 hours before delivery. In cases where this is not possible, strict monitoring of newborns should be ensured within 48-72 hours after delivery.

Special notes

Nebivolol should be used with caution in patients with renal insufficiency, diabetes, hyperthyroidism, history of allergies, psoriasis, COPD, AV-grade I blockade, Prinzmetal angina, as well as in patients over 75 years of age.
Cancellation 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 non-smokers.
Nebivolol does not affect glucose levels in patients with diabetes mellitus, however, under the action of nebivolol, certain signs of hypoglycemia (tachycardia, rapid heartbeat) caused by the use of hypoglycemic drugs may be masked.
If nebivolol is needed in patients with psoriasis, the expected benefit of therapy and the possible risk of exacerbation of psoriasis should be carefully evaluated.
Beta-blockers should be used with caution with increased thyroid function due to the fact that under the influence of beta-blockers tachycardia can be leveled.
Nebivolol may exacerbate the symptoms of peripheral circulation disorders.
Patients wearing contact lenses should take into account that, with the use of beta-blockers, it is possible to reduce the production of tear fluid.
When performing surgical interventions, the anesthesiologist should be warned that the patient is taking beta-blockers.
Control of glucose in the blood plasma should be carried out 1 time in 4-5 months (in patients with diabetes mellitus).
Monitoring laboratory parameters of renal function should be carried out 1 time in 4-5 months (in elderly patients).
Use in children is not recommended.

Composition

1 pill contains:

Active substance: nebivolol (nebivolol hydrochloride) 5.00 mg;

Excipients: lactose monohydrate 142.21 mg, corn starch 46.00 mg, croscarmellose sodium 13.8 mg, microcrystalline cellulose 16.10 mg, hypromellose-E15 4.6 mg, colloidal silicon dioxide 0.69 mg, Magnesium stearate 1.15 mg.

Dosage and administration

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 to 10 mg / day.
For patients over the age of 65, the initial dose is 2.5 mg / day. If necessary, the daily dose can be increased to 5 mg.

Adverse reactions

The frequency of adverse reactions listed below was determined accordingly to the following (classification of the World Health Organization): very often - at least 10%; often not less than 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including individual messages.
Since the cardiovascular system (CCC): infrequently - bradycardia, worsening of CHF, slowing of atrioventricular conduction, atrioventricular blockade, marked reduction of blood pressure, orthostatic hypotension, cardiac rhythm disturbances, cardialgia, progression of concomitant intermittent claudication, peripheral edema.
Nervous system: often - increased fatigue, headache, dizziness, paresthesias; infrequently - “nightmares”, reduced ability to concentrate, drowsiness, insomnia, depression; very rarely - hallucinations, fainting.
Special senses: infrequently - weakening of sight.
Respiratory: often - shortness of breath; infrequently - bronchospasm, rhinitis.
Gastrointestinal: often - dryness of the oral mucosa, constipation, nausea, diarrhea; infrequently - vomiting, flatulence.
From the skin: very rarely - exacerbation during psoriasis, photodermatosis, hyperhidrosis.
Allergic reactions: infrequently - pruritus, erythematous rash; very rarely - angioedema.
From the reproductive system: infrequently - impotence.

Drug Interactions

With simultaneous use with class I antiarrhythmic drugs, Amiodarone, it is possible to enhance the negative inotropic effect and suppress AV conductivity.
When applied simultaneously with Calcium channel blockers (verapamil and diltiazem), the negative inotropic effect and inhibition of AV conduction is enhanced.
With the on / in the introduction of Verapamil with nebivolol intake there is a threat of cardiac arrest (simultaneous use is contraindicated).
With the simultaneous use of nebivolol with antihypertensive drugs, Nitroglycerin or slow calcium channel blockers, severe hypotension may develop (special caution is necessary when combined with prazosin).
When applied simultaneously with sympathomimetics, the pharmacological activity of nebivolol is suppressed.
With simultaneous use with drugs for anesthesia, it is possible to suppress reflex tachycardia and increase the risk of arterial hypotension.
With simultaneous use with tricyclic antidepressants, barbiturates, phenothiazine derivatives, the antihypertensive effect of nebivolol may be enhanced.
With simultaneous use with cimetidine may increase the concentration of nebivolol in the blood plasma.
With simultaneous use of nebivolol with drugs that inhibit serotonin reuptake, or other biotransforming drugs involving the CYP2D6 isoenzyme, plasma concentration of nebivolol increases, the metabolism of nebivolol slows down, which may increase the risk of bradycardia.
When nebivolol is used together with insulin and hypoglycemic agents for oral administration, symptoms of hypoglycemia (tachycardia) can be masked.

There are no data on cases of overdose of nebivolol.
Symptoms: bradycardia, marked reduction in blood pressure, severe bradycardia, AV blockade, cardiogenic shock, cardiac arrest, loss of consciousness, coma, nausea, vomiting, cyanosis, bronchospasm, acute heart failure.
Treatment: the patient is hospitalized and placed in an intensive care unit. Immediately it is necessary to determine the concentration of glucose in the blood. Conduct gastric lavage, taking Activated carbon, maintaining the function of the cardiovascular system, monitoring the performance of the heart and lungs, monitoring blood volume and diuresis.
If necessary, a complex resuscitation measures.
The effect of beta-blockers can be neutralized by slow intravenous (IV) administration of isoprenaline at an initial dose of about 5 μg / min or dobutamine at an initial dose of about 2.5 μg / min. In case of severe bradycardia, 0.5-2 mg of atropine is introduced into / in the absence of a positive effect, the transvenous pacemaker can be set. In heart failure, treatment begins with the introduction of cardiac glycosides and diuretics, in the absence of effect, it is advisable to introduce dopamine, dobutamine or vasodilators. When bronchospasm is used in / in stimulators β2-activated receptors. With ventricular ematrasystole - Lidocaine (antiarrhythmic agent class IA should not be administered).

Store at a temperature not higher than 25 ° С.