Nebivator, pills 5mg 28pcs

Composition

Pharmacological action

Cardioselective beta_-1-adrenoblocker of the third generation with vasodilating properties. The Active ingredient is a racemate consisting of two enantiomers: D-nebivolol and L-nebivolol. D-nebivolol is a competitive and highly selective blocker of β1-adrenergic receptors; 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 during exercise, reduces the final diastolic pressure of the left ventricle, reduces OPSS, improves diastolic function of the heart (reduces filling pressure), increases the ejection fraction; causes an antianginal effect in patients with coronary heart disease.

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 blood plasma).

The antiarrhythmic effect is due to the suppression of pathological automatism of the heart (including in the pathological focus) and a slowdown in AV conduction.

Stable hypotensive effect develops after 1-2 weeks of regular use of the drug, and in some cases – after 4 weeks, stable effect is noted after 1-2 months.

Pharmacokinetics

After oral use, nebivolol is rapidly absorbed from the gastrointestinal tract. Food intake does not affect absorption. Bioavailability is on average 12% in individuals with a fast metabolism (the “first pass” effect through the liver) and is almost complete in individuals with a slow metabolism.

In blood plasma, both enantiomers preferentially bind to albumin. Binding to plasma proteins of D-nebivolol is 98.1%, L-nebivolol-97.9%.

It is metabolized by acyclic and aromatic hydroxylation and partial N-dealkylation. The resulting hydroxy and amino derivatives are conjugated with glucuronic acid and are excreted as O-and N-glucuronides.

It is excreted by the kidneys (38%) and through the intestines (48%).

In individuals with fast metabolism, T_1/2 of hydroxymetabolites – 24 hours, nebivolol enantiomers-10 hours; in individuals with slow metabolism: hydroxymetabolites-48 hours, nebivolol enantiomers-30-50 hours.

Excretion of unchanged nebivolol in the urine is less than 0.5%.

Indications

• Arterial hypertension.
• IHD: prevention of angina attacks of tension.
• Chronic heart failure (as part of combination therapy).

Contraindications

Bronchial asthma, decompensated chronic heart failure, untreated pheochromocytoma, severe liver function disorders, depression, angiospastic angina (Prinzmetal angina), peripheral vascular obliterating diseases (intermittent claudication syndrome), arterial hypotension, cardiogenic shock, bradycardia (heart rate less than 50 beats/min), SSR, AV block II and III degrees, myasthenia gravis, muscle weakness, children and adolescents under 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; very rarely-fainting, hallucinations.

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

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

From the skin and subcutaneous tissues: erythematous skin rash, pruritus; very rarely-aggravation of the course of psoriasis.

Allergic reactions: in some cases – angioedema.

Other: bronchospasm, dry eyes.

Interaction

When used concomitantly with Class I antiarrhythmic drugs, amiodarone may increase the negative inotropic effect and inhibit AV conduction.

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

With intravenous use of verapamil while taking nebivolol, there is a risk of cardiac arrest (simultaneous use is contraindicated).

Concomitant use of nebivolol with antihypertensive agents, nitroglycerin or slow calcium channel blockers may result in severe hypotension (special caution is necessary when combined with prazosin).

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

When used concomitantly with anaesthetic agents, reflex tachycardia may be suppressed and the risk of hypotension may increase.

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

Concomitant use with cimetidine may increase the concentration of nebivolol in blood plasma.

Concomitant use of nebivolol with drugs that inhibit serotonin reuptake or other agents that biotransform with the participation of the CYP2D6 isoenzyme increases the concentration of nebivolol in blood plasma, the metabolism of nebivolol slows down, which may increase the risk of bradycardia.

Concomitant use of nebivolol with insulin and oral hypoglycemic agents may mask the symptoms of hypoglycemia (tachycardia).

How to take, course of use and dosage

Adults for oral use-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 65 years of age, the initial dose is 2.5 mg / day. If necessary, the daily dose can be increased to 5 mg.

Special instructions

Discontinue therapy gradually (within 1-2 weeks). Reducing the heart rate to 55 beats / min requires reducing the dose. Against the background of diabetes mellitus, signs of hypoglycemia can be masked, with hyperthyroidism — tachycardia. May increase reactions to pollen and other allergens.

It should be discontinued 24 hours before surgery using general anesthesia (including surgical dentistry) or choose an anesthetic with the least negative inotropic effect.

If it is necessary to simultaneously prescribe antacids, nebivolol is taken during meals, and antacids-between meals.

Use with caution when working for drivers of vehicles and people whose profession is associated with increased concentration of attention. For the duration of treatment, it is recommended to exclude alcohol intake.

Form of production

Pills.

Storage conditions

In a dark place, at a temperature not exceeding 25 °C.

Shelf

life is 2 years.

Active ingredient

Nebivolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as prescribed by a doctor, Pregnant women as prescribed by a doctor, Nursing mothers as prescribed by a doctor

Indications

Heart Failure, Hypertension, Angina, Arrhythmia