Nebivolol

Nebivolol is a racemate that includes 2 enantiomers - D-, as well as L-nebivolol.

[1], [2], [3], [4]

Indications Nebivolola

It is used in the treatment of the following disorders:

• increase in blood pressure;
• SWF;
• IHD (for the prevention of the development of the disease).

[5], [6]

Release form

The substance is released in tablets packed in a blister plate of 30 pieces each.

[7], [8], [9], [10]

Pharmacodynamics

With a single dose of medication, there is a decrease in blood pressure and a decrease in heart rate (both under loads and in a calm state). Also, 1-fold reception leads to the development of antianginal effect in individuals with IHD, raises the level of the ejection fraction, lowers the final values of left ventricular diastolic pressure, and weakens OPSS and filling pressure.

A stable antihypertensive effect occurs after 1-2 weeks of continuous use of drugs (but sometimes it may take 1 month). A stable therapeutic effect is observed after 1-2 months.

The antiarrhythmic effect of the drug develops by inhibiting pathological cardiac automatism and inhibition of AV conduction. Antihypertensive effect is carried out by reducing the activity of RAS.

[11], [12],

Pharmacokinetics

Both enantiomers of LS at high speed are absorbed inside the gastrointestinal tract; while the food does not have any effect on the degree of absorption.

People who have a fast metabolism have an average bioavailability of 12%, and those who have a slow metabolism have almost complete bioavailability. Because of this, taking into account the intensity of metabolism, you need to assign the sizes of portions individually. Inside the blood plasma, the substance is synthesized mostly with albumin.

Excretion of the substance occurs through the kidneys (38%) and the intestine (48%).

[13], [14], [15], [16], [17], [18]

Dosing and administration

Adults should ingest 2.5-5 mg of medicinal substance per day (do this in the first half of the day). If necessary, it is possible to increase the dosage to 10 mg of the drug. It is possible to achieve stable medication after 7-14 days of constant drug intake (sometimes it takes 1 month).

Elderly people need to take an initial dosage of 2.5 mg per day. The maximum allowable dose for them is 5 mg.

[24], [25]

Use Nebivolola during pregnancy

Nebivolol is prohibited from use in pregnant women, because substances that block the activity of β-adrenergic receptors, weaken the blood circulation inside the placenta and can lead to a delay in fetal growth and disorders of its intrauterine development. Women who used the drug during pregnancy should monitor the condition of the newborn baby (hypoglycemia with bradycardia may develop, especially during the first 3 days after birth).

When lactating, the drug can be used only if you refuse to breast-feed during therapy.

Contraindications

The main contraindications:

• presence of hypersensitivity to nebivolol;
• state of depression;
• obliterating pathologies in the peripheral vascular region in a severe degree (intermittent claudication or Raynaud's disease);
• presence of bronchial spasms or asthma in the anamnesis;
• cardiogenic shock;
• myasthenia gravis;
• expressed disorders in hepatic work;
• metabolic acidosis;
• feohromocytoma;
• bradycardia (HR values below 60 beats / minute);
• AV blockade of the 2nd or 3rd degree (in the absence of an electrocardiostimulator);
• SSSU (also blockade of the sinoatrial type);
• a pronounced decrease in blood pressure (systolic blood pressure is less than 90 mm Hg);
• CHF in the phase of decompensation or heart failure of an acute nature.

[19], [20], [21], [22]

Side effects Nebivolola

Taking medication can cause a variety of adverse events:

• in people with CHF: most often there is a bradycardia with dizziness, and in addition, swelling of the legs, orthostatic collapse, blockade of the 1st degree and potentiation of the symptoms of the disease;
• lesions affecting the reproductive organs: occasionally impotence develops;
• violations in the epidermis: sometimes there is itching and eruptive rash. Individual signs of intolerance appear and potentiation of psoriasis occurs;
• disorders associated with the function of the gastrointestinal tract: often there is constipation, nausea, or diarrhea. Sometimes there may be a dyspeptic syndrome;
• problems with the work of respiratory organs: often there is dyspnea; sometimes spasms of bronchi develop;
• lesions in the CCC region: sometimes there is a potentiation of intermittent claudication, cardialgia develops, bradycardia, heart rhythm disorder, heart failure. In addition, the values of blood pressure decrease or the activity of AV-conduction / blockade slows down;
• problems with visual function: visual disturbances can be observed;
• disruption of the CNS or PNS: there may be a feeling of drowsiness or fatigue, nightmarish dreams, paresthesias, headaches, insomnia and dizziness, and in addition, the development of depression and a weakening of concentration.

[23]

Overdose

Poisoning with medication can provoke the appearance of such manifestations as spasms of the bronchi, heart failure in the acute stage, bradycardia and a decrease in the values of blood pressure.

To eliminate violations, the patient is washed with a stomach and given activated charcoal with laxatives. If there is such a need, intensive care is provided in a hospital.

[26], [27], [28]

Interactions with other drugs

With the combined use of nebivolol with insulin or antidiabetics, masking of symptoms of hypoglycemia (tachycardia) can occur.

The combination of a drug with SSRIs can lead to an increase in the plasma values of nebivolol, as well as slowing down metabolic processes, which increases the likelihood of bradycardia.

Combination with cimetidine increases the plasma indices of the drug.

Application together with phenothiazine derivatives, tricyclics and barbiturates potentiates the antihypertensive properties of the drug.

Simultaneous use with anesthetic agents increases the probability of lowering blood pressure and depresses the processes of reflex tachycardia.

The combination with sympathomimetics suppresses drug activity of the drug.

Combination with drugs that block slow channels of Ca, antihypertensive drugs or nitroglycerin leads to a significant decrease in blood pressure.

The use of medication with verapamil may lead to cardiac arrest.

Simultaneous administration with antiarrhythmic drugs of the 1st class can potentiate a negative inotropic effect, and also suppresses AV-conduction processes.

[29], [30], [31], [32]

Storage conditions

Nebivolol should be kept at temperatures not exceeding 25 ° C.

[33], [34]

Shelf life

Nebivolol can be used within 36 months from the date of manufacture of the drug.

Application for children

Therapeutic agent is not used in pediatrics (before the age of 18).

[35], [36]

Analogues

Analogues of the drug are Binelol, Nebilet and Nebivator with Nevotenz.

[37], [38]

Reviews

Nebivolol receives excellent reviews from most people regarding his therapeutic effectiveness (many say that she is very high). But at the same time there is a large number of negative signs, which are manifested often enough.