Nebivolol

Nebivolol is a racemate that contains two enantiomers, D- and L-nebivolol.

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Indications Nebivolol

It is used in the treatment of the following disorders:

• increase in blood pressure values;
• CHF;
• IHD (to prevent the development of the disease).

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Release form

The substance is released in tablets, packed in blister packs of 30 pieces.

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Pharmacodynamics

A single dose of the drug lowers blood pressure and reduces heart rate (both under load and at rest). A single dose also results in an antianginal effect in people with coronary heart disease, increases the ejection fraction, lowers the final values of left ventricular diastolic pressure, and reduces total peripheral vascular resistance and filling pressure.

A stable antihypertensive effect occurs after 1-2 weeks of continuous use of the drug (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 suppressing pathological cardiac automatism and inhibiting AV conduction. The antihypertensive effect is achieved by reducing the activity of the RAS.

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Pharmacokinetics

Both enantiomers of the drug are absorbed at high speed in the gastrointestinal tract; however, food does not affect the degree of absorption.

People with fast metabolism have average bioavailability of the drug equal to 12%, and people with slow metabolism have almost complete bioavailability. Because of this, taking into account the intensity of metabolism, it is necessary to prescribe portion sizes individually. In the blood plasma, the substance is synthesized mainly with albumin.

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

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Dosing and administration

Adults should take 2.5-5 mg of the drug orally per day (this should be done in the first half of the day). If necessary, the dosage can be increased to 10 mg of the drug. A stable medicinal effect can be achieved after 7-14 days of continuous use of the drug (sometimes this takes 1 month).

Older adults are required to take an initial dosage of 2.5 mg per day. The maximum allowable dose for them is 5 mg.

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Use Nebivolol during pregnancy

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

During lactation, the drug can be used only on condition that breastfeeding is stopped during therapy.

Contraindications

Main contraindications:

• presence of hypersensitivity to nebivolol;
• state of depression;
• severe obliterating pathologies in the peripheral vascular area (intermittent claudication or Raynaud's disease);
• history of bronchospasms or bronchial asthma;
• cardiogenic shock;
• myasthenia;
• severe disorders in liver function;
• metabolic acidosis;
• pheochromocytoma;
• bradycardia (heart rate below 60 beats/minute);
• AV block of the 2nd or 3rd degree (in the absence of a pacemaker);
• SSSU (also sinoatrial block);
• a marked decrease in blood pressure (systolic blood pressure is less than 90 mm Hg);
• CHF in the decompensation phase or acute heart failure.

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Side effects Nebivolol

Taking the medication can cause a variety of side effects:

• in people with CHF: most often bradycardia with dizziness appears, as well as swelling of the legs, orthostatic collapse, first-degree block and potentiation of disease symptoms;
• lesions affecting the reproductive organs: impotence occasionally develops;
• disorders in the epidermis: sometimes itching and erythematous rashes occur. Signs of intolerance appear sporadically and the manifestations of psoriasis are potentiated;
• disorders associated with the gastrointestinal tract: constipation, nausea or diarrhea are often observed. Dyspeptic syndrome may sometimes occur;
• problems with the functioning of the respiratory organs: dyspnea often appears; sometimes bronchial spasms develop;
• lesions in the cardiovascular system: sometimes intermittent claudication is potentiated, cardialgia, bradycardia, heart rhythm disorder, and heart failure develop. In addition, blood pressure values decrease or the activity of AV conduction/blockade slows down;
• problems with visual function: visual disturbances may be observed;
• disorders of the central nervous system or the peripheral nervous system: a feeling of drowsiness or fatigue, nightmares, paresthesia, headaches, insomnia and dizziness may appear, as well as the development of depression and a weakening of concentration.

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Overdose

Poisoning with the drug can provoke the occurrence of such manifestations as bronchial spasms, acute cardiac failure, bradycardia and decreased blood pressure.

To eliminate the disorders, the patient's stomach is washed and activated carbon with laxatives is given. If there is such a need, intensive therapy is carried out in a hospital setting.

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Interactions with other drugs

When Nebivolol is used in combination with insulin or antidiabetic drugs, symptoms of hypoglycemia (tachycardia) may be masked.

The combination of the drug with SSRIs may lead to an increase in plasma levels of nebivolol, as well as a slowdown in metabolic processes, which increases the likelihood of bradycardia.

Combination with cimetidine increases plasma levels of the drug.

Use together with phenothiazine derivatives, tricyclics and barbiturates potentiates the hypotensive properties of the drug.

Concomitant use with anesthetics increases the likelihood of a decrease in blood pressure and inhibits reflex tachycardia processes.

Combination with sympathomimetics suppresses the medicinal activity of the drug.

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

Using the medication together with verapamil can lead to cardiac arrest.

Simultaneous administration with class 1 antiarrhythmic drugs can potentiate the negative inotropic effect and also suppress AV conduction processes.

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Storage conditions

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

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Shelf life

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

Application for children

The therapeutic agent is not used in pediatrics (under 18 years of age).

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Analogues

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

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Reviews

Nebivolol gets excellent reviews from most people regarding its therapeutic effectiveness (many say that it is very high). However, there are also a large number of negative signs that appear quite often.