Nebival

Nebival is a medication with pronounced hypotensive activity.

Indications Nebiwala

It is used for therapy in people with primary hypertension.

In addition, it can be used in combination treatment in elderly people with CHF when standard treatment methods do not provide the desired result.

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Release form

The drug is released in tablets, packed in blister cells of 10 pieces. There are 2 such cells inside the box.

Pharmacodynamics

The active ingredient of Nebival is nebivolol (a combination of 2 enantiomers – L- and D-nebivolol). The drug has a hypotensive effect, developing through 2 main therapeutic mechanisms – competitive selective blockade of β1-adrenoreceptor activity (element D-nebivolol), as well as metabolic connection with L-arginine/NO (element L-nebivolol).

After using the drug, a decrease in heart rate values is observed (without reference to blood pressure level and intensity of exercise), a decrease in blood pressure and systemic resistance of peripheral vessels (this occurs due to a decrease in the tone of smooth muscles inside the vascular membrane layer).

Using the drug in combination with other drugs to treat heart failure results in increased life expectancy and a reduced need for hospitalization due to cardiovascular diseases.

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Pharmacokinetics

After oral administration, nebivolol is well absorbed in the small intestine. The intensity and rate of absorption of the drug are not tied to food intake.

The active element of the drug participates in metabolic processes inside the liver, forming active metabolic products. The half-life of the component can vary significantly in different patients and range from 10 to 30-50 hours.

Approximately 40% of the active substance is excreted through the kidneys, and another approximately 50% in the feces.

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Dosing and administration

Nebival should be taken orally, without reference to food intake. If necessary, it is allowed to divide the tablet into halves. The daily dose of the drug is usually taken in 1 dose. To obtain the maximum medicinal effect, the medicine should be taken at the same time of day. The duration of treatment and dosage sizes are selected by the attending physician.

People with elevated blood pressure are usually given 1 tablet of the drug per day. If optimal control of blood pressure values cannot be achieved after 4 weeks from the start of treatment, an antihypertensive drug from another category or a diuretic (for example, hydrochlorothiazide in a dose of 12.5-25 mg per day) should be additionally prescribed.

People with CHF are often prescribed to take 12.5 mg of the drug per day. If the drug is well tolerated, the dose can be increased at 2-week intervals until the daily dose is 10 mg of the substance.

Before starting to use Nebival, people taking other medications should already have the optimal dosage of these drugs selected (the last dosage adjustment of such drugs should be made no earlier than 14 days before starting to use nebivolol).

A maximum of 10 mg of the medicinal substance is allowed per day.

If it is necessary to stop taking the medication, it is recommended to reduce its dosage gradually (except in situations where the patient’s condition worsens due to taking the drug).

People with kidney disorders can take no more than 5 mg of the therapeutic drug per day.

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Use Nebiwala during pregnancy

Since nebivolol can negatively affect the development of the fetus, the drug is prohibited for use during pregnancy. Before starting treatment, women of reproductive age should exclude the possibility of pregnancy.

When planning conception, you should stop taking Nebival and choose an analogue that will be safer for the fetus.

During lactation, the use of the medicine is allowed only on condition that breastfeeding is stopped.

Contraindications

Main contraindications:

• use in people with intolerance to nebivolol hydrochloride;
• hypolactasia (also people with lactase deficiency), galactosemia and glucose-galactose malabsorption in the intestine;
• severe forms of liver and kidney dysfunction;
• acute stage of heart failure, as well as heart failure, against the background of which episodes of decompensation are observed (in these situations, it is necessary to administer drugs with a positive inotropic effect);
• decreased blood pressure and cardiogenic shock;
• severe bradycardia, SSSU, 2-3 degree AV block;
• untreated pheochromocytoma, bronchial asthma (also in the anamnesis), metabolic acidosis and a tendency to develop bronchospasms;
• severe peripheral circulatory disorders.

Nebivolol hydrochloride should be discontinued at least 24 hours prior to elective surgical procedures that require general anesthesia.

The drug is prescribed with caution in moderate forms of peripheral circulatory disorders, first-degree AV block, diabetes mellitus, spontaneous angina, obstructive forms of chronic pulmonary pathologies, and also in psoriasis (also in the anamnesis).

At the same time, caution is required when using the drug in people with depression or myasthenia, as well as in people over 75 years of age.

You should refrain from operating life-threatening machinery and from driving a car during treatment with Nebival.

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Side effects Nebiwala

After using the drug, various side effects may develop, caused by the activity of nebivolol hydrochloride:

• disorders in the functioning of the cardiovascular system and circulatory system: disturbances in the heart rhythm, a sharp decrease in blood pressure, deterioration of the condition in people with impaired peripheral circulation, acute heart failure, as well as AV block, pain in the heart and peripheral swelling;
• problems with the nervous system function: headaches, syncope, increased fatigue, paresthesia, dizziness, nightmares, depression, and also decreased visual acuity. Along with this, the appearance of hallucinations, mental disorders and Raynaud's disease was observed sporadically;
• digestive disorders: nausea, bowel movements, bloating and symptoms of dyspepsia;
• signs of allergy: itching, erythema, Quincke's edema, bronchospasms, urticaria, anaphylaxis and exacerbation of existing psoriasis;
• Others: cyanosis in the extremities, impotence and dry keratoconjunctivitis.

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Overdose

Using the drug in excessively large doses can cause bradycardia or bronchial spasms, as well as a decrease in blood pressure and the development of acute heart failure or collapse.

In case of poisoning with a large dose of drugs, it is necessary to perform gastric lavage and give the victim enterosorbents. In addition, laxatives may be prescribed to reduce the absorption of nebivolol. In case of overdose, it is necessary to monitor the ECG values, blood pressure levels, blood glucose levels and monitor the general condition of the patient.

In severe forms of intoxication, intensive therapy procedures are carried out.

If bradycardia develops, the patient should be given atropine.

If a significant decrease in blood pressure is observed, the patient should be given plasma substitutes to increase the total circulating blood volume, as well as catecholamines.

When blocking the activity of β-adrenergic receptors, it is necessary to use isoprenaline hydrochloride or dobutamine in selected dosages.

If the above measures are ineffective, the patient should be given glucagon in a dose of 50-100 mcg/kg.

In severe cases, artificial ventilation and the use of a pacemaker may be required.

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Interactions with other drugs

The drug should not be combined with sultopride or floctafenine.

It is prohibited to combine Nebival with antiarrhythmic drugs from the 1st category, calcium antagonists (for example, dihydropyridine or verapamil), and also with antihypertensive drugs that have a central effect. This is due to an increased likelihood of AV block or acute heart failure.

The drug should be used with caution in combination with amiodarone and halogenated volatile painkillers.

Nebivolol can mask the signs of hypoglycemia, which is why it should be used with caution in combination with insulin and oral antidiabetic drugs.

Amifostine and baclofen with antidepressants and antipsychotics when used in combination with the drug potentiate its antihypertensive effect.

When combined with sympathomimetics, the medicinal effect of the drug is weakened.

Substances that inhibit the activity of the CYP2 D6 enzyme (including quinidine with paroxetine, thioridazine and dextromethorphan with fluoxetine) increase the levels of unchanged nebivolol in plasma.

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Storage conditions

Nebival must be kept at temperatures not exceeding 30°C.

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Shelf life

Nebival can be used within 24 months from the date of release of the drug.

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Use in children

Nebival is prohibited for use in pediatrics.

Analogues

Analogues of the drug are the medications Nebilet and Nebivolol.

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Reviews

Nebival generally receives positive reviews from both patients and doctors. With constant use of the drug as prescribed by a doctor, it demonstrates high efficiency in ischemia or high blood pressure.

It should be taken into account that the drug should be used with extreme caution - without allowing non-compliance with the prescribed regimen, because this can weaken its therapeutic effectiveness. At the same time, it should be remembered that poisoning with the drug can lead to very serious consequences, up to and including the death of the patient. Because of this, it is extremely important to follow the instructions prescribed by the specialist in everything.

At the same time, it should be noted that combination therapy is often used (especially in the elderly) using several different drugs. In these cases, the patient's well-being should be carefully monitored to prevent negative consequences associated with the interaction of these drugs.

Another advantage of the medication is its fairly reasonable cost.