Drugs from the group of adrenergic blockers are widely used in the treatment of many cardiac diseases. Among the drugs of this group, Nebivolol stands out significantly. The analogues of this medicine have also gained great fame due to its effectiveness. What kind of medicine is this, how does it work, and in what cases can it be used?
What is this drug?
"Nebivolol" refers to a group of beta-blockers. The main effect of this drug is antihypertensive (the drug reduces pressure). The effect is observed due to the selective blocking of beta receptors located in the vessels (affects beta-1-adrenergic receptors).
Currently used "Nebivolol Sandoz".
This drug is a combination of several isomers (D- and L-rotating). Such a combination of substances favorably affects the development of the clinical effect. One of the isomers is responsible for the development of antihypertensive action, while the second has a greater effect on heart rate.
The drug appeared relatively recently, in the middle of the last century. Since then, it has become widespread in the cardiological environment. "Nebivolol Sandoz" is the drug of choice in the treatment of hypertension, as well as some heart rhythm disturbances.
How does the drug work and what organs are responsible for its digestibility?
Pharmacokinetics
"Nebivolol Sandoz" is best absorbed. The drug is well absorbed in the gastrointestinal tract. It can be taken with food (absorption does not worsen). Bioavailability is relatively low - about 12 percent. If possible, co-administration of the drug with alcohol should be avoided, as the development of side effects is possible.
Once in the blood plasma, the drug binds to albumin and forms insoluble complexes. In such a connected form, the availability of the drug is about 98 percent, that is, almost the entire Nebivolol Sandoz is absorbed. Its analogs go the same way before they get into the blood plasma and do not bind to the protein.
Not absorbed drug is excreted through the gastrointestinal tract and kidneys. It is processed in the liver, where it binds to glucuronic acid.
The half-life of the drug in people with an accelerated metabolite is about a day. In the case of slow metabolism, Nebivolol can accumulate and remain in the blood plasma for about 48 hours.
The drug does not accumulate in the tissues, which avoids its overdose (it is possible only if it is used in patients with kidney or liver pathology).
Indications for use
In what cases is "Nebivolol" prescribed, analogues of this drug or drugs with a similar pharmacological effect?
The first indication for the appointment of the drug is arterial hypertension. The use of beta-blockers is resorted to when the use of ACE inhibitors is ineffective (Enalapril, Captopril). In addition, Nebivolol is also used for endocrine hypertension.
Another, equally important indication for the use of Nebivolol is coronary heart disease. With frequent exacerbations of angina pectoris, as well as for the prevention of such attacks, Nebivolol is indicated. Analogs of it in this case may be even more effective than the pure drug itself.
Included "Nebivolol" and in the combination therapy in the treatment of chronic heart failure. In this case, the drug helps to improve heart function, reduce pre- and afterload on the organ chambers, as well as reduce pressure.
You can use this medicine to prevent the development of hypertensive crises, as well as in individuals prone to atherosclerotic lesions of the vessels of the brain.
Contraindications
When is it not worth using Nebivolol? Instructions for use usually include all those cases that have been clinically identified when the development of certain complications was observed against the background of the use of the drug. Due to the strong antihypertensive effect, one cannot prescribe a remedy for severe arterial hypotension.
First of all, it is forbidden to use the drug in acute heart failure. This is due to the fact that it has an inotropic effect, which can adversely affect the body due to insufficient heart function.
With the development of pheochromocytoma, it is also forbidden to use Nebivolol. Instructions for use indicate that with this endocrine tumor, the drug can only be used in conjunction with alpha receptor blockers.
You should not prescribe the drug to children, as well as to people with existing mental health disorders.
"Nebivolol" is contraindicated in individuals with individual drug intolerance. When the first signs appear (lacrimation, difficulty breathing), you should immediately abandon the further use of the drug and switch to a safer option.
Side effects
Like any drug, Nebivolol has its own side effects. The main ones are:
From the side of the nervous system - headache, depression, drowsiness, insomnia, hallucinations, fainting, dizziness.
A side effect of the digestive system is nausea, constipation, dry mouth, and vomiting. Dyspeptic disorders may occur, and when taken together with antibiotics, dysbiosis.
The cardiovascular system responds to the administration of Nebivolol with bradycardia, dyspnea, edema, the development of acute heart failure, atrioventricular block, Raynaud's syndrome. An overdose can lead to uncontrolled arterial hypotension, which can be complicated by collapse and fainting. In severe cases, shock develops.
Side effect of "Nebivolol" may occur in the form of an erythematous rash, psoriasis.
In severe cases, angioedema develops (Quincke's edema). In milder cases, the development of indomitable sneezing or coughing is observed.
Features of the use of the drug
The drug is used with caution in patients with renal failure, diabetes mellitus or hyperproduction of thyroid hormones. Drug withdrawal is carried out gradually, within 10-14 days. At the beginning of the course of treatment, hell and heart rate should be monitored. If possible, smoking should be abandoned while using the drug. Before the upcoming operation, the anesthesiologist should be warned that the patient is using beta-blockers.
During the entire period of use of the drug, blood sugar levels should be monitored, especially in diabetics. In addition, the filtration capacity of the kidneys (especially creatinia and urea levels) should be evaluated if Nebivolol is prescribed for a long time. Instructions for use (analogues have a similar effect) warns that it is possible to develop renal failure with the irrational use of this drug.
It is forbidden to use the drug for children under 18 years of age, as well as elderly patients with decompensated heart failure. This ban is primarily due to the possibility of metabolic disorders and the appearance of problems with pressure.
Since the use of the drug may cause dizziness, it should not be prescribed to drivers and doctors.
Use of the drug by pregnant women
The appointment of this medicine to a pregnant woman is possible only after consultation with a gynecologist and therapist. The drug is used quite rarely due to the negative effect on the mother and child.
The drug is prescribed only in case of emergency, since the development of bradycardia, arterial hypotension, hypoglycemia, paralysis of the respiratory center, and seizures is possible.
Three days before the expected birth, you must refuse to use this medication. If this is not possible, in the early postpartum period, careful monitoring of the state of health of the mother and child is necessary. Be sure to use spinal anesthesia to warn the anesthetist about ongoing treatment with adrenergic blockers.
It should be remembered that against the background of the use of the drug, fetal hypoxia may develop. The teratogenic effect of the drug has not been proven, however, cases of such an effect on the fetus are known.
If nebivolol is prescribed to the pregnant woman, the instructions for use warns that it is possible to distort the therapeutic effect of the drug when prescribed with intravenous administration of magnesia.
Interaction with drugs of other drug groups
The combined use of Nebivolol and class 1 antiarrhythmics can lead to an increase in the negative inotropic effect. Perhaps the development of AV blockade. A similar effect is observed if you simultaneously use calcium channel blockers and Nebivolol Sandoz.
Instructions for prescribing the drug warns that when it is administered intravenously, cardiac arrest is possible (provided that the medicine is administered together with Verapamil). In this case, emergency cardioversion using electropulse therapy will be required.
There is a significant risk of developing severe arterial hypotension when prescribing a drug with Nitroglycerin.
The simultaneous administration of sympathomimetics and Nebivolol inhibits the action of the latter.
Joint use with drugs for anesthesia can lead to a sharp drop in blood pressure, which will serve as an indication for mechanical ventilation and the use of hypertensive drugs.
When prescribing a drug with insulin, it is possible to develop an overdose of the hormone and conceal the clinical signs of hypoglycemia.
Drug dosage
So in what doses should you use the drug to develop the necessary clinical effect? If Nebivolol Sandoz is used, the instructions for use suggest the following dosage.
The most optimal dose for an adult is 20 milligrams per day. The drug is administered orally in the morning on an empty stomach. The maximum effect of the dose used develops after one to two weeks from the start of treatment. If necessary, the daily amount of the drug can be increased to 10 milligrams. For elderly patients, the maximum daily dose is 5 milligrams, and the optimal for treatment is 2.5 milligrams per day. For pregnant women, the amount of the drug is selected according to clinical signs and body weight. It is best to use Nebivolol Sandoz (5 mg) in tablets.
In case of impaired liver or kidney function, it is better to abandon the use of Nebivolol or prescribe it in minimum dosages.
With the simultaneous administration of sympathomimetics and Nebivolol, a potentiation of the effect is possible, due to which the prescribed dose of the drug can be slightly reduced.
The appointment of the drug in smaller doses does not have an effect on the body. Perhaps the development of receptor tolerance to the drug with prolonged administration of small doses of the drug.
Analogues of the drug
It is not always possible to find the necessary drug in pharmacies, so you have to resort to the use of analogues. Due to the expansion of the drug market, finding similar drugs is not difficult. What medicines can replace "Nebivolol"?
The analogs (synonyms) of this drug are as follows:
- "Binelol";
- "Nebivator";
- "Nebivolol Canon";
- "Nebivolol stada";
- "Nebivolol teva;
- Nebikar
- "Non-ticket";
- Nebilong
- "One heaven."
Each of these drugs has its positive and negative traits. Some of them are enhanced better than the classic Nebivolol. Instructions for use of each of them, however, warns of a greater number of negative effects. Therefore, only a qualified and competent doctor can help determine the question of which drug is better.
You should not use these funds on your own without first consulting a doctor, since in this way you can only significantly worsen your condition and harm both your health and the health of friends and relatives.
Drug Reviews
Many patients actively praise a drug such as Nebivolol Sandoz on the forums. Reviews about it are mostly positive, since this drug helped to cure or stop the symptoms of the disease in most patients.
Despite the number of side effects that the drug has, it is considered one of the main in the treatment of high blood pressure and heart failure.
Pure Nebivolol has a lot of positive reviews. The analogs of the drug are more suitable for someone, for someone less, as a result of which the opinions of patients differ. It is also necessary to take into account the concomitant pathology, which can significantly worsen the effect of the drug.
Be sure to consider the age of patients who have used this medicine.
Of all beta-blockers used in cardiac patients, Nebivolol (analogues) is in the first place. Reviews about this medicine allow us to call it the most effective drug of this drug group.