Nebivolol
Updated onBenjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.
More about the experts All content is checked by medical journalists.Nebivolol is a blood pressure lowering drug from the group of beta blockers. As a relatively new active ingredient of the third generation of beta blockers, it has a particularly advantageous profile of effects and side effects compared to older active ingredients. Here you can read everything you need to know about the effects and use of nebivolol, side effects and interactions.
This is how nebivolol works
Nebivolol is a drug from the group of beta-1 selective beta blockers. Beta-1 receptors are specific docking points for messenger substances and are found primarily in the heart. By docking to these receptors, nebivolol can lower the heart rate (negative chronotropic) and reduce the heart's beating power (negative inotropic).
In addition, the active ingredient influences the conduction of excitation (negative dromotropic; antiarrhythmic effect) and lowers blood pressure (antihypertensive).
The mechanism of action in detail
In stressful situations, the body has an increased need for oxygen and nutrients. In order to optimally supply every organ and tissue during such a stressful situation, stress hormones such as adrenaline are released into the bloodstream. In addition, individual organs are stimulated directly via activating nerve pathways with messenger substances such as norepinephrine to increase their performance.
As a result, the airways widen to allow the lungs to absorb more oxygen. The heartbeat is accelerated to move oxygen and nutrients around the body faster. Digestion is slowed down in order to be able to provide more energy for other essential processes in the body. In addition, the blood flow to internal organs and muscles is increased, while that of the extremities and the surface of the skin is decreased.
In the case of high blood pressure patients and patients with cardiac insufficiency, this system is excessively regulated even in the normal state, which leads to permanent unnecessary stress, especially on the heart and blood vessels. Then beta blockers like nebivolol can help:
They block the docking points for adrenaline and noradrenaline. The messenger substances can then no longer bind to it, so they can no longer trigger an effect.
Newer beta blockers work primarily on the heart, where they reduce the heartbeat to a normal level. The active ingredient nevivolol also has the special feature that it leads to vasodilation via a further mechanism of action in the blood vessels - the blood pressure drops and the blood flow rate in small and large vessels improves.
Uptake, breakdown and excretion
After ingestion, nebivolol is quickly absorbed into the blood through the intestinal wall. In the liver, the active ingredient is extensively metabolized, sometimes into effective metabolic products.
The ability to break down nebivolol is different in each patient, depending on their genetic makeup. The attending physician may have to take this into account when determining the dosage. In patients who metabolize the active ingredient quickly (so-called "fast metabolizer"), half of the active ingredient is excreted after about ten hours. In the case of slow metabolisers, on the other hand, this process can take three to five times longer.
The breakdown products are excreted in roughly equal parts with the stool and urine.
When is nebivolol used?
The areas of application (indications) of nebivolol are:
- High blood pressure (hypertension)
- chronic heart failure (heart failure) mild to moderate severity
Generally, nebivolol is taken permanently.
This is how nebivolol is used
Nebivolol is taken in the form of tablets, which can be divided if necessary. The dose is swallowed once a day, at the same time each day, regardless of what you eat.
The blood pressure lowering effect occurs one to two weeks after the start of therapy, the full effect of nebivolol may not take place until four weeks. In the case of heart failure, a particularly low dose is started, which is then gradually increased.
In the case of high blood pressure, it can be useful to combine nebivolol with another antihypertensive agent in order to achieve a greater reduction in blood pressure. Fixed combinations of nebivolol with other active ingredients (e.g. hydrochlorothiazide = HCT) are also available for this purpose.
If treatment with nebivolol is ended, the active ingredient should not be discontinued suddenly, but rather slowly, gradually reducing the dosage ("tapering off").
What are the side effects of nebivolol?
In more than every tenth person treated, taking it triggers side effects such as slow heartbeat and dizziness (the latter occurs particularly at the start of therapy). Headaches, tiredness and a drop in blood pressure when changing position (orthostasis) are also possible.
Furthermore, every tenth to one hundredth patient experience headaches, shortness of breath, constipation, nausea, diarrhea and / or water retention in the body.
What should be considered when taking nebivolol?
Contraindications
The use of nebivolol in combination with active substances against cardiac arrhythmias is not recommended. The combined effect on the heart could lead to impulse conduction disorders. Examples of such active ingredients are quinidine, flecainide, lidocaine, propafenone and calcium channel blockers such as verapamil or diltiazem.
Centrally acting high blood pressure drugs such as clonidine, monoxidine and methyldopa should not be taken together with nebivolol.
Other contraindications are:
- very low blood pressure (severe hypotension with blood pressure values below 90/50 mmHg)
- certain types of cardiac arrhythmias and conduction disorders
- slow heartbeat (bradycardia: less than 60 heartbeats per minute)
- Spasms of the airways muscles (bronchospasm) or known bronchial asthma
- Metabolic acidosis (acidification of the blood)
Interactions
In diabetics who are being treated with insulin or oral antidiabetic drugs, the active substance nebivolol can mask hypoglycaemia by delaying the rise in blood sugar levels after administration of the diabetes medication. Therefore, diabetics should be particularly careful when using nebivolol.
The simultaneous use of antipsychotics (agents against psychoses and schizophrenia), antidepressants or sleeping pills of the barbiturate type can lead to an increased decrease in blood pressure.
People with COPD (Chronic Obstructive Pulmonary Disease) should take nebivolol with caution as it can exacerbate respiratory problems.
The enzyme CYP2D6 is involved in the breakdown of nebivolol. The simultaneous use of substances that inhibit this enzyme can therefore increase the plasma level and thus the effect of nebivolol. These substances include in particular the antidepressants paroxetine and fluoxetine, the antipsychotic thioridazine and quinidine - a remedy for cardiac arrhythmias.
Age restriction
Nebivolol is approved for ages 18+. Due to a lack of data, its use in children and adolescents under 18 years of age is not recommended.
pregnancy and breast feeding period
Beta blockers such as nebivolol generally reduce blood flow to the placenta, which can lead to an undersupply of the unborn child. Therefore, nebivolol should only be used in pregnant women if absolutely necessary.
In animal experiments, the active ingredient is excreted in breast milk. It is not known if this is also the case in humans. For this reason, breastfeeding is not recommended during treatment with nebivolol.
How to get medication with nebivolol
In Germany, Austria and Switzerland, nebivolol requires a prescription in every dosage and is only available in pharmacies.
How long has nebivolol been known?
Nebivolol was jointly developed by two research-based pharmaceutical companies. It was approved in Germany in 1996 and launched on the market in 1997.
The first generics came on the market from 2008, but were then withdrawn due to patent disputes. In 2010, after the patent protection finally expired, generics with the active ingredient nebivolol came onto the market again.
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