Betahistine

Benjamin 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.

The active ingredient betahistine is one of the antivertiginous drugs used to treat dizziness. These occur, for example, in Menière's disease of the inner ear (Menière's disease), for the treatment of which betahistine is often used. Here you can read everything interesting about the effect of betahistine, side effects and use.

This is how betahistine works

The structure of the active ingredient betahistine is similar to the natural messenger substance histamine. With the help of histamine, nerve cells can transmit signals that are perceived by downstream cells via docking points, so-called receptors. Depending on the location in the body and the exact function, different subtypes of histamine receptors can be distinguished:

The H1 receptor, for example, is important for allergic reactions, the H2 receptor promotes the production of stomach acid.

The H3 receptor plays a crucial role in the treatment of dizziness with betahistine. It is present in the central nervous system, i.e. the brain and spinal cord, as well as in the rest of the body and regulates a whole series of the body's own control circuits such as eating behavior, sleeping behavior and the perception of reality (which is disturbed in diseases such as schizophrenia).

The active ingredient betahistine specifically docks to H3 receptors and inhibits them so that they cannot be activated by the body's own histamine. This leads to an increase in other messenger substances, as a result of which, among other things, the blood vessels in the inner ear expand - the pressure prevailing here drops. Experts believe that such overpressure in the cochlea, which affects the balance organ in the ear, is the cause of vertigo. Vascular relaxation with betahistine can therefore often relieve dizziness. The active ingredient also binds somewhat weaker to H1 receptors, which also leads to vascular relaxation in the inner ear.

Uptake, breakdown and excretion of betahistine

After ingestion by mouth, the active ingredient is quickly absorbed from the intestine into the blood, where it reaches its highest concentration after about half an hour. After about three hours, half of the amount of active substance in the blood is broken down and excreted in the urine.

When is betahistine used?

The active ingredient betahistine is used to treat dizziness, such as those that occur in Menière's disease. With this inner ear disease, there are often noises in the ears, ear pain and hearing loss.

It is used for the long term, as taking it only improves the symptoms, but does not eliminate the cause.

This is how betahistine is used

The active ingredient is taken in the form of tablets. Drops are also available for patients who have problems swallowing or who are fed through a tube.

It is usually taken one to three times a day. The total daily dose is generally 18 to 36 milligrams of betahistine. The dosage should be high enough to relieve dizziness but as low as possible to avoid side effects. To do this, the tablets sometimes have to be halved.

What are the side effects of betahistine?

One in ten to one hundredth treated people experience betahistine side effects of headache, nausea and indigestion. The latter can be reduced if the active ingredient is taken with a meal.

Hypersensitivity reactions, skin reactions and abdominal pain can occur as less common side effects.

What should be considered when taking betahistine?

Betahistine is broken down by the same enzymes as the body's own messenger substances (for example dopamine). Therefore, drugs that block such enzymes (such as the Parkinson's drug selegiline to inhibit the breakdown of dopamine) can lead to increased betahistine levels and thus to increased side effects.

The simultaneous intake of antihistamines against allergies sometimes leads to a weakening of the betahistine effect and should therefore be avoided.

The use of betahistine is not recommended in children and adolescents under 18 years of age or in pregnant and breastfeeding women because no studies are available.

The use of betahistine does not slow down the ability to react, nor does it impair the ability to drive or use machines. However, these skills are often compromised because of the underlying medical condition and should therefore be avoided.

This is how you get drugs with the active ingredient betahistine

The active ingredient betahistine requires a prescription in every dosage.

Since when is Betahistine known?

The active ingredient betahistine was first approved in the USA in 1963. After about five years, however, his approval was withdrawn again because no studies existed that showed sufficient effectiveness. These studies were then made up for in the following years, but the effect for betahistine was only very moderate. Due to the low side effects, the US FDA (food and drug administration) granted approval for the active ingredient betahistine again in 1999.

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