Betahistine

Betahistine is a synthetic analogue of the substance histamine.

[ 1 ], [ 2 ], [ 3 ], [ 4 ]

Indications Betahistine

It is used to treat padalemixia, and other symptoms that sometimes include tinnitus, dizziness, nausea, partial hearing loss, and problems with coordination.

[ 5 ], [ 6 ]

Release form

The release is made in tablets of 8, 16 or 24 mg, 10 pieces inside a blister pack. There are 3 such tablets in a box.

[ 7 ], [ 8 ]

Pharmacodynamics

Often, the active element of the drug has the ability to influence the action of histamine endings H1, as well as H3 (weak and strong antagonists) in the CNS. In this case, we are talking about endings located in the vestibular nuclei and the inner ear.

Betahistine dihydrochloride affects the circulatory function, stimulating microcirculation processes, and also affecting the strength of capillaries in the inner ear. At the same time, the active element helps to normalize the level of endolymphatic pressure inside the labyrinth and cochlea.

Since Betahistine is a drug that inhibits the activity of H3-endings of the labyrinthine nuclei, it has a significant effect on the function of the central nervous system, normalizing neuronal transmission within the vestibular nucleus.

Correct use of the drug leads to rapid neutralization of the signs of vestibular dizziness. The duration of action of the active component of the drug is at least several minutes, and at most 24 hours.

Regular use of the medication under the supervision of a doctor reduces the frequency and severity of dizziness, reduces tinnitus and noise, and at the same time restores the quality of hearing if it has deteriorated.

The drug has no sedative properties and does not lead to the development of various problems with coordination. It does not affect the endogenous secretory glands.

[ 9 ], [ 10 ]

Pharmacokinetics

The substance taken orally is absorbed completely and quickly. Peak plasma levels of the drug are observed approximately 60 minutes after taking the tablet on an empty stomach. The drug is then synthesized in the blood plasma with proteins, but the rates of this binding are extremely low - less than 5%.

The excretion of the component is carried out by a metabolic pathway, during which inactive metabolic products are formed (the main element is 2-pyridylacetic acid, and the additional one is demethylbetahistine).

Almost complete excretion of drug components occurs within 24 hours; the main route is the kidneys (about 90%), and the remainder (10%) is excreted through the liver and intestines.

[ 11 ], [ 12 ], [ 13 ]

Dosing and administration

Adult Dose Sizes.

In case of dizziness, tablets should be taken with or after food in a dose of 8 or 16 mg, three times a day (at the initial stage of therapy using the medication).

The sizes of maintenance doses usually fluctuate between 24-48 mg/day (the exact dose is selected by the doctor). The daily dosage can be a maximum of 48 mg.

Portion sizes may be adjusted to suit individual patient characteristics. In some cases, improvement is noted only after several weeks of therapy.

Use in people with kidney, liver or heart failure:

People with liver failure should undergo a thorough examination before starting therapy with Betahistine. The same conditions are required for prescribing to people with cardiac/renal failure.

Purpose for the elderly:

The drug should be prescribed to elderly patients with great caution, because this category of patients has a high risk of developing negative symptoms under the influence of the active and auxiliary elements of the drug.

[ 17 ], [ 18 ], [ 19 ], [ 20 ]

Use Betahistine during pregnancy

There are not enough data regarding the use of Betahistine in pregnant or breastfeeding women.

Contraindications

Main contraindications:

• pheochromocytoma - because the drug is an artificial histamine analogue, its use can lead to the release of catecholamines, which causes a strong increase in blood pressure;
• the patient has an intolerance to medicinal elements - both the active ingredient and additional substances contained in the drug;
• It is prohibited to prescribe the drug to persons under 18 years of age, because there is no information about the effectiveness and safety of its use in this category of patients.

[ 14 ]

Side effects Betahistine

Side effects that may occur as a result of taking the pills:

• general deterioration of the patient's well-being;
• stomach upset (usually occurs if you take the medicine before eating, which is prohibited);
• headaches (if you experience this type of disorder, you should take a painkiller after consulting a specialist);
• abdominal discomfort or flatulence;
• symptoms of skin allergies, such as rashes or itching (such disorders can be eliminated with the help of an antihistamine or by lubricating the affected areas with a simple moisturizer).

If the above recommendations do not produce results, you must stop using Betahistine and be sure to consult a doctor.

[ 15 ], [ 16 ]

Overdose

There is no general information about the development of intoxication. There is some data that some people experienced mild or moderate symptoms in the form of nausea, headaches or abdominal pain, and also a feeling of drowsiness - when using the drug in a dose of up to 640 mg.

Other signs of poisoning: dyspeptic symptoms, convulsions, vomiting, and ataxia.

More severe disorders may also occur, such as complications affecting the function of the cardiovascular system or lungs. Such symptoms have developed with deliberate administration of extremely high doses of the drug, especially in combination with other drugs.

The drug does not have a specific antidote, so if an overdose occurs, gastric lavage must be performed within 60 minutes after taking the drug.

[ 21 ], [ 22 ]

Storage conditions

Betahistine should be kept in a sealed container, in a dark and dry place, out of the reach of small children. The temperature level should be within 25°C.

[ 23 ]

Shelf life

Betahistine can be used for 2 years from the date of manufacture of the drug.

[ 24 ], [ 25 ]

Reviews

Betahistine does not always receive positive reviews. Some comments on medical forums indicate that the drug does not have a stable effect. Therefore, many people who have chronic disorders of the cardiovascular system need to take the drug constantly. Although such a treatment regimen does not guarantee that dizziness with headaches will disappear.

But there are also many positive opinions about the effect of the drug. Some women noted that during menopause they developed severe headaches, and in addition to this, sharp attacks of dizziness, during which it was impossible to even slightly tilt the head down, because this led to a complete loss of coordination. The use of Betahistine made it possible to completely eliminate all the described negative manifestations.

Both negative and positive reviews show that the drug must be used very carefully and correctly - for some disorders, the drug can show high efficiency, completely eliminating the problems, but for others, on the contrary, it only leads to a weakening of the symptoms of the disease, without eliminating its main cause.