Maxigistine

Maxigistine is a medicine used to eliminate various vestibular disorders.

Indications Maxigistine

Among the indications for the use of the drug:

• Meniere's disease, which is characterized by 3 main signs - dizziness (in some cases, with vomiting and nausea), hearing loss, and the appearance of noise in the ears;
• symptomatic therapy to eliminate vestibular vertigo, which has a different nature.

Release form

Produced in the form of tablets. One blister contains 10 tablets. Packed in 3 or 6 blister plates.

Pharmacodynamics

The mechanism of action on the body of the active component of the drug (betagistine) is poorly understood. Among the most reliable hypotheses are the following:

The effect of the active substance on the histaminergic structure: has a partial internal activity against the H1 receptors, and besides it acts as an antagonist of the histamine receptors (H3) inside the nerve tissues and has little effect on the H2 histamine receptors. In addition, betahistine increases the rate of metabolism and release of this component by blocking H3 receptors (presynaptic) - thereby inducing a decrease in their number.

Betagistin increases the flow of blood to the cochlear region and the brain - the circulatory process in the vessels located in the inner ear (stria vascularis) improves - as a result of attenuation of tension in precapillary sphincters participating in the process of microcirculation in the inner ear. In addition, the active substance helps to accelerate the intensity of cerebral blood flow.

Betagistin stimulates vestibular compensation - increases the rate of recovery of vestibular apparatus in animals with unilateral neurrectomy. This substance is achieved by improving the regulation of the release and metabolism of histamine, and in addition acting as an antagonist of H3 receptors. In the treatment of this drug after neyrektomii in humans, too, the period of restoration of the functionality of the vestibular apparatus is shortened.

Betagistin influences neuronal activity within vestibular nuclei - in accordance with the dosage it slows the formation of their peak potentials inside the medial as well as lateral nuclei.

Pharmacokinetics

After internal use, betahistine is almost completely absorbed from the digestive tracts rather quickly. Further, the drug rapidly passes the process of metabolism, as a result of which pyridyl-2-acetic acid is formed, which is the product of disintegration. The accumulation of beta-histidine in the blood plasma is very low, which is why all pharmacokinetic tests are performed by determining the concentration level of its decay product in the urine.

In the case of eating the drug with food, the peak concentration index decreases compared to the same level when administered on an empty stomach. But the complete absorption of the active substance in both situations is the same - this is a sign that the food is inhibited only by the absorption process.

With plasma proteins, beta-histidine binds less than 5%.

Absorbed betahistine is almost completely converted to pyridyl-2-acetic acid (which has no pharmacological activity). The internal accumulation of this metabolite in the urine and blood plasma reaches a peak 1 hour after the drug is consumed. This figure decreases with a half-life of about 3.5 hours.

Excretion of pyridyl-2-acetic acid occurs together with urine. After consuming the drug in a dosage of 8-48 mg, about 85% of the substance is detected in the urine. Through the kidneys, or together with the feces, the active ingredient is excreted in small amounts.

The rate of excretion does not change depending on the dosage of the drug - this indicates that the pharmacokinetics of betagistin is linear. This allows us to consider the used metabolic pathway to be unsaturated.

Dosing and administration

In a 24-48 mg dose should be taken (the dose should be divided into several methods). Tablets with a volume of 8 mg should be drunk 1-2 times a day, three times a day. Tablets with a volume of 16 mg should be drunk for 0.5-1 pieces also three times a day. Tablets with a volume of 24 mg should be taken twice a day for the first item.

Drinking the medicine is recommended after eating, and the dosage should be selected individually for each patient in accordance with the effect obtained.

Relaxation of symptoms in individual cases begins to manifest only after 2-3 weeks of therapy. Sometimes the necessary effect can be achieved only after several months of drug use. There is information that when prescribing therapy in the early stages of the disease it is possible to prevent its progression or hearing loss at a later stage.

Use Maxigistine during pregnancy

Since there is no necessary information on the use of the drug in pregnancy, it is not recommended to use it during this period. Exceptions are only cases of urgent necessity.

Contraindications

Among the contraindications:

• presence of individual intolerance of elements of drugs;
• pheochromocytoma.

Side effects Maxigistine

Among the side effects of taking Maxigistin:

• organs of the digestive system: dyspeptic manifestations and nausea, minor manifestations of indigestion (flatulence, as well as vomiting and gastrointestinal syndrome). All these manifestations usually occur after a reduction in the dosage or intake of drugs along with food;
• organs of the National Assembly: the appearance of headaches;
• immune system: hypersensitivity in the form of anaphylaxis, etc .;
• skin with subcutaneous tissue: allergic reactions to fatty tissue under the skin, as well as the skin - such as rashes, urticaria, itching or Quincke edema.

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Overdose

There are data on several cases of overdose by Maxigistin - when using the drug in a dosage of up to 640-mg mg. In this case, the patients showed moderate or mild symptoms - such as a feeling of drowsiness, nausea and pain in the abdomen. More dangerous complications (such as the onset of seizures, the development of cardiopulmonary disorders) developed in the case of intentional use of betagistin in high doses (especially when combined with an overdose of other drugs).

For the elimination of disorders, supportive and symptomatic treatment is prescribed.

Interactions with other drugs

The information obtained after in vitro studies shows that the metabolism of the active substance of Maxigistin is suppressed when combined with drugs that slow down the activity of MAO (among these elements is selegiline, which is a subtype of MAO). Therefore, care should be taken when combining these drugs during treatment.

Since betahistine is an analog of histamine, in the case of interaction of this component with antihistamines in theory, the effectiveness of any of these drugs may be affected.

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Storage conditions

It is necessary to keep the medicine under standard conditions that are inaccessible to children. The temperature should not exceed 25 ° C.

Shelf life

Maxigistine is allowed to be used for 2 years after the manufacture of the medicine.