Betahistine

• 2- Pyridinethanmethylamin
• N- methyl-2- (2-pyridyl ) ethylamine

N07CA01

• Antivertiginous
• Antiemetics

0.98 g · cm -3

113-114 ° C ( at 40 hPa)

Attention

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Betahistine is a drug from the group of antivertiginous, which is used in the treatment of vertigo, especially Meniere's disease and cochlear hydrops. It acts as an antihistamine H3, which is effective as an agonist at the H1-receptor at a time.

• 2.1 Mechanism of action ( pharmacodynamics )
• 2.2 bioavailability and metabolism
• 2.3 Toxicology

Clinical information

Areas of application (indications )

Betahistine is used in disorders of the vestibular apparatus, such as the symptoms of Meniere's disease, these include, inter alia, Dizziness, ringing in the ears, headache, nausea, vomiting, and hearing impairments.

Posology and method of administration

Three times a day 8 mg to 16 mg three times daily for a period of at least three months. In practice, a dosage of 6-12 mg three times a day is common. These details refer to the common salt of the active ingredient Betahistindimesilat. To avoid stomach incompatibilities, the taken after a meal is recommended.

Contraindications ( contraindications)

Pheochromocytoma, stomach and intestinal ulcers, bronchial asthma, hypersensitivity to betahistine pregnancy.

Interactions with other drugs

Antihistamines reduce the efficacy of betahistine.

Use during pregnancy and lactation

The use of Betahistine is contraindicated during pregnancy and lactation.

Adverse effects (side effects)

Frequency not known:

• Rash with redness and hives
• Headache, dizziness
• Palpitation
• Gastrointestinal intolerance
• Feeling hot

Pharmacological properties

Mechanism of action ( pharmacodynamics )

Betahistine attacks, among others, the histamine H1 receptors of the inner ear, where it acts a vasodilator. In addition, the excitation of nerve cells, the equilibrium nuclei is inhibited, which together with the increased blood flow has a beneficial effect on the above -mentioned symptoms.

Bioavailability and metabolism

The absorption of betahistine is rapid and complete. Betahistine is not detectable in the blood, but its inactive metabolite 2- pyridyl acetic acid. Meanwhile, peak plasma levels are reached after about half an hour, after 24 hours, the substance is completely excreted in the urine.

Toxicology

The following information on the LD50 (acute toxicity ) are known: Betahistindimesilat

• Rat: 3030 mg / kg bw orally, 604 mg / kg bw i.v.

Betahistine dihydrochloride

• Rat: 3000 mg / kg bw orally, 505 mg / kg bw i.v.
• Dog: 129 mg / kg bw i.v.

Trade names

Aequamen (D), Betaserc (A, CH), Betavert (D), Vasomotal (D ), numerous generics