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Betahistine
Systematic (IUPAC) name
N-methyl-2-(pyridin-2-yl)ethanamine
Identifiers
CAS number 5638-76-6
ATC code N07CA01
PubChem 2366
ChemSpider 2276
Chemical data
Formula C 8H12N2  
Mol. mass 136.194 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Protein binding Very low
Metabolism To 2-(2-aminoethyl)pyridine and 2-pyridylacetic acid[1]
Half life 3–4 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral
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Betahistine hydrochloride (SERC, Betaserc) is an antivertigo drug. It was first registered in Europe in 1970 for the treatment of Ménière's disease. It is commonly prescribed to patients with balance disorders or to alleviate vertigo symptoms associated with Ménière's disease.

Betahistine is available in 8 mg, 16 mg, or 24 mg tablets. It is contraindicated for people with peptic ulcers or tumours of the adrenal gland. People with bronchial asthma should be closely monitored.

Contents

Chemistry

Betahistine chemically is 2-[2-(methylamino)ethyl]pyridine, and is formulated as the dihydrochloride salt. Its structure closely resembles that of phenethylamine and histamine.

Pharmacology

Betahistine comes in tablet form and is taken orally. It is rapidly and completely absorbed. The mean plasma half-life is 3-4 hours, and excretion is virtually complete in the urine within 24 hours. Plasma protein binding is very low. Betahistine is transformed into aminoethylpyridine and hydroxyethylpyridine and excreted with the urine as pyridylacetic acid. There is some evidence that one of these metabolites, aminoethylpyridine, may be active and exert effects similar to those of betahistine on ampullar receptors.[2]

Mode of action

Betahistine has a very strong affinity for histamine H3 receptors and a weak affinity for histamine H1 receptors. Betahistine seems to dilate the blood vessels within the middle ear which can relieve pressure from excess fluid and act on the smooth muscle.

The mode of action of betahistine was believed to be a direct stimulating (agonistic) effect on H1 receptors located on blood vessels in the inner ear. This would give rise to local vasodilation and increased permeability, which would help reverse the underlying problem of endolymphatic hydrops.

In addition, betahistine has a powerful antagonistic effects at H3 receptors, and increases the levels of neurotransmitters released from the nerve endings. This is thought to have two consequences;

  • The increased amounts of histamine released from histaminergic nerve endings can stimulate H1 receptors, thus augmenting the direct agonistic effects of betahistine on these receptors. This explains the potent vasodilatory effects of betahistine in the inner ear, which are well documented.
  • It is postulated that betahistine increases the levels of neurotransmitters such as serotonin in the brainstem, which inhibits the activity of vestibular nuclei.

Side effects

  • Low level of gastric side effects
  • No significant antidopaminergic effects
  • Nausea can be a side effect, but the patient is generally already experiencing nausea due to the vertigo so it goes largely unnoticed.

Recent updates

A new use for betahistine may be in the field of obesity management. Dr Nir Barak of the Rabin Medical Centre in Tel Aviv has undertaken trials[3] and it is reported (Telegraph, UK, 19 February 2007) that volunteers lost more than 1.5 kg/week over twelve weeks and experienced a distaste for fatty foods.

A recent Phase II clinical trial of the new drug in the U.S. suggests that women under the age of 50 who took Histalean (Betahistine) for 12 weeks lost 7 times the weight of those taking a placebo. What's most important to the researchers involved is that none of the 281 patients, males and females aged 18-65, complained of any serious side effects. The recent results were based on a double-blind, placebo-controlled study on people with a Body Mass Index ranging from 30 to 40. (A BMI of 30 and above indicate obesity.) The study was conducted at 19 investigation sites across the U.S. over a 12 week treatment period. The subgroup of high-dose Histalean (Betahistine)-treated women lost an average of 2.91% of their weight versus placebo group which lost only 0.4 %.[4]

Footnotes

  1. ^ (French) "Betahistine Dichlorhydrate". BIAM. June 30, 1999. http://www.biam2.org/www/Sub1291.html.   Retrieved on November 7, 2008.
  2. ^ Botta L, Mira E, Valli S, Zucca G, Perin P, Benvenuti C, Fossati A, Valli P (June 2001). "Effects of betahistine and of its metabolites on vestibular sensory organs.". Acta Otorhinolaryngol Ital. 21 (3 Suppl 66): 24–30. PMID 11677836.  
  3. ^ "Vertigo pill is new obesity wonderdrug". http://www.dailymail.co.uk/pages/live/articles/health/healthmain.html?in_article_id=437291&in_page_id=1774. Retrieved 2007-06-20.  
  4. ^ "New drug makes weight loss safer". http://www.brightsurf.com/news/headlines/33188/New_drug_makes_weight_loss_safer.html. Retrieved 2007-09-27.  







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