Betahistine hydrochloride is the generic name for the anti vertigo drug SERC. It was first registered in Europe in 1970 for the treatment of Ménière's disease. It is commonly prescribed for people who have balance disorders or to alleviate the 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.
A new use may be in the field of obesity management. Dr Nir Barak, of the Rabin Medical Centre in Tel Aviv has undertaken trials and it is reported (Telegraph, UK, 19 February 2007) that volunteers lost better 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 %.
Chemistry and pharmacokinetics
Betahistine chemically is 2-[2-(methylamino) ethyl] pyridine, and is formulated as the dihydrochloride salt. Its structure closely resembles that of histamine.
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 not be inactive and exerts effects similar to those of betahistine on ampullar receptors.
Mode of action
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 endolympathic 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;