Betahistine
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| Trade names | Serc, Veserc |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Protein binding | Very low |
| Metabolism | To 2-(2-aminoethyl)pyridine and 2-pyridylacetic acid |
| Biological half-life | 3–4 hours |
| Excretion | Renal |
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| ChEMBL | |
| ECHA InfoCard | 100.024.625 |
| Chemical and physical data | |
| Formula | C8H12N2 |
| Molar mass | 136.194 g/mol |
| 3D model (Jmol) | |
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Betahistine dihydrochloride (brand names Veserc, Serc, Hiserk, Betaserc, Vergo) is an anti-vertigo drug. It is commonly prescribed for balance disorders or to alleviate vertigo symptoms associated with Ménière's disease.
It was first registered in Europe in 1970 for the treatment of Ménière's disease.
Patients taking betahistine dihydrochloride may experience following side effects
Betahistine may also cause several digestive-related side effects. The package insert for Serc, a trade name for betahistine, states that patients may experience several gastrointestinal side effects. These may include nausea, upset stomach, vomiting, diarrhea and stomach cramping. These symptoms are usually not serious and subside between doses. Patients experiencing chronic digestive problems may lower their dose to the minimum effective range and by taking betahistine with meals. Additional digestive problems may require that patients consult their physician in order to find a possible suitable alternative.
People taking betahistine may experience several other side effects ranging from mild to serious. The package insert for Serc states that patients may experience nervous-system side effects, including headache. Some nervous system events may also partly be attributable to the underlying condition rather than the medication used to treat it. The study by Jeck-Thole and Wagner also reports that patients may experience headache and liver problems, including increased liver enzymes and bile-flow disturbances. Any side effects that persist or outweigh the relief of symptoms of the original condition may warrant that the patient consult their physician to adjust or change the medication.
Betahistine is contraindicated for people with pheochromocytoma. People with bronchial asthma and history of peptic ulcer need to be closely monitored.
Betahistine chemically is 2-[2-(methylamino)ethyl]pyridine, and is formulated as the dihydrochloride salt. Its structure closely resembles that of phenethylamine and histamine.
Betahistine comes in both a tablet form as well as an oral solution, 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.
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Wikipedia