Products
Betahistine is commercially available in the form of tablets and drops (Betaserc, generic). It has been approved in many countries since 1971.
Structure and properties
Betahistine (C8H12N2, Mr = 136.19 g/mol) exists as betahistine dihydrochloride, a white to pale yellow, very hygroscopic powder that is very soluble in water. Betahistine dimesilate is also present in some drugs. Betahistine is a pyridine derivative (pyridylalkylamine) and has similarities to histamine.
Effects
Betahistine (ATC N07CA01) has antivertiginous and circulatory properties in the inner ear and brain. It is a partial agonist at the histamine H1 receptor and a partial antagonist at the histamine H3 receptor and, unlike histamine, also crosses the blood–brain barrier.
Indications
- Vertigo due to circulatory disturbances of the inner ear.
- Ménière’s syndrome and Ménière-like syndromes (vertigo, ringing in the ears, hearing loss).
Dosage
According to the professional information. Tablets are usually taken two to three times daily with a meal. Taking with food may reduce gastrointestinal side effects.
Contraindications
- Hypersensitivity
- Pheochromocytoma
For complete precautions, see the drug label.
Interactions
Drug-drug interactions are possible with MAO inhibitors and antihistamines.
Adverse effects
The most common possible adverse effects include nausea, dyspepsia, and headache.