Betahistine

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 bloodbrain 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.