Ménière disease (to decrease episodes of vertigo): Oral: 8 to 16 mg 3 times daily or 24 mg twice daily; usual dosage range: 24 to 48 mg daily in divided doses.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); use with caution.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). Betahistine primarily undergoes hepatic metabolism; use with caution.
Refer to adult dosing. Use with caution due to likelihood of decreased hepatic/renal function.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Serc: 16 mg, 24 mg
Generic: 8 mg, 16 mg, 24 mg
Not available in the US
Oral: Administer with or without meals; administer with meals if adverse GI effects occur.
Note: Not approved in the US.
Ménière disease: Treatment of Ménière disease (to decrease episodes of vertigo).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Central nervous system: Headache (5%)
Gastrointestinal: Nausea (2%), dyspepsia
Frequency not defined:
Central nervous system: Confusion, convulsions, drowsiness (case reports), hallucination, paraesthesia
Cardiovascular: Hypotension (including orthostatic and postural hypotension), tachycardia, ventricular premature contractions (case reports)
Dermatologic: Pruritus, skin rash, Stevens-Johnson syndrome, urticaria
Gastrointestinal: Abdominal distension, abdominal pain, bloating, peptic ulcer (including exacerbation of previous disease), vomiting
Hypersensitivity: Anaphylaxis, angioedema, hypersensitivity reaction
Respiratory: Dyspnea
Hypersensitivity to betahistine or any component of the formulation; presence or history of active peptic ulcer disease; pheochromocytoma
Disease-related concerns:
• Asthma: Use with caution; clinical intolerance has been reported in a few asthmatic patients.
• Cardiovascular disease: Use with caution in patients with cardiovascular disease; post-market cases of ventricular extrasystoles, hypotension, and tachycardia have been reported during use.
• Hepatic impairment: Use with caution; primarily undergoes hepatic metabolism.
• Peptic ulcer: Exacerbation of symptoms has been observed in patients with a history of peptic ulcer; use is contraindicated in the presence or history of peptic ulcer.
None known.
Antihistamines: May diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
Beta2-Agonists: Betahistine may diminish the therapeutic effect of Beta2-Agonists. Risk C: Monitor therapy
Monoamine Oxidase Inhibitors: May increase the serum concentration of Betahistine. Risk C: Monitor therapy
Adverse events were observed in some animal reproduction studies.
It is not known if betahistine is present in breast milk. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Partial agonist of histamine at H1 receptor and antagonist at H3 receptor; relatively inactive at H2 receptor. Animal studies suggest that betahistine may increase cochlear blood flow and produce excitatory effects on neuronal activity of cortical and subcortical structures via H1-receptor agonism and decrease vestibular sensory input and increase synthesis and release of histamine from the hypothalamus via H3-receptor antagonism (Ihler 2012; Lacour 2007).
Absorption: Rapid, complete; delayed by food
Tmax: 1 hour to reach peak levels of inactive metabolite
Protein binding: <5%
Metabolism: Rapid and almost complete hepatic metabolism to 2-pyridylacetic acid (inactive metabolite)
Half-life elimination: ~3.5 hours (inactive metabolite)
Excretion: Urine (~91%; primarily as inactive metabolite)
