Meniere disease, chronic management:
Note: Reserve pharmacotherapy for patients in whom lifestyle modifications do not result in sufficient response. Provide as-needed vestibular suppressants and antiemetics for acute relief of vertigo (AAO/HNS [Basura 2020]; Coelho 2008).
Oral: Initial: 24 to 48 mg/day in 2 to 3 divided doses (manufacturer's labeling [Canadian product]). Some experts initiate at a lower dose (eg, 8 to 16 mg once daily) and increase at 2- to 4-week intervals as needed to twice daily, then 3 times daily based on response and tolerability (Moskowitz 2022). May taper and discontinue after 3 to 6 months of prolonged control (AAO/HNS [Basura 2020]; Magnan 2018; Moskowitz 2022).
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.
May be product dependent
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 United States.
Meniere disease: Treatment of Meniere 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.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Antihistamines: Betahistine may diminish the therapeutic effect of Antihistamines. Antihistamines may diminish the therapeutic effect of Betahistine. 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)
