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Name
Betahistine

Brand Names: International

Acuver (RO); Aequamen (DE); Agihistine (VN); Agiserc (IL); Alfinor (HK, LK, MY); Alvigo (LB); Avertid
(UA); Be-Stedy (BH); Beanorm (UA); Beautipex (KR); Behistin (TH); Bertigo (BH, QA); Besutin (TW);
Betabere (NL); Betagen (AE, BH, QA); Betagis (UA); Betahist (LK); Betahistine-Eurogenerics (LU);
Betakule (NL); Betasaerc (JO); Betaserc (AE, AT, BE, BG, BH, BR, CH, CY, CZ, DK, EC, EE, EG, FI, GR,
HK, HR, HU, ID, KW, LK, LT, LU, LV, MT, MY, NL, PE, PH, PL, PT, QA, RO, RU, SA, SG, SI, TR, TW, TZ,
UA, VN); Betastin (JO); Betavert (BD, PH); Betistin (UY); Betris (TH); By-Vertin (IE); Clensan (TW);
Ergo (PH); Exigo (PH); Fidium (ES); Histigo (ID, TH); Histine (EG); Kernhistine (VN); Lectil (FR); Lexigo
(ID); Lobione (LU); Menaril (BD); Meniace (JP, KR); Menistin (PE); Merislon (CN, HK, ID, JP, MY, PH,
QA, SG, TH, TW, VN); Merison (HK); Meristin (ID); Mertigo (ID, TH); Mertigo SR (ID); Meslon (TW);
Microser (AR, CL, EC, IT, PE, PK, VE); Microserc (EG); Misoserc (QA); Nisulin (TW); Novertin (PY);
Nuveat (PH); Rotaver (ID); Seniere (AU); Serc (AU, GB, HR, IE, MX, NZ, PK, TH, ZA); Stei (TH);
Suzutolon (JP); Theohist (LK); Tiniril (BD); Urutal (HR); Vasomotal (DE, PY); Vasoserc (LB, UA);
Vasoserc Forte (LB); Vasotal (UY); Verdiz (PH); Vergo (NZ); Vert (PH); Vertigal (HR); Vertigon (IE);
Vertihof (TH); Vertikind (PH); Vertimed (MT, RO, TR); Vertin (IN); Vertinex (LB); Vertrol (PH); Verum
(CO); Vestibo (UA); Veszrc (BD)

International Nonproprietary Names (INN)

Betahistina [Spanish]; Betahistine [English]; Betahistinum [Latin]; Bétahistine [French];
Бетагистин [Russian]; ‫[ ﺑﻴﺘﺎﻫﻴﺴﺘﻴﻦ‬Arabic]; 倍他司汀 [Chinese]

Brazilian Nonproprietary Names (DCB)

Betaistina

Japanese Accepted Name (JAN)

ベタヒスチンメシル酸塩
Anatomic Therapeutic Chemical (ATC) Classification
N07CA01

Pharmacologic Category
Histamine H1 Agonist; Histamine H3 Antagonist

Dosing: Adult
Ménière disease (to decrease episodes of vertigo): Oral:
Betahistine dihydrochloride [Canadian/International product]: 8 to 16 mg 3 times daily or 24
mg twice daily; usual dosage range: 24 to 48 mg daily in divided doses.
Betahistine mesilate [International product]: 6 to 12 mg 3 times daily. Significantly higher
doses of the active ingredient (as dihydrochloride salt) have been studied in a small
number of cases with severe, resistant disease (Lezius 2011).

Dosing: Geriatric
Refer to adult dosing. Use with caution due to likelihood of decreased hepatic/renal function.

Dosing: Renal Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied);
use with caution.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Betahistine primarily undergoes hepatic metabolism; use with caution.

Use: Labeled Indications

Note: Not approved in the US.
Ménière disease: Treatment of Ménière disease (to decrease episodes of vertigo).

Clinical Practice Guidelines

Ménière disease:
American Academy of Otolaryngology–Head and Neck Surgery Foundation, "Clinical Practice
Guideline: Ménière's Disease," April 2020

Administration: Oral
Administer with or without meals; administer with meals if adverse GI effects occur.

Storage/Stability
Store at 15°C to 30°C (59°F to 86°F). Protect from moisture.

Contraindications
Hypersensitivity to betahistine or any component of the formulation; presence or history of
active peptic ulcer disease; pheochromocytoma
Warnings/Precautions
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.

Pregnancy Considerations
Adverse events were observed in some animal reproduction studies.

Breast-Feeding Considerations
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.

Adverse Reactions
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

Allergy and Idiosyncratic Reactions

Betahistine Allergy

Metabolism/Transport Effects
None known.
Drug Interactions
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

Product Availability (US)

Not available in the US

Dosage Forms: Canada

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

Dosage Forms: International

Excipient information presented when available (limited, particularly for generics); consult
specific product labeling. Note: Availability of specific dosage forms may vary by region/country
Additional dosage forms not available in US and/or Canada:
Tablet, Oral, as mesilate: 6 mg, 12 mg

Generic Available (US)

Yes

Mechanism of Action
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).

Pharmacodynamics/Kinetics
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)
Dental: Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions

Dental: Effects on Dental Treatment

No significant effects or complications reported

Dental: Effects on Bleeding

No information available to require special precautions

Index Terms
Betahistine Dihydrochloride; Betahistine HCl

References
Ihler F, Bertlich M, Sharaf K, et al. Betahistine Exerts a Dose-Dependent Effect on Cochlear Stria
Vascularis Blood Flow in Guinea Pigs In Vivo. PLoS One. 2012;7(6):e39086.[PubMed 22745706]
Lacour M, van de Heyning PH, Novotny M, et al. Betahistine in the treatment of Ménière’s disease.
Neuropsychiatr Dis Treat. 2007;3(4):429-440.[PubMed 19300572]
Serc (betahistine) [product monograph].Etobicoke, Ontario, Canada: BGP Pharma ULC: August
2017.

References: International
Meniace (betahistine) tablets [KR prescribing information]. Available at:
https://nedrug.mfds.go.kr/pbp/CCBBB01/getItemDetail?itemSeq=197700201. Accessed
December 20, 2018.

Brand Names: Canada

ACT Betahistine [DSC]; Auro-Betahistine; PMS-Betahistine; Serc; TEVA-Betahistine