関: betahistine hydrochloride、betahistine mesilate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/06/29 17:02:25」(JST)

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Betahistine dihydrochloride (brand names Veserc, Serc, Hiserk, Betaserc) is an antivertigo drug. It was first registered in Europe in 1970 for the treatment of Ménière's disease. It is commonly prescribed to patients with balance disorders or to alleviate vertigo symptoms associated with Ménière's disease.

Chemistry

Betahistine chemically is 2-[2-(methylamino)ethyl]pyridine, and is formulated as the dihydrochloride salt. Its structure closely resembles that of phenethylamine and histamine.^{[citation needed]}

Pharmacokinetics

Betahistine comes in both a tablet form as well as an oral solution, and is taken orally. It is rapidly and completely absorbed. The mean plasma half-life is 3–4 hours, and excretion is virtually complete in the urine within 24 hours. Plasma protein binding is very low. Betahistine is transformed into aminoethylpyridine and hydroxyethylpyridine and excreted with the urine as pyridylacetic acid. There is some evidence that one of these metabolites, aminoethylpyridine, may be active and exert effects similar to those of betahistine on ampullar receptors.^[1]

Mode of action

Betahistine has a very strong affinity as an antagonist for histamine H₃ receptors and a weak affinity as an agonist for histamine H₁ receptors. Betahistine seems to dilate the blood vessels within the inner ear which can relieve pressure from excess fluid and act on the smooth muscle.

Betahistine has two modes of action. Primarily, it has a direct stimulating (agonistic) effect on H₁ receptors located on blood vessels in the inner ear. This gives rise to local vasodilation and increased permeability, which helps to reverse the underlying problem of endolymphatic hydrops.

More importantly, betahistine has a powerful antagonistic effects at H₃ receptors, thereby increasing the levels of neurotransmitters histamine, acetylcholine, norepinephrine, and serotonin released from the nerve endings. The increased amounts of histamine released from histaminergic nerve endings can stimulate receptors. This stimulation explains the potent vasodilatory effects of betahistine in the inner ear, that are well documented.

It is postulated that betahistine's increase in the level of serotonin in the brainstem inhibits the activity of vestibular nuclei.

Adverse effects

Headache.
Low level of gastric side effects.
Insomnia
Nausea can be a side effect, but the patient is generally already experiencing nausea due to the vertigo so it goes largely unnoticed.
Patients taking betahistine hydrochloride may experience several hypersensitivity and allergic reactions. In the November 2006 issue of "Drug Safety," Dr. Sabine Jeck-Thole and Dr. Wolfgang Wagner reported that betahistine hydrochloride may cause several allergic and skin-related side effects. These include rash in several areas of the body; itching and hives; and swelling of the face, tongue and mouth. Other hypersensitivity reactions reported include tingling, numbness, burning sensations, shortness of breath and laboured breathing. The study authors suggest that hypersensitivity reactions may be a direct result of betahistine's role in increasing histamine levels throughout the body. Hypersensitivity reactions quickly subside after betahistine has been discontinued.

Digestive side effects Betahistine may also cause several digestive-related side effects. The package insert for Serc, a trade name for betahistine, states that patients may experience several gastrointestinal side effects. These may include nausea, upset stomach, vomiting, diarrhea and stomach cramping. These symptoms are usually not serious and subside between doses. Patients experiencing chronic digestive problems may lower their dose to the minimum effective range and by taking betahistine with meals. Additional digestive problems may require that patients consult their physician in order to find a possible suitable alternative.

Other side effects Patients taking betahistine may experience several other side effects ranging from mild to serious. The package insert for Serc states that patients may experience nervous-system side effects, including headache. Some nervous system events may also partly be attributable to the underlying condition rather than the medication used to treat it. The study by Jeck-Thole and Wagner also reports that patients may experience headache and liver problems, including increased liver enzymes and bile-flow disturbances. Any side effects that persist or outweigh the relief of symptoms of the original condition may warrant that the patient consult their physician to adjust or change the medication.

Contraindications

Betahistine is contraindicated for people with pheochromocytoma. People with bronchial asthma and history of peptic ulcer need to be closely monitored.^{[citation needed]}

References

^ Botta L, Mira E, Valli S, Zucca G, Perin P, Benvenuti C, Fossati A, Valli P (June 2001). "Effects of betahistine and of its metabolites on vestibular sensory organs.". Acta Otorhinolaryngol Ital. 21 (3 Suppl 66): 24–30. PMID 11677836.

UpToDate Contents

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1. 回転性めまいの治療 treatment of vertigo
2. メニエール病 meniere disease

English Journal

Clinical and Demographic Features of Vertigo: Findings from the REVERT Registry.

Agus S, Benecke H, Thum C, Strupp M.SourceAbbott Products Operations AG Allschwil, Switzerland.
Frontiers in neurology.Front Neurol.2013 May 10;4:48. doi: 10.3389/fneur.2013.00048. Print 2013.
Introduction: Despite being a common disease, data on vertigo management in a real-world setting are scarce. Aims: To provide information on the vertigo and its management in a real-world setting. Methods: Data were collected from 4,294 patients with vertigo in 13 countries over 28 months via a mu
PMID 23675366

Sudden Hearing Loss After Dental Treatment.

Kansu L, Yilmaz I.SourceAssociate Professor, Department of Otolaryngology-Head and Neck Surgery, Baskent University, Ankara, Turkey. Electronic address: leylakansu@hotmail.com.
Journal of oral and maxillofacial surgery : official journal of the American Association of Oral and Maxillofacial Surgeons.J Oral Maxillofac Surg.2013 May 1. pii: S0278-2391(13)00304-2. doi: 10.1016/j.joms.2013.03.014. [Epub ahead of print]
A 66-year-old man presented with impaired balance, tinnitus, sensation of blockage, and hearing loss in his left ear, which developed after dental treatment for dental pain 4 days previously. Treatment of the carious left upper second molar tooth had included pulp extirpation, canal expansion, and t
PMID 23642550

Japanese Journal

めまい集団リハビリテーションと補中益気湯の併用療法 : 抑うつ傾向がみられるめまい患者の治療

新井基洋,五島史行,保坂隆
心身医学 52(3), 221-228, 2012-03-01
… いリハビリテーションと補中益気湯を併用しQOLの改善効果を検討した.対象は入院治療前にSelf-rating Depression Scale(以下,SDS)検査を施行し,抑うつ傾向(50>SDS≧40)を呈する患者275例である.全例にめまい薬物治療(betahistine mesilateおよびATP製剤の内服)と集団めまいリハビリテーションを施行し,補中益気湯投与群は入院期間中から前記治療に加えて本剤を併用した.結果:投与群,非投与群ともにQOLの改善が認められた.また両群間で …
NAID 110009418965

めまい集団リハビリテーションとSSRIの併用療法(第2報) : うつ状態の併存がみられるめまい患者の治療

新井基洋,五島史行,保坂隆
心身医学 51(10), 919-926, 2011-10-01
… リハビリテーションとSSRIの併用療法によるQOLの改善内容を明らかにする目的で,入院時のSDS検査におけるスコアが50以上の患者を対象としたレトロスペクティブな検討を行った.めまい治療は,薬物治療としてbetahistine mesilate(メリスロン^[○!R])18mg/日とATP製剤(10%アデホス顆粒^[○!R])3g/日の内服とし,さらに集団めまいリハビリテーション併用加療を施行した.また,うつ状態の治療にはSSRIのfluvoxamine(デプロメール^[○!R])50mg/日 …
NAID 110008722825

「ベタヒスチン」

Betahistine
Systematic (IUPAC) name
	N-methyl-2-(pyridin-2-yl)ethanamine
Clinical data
Trade names	Serc, Veserc
AHFS/Drugs.com	International Drug Names
Legal status	?
Routes	Oral
Pharmacokinetic data
Protein binding	Very low
Metabolism	To 2-(2-aminoethyl)pyridine and 2-pyridylacetic acid
Half-life	3–4 hours
Excretion	Renal
Identifiers
CAS number	5638-76-6
ATC code	N07CA01
PubChem	CID 2366
DrugBank	DB06698
ChemSpider	2276
UNII	X32KK4201D
KEGG	D07522
ChEBI	CHEBI:35677
ChEMBL	CHEMBL24441
Chemical data
Formula	C8H12N2
Mol. mass	136.194 g/mol
	SMILES n1ccccc1CCNC;
	InChI InChI=1S/C8H12N2/c1-9-7-5-8-4-2-3-6-10-8/h2-4,6,9H,5,7H2,1H3 ; Key:UUQMNUMQCIQDMZ-UHFFFAOYSA-N ;
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