ベタヒスチン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P271：屋外または換気の良い場所でのみ使用すること。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

ベタヒスチン 価格

ベタヒスチン 化学特性,用途語,生産方法

• 効能

  鎮暈薬, 血管拡張薬, 抗ヒスタミン薬

• 説明

  Betahistine is an analogue of histamine with weak agonist properties at histamine H1 receptors and more potent antagonistic effects at histamine H3 receptors.
  This drug is broadly used worldwide, except for the USA, since it has not been approved by the US Food and Drug Administration. Betahistine is a structural analog of histamine that acts as a weak partial postsynaptic histamine H1 receptor agonist and presynaptic H3 receptor antagonist, with no effect on postsynaptic H2 receptors (Gbahou et al, 2010). The mechanism of action of the drug appears to depend mainly on its action on H3 receptors mediated by two metabolites, aminoethylpyridine and hydroxyethylpyridine (Bertich et al, 2014).

• 使用

  Betahistine is a vasodilator, a mild H1 histamine agonist, and a potent H3 histamine antagonist. The mechanism of action in Meniere's disease is unknown, but theories include reducing the endolymphatic pressure through improved circulation in the stria vascularis or inhibiting activity in the vestibular nuclei. It has been found to be a safe drug with a very low side effect profile. Betahistine was FDA approved for Meniere's disease in the US market for a short period of time in the 1970s, but approval was then rescinded due to lack of evidence supporting its efficacy. However, based on clinical experience and several observational studies, it is still widely used elsewhere in the world.

• 適応症

  Betahistine is indicated in treatment of Meniere's disease (vertigo, hearing loss and tinnitus); it is not effective in preventing vertigo attacks.

• 作用機序

  The precise mechanism of betahistine's actions is unclear; it has antagonistic actions on histamine H3 receptors, and is a weak agonist at H receptors. In animal studies, it inhibits generation of spikes in vestibular nuclei. Its vasodilator activity (similar to histamine's) presumably improves blood flow in the inner ear and brainstem.

• 薬物動態学

  After oral administration, betahistine is rapidly and completely absorbed, rapidly metabolised (to one major metabolite, 2-pyridylacetic acid) and 90% excreted within 24 hours. Plasma and urinary half-lives are about 3.5 hours.

• 副作用

  Common adverse reactions include headache, nausea and dyspepsia. More rarely, hypersensitivity reactions (rash, pruritis, bronchospasm) and hypotension may occur.

• 薬物相互作用

  Co-administration of betahistine and monoamine oxidase inhibitors type B reduces metabolism of betahistine. Theoretically, interactions might occur with concurrent antihistamines; however, no significant problems have been reported.

• 予防処置

  Betahistine should be used with caution in individuals with asthma, urticaria, phaeochromocytoma or hypersensitivity to any components of tablets. Betahistine is contraindicated in people with active or history of peptic ulcer. Betahistine is classified in Pregnancy Safety Category B2: insufficient data available; it is contraindicated in pregnancy and lactation, and in children under 18.

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