Betahistine

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H315：피부에 자극을 일으킴

  H319：눈에 심한 자극을 일으킴

  H335：호흡 자극성을 일으킬 수 있음

• 예방조치문구

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P271：옥외 또는 환기가 잘 되는 곳에서만 취급하시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P302+P352：피부에 묻으면 다량의 물로 씻으시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

Betahistine 화학적 특성, 용도, 생산

• 개요

  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).

• 용도

  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was FDA approved for Meniere's disease in the US market for a short period of time in the 1970s, but approval was then rescinded due to lack of evidence supporting its efficacy.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.

• Indications

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

• Mechanism of action

  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.

• Pharmacokinetics

  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.

• 부작용

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

• Drug interactions

  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.

• 주의 사항

  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.

Betahistine 준비 용품 및 원자재

Betahistine 공급 업체

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