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解説
スボレキサント，催眠薬の一。覚醒状態を維持する上で必要なオレキシンが、受容体に結合することを阻害する作用をもつ。不眠症などに用いられる。商標名ベルソムラ。
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効能
催眠薬, オレキシン受容体拮抗薬
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商品名
ベルソムラ (MSD)
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説明
Suvorexant, a dual orexin receptor antagonist marketed under
the trade name Belsomra®, discovered and developed by Merck
for the treatment of insomnia, was approved by the US FDA in
August 2014 and became available in Japan in November of the
same year. The drug’s mechanism of action operates through
the competitive blockade of wake-promoting neuropeptides orexin
A and orexin B toward receptors orexin receptor type 1 and orexin
receptor type 2, which are believed to modulate sleep-wake
cycles.
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使用
Suvorexant (MK-4305) is a dual (non-selective) orexin receptor antagonist in development by Merck & Co. for the treatment of insomnia. It works by turning off wakefulness rather than by inducing sleep. Users of higher doses had an increased rate of suicidal ideation.
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定義
ChEBI: Suvorexant is an aromatic amide obtained by formal condensation of the carboxy group of 5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid with the secondary amino group of 5-chloro-2-[(5R)-5-methyl-1,4-diazepan-1-yl]-1,3-benzoxazole. An orexin receptor antagonist used for the management of insomnia. It has a role as a central nervous system depressant and an orexin receptor antagonist. It is a member of 1,3-benzoxazoles, a member of triazoles, a diazepine, an aromatic amide and an organochlorine compound.
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生物活性
Suvorexant is a dual orexin receptor (OXR) antagonist that blocks both OX1R and OX2R (Kis = 1.2 and 0.60 nM, respectively). It reduces locomotor activity and promotes sleep by inhibiting the binding of orexin A and B. In rats, suvorexant decreases self-administration of, and conditioned place preference for, cocaine ( | 16186 | ISO60176). It also decreases dopamine levels in the rat ventral striatum following a cocaine-induced increase. Formulations containing suvorexant are used in the treatment of insomnia. Suvorexant is regulated as a Schedule IV compound in the United States. This compound is also available as an analytical reference standard.
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代謝
Suvorexant is primarily metabolized by cytochrome-P450 3A4 enzyme (CYP3A4) with a minor contribution from CYP2C19. Major circulating metabolites are suvorexant and a hydroxy-suvorexant metabolite, which is not expected to be pharmacologically active. There is potential for drug-drug interactions with drugs that inhibit or induce CYP3A4 activity.
