Recent Development of Zolmitriptan Formulation in Migraine Therapy: Production, Metabolism and Pharmaceutical Aspects.

Farha Bano, Faris F Aba Alkhayl, Mohammad Rashid, Mohammed Ghanim Alqethami, Mohammed Omair Alsufyani, Khadijah Oudah R Alhothali, Mohammed Japer Mohammed Hakme, Abdulrahman Mohammed Al-Jarallah, Rikeshwer Prasad Dewangan, Asif Husain
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Abstract

The triptans class of pharmaceuticals, which was created to treat acute migraine, is made up of indole-containing drugs that bind to a subset (1B/1D) of 5-hydroxytryptamine receptors and are agonists of serotonin receptors. At the moment, naratriptan, eletriptan, zolmitriptan, rizatriptan, almotriptan, and frovatriptan are the seven types of triptans available on the market. Among these are the FDA-approved triptans, Zolmitriptan and Sumatriptan, which are selective serotonin (5-hydroxytryptamine) agonists. Zolmitriptan, a synthetic tryptamine derivative and a well-known member of the triptan family, is available as an orally disintegrating tablet, nasal spray, and tablet. There are melt formulations of rizatriptan and zolmitriptan available on the market that are easier to use and absorb, comparable to regular pills. Recently, the FDA approved zolmitriptan, a medication with tolerability comparable to sumatriptan. Whereas zolmitriptan is only available as an oral melt or tablet, sumatriptan is available as a nasal spray, oral preparation, or self-injectable kit. The only known antimigraine drugs that were widely utilized before the triptan period were ergotamine and dihydroergotamine. However, zolmitriptan binds to plasma proteins only 25% of the time because of significant first-pass degradation. Researchers have looked into fresh ideas for solving this issue and innovations to overcome its pharmacokinetic difficulties. This article emphasizes the role of zolmitriptan in the treatment of migraines, highlighting its pharmacological properties, production, metabolism, and structural features.

用于偏头痛治疗的佐米曲普坦制剂的最新发展:生产、代谢和制药方面。
三苯氧胺类药物是为治疗急性偏头痛而诞生的,由含有吲哚的药物组成,这些药物与5-羟色胺受体的一个子集(1B/1D)结合,是血清素受体的激动剂。目前,市场上有纳拉曲坦、依利曲坦、佐米曲坦、利扎曲坦、阿莫曲坦和弗罗伐曲坦等七种曲坦类药物。其中,佐米曲普坦(Zolmitriptan)和舒马普坦(Sumatriptan)是美国食品及药物管理局批准的三普坦,它们是选择性 5-羟色胺(5-hydroxytryptamine)激动剂。佐米曲普坦(Zolmitriptan)是一种合成色胺衍生物,也是众所周知的曲坦类药物,有口腔崩解片、鼻喷剂和片剂等剂型。市场上有更易于使用和吸收的利扎曲普坦和佐米曲普坦的融化配方,可与普通药片相媲美。最近,美国食品及药物管理局批准了佐米曲普坦(zolmitriptan),这种药物的耐受性与舒马曲普坦相当。佐米曲普坦只有口服溶液或片剂,而舒马曲普坦则有鼻腔喷雾剂、口服制剂或自我注射试剂盒。在三普坦时期之前,唯一被广泛使用的已知抗偏头痛药物是麦角胺和双氢麦角胺。然而,由于存在明显的首过降解,佐米曲普坦与血浆蛋白的结合率仅为 25%。研究人员一直在寻找解决这一问题的新思路,并通过创新来克服其药代动力学方面的困难。本文强调了佐米曲普坦在偏头痛治疗中的作用,重点介绍了其药理特性、生产、代谢和结构特点。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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