Zolmitriptan

Zolmitriptan 속성

Zolmitriptan MSDS

(4R)-4-[[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]methyl]oxazolidin-2-one

Zolmitriptan C화학적 특성, 용도, 생산

개요

Zolmitriptan is a selective serotonin receptor agonist of the 1B and 1D subtypes. It is mainly used in the acute treatment of migraine attacks with or without aura and cluster headaches. Zolmitriptan takes effect through binding to human 5-HT1Band 5-HT1Dreceptors, leading to cranial blood vessel constriction and the release of sensory neuropeptides through nerve endings in the trigeminal system.

화학적 성질

White Crystalline Powder

용도

Zolmitriptan is a serotonin 5HTID-receptor agonist and used to treat migraine (1,2,3).

일반 설명

Zolmitriptan, the second triptan marketed (approved in1997), has a much better bioavailability (40%–48%) thansumatriptan. It is rapidly absorbed after oral or nasal sprayadministration. It also has an orally disintegrating tablet formulation(Zomig ZMT), which can be taken without water.Zolmitriptan undergoes rapid N-demethylation via CYP1A2to a more potent, active metabolite, N-desmethylzolmitriptan,which is 2 to 6 times more potent than the parentdrug. This active metabolite was detected 5 minutesafter dosing and accounts for about two thirds of the plasmaconcentration of the administered dose of the parent drug.284Thus, it is reasonable to assume that the therapeutic effectsand especially the CNS side effects of zolmitriptan must bein part attributed to the plasma levels of this active metabolite,at least until it is further degraded by hepatic MAO-Ato its inactive indole acetic acid derivatives.

Clinical Use

Zomig was launched in Germany, Denmark, Sweden and the UK for use as an antimigraine agent (with and without aura). It can be prepared by three related routes of 5 to 7 steps starting from L-4-nitrophenylalanine. Zomig is a 5-HT_1D/1B receptor agonist (10 fold ratio) with modest (< 100x) affinity for 5-HT_1A and 5-HT_1F receptors. It has no affinity for other serotonin receptors or receptors of other neurotransmitters. It has a novel dual action mechanism: centrally it acts on the trigeminal nucleus caudalis and peripherally is acts on the trigeminovascular system. Zomig was effective in treating headaches and nonheadache (photophobia, phonophobia and nausea) symptoms. It was 2-3 times more potent than sumatriptan and is metabolized to three compounds, one of which is 2-8 times more active than the parent. It caused a 40-50% decrease in headache after 1 h and a 73-77% after 4 h. There was a 30% reoccurance of headache but 90% effective treatment with a second dose. It blocks neurogenic inflammation by inhibiting release of peptides, causes vasoconstriction, and inhibits neuronal depolarization at peripheral sites in the cranium. It is 40% bioavailable and a 10 time theraputic dose showed no safety concerns.

참고 문헌

https://www.drugbank.ca/drugs/DB00315
Rothner, A. D., et al. "Zolmitriptan oral tablet in migraine treatment: high placebo responses in adolescents." Headache the Journal of Head & Face Pain 46.1(2006):101.
Hedlund, C, et al. "Zolmitriptan nasal spray in the acute treatment of cluster headache: a meta-analysis of two studies. " Neurology49.9(2009):1315–1323.

Zolmitriptan 준비 용품 및 원자재

원자재

준비 용품

Zolmitriptan 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Shandong Hengshannuode Pharmaceutical Technology Co., Ltd.	+8615065888978	admin@hsnordpharma.com	China	92	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	6011	58
Sinoway Industrial co., ltd.	0592-5800732; +8613806035118	xie@china-sinoway.com	China	992	58
Henan Bao Enluo International TradeCo.，LTD	+86-17331933971 +86-17331933971	deasea125996@gmail.com	China	2503	58
Zibo Hangyu Biotechnology Development Co., Ltd	+86-0533-2185556 +8617865335152	Mandy@hangyubiotech.com	China	11013	58
Hebei Zhuanglai Chemical Trading Co.,Ltd	+8613343047651	admin@zlchemi.com	China	2852	58
Hebei Shengyang Water Conservancy Engineering Co., Ltd.	+8615373025980	clara@hbshengyang.com	China	783	58
Nanjing Gold Pharmaceutical Technology Co. Ltd.	025-84209270 15906146951		CHINA	115	55
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21687	55
Shanghai Time Chemicals CO., Ltd.	+86-021-57951555 +8617317452075	jack.li@time-chemicals.com	China	1807	55

Zolmitriptan 관련 검색: