2790 Zolmitriptan Zolmitriptan is only found in individuals that have used or taken this drug. It is a synthetic tryptamine derivative and appears as a white powder that is readily soluble in water. Zolmitriptan binds with high affinity to human 5-HT_1B and 5-HT_1D receptors leading to cranial blood vessel constriction. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. 139264-17-8 60857 C16H21N3O2 287.163380 White powder. 1.90e-01 g/L Topical(nasal); Oral. Mean absolute oral bioavailability is approximately 40%. Food has no affect on the rate and extent of absorption. Zolmitriptan binds with high affinity to human 5-HT_1B and 5-HT_1D receptors leading to cranial blood vessel constriction. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. Hepatic. There have been three metabolites identified: indole acetic acid, N -oxide, and N-desmethyl metabolites. However, the N-desmethyl is the only active metabolite. Half Life: The mean elimination half-life of zolmitriptan and of the active N-desmethyl metabolite is 3 hours. No indication of carcinogenicity to humans (not listed by IARC). Used in the acute treatment of migraine attacks with or without aura and cluster headaches. Serious cardiac events, including myocardial infarction migth occur. [Wikipedia] There is no specific antidote to zolmitriptan. In cases of severe intoxication, intensive care procedures are recommended, including establishing and maintaining a patent airway, ensuring adequate oxygenation and ventilation, and monitoring and support of the cardiovascular system. (L1712) 2009-07-21T20:26:34Z 2026-03-27T01:32:06Z Zolmitriptan C07218 10124 Zolmitriptan DB00315 true CN(C)CCC1=CNC2=CC=C(C[C@H]3COC(=O)N3)C=C12 C16H21N3O2 InChI=1S/C16H21N3O2/c1-19(2)6-5-12-9-17-15-4-3-11(8-14(12)15)7-13-10-21-16(20)18-13/h3-4,8-9,13,17H,5-7,10H2,1-2H3,(H,18,20)/t13-/m0/s1 ULSDMUVEXKOYBU-ZDUSSCGKSA-N 287.3568 287.163376931 Exogenous Solid 1.6 HMDB14460 CHEMBL1185 54844 <p>Islam Aminul, Bhar Chandan, Katam Sahadev, &#8220;Process for preparing optically pure zolmitriptan.&#8221; U.S. Patent US20050245585, issued November 03, 2005.</p> CHEM002167 DTXSID8045933 NS00007368 (4S)-4-({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-one