{"id":1062,"date":"2012-08-01T00:00:39","date_gmt":"2012-08-01T07:00:39","guid":{"rendered":"http:\/\/rhochistj.org\/RhoChiPost\/?p=1062"},"modified":"2014-02-17T22:14:11","modified_gmt":"2014-02-18T05:14:11","slug":"quick-update-triptan-pharmacology","status":"publish","type":"post","link":"https:\/\/rhochistj.org\/RhoChiPost\/quick-update-triptan-pharmacology\/","title":{"rendered":"Quick Update: Triptan Pharmacology"},"content":{"rendered":"<p><span style=\"font-size: 11pt; line-height: 1.5em;\">By: Neal Shah, Co-Editor-In-Chief<\/span><\/p>\n<p>&#8211;<\/p>\n<p>Migraines can be \u201cclassic\u201d or \u201ccommon.\u201d \u00a0While all migraines feature unilateral, pulsating headaches, classic migraines feature an \u201caura\u201d upon onset (whereas common migraines do not). \u00a0Pharmacologic treatment of migraines generally includes serotonin agonists (triptans).<sup>1<\/sup><\/p>\n<p>Triptans are selective agonists of the 5-hydroxytryptamine 1B and 1D (5HT<sub>1B\/1D<\/sub>) subtypes. \u00a0By activating these receptors, triptans cause vasoconstriction and inhibit the release of vasodilatory mediators.\u00a0 5HT<sub>1D<\/sub> is found on neurons, whereas 5HT<sub>1B<\/sub> is found on cerebral vessels.<sup>2<\/sup>\u00a0 Cerebral vasodilation causes pressure against nerves and initiates migraines<sup>3<\/sup>, whereas triptans act to relieve this pressure to abort migraines.<\/p>\n<p>Interestingly, a there is an experimental drug called lasmiditan (COL-144) currently in Phase II trials.<sup>4<\/sup>\u00a0 It differs from current triptans because it is an oral 5HT<sub>1F<\/sub> agonist devoid of vasoconstrictive activity.<sup>4<\/sup><\/p>\n<p><b><span style=\"text-decoration: underline;\">SOURCES:<\/span><\/b><\/p>\n<ol>\n<li>Katzung B, Masters S, Trevor A. Basic and Clinical Pharmacology, 11th edition.\u00a0 Lange Medical Publications, McGraw-Hill, 2006.\u00a0 P 283 \u2013 284.<\/li>\n<li>Longmore J, Shaw D, Smith D et. al. Differential distribution of 5HT1D- and 5HT1B-immunoreactivity within the human trigemino-cerebrovascular system: implications for the discovery of new antimigraine drugs.\u00a0 Cephalgia.\u00a0 1997 Dec;17(8):833-42.<\/li>\n<li>Ward RC, Hruby R, Jerome JA, et. al. Foundations for Osteopathic Medicine, 2nd edition.\u00a0 Lippincott Williams &amp; Wilkins, 2002.\u00a0 P 679.<\/li>\n<li>F\u00e4rkkil\u00e4 M, Diener HC, G\u00e9raud G, et. al. Efficacy and tolerability of lasmiditan, an oral 5-HT(1F) receptor agonist, for the acute treatment of migraine: a phase 2 randomised, placebo-controlled, parallel-group, dose-ranging study.\u00a0 Lancet Neurol. 2012 May;11(5):405-13.<\/li>\n<\/ol>\n","protected":false},"excerpt":{"rendered":"<p>By: Neal Shah, Co-Editor-In-Chief &#8211; Migraines can be \u201cclassic\u201d or \u201ccommon.\u201d \u00a0While all migraines feature unilateral, pulsating headaches, classic migraines feature an \u201caura\u201d upon onset (whereas common migraines do not). \u00a0Pharmacologic treatment of migraines generally includes serotonin agonists (triptans).1 Triptans are selective agonists of the 5-hydroxytryptamine 1B and 1D (5HT1B\/1D) subtypes. \u00a0By activating these receptors,&hellip;<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[7],"tags":[1822,343,163,13,2229,2227,29,314,376,26,363,1625,657,2244,2260,671,447,21,453,16],"class_list":["post-1062","post","type-post","status-publish","format-standard","hentry","category-clinical","tag-against","tag-and","tag-dose","tag-drug","tag-drugs","tag-ebola-virus-disease","tag-editor","tag-for","tag-human","tag-migraine","tag-of","tag-or","tag-oral","tag-pharmacology","tag-pressure","tag-r","tag-release","tag-study","tag-system","tag-treatment"],"views":583,"_links":{"self":[{"href":"https:\/\/rhochistj.org\/RhoChiPost\/wp-json\/wp\/v2\/posts\/1062","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/rhochistj.org\/RhoChiPost\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/rhochistj.org\/RhoChiPost\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/rhochistj.org\/RhoChiPost\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/rhochistj.org\/RhoChiPost\/wp-json\/wp\/v2\/comments?post=1062"}],"version-history":[{"count":0,"href":"https:\/\/rhochistj.org\/RhoChiPost\/wp-json\/wp\/v2\/posts\/1062\/revisions"}],"wp:attachment":[{"href":"https:\/\/rhochistj.org\/RhoChiPost\/wp-json\/wp\/v2\/media?parent=1062"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/rhochistj.org\/RhoChiPost\/wp-json\/wp\/v2\/categories?post=1062"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/rhochistj.org\/RhoChiPost\/wp-json\/wp\/v2\/tags?post=1062"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}