International Journal of Basic & Clinical Pharmacology | June 2021 | Vol 10 | Issue 6 Page 745 International Journal of Basic & Clinical Pharmacology Bhanwra S et al. Int J Basic Clin Pharmacol. 2021 Jun;10(6):745-747 http://www.ijbcp.com pISSN2319-2003 | eISSN2279-0780 Review Article Lasmiditan: the first neurally acting anti-migraine drug Sangeeta Bhanwra*, Sonia S. Mahajan, Rajiv Kumar INTRODUCTION Migraine is a primarily a headache disorder characterized by pulsating headache, moderate to severe in intensity, usually restricted to one side, often associated with nausea, vomiting, sensitivity to light and sound which often aggravates by routine physical activity. It is more common in women due to hormonal influences. 1 It ranks sixth in the years lost due to disability (YLD) worldwide. 2 Therefore, prompt treatment and prophylaxis of the chronic patients becomes imperative. There are various classes of drugs used for the treatment and prophylaxis of migraine, depending upon the severity, such as non-steroidal anti-inflammatory drugs like paracetamol, aspirin, metamizole, ibuprofen and indomethacin and their combinations, selective 5-HT1D/1B agonists (triptans), ergot alkaloids, antiemetics, beta blockers, tricyclic antidepressants, calcium channel blockers and antiepileptics. Cardiovascular diseases like uncontrolled hypertension, myocardial infarction and arrhythmias, stroke and hemiplegic migraine require the restricted and cautious use of triptans. 3 This led to the search for newer effective drugs for the treatment of migraine without vasoactive properties. Calcitonin gene related peptides (CGRP) receptor antagonists or “gepants” have been found to be effective for the prevention and treatment of acute migraine. Ubrogepant and rimegepant are the orally active drugs belonging to this class which have been approved by the United States food and drug administration (USFDA) in December 2019 and February 2020 respectively. 4,5 A new drug, lasmiditan, a member of the novel class “ditans”, a serotonin (5-HT)1F receptor agonist, has been approved for the treatment of adult patients suffering from acute migraine with or without aura in October 2019. Lasmiditan is devoid of vasoconstricting action and is the first neurally acting antimigraine agent (NAAM). 3,6 5-HT1F RECEPTOR AND MIGRAINE The trigemino-vascular system has a pivotal role in the migraine headache. It comprises of the trigeminal nucleus caudalis, trigeminal ganglia and the C1-C2 segments of the spinal cord. The activation of this system results in a cascade of events leading to the symptomatology of migraine. 7 The 5-HT1F receptors are widely expressed in the CNS. They are found centrally and peripherally in trigeminal DOI: https://dx.doi.org/10.18203/2319-2003.ijbcp20212088 Department of Pharmacology, Government Medical College, Chandigarh, India Received: 21 April 2021 Accepted: 03 May 2021 *Correspondence: Dr. Sangeeta Bhanwra, Email: doc_sangeeta@yahoo.com Copyright: © the author(s), publisher and licensee Medip Academy. This is an open-access article distributed under the terms of the Creative Commons Attribution Non-Commercial License, which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. ABSTRACT Lasmiditan is the first neurally acting drug for the treatment of acute migraine. It is a highly selective, orally acting 5- HT1F agonist that was approved in November 2019, for the acute treatment of migraine in adults, with or without aura, by USFDA. Lesmiditan may help in terminating the acute attack of migraine by inhibiting the central and peripheral neuronal activity and the release of CGRP. Keywords: Lasmiditan, 5-HT1F agonist, Migraine