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Headache
Published in Philip B. Gorelick, Fernando D. Testai, Graeme J. Hankey, Joanna M. Wardlaw, Hankey's Clinical Neurology, 2020
Ditans, serotonin 5-HT1F receptor agonists, are neurally active acute treatments of migraine with no vasoconstrictor liability. One is currently available, lasmiditan, which was more effective than placebo at 2 hours on pain-free and the most bothersome symptom endpoints.28,29 Dizziness occurs in about 15% of patients.30 Ditans offer an effective and safer option in patients in whom one is concerned about triptans use.
Safety profile of lasmiditan in patients with migraine in an Asian population
Published in Expert Opinion on Drug Safety, 2023
Koichi Hirata, Yasuhiko Matsumori, Yuka Tanji, Rashna Khanna, Akichika Ozeki, Mika Komori
Lasmiditan is an acute treatment for migraine with a novel mechanism of action. As a centrally penetrant, high-affinity and highly selective 5-HT1F receptor agonist, lasmiditan acts on the trigeminal system to suppress hyperactivation of trigeminal neurons and inhibits neurotransmitter release without causing vasoconstriction [12,13]. Lasmiditan has been studied in four global phase 3 studies [14–17] and is approved as an oral acute treatment for migraine in the United States. Consistent with these studies, findings from a randomized, double-blind, placebo-controlled phase 2 trial (MONONOFU) showed that, in general, lasmiditan is a well-tolerated and effective acute treatment for migraine in Japan [18]. Although the types of treatment-emergent adverse events (TEAEs) reported in the MONONOFU study were similar to those in the global studies, the incidence of TEAEs in the 100-mg and 200-mg lasmiditan treatment groups in Japanese patients appeared to be higher than in non-Japanese patients enrolled in phase 3 studies [17–19].
Are 5-HT1 receptor agonists effective anti-migraine drugs?
Published in Expert Opinion on Pharmacotherapy, 2021
Masaru Tanaka, Nóra Török, László Vécsei
Another target for the treatment of migraine is the 5-HT1F receptor expressed centrally in the cortex, the hypothalamus, the trigeminal ganglia, the locus coeruleus, the middle cerebral artery, and the upper cervical cord. The 5-HT1F receptor is also expressed peripherally, but the expression is low in the coronary artery and absent in the heart. Lasmiditan is the first clinically approved drug of the pyridine/piperidine-containing ditans which have a high affinity for 5-HT1F receptors (Figure 1). Lasmiditan does not cause vasoconstriction. The precise mechanism of action is unknown, but the high selectivity for 5-HT1F receptors successfully terminates migraine by inhibiting the release of CGRP and probably substance P from the peripheral trigeminal endings in the dura and centrally acting in the trigeminal nucleus caudalis or the thalamus (Table 1 and Table 2) [5]. Drowsiness, dizziness, tiredness, and numbness or tingling of the skin or mouth are main side effects of Lasmiditan.
Effect of a change in lasmiditan dose on efficacy and safety in patients with migraine
Published in Postgraduate Medicine, 2021
David B. Clemow, Helen M. Hochstetler, Yan Dong, Paula Hauck, Mario F. P. Peres, Jessica Ailani
In the current analyses, increasing the subsequent dose improved the rate of pain freedom, migraine-related functional disability freedom, MBS freedom, and pain relief. While mean differences were small and generally not statistically significant, the trends in these exploratory analyses were consistent and suggestive of a positive efficacy-TEAE balance when increasing lasmiditan dose over time. For example, if a patient took 50 mg and then 100 or 200 mg, they had a greater chance of efficacy as well as an increased chance at having ≥1 MC-TEAE; however, the efficacy-TEAE balance was positive. For patients who started on 50 mg for treatment of their first attack and then switched to 200 mg for treatment of their second attack, the increase in incidence of pain relief was 2.6-fold greater than the increase of ≥1 MC-TEAE. Increasing an initial lasmiditan dose from 50 or 100 mg to 200 mg for future migraine attacks may be beneficial to maximize the patients’ chance at pain freedom, while still providing a tolerable safety profile. If tolerability is not adequate, waiting to increase the dose may be a preferred option. This conclusion is supported with data showing that lasmiditan efficacy is maintained over multiple-treated migraine attacks while the likelihood of having a MC-TEAE goes down [16,18].