Peringatan Keamanan

Data regarding overdose of lasmiditan is currently unavailable. Non-clinical murine toxicology studies revealed no evidence of carcinogenesis, mutagenesis, or impairment of fertilityL9338 at plasma concentrations well above those seen in humans.

Lasmiditan

DB11732

small molecule approved investigational

Deskripsi

Lasmiditan is an oral medication used in the termination of migraine headaches that was first approved for use in the United States in October 2019.L9338,L9356 It was also approved by the European Commission on August 17, 2022.L43997

Traditionally, the triptan class of anti-migraine medications (e.g. sumatriptan) have seen preferential use in the acute treatment of migraines due to their relatively favourable efficacy and safety. Their use is not devoid of concerns, however, and their vasoconstrictive activity can lead to blood pressure lability and other cardiovascular side effects - for this reason, these medications are less suitable for use in patients with pre-existing cardiovascular disorders.A187316 Triptans abort migraines via action at several serotonin receptors, including 5-HT1D and 5-HT1B receptors, and activity at the 5-HT1B receptor has been specifically implicated in their vasoconstrictive activity.A187316,A187322

Lasmiditan, in contrast, is a highly selective agonist of 5-HT1F receptors, carrying virtually no affinity for other receptors which appear to be largely responsible for the adverse effect profile of its predecessors - in other words, lasmiditan’s selectivity allows for the successful termination of migraines without causing vasoconstriction.A187322,A187319 Selectivity for 5-HT1F, a lack of vasoconstrictive activity, and the ability to terminate migraines through neuronal inhibition has resulted in the creation of a new class of anti-migraine medications in which lasmiditan is the first and only member: the neurally-acting anti-migraine medications (NAAMAs).A187322,A187307

Struktur Molekul 2D

Berat 377.367
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life of lasmiditan is 5.7 hours.[L9338]
Volume Distribusi Lasmiditan has been shown to penetrate the blood-brain barrier.[A187307]
Klirens (Clearance) -

Absorpsi

Oral absorption of lasmiditan is quick, with a median tmax of 1.8 hours.L9338 An open-label study looking at absorption pharmacokinetics found the Cmax and AUC0-t of lasmiditan following oral administration to be 322.8 ± 122.0 ng/mL and 1892 ± 746.0 ng.h/mL, respectively.A187307 The oral bioavailability of lasmiditan has been reported as approximately 40%.A187316 Co-administration of lasmiditan with a high-fat meal increased its Cmax and AUC by 22% and 19%, respectively, and delayed Tmax by approximately 1 hour - these differences in absorption are relatively minor and unlikely to be clinically significant.L9338 Similarly, severe renal impairment and mild-moderate hepatic impairment were found to increase both AUC and Cmax, but not to a clinically significant extent.L9338

Metabolisme

The hepatic and extra-hepatic metabolism of lasmiditan is catalyzed primarily by non-CYP enzymes, with ketone reduction appearing to be the primary pathway.L9338 While the specific enzymes involved in the metabolism of lasmiditan have not been elucidated, FDA labeling states that the following enzymes are not involved in its metabolism: monoamine oxidases, CYP450 reductase, xanthine oxidase, alcohol dehydrogenase, aldehyde dehydrogenase, and aldo-keto reductases.L9338 The metabolites of lasmiditan have not been characterized in published research, but two of its metabolites (M7 and M18) are considered to be pharmacologically inactive.L9338

Rute Eliminasi

Lasmiditan is eliminated primarily via metabolism,L9338 with renal excretion accounting for a small fraction of its total elimination. Of the small amount of drug found in the urine post-dose, approximately 66% is comprised of lasmiditan's S-M8 metabolite. Only 3% of an administered dose of lasmiditan was recovered unchanged in the urine,L9338 further implying a relatively extensive metabolism of this drug.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Interaksi Obat

1066 Data
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Lasmiditan.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Lasmiditan.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Lasmiditan.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Lasmiditan.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Lasmiditan.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Lasmiditan.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Lasmiditan.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Lasmiditan.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Lasmiditan.
Silodosin The excretion of Silodosin can be decreased when combined with Lasmiditan.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Lasmiditan.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Lasmiditan.
Mirtazapine The risk or severity of serotonin syndrome can be increased when Lasmiditan is combined with Mirtazapine.
Methylene blue Lasmiditan may increase the serotonergic activities of Methylene blue.
Lumacaftor The serum concentration of Lasmiditan can be decreased when it is combined with Lumacaftor.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Lasmiditan.
Vemurafenib The serum concentration of Lasmiditan can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Lasmiditan can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Lasmiditan can be increased when it is combined with Pitolisant.
Isavuconazole The serum concentration of Lasmiditan can be increased when it is combined with Isavuconazole.
Isavuconazonium The serum concentration of Lasmiditan can be increased when it is combined with Isavuconazonium.
Fluconazole The serum concentration of Lasmiditan can be increased when it is combined with Fluconazole.
Mifepristone The serum concentration of Lasmiditan can be increased when it is combined with Mifepristone.
Conivaptan The serum concentration of Lasmiditan can be increased when it is combined with Conivaptan.
Lapatinib The serum concentration of Lasmiditan can be increased when it is combined with Lapatinib.
Lopinavir The serum concentration of Lasmiditan can be increased when it is combined with Lopinavir.
Biricodar The serum concentration of Lasmiditan can be increased when it is combined with Biricodar.
Elacridar The serum concentration of Lasmiditan can be increased when it is combined with Elacridar.
Vandetanib The serum concentration of Lasmiditan can be increased when it is combined with Vandetanib.
Zosuquidar The serum concentration of Lasmiditan can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Lasmiditan can be increased when it is combined with Tariquidar.
Brefeldin A The serum concentration of Lasmiditan can be increased when it is combined with Brefeldin A.
Ivacaftor The serum concentration of Lasmiditan can be increased when it is combined with Ivacaftor.
Lomitapide The serum concentration of Lasmiditan can be increased when it is combined with Lomitapide.
Vorapaxar The serum concentration of Lasmiditan can be increased when it is combined with Vorapaxar.
Netupitant The serum concentration of Lasmiditan can be increased when it is combined with Netupitant.
Cobicistat The serum concentration of Lasmiditan can be increased when it is combined with Cobicistat.
Daclatasvir The serum concentration of Lasmiditan can be increased when it is combined with Daclatasvir.
Rolapitant The serum concentration of Lasmiditan can be increased when it is combined with Rolapitant.
Istradefylline The serum concentration of Lasmiditan can be increased when it is combined with Istradefylline.
Neratinib The serum concentration of Lasmiditan can be increased when it is combined with Neratinib.
Sarecycline The serum concentration of Lasmiditan can be increased when it is combined with Sarecycline.
Laniquidar The serum concentration of Lasmiditan can be increased when it is combined with Laniquidar.
ONT-093 The serum concentration of Lasmiditan can be increased when it is combined with ONT-093.
Norgestimate The serum concentration of Lasmiditan can be increased when it is combined with Norgestimate.
Erythromycin The serum concentration of Lasmiditan can be increased when it is combined with Erythromycin.
Tacrolimus The serum concentration of Lasmiditan can be increased when it is combined with Tacrolimus.
Ketoconazole The serum concentration of Lasmiditan can be increased when it is combined with Ketoconazole.
Itraconazole The serum concentration of Lasmiditan can be increased when it is combined with Itraconazole.
Clarithromycin The serum concentration of Lasmiditan can be increased when it is combined with Clarithromycin.
Entrectinib The serum concentration of Lasmiditan can be increased when it is combined with Entrectinib.
Asunaprevir The serum concentration of Lasmiditan can be increased when it is combined with Asunaprevir.
Favipiravir The serum concentration of Lasmiditan can be increased when it is combined with Favipiravir.
Lonafarnib The serum concentration of Lasmiditan can be increased when it is combined with Lonafarnib.
Clofazimine The serum concentration of Lasmiditan can be increased when it is combined with Clofazimine.
Arsenic trioxide The serum concentration of Lasmiditan can be increased when it is combined with Arsenic trioxide.
Ixabepilone The serum concentration of Lasmiditan can be increased when it is combined with Ixabepilone.
Eliglustat The serum concentration of Lasmiditan can be increased when it is combined with Eliglustat.
Umbralisib The serum concentration of Lasmiditan can be increased when it is combined with Umbralisib.
Diosmin The serum concentration of Lasmiditan can be increased when it is combined with Diosmin.
Sapropterin The serum concentration of Lasmiditan can be increased when it is combined with Sapropterin.
Levoketoconazole The serum concentration of Lasmiditan can be increased when it is combined with Levoketoconazole.
Capmatinib The serum concentration of Lasmiditan can be increased when it is combined with Capmatinib.
Belumosudil The serum concentration of Lasmiditan can be increased when it is combined with Belumosudil.
Dabigatran etexilate The serum concentration of Dabigatran etexilate can be increased when it is combined with Lasmiditan.
Carfilzomib The serum concentration of Carfilzomib can be increased when it is combined with Lasmiditan.
Bendamustine The serum concentration of Bendamustine can be increased when it is combined with Lasmiditan.
Binimetinib The serum concentration of Binimetinib can be increased when it is combined with Lasmiditan.
Axitinib The serum concentration of Axitinib can be increased when it is combined with Lasmiditan.
Erdafitinib The serum concentration of Lasmiditan can be increased when it is combined with Erdafitinib.
Metildigoxin Lasmiditan may decrease the excretion rate of Metildigoxin which could result in a higher serum level.
Acetyldigoxin Lasmiditan may decrease the excretion rate of Acetyldigoxin which could result in a higher serum level.
Hydrocodone Lasmiditan may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Trazodone The risk or severity of serotonin syndrome can be increased when Trazodone is combined with Lasmiditan.
Lefamulin Lasmiditan may decrease the excretion rate of Lefamulin which could result in a higher serum level.
Escitalopram The risk or severity of serotonin syndrome can be increased when Lasmiditan is combined with Escitalopram.
Droperidol The risk or severity of adverse effects can be increased when Lasmiditan is combined with Droperidol.
Orphenadrine The risk or severity of adverse effects can be increased when Lasmiditan is combined with Orphenadrine.
Paraldehyde The risk or severity of adverse effects can be increased when Lasmiditan is combined with Paraldehyde.
Perampanel The risk or severity of adverse effects can be increased when Lasmiditan is combined with Perampanel.
Rufinamide The risk or severity of adverse effects can be increased when Lasmiditan is combined with Rufinamide.
Sodium oxybate Lasmiditan may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Brimonidine The risk or severity of adverse effects can be increased when Lasmiditan is combined with Brimonidine.
Seproxetine The risk or severity of adverse effects can be increased when Lasmiditan is combined with Seproxetine.
Zopiclone The risk or severity of adverse effects can be increased when Lasmiditan is combined with Zopiclone.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Lasmiditan is combined with Botulinum toxin type B.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Lasmiditan is combined with Botulinum toxin type A.
Baclofen The risk or severity of adverse effects can be increased when Lasmiditan is combined with Baclofen.
Lorazepam The risk or severity of adverse effects can be increased when Lasmiditan is combined with Lorazepam.
Ethchlorvynol The risk or severity of adverse effects can be increased when Lasmiditan is combined with Ethchlorvynol.
Succinylcholine The risk or severity of adverse effects can be increased when Lasmiditan is combined with Succinylcholine.
Enflurane The risk or severity of adverse effects can be increased when Lasmiditan is combined with Enflurane.
Temazepam The risk or severity of adverse effects can be increased when Lasmiditan is combined with Temazepam.
Reboxetine The risk or severity of adverse effects can be increased when Lasmiditan is combined with Reboxetine.
Butabarbital The risk or severity of adverse effects can be increased when Lasmiditan is combined with Butabarbital.
Butalbital The risk or severity of adverse effects can be increased when Lasmiditan is combined with Butalbital.
Methysergide The risk or severity of adverse effects can be increased when Lasmiditan is combined with Methysergide.
Clemastine The risk or severity of adverse effects can be increased when Lasmiditan is combined with Clemastine.
Etomidate The risk or severity of adverse effects can be increased when Lasmiditan is combined with Etomidate.
Talbutal The risk or severity of adverse effects can be increased when Lasmiditan is combined with Talbutal.

Target Protein

5-hydroxytryptamine receptor 1F HTR1F

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28076702
    Capi M, de Andres F, Lionetto L, Gentile G, Cipolla F, Negro A, Borro M, Martelletti P, Curto M: Lasmiditan for the treatment of migraine. Expert Opin Investig Drugs. 2017 Feb;26(2):227-234. doi: 10.1080/13543784.2017.1280457.
  • PMID: 20855361
    Nelson DL, Phebus LA, Johnson KW, Wainscott DB, Cohen ML, Calligaro DO, Xu YC: Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. Cephalalgia. 2010 Oct;30(10):1159-69. doi: 10.1177/0333102410370873. Epub 2010 Jun 15.
  • PMID: 30714429
    Lupi C, Benemei S, Guerzoni S, Pellesi L, Negro A: Pharmacokinetics and pharmacodynamics of new acute treatments for migraine. Expert Opin Drug Metab Toxicol. 2019 Mar;15(3):189-198. doi: 10.1080/17425255.2019.1578749. Epub 2019 Feb 12.
  • PMID: 29488143
    Vila-Pueyo M: Targeted 5-HT1F Therapies for Migraine. Neurotherapeutics. 2018 Apr;15(2):291-303. doi: 10.1007/s13311-018-0615-6.
  • PMID: 31418454
    Rubio-Beltran E, Labastida-Ramirez A, Haanes KA, van den Bogaerdt A, Bogers AJJC, Zanelli E, Meeus L, Danser AHJ, Gralinski MR, Senese PB, Johnson KW, Kovalchin J, Villalon CM, MaassenVanDenBrink A: Characterization of binding, functional activity and contractile responses of the selective 5-HT1F receptor agonist lasmiditan. Br J Pharmacol. 2019 Aug 16. doi: 10.1111/bph.14832.
  • PMID: 25584073
    Reuter U, Israel H, Neeb L: The pharmacological profile and clinical prospects of the oral 5-HT1F receptor agonist lasmiditan in the acute treatment of migraine. Ther Adv Neurol Disord. 2015 Jan;8(1):46-54. doi: 10.1177/1756285614562419.

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