Lasmiditan

Last updated on: 22.02.2026

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Definition
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Lasmiditan is a new drug for the acute treatment of migraine attacks with or without aura in adults. It is the first representative of a new class of active ingredients, the ditanes. Lasmiditan selectively targets the 5-HT1F receptor and, like triptans, causes vasoconstriction in the blood vessels, but only in the brain and not in the periphery. This makes the drug suitable for migraine patients who are not allowed to use triptans due to cardiovascular disease or who do not respond sufficiently to them. The drug is available as hemisuccinate in the form of film-coated tablets in strengths of 50, 100 and 200 mg.

Pharmacodynamics (Effect)
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Lasmiditan belongs to the Ditane class of active ingredients and was the first representative of this group to be approved. It has a vasoconstrictive effect on the blood vessels in the brain. However, it binds selectively to the 5-HT1F receptor. This means that it does not cause vasoconstriction in the periphery. In contrast to lasmiditan, triptans bind as agonists to the 5-HT1B/5-HT1D subtypes and cause vasoconstriction in the blood vessels in the brain as well as in the peripheral blood vessels.

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Pregnancy/nursing period
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Only limited data are available on the use of Lasmiditan in pregnant women. It is therefore not known what effects Lasmiditan has on the development of the human fetus. It is not recommended to take Lasmiditan during pregnancy.

Lactation: Lasmiditan and/or its metabolites have been found to be excreted in the milk of lactating rats. There are no data on whether lasmiditan is present in human breast milk or what effects it has on the breastfed infant.

Dosage and method of use
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The standard initial dose is 100 mg. If necessary, this can be increased to 200 mg or reduced to 50 mg for better tolerability. No more than 200 mg lasmiditan may be taken within 24 hours.

A second dose of the same strength (50 or 100 mg) may be taken if the headache recurs within 24 hours, but not within two hours of the first dose.

Dose adjustment is not necessary in persons >65 years of age or in persons with renal or hepatic impairment.

Undesirable effects
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The most common adverse events reported were drowsiness, dizziness, fatigue, paraesthesia, nausea, dizziness, hypaesthesia and muscle weakness. Most adverse events showed a dose dependency.

Lasmiditan impairs the ability to drive and operate machinery. This effect can last up to 8 hours.

Interactions
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Patients taking medicines that lower the heart rate should exercise caution when taking Lasmiditan as it has been associated with a decrease in heart rate. Concomitant use of Lasmiditan and serotonergic drugs may increase the risk of serotonin syndrome.

Note(s)
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Lasmiditan and its metabolites are inducers of CYP enzymes.

Treatment alternatives to lasmiditan for acute migraine are:

  • Triptans (e.g. sumatriptan, eletriptan)
  • Ergotamine derivatives (e.g. dihydroergotamine)
  • Non-steroidal anti-inflammatory drugs (e.g. ibuprofen, naproxen)
  • Combinations of triptans and NSAIDs (e.g. sumatriptan/naproxen)
  • Opioid analgesics (e.g. tramadol)
  • Antiemetics (e.g. metoclopramide)
  • Corticosteroids (e.g. dexamethasone)

The choice of suitable medication depends on various factors, such as the severity of the migraine, the presence of accompanying symptoms such as nausea or vomiting, the patient's history and possible contraindications.

Literature
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  1. Lovenberg TW et al. (1993) Molecular cloning and functional expression of rat and human 5-HT1E-like 5-hydroxytryptamine receptor genes. Proceedings of the National Academy of Sciences of the United States of America 90: 2184-2188 .
  2. Erdmann J et al. (1997) Assignment of the human serotonin 1F receptor gene (HTR1F) to the short arm of chromosome 3 (3p13-p14.1). Molecular Membrane Biology. 14 133-135 .
  3. Maassen VanDenBrink A et al. (1998) Chromosomal localization of the 5-HT1F receptor gene: No evidence for involvement in sumatriptan action in migraine patients". American Journal of Medical Genetics 77: 415-420 .
  4. Wainscott DB et al. (2005) [3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties. Naunyn -Schmiedeberg's Archives of Pharmacology 371: 169-177 .

Last updated on: 22.02.2026