Lasmiditan

Products

Lasmiditan was approved in the United States in 2019 in film-coated tablet form (Reyvow).

Structure and properties

Lasmiditan (C19H18F3N3O2, Mr = 377.4 g/mol) is present in the drug as lasmiditanhemisuccinate, a white crystalline powder that is sparingly soluble in water. It is a piperidine and pyridine derivative and has no indole structure.

Effects

Lasmiditan binds with high affinity as an agonist to the 5-HT1F receptor, a serotonin receptor subtype and GPCR. It has little or no effect on the vasculature, unlike the triptans. The half-life is in the range of 5.7 hours.

Indications

For acute treatment of migraine with or without aura.

Dosage

According to the SmPC. Tablets are taken once a day as needed, regardless of meals.

Abuse

Due to the depressant properties, abuse cannot be ruled out. Rarely, euphoria also occurs after ingestion.

Contraindications

For complete precautions, see the drug label.

Interactions

Interactions have been described with central depressant drugs, serotonergic agents (risk for serotonin syndrome), and drugs that lower heart rate. Lasmiditan is an inhibitor of P-glycoprotein and BCRP. In contrast, it does not interact with CYP450 isoenzymes.

Adverse effects

The most common potential adverse effects include dizziness, fatigue, sensory disturbances, and dullness. Because of these side effects, responsiveness is impaired. Driving should be avoided after taking the medication. The profile is different from painkillers (NSAIDs), which can cause organ damage.