lasmiditan
Brand: Reyvow
Prototype Drug
Drug Class: serotonin 5-HT1F receptor agonist (ditan)
Drug Family: antimigraine
Subclass: first-in-class ditan
Organ Systems: cns
Mechanism of Action
Highly selective 5-HT1F receptor agonist; unlike triptans, it has no 5-HT1B activity (no vasoconstriction) and no clinically significant 5-HT1D activity. 5-HT1F receptors are expressed on trigeminal neurons; inhibiting trigeminal activation aborts migraine without vascular effects.
5-HT1F receptor
Indications
- acute migraine with or without aura
Contraindications
- no absolute contraindications related to cardiovascular disease (unlike triptans)
Adverse Effects
Common
- dizziness
- somnolence
- paresthesia
- fatigue
- nausea
Serious
- CNS depression (driving impairment for 8 hours after dose)
- serotonin syndrome (theoretical with serotonergic drugs)
- Schedule V controlled substance (abuse potential)
Pharmacokinetics (ADME)
| Absorption | oral; bioavailability ~40%; food delays but does not reduce absorption |
| Distribution | protein binding ~55-60% |
| Metabolism | hepatic; multiple CYP and non-CYP pathways |
| Excretion | renal (~74%) |
| Half-life | 5.7 hours |
| Onset | 1-2 hours |
| Peak | 1.8 hours |
| Duration | 24 hours (once per migraine attack) |
| Protein Binding | 55-60% |
| Vd | not well characterized |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| P-glycoprotein inhibitors | increase lasmiditan exposure | moderate |
| serotonergic agents | theoretical serotonin syndrome risk | moderate |
| CNS depressants | additive CNS depression; driving impairment | moderate |
Nursing Considerations
- Patients must not drive or operate heavy machinery for at least 8 hours after lasmiditan administration due to CNS impairment risk.
- Does not cause vasoconstriction; can be used in migraine patients with cardiovascular contraindications to triptans.
- Schedule V controlled substance; diversion and abuse screening per PDMP as with other controlled substances.
- Maximum 1 dose per 24 hours; do not use more than 1 lasmiditan dose per migraine attack.
Clinical Pearls
- Lasmiditan represents the first mechanistically distinct acute migraine therapy in decades; its lack of vasoconstriction via 5-HT1F selectivity opens triptan-type acute treatment to patients with cardiovascular contraindications.
- The drivability restriction (8 hours) significantly affects patient lifestyle compared to triptans; this pharmacodynamic property must be incorporated into patient counseling and medication selection.
Safety Profile
Pregnancy avoid
Lactation avoid
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Guideline Update pending
Concordance Terms
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