Dosing & Uses
Dosage Forms & Strengths
tablet
- 50mg
- 100mg
Acute Migraine
Indicated for treatment of acute migraine with or without aura
50 mg, 100 mg, or 200 mg PO PRN
Not to exceed more than 1 dose/24 hr
Do not take unless patient can wait at least 8 hr between dosing and driving or operating machinery
Second dose has not been shown to be effective for the same migraine attack
The safety of treating an average of >4 migraine attacks/30 days has not been established
Dosage Modifications
Renal impairment
- No dosage adjustment needed for any degree of renal impairment
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dosage adjustment needed
- Severe (Child-Pugh C): Not recommended
Dosing Considerations
Limitations of use
- Not indicated for prevention of migraine
Safety and efficacy not established
Acute Migraine
Indicated for treatment of acute migraine with or without aura
50 mg, 100 mg, or 200 mg PO PRN; initiate at lower end of dosage range for geriatric patients
Not to exceed more than 1 dose/24 hr
Do not take unless patient can wait at least 8 hr between dosing and driving or operating machinery
Second dose has not been shown to be effective for the same migraine attack
The safety of treating an average of >4 migraine attacks/30 days has not been established
Dosage Modifications
Renal impairment
- No dosage adjustment needed for any degree of renal impairment
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dosage adjustment needed
- Severe (Child-Pugh C): Not recommended
Dosing Considerations
Generally start dose at low end of dosing range for geriatric patients
Dizziness occurred more frequently in patients aged >65 yr (19% vs 2% for placebo) compared with patients aged <65 yr (14% vs 3% for placebo)
A larger increase in systolic blood pressure also occurred in patients aged >65 yr compared with those aged <65 yr
Limitations of use
- Not indicated for prevention of migraine
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
Dizziness (9-17%)
1-10%
Paresthesia (3-9%)
Sedation (6-7%)
Fatigue (4-6%)
Nausea and/or vomiting (3-4%)
Muscle weakness (1-2%)
<2%
- Vertigo
- Incoordination
- Lethargy
- Visual impairment
- Feeling abnormal
- Palpitations
- Anxiety
- Tremor
- Restlessness
- Sleep abnormalities (eg, sleep disturbance, abnormal dreams)
- Muscle spasm
- Limb discomfort
- Cognitive changes
- Confusion
- Euphoric mood
- Chest discomfort
- Speech abnormalities
- Dyspnea
- Hallucinations
<1%
Hypersensitivity (eg, angioedema, rash, photosensitivity reaction)
Warnings
Contraindications
None
Cautions
Significant driving impairment may occur; advise patients not to engage in potentially hazardous activities requiring complete mental alertness eg, driving a motor vehicle, operating machinery) for at least 8 hr after each dose; avoid use in patients who are unable to follow this advice
Reactions consistent with serotonin syndrome reported; discontinue if symptoms of serotonin syndrome occur
CNS depression (eg, dizziness, sedation) reported
Overuse of acute migraine drugs (eg, ergotamines, triptans, opioids, or a combination of these drugs for ≥10 per month) may lead to exacerbation of headache (ie, medication overuse headache); may present as migrainelike daily headaches or as a marked increase in frequency of migraine attacks; detoxification and treatment of withdrawal symptoms (which often includes a transient worsening of headache) may be necessary
Drug interaction overview
- Lasmiditan inhibits P-gp and breast cancer-resistant protein (BCRP); avoid coadministration
- Owing to the potential for sedation, other cognitive and/or neuropsychiatric adverse reactions, and driving impairment, use with caution if used in combination with alcohol or other CNS depressants
- Coadministration of lasmiditan and drugs (eg, SSRIs, SNRIs, TCAs, MAO inhibitors, trazodone), over-the-counter medications (eg, dextromethorphan), or herbal supplements (eg, St. John’s wort) that increase serotonin may increase the risk of serotonin syndrome; use with caution in patients taking medications that increase serotonin.
- In a drug interaction study, addition of a single lasmiditan 200-mg dose to propranolol decreased heart rate by an additional 5 bpm compared with propranolol alone, for a mean maximum of 19 bpm; use with caution in patients taking concomitant medications that lower heart rate
Pregnancy & Lactation
Pregnancy
No adequate data are available on the developmental risk associated with use in pregnant women
Clinical considerations
- Data suggest women with migraine may be at increased risk for preeclampsia and gestational hypertension during pregnancy
Animal data
- In animal studies, adverse effects on development (increased incidences of fetal abnormalities, increased embryofetal and offspring mortality, decreased fetal body weight) occurred at maternal exposures less than (rabbit) or greater than (rat) those observed clinically
Lactation
There are no data on the presence in human milk, effects on breastfed infants, or effects on milk production
Excretion of lasmiditan and/or metabolites into milk, at levels ~3 times those in maternal plasma, was observed in lactating rats following oral administration
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Lasmiditan binds with high affinity to the 5-HT1F receptor; it presumably exerts its therapeutic effects for acute migraine through agonist effects at the 5-HT1F receptor; however, the precise mechanism is unknown
Serotonin 5-HT1F agonists (ie, ditans) do not elicit a vasoconstrictive effect
Absorption
Peak plasma time: 1.8 hr
Distribution
Protein bound: 55-60%
Metabolism
Undergoes hepatic and extrahepatic metabolism primarily by non-CYP enzymes
Also metabolized to M7 (oxidation on piperidine ring) and M18 (combination of M7 and M8 pathways); these metabolites are considered pharmacologically inactive
Elimination
Half-life: 5.7 hr
Primarily eliminated via metabolism, with ketone reduction representing the major pathway
Excretion: Urine (3% [unchanged], ~66% [metabolite S-M8])
Administration
Oral Administration
May take with or without food
Storage
Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
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Patient Handout
Formulary
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