REYVOW
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REYVOW (REYVOW).
Selective serotonin 1F (5-HT1F) receptor agonist; modulates trigeminal nerve activity and reduces release of vasoactive neuropeptides.
| Metabolism | Primarily metabolized by CYP3A4 and CYP2D6; minor contributions from CYP1A2 and CYP2C9. |
| Excretion | Primarily hepatic metabolism via CYP3A4; renal excretion accounts for <2% of unchanged drug; fecal excretion is minimal. Approximately 50% of the dose is eliminated as metabolites in urine and 50% in feces. |
| Half-life | Terminal elimination half-life is approximately 7 hours. In clinical context, this supports a twice-daily dosing regimen to maintain therapeutic levels. |
| Protein binding | Approximately 95% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 50 L (0.7 L/kg for a 70 kg adult), indicating moderate tissue distribution beyond plasma. |
| Bioavailability | Oral bioavailability is approximately 40–60% when taken as the 50 mg capsule, with lower bioavailability at higher doses due to saturation of absorption. |
| Onset of Action | For the 50 mg capsule, onset of pain relief is observed within 1 hour, with peak plasma concentrations reached at 1.5–2 hours. For the same dose, significant headache response occurs at 2 hours post-dose. |
| Duration of Action | Duration of clinical effect is approximately 24 hours per dose for acute migraine treatment. Pain-freedom and sustained pain-free responses are maintained for up to 48 hours in clinical trials. Multiple doses are not recommended within 24 hours. |
50 mg orally once, may repeat once after at least 2 hours; maximum 100 mg per 24 hours.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment; not studied in severe renal impairment (eGFR <30 mL/min) or ESRD. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: use is not recommended; Child-Pugh C: contraindicated. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment; consider lower starting dose due to increased sensitivity and comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REYVOW (REYVOW).
| Breastfeeding | No data on presence in human milk; lasmiditan is lipophilic and likely excreted. M/P ratio unknown. Consider risk of infant sedation and withdrawal. Avoid breastfeeding for at least 8 hours after dose, or discontinue drug or nursing. |
| Teratogenic Risk | Pregnancy Category C; no adequate studies in pregnant women. In animal studies, lasmiditan (active metabolite) caused developmental toxicity (reduced fetal weight, skeletal variations) at doses similar to human exposure. Risk cannot be ruled out; use only if benefit justifies potential risk. First trimester: potential for teratogenicity unknown. Second/third trimester: may cause fetal CNS depression or withdrawal if used chronically. |
■ FDA Black Box Warning
No FDA-required black box warning.
| Serious Effects |
["Concomitant use with monoamine oxidase inhibitors (MAOIs)","Use within 24 hours of another 5-HT1F agonist or ergotamine","Severe hepatic impairment"]
| Precautions | ["Serotonin syndrome (especially with concomitant serotonergic drugs)","Hypersensitivity reactions (angioedema, rash)","Avoid use in patients with hepatic impairment","Potential for drug interactions with CYP3A4 and CYP2D6 inhibitors/inducers"] |
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| Fetal Monitoring | Monitor maternal blood pressure and heart rate; lasmiditan may cause bradycardia or hypotension. Assess fetal heart rate during labor if used near term for potential CNS depression. No specific fetal monitoring required otherwise. |
| Fertility Effects | No human data; animal studies showed no impairment of fertility at exposures up to 30 times human exposure. Potential for dizziness and somnolence may impair sexual function transiently. |