DAYVIGO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DAYVIGO (DAYVIGO).
Orexin receptor antagonist; blocks the binding of neuropeptides orexin A and orexin B to OX1R and OX2R receptors, promoting sleep initiation and maintenance.
| Metabolism | Primarily metabolized by CYP3A4; minor contribution from CYP2C19 and CYP2D6. |
| Excretion | Fecal (67%) as unchanged drug; renal (32%) as unchanged drug and minor metabolites |
| Half-life | Terminal elimination half-life is approximately 17–19 hours; supports once-daily evening dosing with sustained receptor occupancy |
| Protein binding | 93–94% bound to human serum albumin |
| Volume of Distribution | Approximately 34–56 L (0.4–0.8 L/kg) indicating extensive tissue distribution |
| Bioavailability | Oral: absolute bioavailability is not determined; relative bioavailability is high with rapid absorption (Tmax ~0.5–1 hour) |
| Onset of Action | Oral: 30–60 minutes based on time to sleep initiation in clinical trials |
| Duration of Action | Approximately 8 hours for sleep maintenance; residual effects may last up to 11 hours |
5 mg orally once daily immediately before bedtime; may increase to 10 mg based on efficacy and tolerability.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Not recommended in severe renal impairment (CrCl <30 mL/min). |
| Liver impairment | For mild hepatic impairment (Child-Pugh A): no dose adjustment. For moderate hepatic impairment (Child-Pugh B): 5 mg maximum. Not recommended in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Safety and effectiveness not established in pediatric patients (<18 years). |
| Geriatric use | Elderly patients (≥65 years): 5 mg once daily; dose may be increased to 10 mg if needed, but with caution due to increased sensitivity and fall risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DAYVIGO (DAYVIGO).
| Breastfeeding | Unknown if excreted in human milk; M/P ratio not established. Risk of infant sedation and respiratory depression. Manufacturer recommends discontinuing drug or breastfeeding. |
| Teratogenic Risk | Pregnancy Category C. Second and third trimester: Risk of neonatal respiratory depression, hypotonia, and withdrawal. No adequate human studies; animal studies show fetal harm. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to daridorexant or any excipients","Narcolepsy"]
| Precautions | ["CNS depressant effects: risk of daytime somnolence, impaired driving ability","Worsening of depression or suicidal ideation","Sleep paralysis, hallucinations, and cataplexy-like symptoms","Decreased efficacy in patients taking strong CYP3A4 inducers","Not recommended for use in patients with narcolepsy"] |
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| Monitor maternal vital signs, sedation level. No specific fetal monitoring required but consider growth ultrasound and fetal movement counts if used late in pregnancy. |
| Fertility Effects | No human data on fertility effects. Animal studies show no impairment at clinically relevant doses. |