SUVOREXANT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SUVOREXANT (SUVOREXANT).
Suvorexant is a dual orexin receptor antagonist that inhibits the action of orexin A and orexin B by binding to orexin receptors OX1R and OX2R, thereby promoting sleep initiation and maintenance.
| Metabolism | Primarily metabolized by CYP3A4, with minor contribution from CYP2C19. |
| Excretion | Primarily hepatic metabolism via CYP3A4 and CYP2C19; minimal renal excretion (approximately 2% as unchanged drug in urine) |
| Half-life | Terminal half-life approximately 12.2 hours; supports once-daily dosing at bedtime |
| Protein binding | ~99% bound primarily to serum albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | Approximately 0.5 L/kg (about 40 L); indicates moderate tissue distribution |
| Bioavailability | Oral bioavailability is approximately 82%; unaffected by food |
| Onset of Action | Oral: Sleep initiation within 30-60 minutes post-dose |
| Duration of Action | Approximately 7-8 hours; maintains sleep maintenance without significant next-day residual effects |
10 mg orally once nightly, within 30 minutes of bedtime; maximum dose 20 mg.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not recommended in severe renal impairment (CrCl <30 mL/min) due to lack of data. |
| Liver impairment | Mild hepatic impairment (Child-Pugh A): no adjustment. Moderate hepatic impairment (Child-Pugh B): maximum 10 mg. Severe hepatic impairment (Child-Pugh C): not recommended. |
| Pediatric use | Safety and efficacy not established in pediatric patients (<18 years); no recommended dosing. |
| Geriatric use | No specific dose adjustment required based on age alone; however, monitor for increased sensitivity and postural instability. Start at 10 mg; may increase to 20 mg if tolerated. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SUVOREXANT (SUVOREXANT).
| Breastfeeding | Unknown if excreted in human milk; M/P ratio not available. Caution recommended due to potential CNS effects in nursing infants. Consider alternative therapies or discontinue breastfeeding. |
| Teratogenic Risk | Pregnancy Category C. Limited human data; animal studies show no teratogenicity at clinically relevant doses but increased fetal resorption at high doses. Risk cannot be ruled out. First trimester: advise caution; second and third trimesters: insufficient data. Use only if benefit outweighs risk. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Concurrent use with strong CYP3A inhibitors (e.g., ketoconazole, clarithromycin) or strong CYP3A inducers (e.g., rifampin).","Narcolepsy."]
| Precautions | ["May impair daytime wakefulness and cause next-day somnolence (including impaired driving ability).","Worsening of depression or suicidal ideation has been reported; monitor for behavioral changes.","Complex sleep behaviors such as sleepwalking, sleep-driving, and other activities while not fully awake.","Respiratory depression risk in patients with compromised respiratory function (e.g., COPD, sleep apnea).","Use with caution in patients with a history of drug or alcohol abuse.","Higher risk of falls in elderly patients."] |
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| Fetal Monitoring |
| Monitor for maternal sedation, CNS depression, and falls. No specific fetal monitoring required; standard prenatal care. Assess for sleep-related behaviors (e.g., driving, eating) during use. |
| Fertility Effects | No human studies on fertility. In animal studies, no impairment of fertility at doses up to 150 mg/kg/day (21 times MRHD). Effects on human reproductive capacity unknown. |