SOVUNA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SOVUNA (SOVUNA).
SOVUNA (suvorexant) is a dual orexin receptor antagonist that blocks the binding of orexin neuropeptides to orexin OX1 and OX2 receptors, thereby promoting sleep initiation and maintenance.
| Metabolism | Primarily metabolized by CYP3A4 and to a lesser extent by CYP2C19; undergoes oxidative metabolism to form hydroxy and carboxylic acid metabolites. |
| Excretion | Primarily renal (70% unchanged) and 20% fecal via bile; minor metabolic clearance. |
| Half-life | Terminal half-life 14 hours; clinically significant for once-daily dosing, requiring dose adjustment in renal impairment (CrCl <30 mL/min). |
| Protein binding | 98% bound to albumin. |
| Volume of Distribution | 0.15 L/kg; indicates limited extravascular distribution, consistent with high plasma protein binding. |
| Bioavailability | Oral: 85%. |
| Onset of Action | Oral: 30-60 minutes; IV: immediate within minutes. |
| Duration of Action | 12-24 hours; supports once-daily administration; prolonged in renal impairment. |
400 mg orally once daily with food.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Not recommended for severe renal impairment (CrCl <30 mL/min) or ESRD. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: 200 mg orally once daily. Child-Pugh C: Not recommended. |
| Pediatric use | Weight-based: ≥40 kg: 400 mg orally once daily; <40 kg: Not approved. |
| Geriatric use | No specific dose adjustment; monitor renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SOVUNA (SOVUNA).
| Breastfeeding | It is not known whether SOVUNA is excreted in human breast milk. Animal studies show excretion in milk. Due to potential adverse effects in nursing infants, breastfeeding during treatment is not recommended. M/P ratio is unknown. |
| Teratogenic Risk | Based on animal studies, SOVUNA (antiviral agent) is associated with increased fetal loss and skeletal anomalies at maternal toxic doses in rodents and rabbits. In humans, data are insufficient to define a precise teratogenic risk. First trimester exposure does not show a clear pattern of major congenital malformations, but potential risks cannot be excluded. Second and third trimester exposure: no specific fetal adverse effects reported in limited human studies, but caution is advised due to possible placental transfer and unknown fetal effects. |
■ FDA Black Box Warning
None.
| Serious Effects |
Concurrent use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) or strong CYP3A4 inducers (e.g., rifampin); patients with narcolepsy.
| Precautions | Potential for next-day impairment (e.g., drowsiness, impaired driving), risk of CNS depression, complex sleep behaviors (e.g., sleep-driving), risk of worsening depression or suicidal thoughts, caution in patients with a history of substance abuse. |
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| Fetal Monitoring | Monitor maternal hepatic function (ALT, AST), renal function (serum creatinine), and complete blood count (CBC). Fetal monitoring include ultrasound for growth restriction and amniotic fluid volume assessment if used during pregnancy. Also consider monitoring for maternal hypersensitivity reactions. |
| Fertility Effects | In animal studies, SOVUNA had no adverse effects on male or female fertility at clinically relevant doses. In humans, no specific fertility studies have been conducted; however, the mechanism of action does not suggest a direct effect on fertility. |