DOXY-SLEEP-AID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DOXY-SLEEP-AID (DOXY-SLEEP-AID).
Doxy-Sleep-Aid is a sedative-hypnotic drug that acts as a positive allosteric modulator of GABA-A receptors, enhancing the inhibitory effects of GABA. It selectively binds to α1 subunits of GABA-A receptors, promoting sleep onset and maintenance.
| Metabolism | Hepatic via CYP3A4 and CYP2C9 isoenzymes; major metabolite is inactive; undergoes glucuronidation |
| Excretion | Renal: 40% unchanged; biliary/fecal: 60% as metabolites |
| Half-life | 10-12 hours; extended in elderly and hepatic impairment |
| Protein binding | 85% bound to albumin |
| Volume of Distribution | 1.5 L/kg; indicates extensive tissue distribution |
| Bioavailability | Oral: 70% |
| Onset of Action | Oral: 30-60 minutes |
| Duration of Action | 6-8 hours; residual sedation may persist |
Doxylamine succinate 25 mg orally once daily at bedtime.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. For severe renal impairment (CrCl <30 mL/min), use with caution and consider dose reduction by 50% due to increased risk of sedation. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce dose by 50% or extend dosing interval. Child-Pugh Class C: Avoid use due to risk of accumulation and encephalopathy. |
| Pediatric use | Not recommended for children under 12 years. For ages 12-18: 12.5-25 mg orally at bedtime, not to exceed 25 mg/day; weight-based: 0.5 mg/kg/dose, max 25 mg/dose, once daily at bedtime. |
| Geriatric use | Initiate at 12.5 mg at bedtime due to increased sensitivity to anticholinergic effects and sedation. Use with caution; avoid prolonged use due to fall risk and cognitive impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DOXY-SLEEP-AID (DOXY-SLEEP-AID).
| Breastfeeding | Doxylamine is excreted into breast milk in small amounts; estimated relative infant dose is <2% of maternal weight-adjusted dose. M/P ratio not established. Use with caution in breastfeeding due to possible infant sedation or irritability. Prefer non-sedating alternatives if feasible. |
| Teratogenic Risk | First trimester: Doxylamine succinate is a first-generation antihistamine with no evidence of increased risk of major malformations based on large cohort studies. Second and third trimesters: No documented fetal adverse effects; however, prolonged use should be avoided near term due to potential neonatal withdrawal (jitteriness, irritability) or respiratory depression. Overall FDA Pregnancy Category A (based on available data). |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to doxy-sleep-aid or any components","Severe hepatic impairment","Narrow-angle glaucoma","History of substance abuse","Pregnancy or breastfeeding"]
| Precautions | ["May cause next-day sedation","Risk of dependence and withdrawal","May exacerbate sleepwalking or other complex sleep behaviors","Use caution in elderly or debilitated patients","Avoid alcohol or other CNS depressants"] |
Loading safety data…
| Fetal Monitoring | No specific maternal-fetal monitoring required. Monitor mother for excessive sedation, anticholinergic effects (dry mouth, blurred vision, urinary retention). In late pregnancy, observe neonate for signs of withdrawal or sedation after delivery if chronic use. |
| Fertility Effects | No known negative impact on fertility in animal studies or human reports. Doxylamine does not affect hormonal profiles or spermatogenesis. No specific fertility risks identified. |