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 |
| Molecular Weight | 432.47 |
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 | Avoid due to limited safety data; potential teratogenic effects in animal studies. |
| 2nd trimester | Use only if clearly needed; no well-controlled studies. |
| 3rd trimester | Avoid near term due to risk of neonatal withdrawal or respiratory depression. |
Clinical note
Comprehensive clinical and safety monograph for DOXY-SLEEP-AID (DOXY-SLEEP-AID).
| Placental transfer | Crosses placenta; evidence based on detection in fetal plasma. |
| Breastfeeding | Excreted in breast milk in low amounts; potential for infant drowsiness. Caution advised, especially with prolonged use. |
| Lactation Rating | L3 (Moderately Safe) |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to doxylamine or any componentAsthma attackNarrow-angle glaucomaStenosing peptic ulcerBladder neck obstructionConcurrent MAO inhibitor therapy
| 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 |
| Food/Dietary | Avoid alcohol and grapefruit juice. Alcohol may enhance the sedative effects of doxylamine. Grapefruit juice may inhibit CYP2D6, although doxylamine is primarily metabolized by CYP1A2 and CYP2C9; clinical relevance is minimal but caution advised. No other significant food interactions documented. |
Loading safety data…
| 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). |
| 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. |
| Clinical Pearls | Doxy-sleep-aid is a fixed-dose combination of doxylamine succinate, an antihistamine with sedative properties, and a sleep aid. It is indicated for short-term management of insomnia. Onset of action is approximately 30 minutes; avoid administration with alcohol or CNS depressants. Anticholinergic effects may be pronounced in elderly patients, increasing risk of confusion, urinary retention, and falls. Use with caution in patients with narrow-angle glaucoma, benign prostatic hyperplasia, or asthma. Tolerance to sedative effects may develop after 2 weeks of continuous use; limit therapy to 7-10 days. Do not use in children under 12 years. |
| Patient Advice | Take this medication 30 minutes before bedtime, only when you have at least 7-8 hours to dedicate to sleep. · Do not take more than the recommended dose; do not take this medication for more than 10 days without consulting a doctor. · Avoid alcohol and other CNS depressants (e.g., benzodiazepines, opioids) while taking this medication. · Do not drive or operate heavy machinery until you know how this medication affects you, as it may cause drowsiness the next day. · Inform your healthcare provider if you have glaucoma, difficulty urinating, or chronic lung disease. · Common side effects include dry mouth, blurred vision, and constipation. If you experience rapid heartbeat or confusion, seek medical attention. · Store at room temperature away from moisture and heat. |