DORMATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DORMATE (DORMATE).
Gamma-aminobutyric acid (GABA) type A receptor positive allosteric modulator; increases chloride ion influx, enhancing inhibitory neurotransmission.
| Metabolism | Hepatic via CYP3A4; major metabolite is zolpidem phenyl-4-carboxylic acid (inactive). |
| Excretion | Primarily renal excretion (60-80% as unchanged drug and metabolites); biliary/fecal excretion accounts for 15-25%. |
| Half-life | Terminal elimination half-life 8-12 hours in healthy adults; prolonged in renal impairment (up to 30 hours) and elderly. |
| Protein binding | 95-98% bound to albumin. |
| Volume of Distribution | 5-10 L/kg; large Vd indicates extensive tissue distribution. |
| Bioavailability | Oral: 80-90% due to extensive absorption and moderate first-pass metabolism. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | 4-8 hours depending on dose and route; shorter with IV due to redistribution. |
| Molecular Weight | 232.28 |
10 mg orally once daily at bedtime, not to exceed 10 mg/day.
| Dosage form | TABLET |
| Renal impairment | CrCl ≥30 mL/min: no adjustment. CrCl <30 mL/min: not recommended due to lack of data. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B or C: not recommended due to increased risk of encephalopathy. |
| Pediatric use | Not approved for use in pediatric patients (<18 years). |
| Geriatric use | 5 mg orally once daily at bedtime; increase to 10 mg if needed and tolerated. Caution due to increased sensitivity and risk of falls. |
| 1st trimester | Avoid. Limited human data; animal studies show risk. Use only if benefit outweighs risk. |
| 2nd trimester | Avoid. Potential fetal effects; use only if clearly needed. |
| 3rd trimester | Avoid in third trimester due to risk of neonatal withdrawal and respiratory depression. |
Clinical note
Comprehensive clinical and safety monograph for DORMATE (DORMATE).
| Placental transfer | Crosses placenta. Detected in fetal plasma at concentrations similar to maternal levels. |
| Breastfeeding | Not recommended due to potential for infant sedation and respiratory depression. If used, monitor infant for drowsiness and feeding difficulties. |
| Lactation Rating |
■ FDA Black Box Warning
Complex sleep behaviors including sleep-driving, making phone calls, preparing and eating food, and other activities while not fully awake have been reported with hypnotic agents like DORMATE. Discontinue immediately if such behaviors occur.
| Serious Effects |
Hypersensitivity to zolpidem or any componentSevere hepatic impairmentNarrow-angle glaucomaMyasthenia gravisRespiratory failureSleep apnea syndrome
| Precautions | Risk of CNS depression, impaired daytime function, anaphylaxis, angioedema, depression exacerbation, respiratory depression (especially in COPD/sleep apnea), withdrawal symptoms upon abrupt discontinuation. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase midazolam levels and prolong sedation. No other significant food interactions. |
Loading safety data…
| L4 (Hazardous) |
| Teratogenic Risk | Dormate (Meprobamate) is classified as FDA Pregnancy Category D. There is evidence of human fetal risk, but potential benefits may warrant use in pregnant women despite risks. First trimester: Increased risk of major malformations, particularly cardiovascular defects, cleft palate, and neural tube defects, as observed in epidemiological studies. Second and third trimesters: Exposure may lead to withdrawal symptoms (e.g., irritability, tremors, hypertonia) in the neonate, and prolonged exposure may cause low birth weight. Neonatal sedation and respiratory depression may occur if used near delivery. |
| Fetal Monitoring | Maternal: Regular monitoring of mental status, sedation level, liver function tests, and complete blood counts (due to risk of agranulocytosis). Fetal/Neonatal: Fetal ultrasound for malformations if exposed in first trimester; after second/third trimester exposure, monitor neonate for signs of withdrawal (jitteriness, hypertonia, poor feeding, respiratory depression) for at least 48 hours. Long-term neurodevelopmental follow-up is recommended. |
| Fertility Effects | Data on human fertility effects are limited. Animal studies have shown no direct impairment of fertility at therapeutic doses, but chronic use may affect hormonal regulation and menstrual cyclicity due to CNS depression and possible disruption of hypothalamic-pituitary-ovarian axis. In males, there is a theoretical risk of reduced libido or erectile dysfunction secondary to sedation. Discontinuation of meprobamate may restore fertility. For reliable contraception, discuss alternative therapies to avoid potential fetal risks. |
| Clinical Pearls | DORMATE (midazolam) is a short-acting benzodiazepine used for anesthesia induction and procedural sedation. Onset is rapid (1-2 min IV), duration 20-30 min. Use with caution in elderly due to prolonged sedation. Reversal agent is flumazenil. |
| Patient Advice | You may experience drowsiness and amnesia after administration. · Do not drive or operate heavy machinery for at least 24 hours. · Avoid alcohol and other CNS depressants. · Inform your doctor if you are pregnant or breastfeeding. · Allergic reactions include rash, difficulty breathing; seek immediate help. |