estazolam

General Information

Estazolam is a benzodiazepine hypnotic indicated for the short-term treatment of insomnia (label; product-dependent). It can improve sleep onset and maintenance but is not a maintenance strategy for chronic insomnia.

Estazolam’s elimination half-life is relatively long for a hypnotic (10–24 hours; longer in some older adults). Longer duration can reduce late-night rebound but increases morning grogginess, falls, and impaired driving risk—especially with polypharmacy (label).

Benzodiazepine risks extend beyond sedation: abuse, misuse, addiction, and withdrawal reactions are core safety constraints and support a time-limited plan with a defined reassessment date (label / safety guidance).

Boxed warning: Concomitant use with opioids can cause profound sedation, respiratory depression, coma, and death; avoid co-prescribing when possible (label).

The estazolam compare view, estazolam evidence feed, and estazolam print page can support shared decision-making and safe-use counseling.

Estazolam is often positioned as an “intermediate-to-long” benzodiazepine hypnotic: it can cover sleep maintenance but has meaningful carryover impairment risk. It is typically paired with a brief course, a follow-up date, and an exit/taper plan, with preference for CBT-I and non-controlled options when insomnia is chronic.

Mechanism of Action

Refer to the Glossary entry on Neurotransmitters for background on receptor systems involved in serious mental illness.

Positive allosteric modulator of GABA-A receptors, increasing inhibitory neurotransmission and producing hypnotic effects.

Sedation and cognitive slowing scale with dose and co-administered CNS depressants; total sedative burden is a major driver of harm.

Repeated nightly use can lead to tolerance and physical dependence; abrupt discontinuation can cause rebound insomnia and withdrawal.

• GABA-A receptor positive allosteric modulation.

Metabolism and Pharmacokinetics

• Mean elimination half-life estimates range from 10–24 hours; in a small older-adult study, mean half-life was 18.4 hours (range 13.5–34.6 hours) (label).
• Hepatic metabolism to hydroxylated metabolites; biotransformation to 4-hydroxy-estazolam is mediated by CYP3A (label).
• After 5 days, 87% of radiolabeled drug was recovered in urine, primarily as metabolites; <5% is excreted unchanged in urine and ~4% in feces (label).
• Longer half-life increases the risk of next-day impairment and interactions with other psychoactive medications and alcohol (label / class).

Dosing and Administration

• Adults: recommended initial dose is 1 mg at bedtime; some may need 2 mg (label).
• Older adults: 1 mg is a typical starting dose, but dose increases are approached cautiously; in small or debilitated older adults, 0.5 mg is sometimes used to reduce falls and confusion (label).
• Use the lowest effective dose and take only when a full sleep window is possible; avoid middle-of-the-night “catch-up” dosing.
• If used beyond a short course, tapering is commonly used to reduce rebound insomnia and withdrawal symptoms (label / class).

Monitoring & Labs

• Reassess benefit and adverse effects within 1–2 weeks; discontinue if benefit is marginal or impairment emerges.
• Screen for opioid co-prescribing, alcohol use, untreated sleep apnea, and fall risk before renewing.
• Review the medication list for CYP3A inhibitors and additive sedatives before initiation and dose changes.
• If used beyond a short course, create a taper plan and monitor for rebound insomnia and withdrawal symptoms.

Sources: FDA/DailyMed label; insomnia guideline context; benzodiazepine safety guidance.

Adverse Effects

Interactions

• CYP3A inhibitors can increase estazolam exposure and adverse effects; review interacting antibiotics/antifungals and antiviral regimens (label).
• Additive CNS/respiratory depression occurs with alcohol, opioids, antihistamines, and sedating antipsychotics; avoid stacking sedatives when possible.
• Grapefruit products and other moderate CYP3A inhibitors can increase exposure; dose reduction or switching hypnotics is commonly considered if carryover impairment emerges.

Other Useful Information

• When insomnia is chronic, guidelines typically prioritize CBT-I and treat underlying contributors (mood episodes, pain, substance use, sleep apnea) rather than escalating hypnotic intensity.
• A time-limited plan often includes documentation of indication, intended duration, quantity limits, and a taper strategy if nightly use persists.
• If next-day impairment is prominent, clinicians often pivot to shorter acting or non-controlled options rather than increasing dose.

References

1. Estazolam tablets prescribing information — DailyMed (2025)
2. Clinical Practice Guideline for the Pharmacologic Treatment of Chronic Insomnia in Adults: An American Academy of Sleep Medicine Clinical Practice Guideline — Journal of Clinical Sleep Medicine (2017)
3. ASAM guideline on benzodiazepines — Journal of Addiction Medicine (2020)
4. Efficacy and Acceptability of Pharmacological Interventions for Insomnia in Patients With Severe Mental Illness — Acta Psychiatrica Scandinavica (2025)
5. Residual effects of medications for sleep disorders on driving performance — European Neuropsychopharmacology (2024)