diazepam

General Information

Diazepam is a long-acting benzodiazepine used for anxiety, alcohol withdrawal, muscle spasm, and seizure-related indications (label varies by product). In psychiatric practice it may be used as a short-term bridge for severe anxiety or agitation when rapid relief is required.

Long half-life and active metabolites can provide smoother coverage but also increase accumulation, next-day impairment, and fall risk—key concerns in older adults and in serious mental illness with polypharmacy.

Because of its long duration, diazepam is sometimes used as part of a structured taper strategy from shorter-acting benzodiazepines, but it still carries substantial misuse and overdose risk; short courses with explicit goals and a stop plan are common.

Generally avoided or used with extreme caution in older adults, significant liver disease, untreated sleep apnea/COPD, and with concurrent opioids or alcohol; the safety risks of carryover sedation and falls can outweigh any benefit.

The diazepam compare view, diazepam evidence feed, and diazepam print page can support safe-use counseling and shared decision-making when aligning short-term calming strategies with safety planning.

Often reserved for targeted, time-limited indications with explicit taper plans and frequent reassessment; open-ended chronic use is generally avoided. Long half-life and active metabolites can smooth coverage but also increase carryover impairment, especially in older adults and with polypharmacy—prescriptions are typically short with a defined stop date and reassessment at renewals.

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 that increases inhibitory neurotransmission.

Produces anxiolysis, sedation, and anticonvulsant effects; long half-life increases carryover impairment risk.

Diazepam treats symptoms but does not address underlying anxiety drivers; it is often paired with psychotherapy and SSRI/SNRI-based plans when ongoing anxiety is present.

• GABA-A receptor facilitation (benzodiazepine class).

Metabolism and Pharmacokinetics

• N-demethylated by CYP3A4 and CYP2C19 to active metabolite N-desmethyldiazepam; further metabolized to oxazepam/temazepam (label).
• Terminal elimination phase half-life up to ~48 hours; active metabolite half-life up to ~100 hours (label).
• Excreted mainly in urine as glucuronide conjugates; accumulates with repeated dosing (label).
• Accumulation is more pronounced in older adults and hepatic impairment; lower doses and avoiding frequent redosing are common, with reassessment of next-day function.

Dosing and Administration

• Anxiety (label ranges vary): the lowest effective dose is typically used in divided doses; dose escalation is generally avoided without a clear, time-limited plan.
• Alcohol withdrawal and seizure protocols vary by setting; coordination with medical teams and close monitoring of vitals and sedation are typical.
• Tapering is typically planned after courses beyond a few weeks, and abrupt discontinuation is generally avoided to reduce withdrawal and seizures.
• Long half-life and active metabolites mean slow washout; rapid dose changes are generally avoided, and tapers are often planned over weeks to months when use has been prolonged.
• Generally not used as a nightly sleep medication; if insomnia is the primary complaint, underlying drivers are addressed and insomnia-specific strategies are considered.

Monitoring & Labs

• Functional benefit and safety at each renewal; open-ended continuation without documented goals is generally avoided.
• Sedation, falls, and driving impairment—especially in older adults and when other CNS depressants are present.
• Screening for substance use disorders and prescription monitoring data review; aligning on a single prescriber and pharmacy is common.
• If discontinuing after more than brief use, tapering is gradual with monitoring for withdrawal symptoms and rebound anxiety.

Sources: FDA/DailyMed label; guideline statements.

Adverse Effects

Interactions

• Additive CNS and respiratory depression with opioids, alcohol, antihistamines, and sedating antipsychotics.
• CYP3A4 and CYP2C19 inhibitors can increase exposure; inducers may reduce effect.
• Stacking with other sedative-hypnotics increases overdose risk and is generally avoided; if combinations are unavoidable, lower dosing, closer follow-up, and a single-prescriber plan are commonly used to reduce risk.

Other Useful Information

• Documentation of indication, time horizon, and taper plan at initiation is typical; necessity is reassessed frequently.
• Prescription monitoring data review and screening for substance use disorders are common when benzodiazepines are used.
• Non-benzodiazepine long-term anxiety strategies are generally preferred, and diazepam necessity is revisited frequently.
• Prescriptions are often short with planned follow-up and without “automatic” refills; when discontinuing, tapering is gradual with monitoring for withdrawal symptoms and rare seizure risk.

References

1. Valium (diazepam) prescribing information — DailyMed (2025)
2. ASAM guideline on benzodiazepines — Journal of Addiction Medicine (2020)
3. Evidence Based Pharmacological Treatment OF Anxiety Disorders — Depression and Anxiety (2014)
4. Guidelines FOR THE Pharmacological Treatment OF Anxiety Disorders, Obsessive Compulsive Disorder AND Posttraumatic Stress Disorder IN Primary Care — International Journal of Psychiatry in Clinical Practice (2012)