Diazepam

Benzodiazepine (long-acting), Anxiolytic, Anticonvulsant, Skeletal muscle relaxant, Schedule IV controlled substance

Diazepam

Valium (oral, IV/IM, rectal), Diastat (rectal gel for breakthrough seizures), Valtoco (nasal spray for breakthrough seizures), Libervant (buccal film)

Experience

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Problems

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Titration strategies

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Effects

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Monitoring

Boxed warning: in September 2020 the FDA required an updated boxed warning across the benzodiazepine class for the risks of abuse, misuse, addiction, physical dependence, and withdrawal reactions. Physical dependence can develop with continued use even at prescribed doses, and abrupt discontinuation or rapid dose reduction can precipitate acute, sometimes life-threatening withdrawal (including seizures), so prolonged use requires a gradual, individualized taper. This is in addition to the earlier boxed warning for fatal respiratory depression, coma, and death when benzodiazepines are combined with opioids or other CNS depressants.

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Pharmacy

Starting dose

Anxiety: 2-10 mg PO 2-4 times daily. Alcohol withdrawal: 10-20 mg PO/IV every 4-6 hours, symptom-triggered. Status epilepticus: 5-10 mg IV. Breakthrough seizures: Diastat rectal 0.2-0.5 mg/kg or Valtoco intranasal 5-20 mg

Preparations

Tablets 2, 5, 10 mg; oral solution 1, 5 mg/mL; injection 5 mg/mL; Diastat rectal gel 2.5, 5, 10, 20 mg; Valtoco nasal spray 5, 7.5, 10 mg/dose; Libervant buccal film

US FDA Max

40 mg/day (oral, anxiety)

Common uses

Classification(s)

Classes

Benzodiazepine (long-acting), Anxiolytic, Anticonvulsant, Skeletal muscle relaxant, Schedule IV controlled substance

Pharmacology

Routes

Oral, IV, IM, rectal, intranasal, buccal

Onset

15-60 minutes (oral); 1-5 minutes (IV); 4-10 minutes (rectal or intranasal)

Duration

6-24 hours (parent); much longer when accounting for the long-lived active metabolites

Half-life

Diazepam 20-50 hours; N-desmethyldiazepam (nordazepam) 30-200 hours is the major active metabolite and accumulates substantially with chronic dosing

Bioavailability

~93% (oral); ~90% (rectal)

Pregnancy

Some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.^{[citation needed]}

Legal status

Schedule IV controlled substance in US. Carries the benzodiazepine class Boxed Warning for risk of fatal respiratory depression, coma, and death when combined with opioids

Purported mechanism

Classic positive allosteric modulator of the GABA-A receptor at the benzodiazepine binding site (α-γ subunit interface), enhancing chloride ion conductance and producing the full benzodiazepine effect spectrum: anxiolysis, anticonvulsant activity, skeletal muscle relaxation, and sedation. The very long elimination half-life combined with the even-longer-lived active metabolite nordazepam is the clinical signature, producing stable plasma levels with infrequent dosing.▲0▼ The pharmacokinetic profile produces self-tapering withdrawal as plasma levels gradually decline, the basis of diazepam's preference in alcohol withdrawal protocols. CYP3A4 and CYP2C19 substrate; CYP3A4 inhibitors substantially raise exposure.

Pharmacopedia is intended for reference. Nothing here is advice. In an emergency call 911; US Poison Control 1-800-222-1222. See the full disclaimer.