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)
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Summary
Classes
Common uses
Anxiety disorders (FDA)0, Alcohol withdrawal (FDA; the classic indication for long-acting benzodiazepines)0, Preoperative sedation (FDA)0, Status epilepticus (FDA, IV)0, Breakthrough seizures (FDA, Diastat rectal gel; Valtoco intranasal)0, Acute muscle spasm (FDA, IV/IM)0, Cerebral palsy spasticity (FDA)0
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)
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[1]
Bioavailability
~93% (oral); ~90% (rectal)[1]
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[1]
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[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Valium (diazepam), Roche/Bausch, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf