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Diazepam: Difference between revisions

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{{MedTemplate
{{MedTemplate
| generic           = Diazepam
| generic           = Diazepam
| brand             = Valium
| brand             = Valium (oral, IV/IM, rectal), Diastat (rectal gel for breakthrough seizures), Valtoco (nasal spray for breakthrough seizures), Libervant (buccal film)
| structure         =  
| structure         =
| classes           = Benzodiazepine, Anxiolytic
| classes           = [[:Category:Benzodiazepines|Benzodiazepine (long-acting)]], [[:Category:Anxiolytics|Anxiolytic]], [[:Category:Anticonvulsants|Anticonvulsant]], [[:Category:Skeletal muscle relaxants|Skeletal muscle relaxant]], [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]]
| mechanism          = GABAA positive allosteric modulator
| uses             = <vote slug="anxiety-disorders-broad-use">Anxiety disorders (FDA)</vote>, <vote slug="alcohol-withdrawal-use">Alcohol withdrawal (FDA; the classic indication for long-acting benzodiazepines)</vote>, <vote slug="preoperative-sedation-use">Preoperative sedation (FDA)</vote>, <vote slug="status-epilepticus-use">Status epilepticus (FDA, IV)</vote>, <vote slug="breakthrough-seizures-use">Breakthrough seizures (FDA, Diastat rectal gel; Valtoco intranasal)</vote>, <vote slug="acute-muscle-spasm-use">Acute muscle spasm (FDA, IV/IM)</vote>, <vote slug="cerebral-palsy-spasticity-use">Cerebral palsy spasticity (FDA)</vote>
| uses               =  
| 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
| starting_dose     =  
| 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
| preparations       =  
| fda_max           = 40 mg/day (oral, anxiety)
| fda_max          =  
| pill_id           =
| routes             =  
| routes           = Oral, IV, IM, rectal, intranasal, buccal
| onset             =  
| onset             = 15-60 minutes (oral); 1-5 minutes (IV); 4-10 minutes (rectal or intranasal)
| duration           =  
| duration         = 6-24 hours (parent); much longer when accounting for the long-lived active metabolites
| halflife           =
| halflife          = Diazepam 20-50 hours; '''N-desmethyldiazepam (nordazepam) 30-200 hours''' is the major active metabolite and accumulates substantially with chronic dosing<ref name="valium-label">FDA Prescribing Information, Valium (diazepam), Roche/Bausch, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf</ref>
| bioavailability    =
| bioavailability   = ~93% (oral); ~90% (rectal)<ref name="valium-label" />
| pregnancy         =  
| pregnancy        = Some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.{{citation needed}}
| legal              =  
| legal             = [[USLegal:Schedule IV|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<ref name="valium-label" />
| intro              =
| mechanism         = <vote slug="diazepam-mech-claim">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.</vote> 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<ref name="valium-label" />.
| pharmacokinetics   =  
| pharmacodynamics  =  
| indications        =  
| dosing             =  
| effects            =  
| contraindications  =
| interactions      =
| pregnancy_details  =
| monitoring         =  
| counseling        =  
| anecdotes          =
| seealso            =
| references        =  
}}
}}


== References ==
<references />
[[Category:Benzodiazepines]]
[[Category:Anxiolytics]]
[[Category:Anxiolytics]]
[[Category:Anticonvulsants]]
[[Category:Skeletal muscle relaxants]]
[[Category:Schedule IV controlled substances]]

Latest revision as of 07:15, 23 May 2026

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