diazepam VALIUM

Class: Benzodiazepine/​2-Keto
FDA Indications: Anxiety Disorders, Acute Alcohol Withdrawal, Muscle Spasm, Seizure Disorders, Status Epilepticus (IM Only), Preanesthetic (IM Only), Cardioversion (IM Only)
Off-Label Use: Muscle Relaxation, Preanesthetic, Tetanus, Catatonia, Delirium Tremens, Insomnia
Prescribing
FDA Schedule IV
Forms: 2, 5, 10mg tablet; 5 mg/mL IM
Dose Range: 2-40 mg/day
Starting: 2-10 mg, 2-4 times/day
Stopping: Taper by 2 mg q3 days, slower for difficult-to-taper patients

NAMI drug fact sheet

Precautions
Contraindications: Sleep apnea
Serious Side Effects: Overdose can result in hypotension, respiratory depression, and coma
Side Effects: sedation/somnolence, dizziness, confusion, disequilibrium, ataxia, lightheadedness, weakness/asthenia, decreased libido, dysarthria, increased appetite, weight gain
Pharmacodynamics
1° MOA: GABAAR PAM
Target: GABAA: α2, α3 (high); α1, γ2, β3 (low to moderate)
Pharmacokinetics
t½: 20 (20-80)° TMAX: 1-2°
Absorption Rate: Rapid
Lipid Solubility: High
Substrate of: 3A4
Inhibits: ∅ ; Induces:
Active Metabolites: oxazepam, N-desmethyldiazepam (100° t½), temazepam
DDIs
  • - CNS depression with combined use of opioids
  • - 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers can ↓ levels
  • - valproate causes twofold ↑ of unbound serum diazepam (via displacement from plasma protein-binding sites)
Misc
  • - ↓ stage 4 sleep
  • - available in rectal gel and oral liquid formulations
  • - longer t½ makes it easier to taper
  • - t½ ↑ by ~1h for each year >40
Special Populations

Category D—↑ risk of oral cleft by 0.01%, use just before delivery associated with floppy infant syndrome, 3rd trimester use can cause withdrawal in newborns

Diazepam's high RID (2.8-7.1%) and its long t½ make it the worst choice of among the benzodiazepines for nursing mothers

2-2.5 mg, 1-2 times/day; ↑ gradually as needed; use with caution; active metabolites with ↑ t½ may lead to accumulation

There are no dosage adjustments provided in the manufacturer's labeling

There are no dosage adjustments provided in the manufacturer's labeling

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Last updated July 08 2018 15:58:23. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.