TaperCommunitydiazepam
Boxed Warning
Concomitant use with opioids may result in profound sedation, respiratory depression, coma, and death. Risks of abuse, misuse, and addiction, which can lead to overdose and death. Physical dependence and life-threatening withdrawal reactions.
Diazepam is a long-acting benzodiazepine approved for anxiety disorders, alcohol withdrawal, muscle spasm, seizures, and as a pre-anesthetic. Due to its long half-life, multiple tablet strengths, and smooth pharmacokinetic profile, it is the preferred benzodiazepine for crossover tapers.
2mg, 5mg, 10mg
Tablets: 2mg, 5mg, 10mg; Oral solution: 5mg/5mL; Oral concentrate (Intensol): 5mg/mL; Injection: 5mg/mL; Rectal gel (Diastat): 2.5mg, 10mg, 20mg
Category D (positive evidence of risk)
Positive allosteric modulator at GABA-A receptors. Enhances GABA-mediated chloride conductance producing anxiolytic, sedative, anticonvulsant, and muscle relaxant effects. Multiple active metabolites (desmethyldiazepam, temazepam, oxazepam) prolong its duration of action.
Very long half-life — often used as the target drug for benzodiazepine crossover tapers. Tablets easily split. Liquid formulation available.
Preferred benzodiazepine for tapering due to long half-life and available small doses. Ashton Manual taper schedules use diazepam as the standard.
Toxicity
CNS and respiratory depression (especially with opioids/alcohol). Physical dependence with chronic use. Extremely long effective half-life due to active metabolites can lead to accumulation in elderly. Abrupt discontinuation can cause seizures.
Pharmacokinetics
Rapidly and completely absorbed after oral administration. Bioavailability ~100%. Tmax 0.5–2 hours. Food may delay absorption.
~0.8–1.0 L/kg
Hepatic via CYP3A4 and CYP2C19 to the long-acting active metabolite desmethyldiazepam (half-life 36–200 hours), then to oxazepam, and via CYP3A4 to temazepam (both active). Final elimination via glucuronidation.
Renal (primarily as glucuronide conjugates of metabolites). Very little unchanged diazepam in urine.
~98%
~20–30 mL/min (total body clearance)
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