Products
Diazepam is commercially available in tablet, drop, solution for injection, and enema form (Valium, generic). It has been approved in many countries since 1962. In 2020, a diazepam nasal spray was released in the United States. Diazepam was developed by Leo Sternbach at Hoffmann-La Roche as the second member of the benzodiazepine group.
Structure and properties
Diazepam (C16H13ClN2O, Mr = 284.7 g/mol) exists as a white crystalline powder that is very sparingly soluble in water. It belongs to the 1,4-benzodiazepines.
Effects
Diazepam (ATC N05BA01) has antianxiety, sedative, sleep-inducing, muscle relaxant, and anticonvulsant properties. The effects are due to binding to GABAA receptors, resulting in enhancement of GABAergic inhibition. Diazepam has a long half-life of 24 to 48 hours. The half-life of the active metabolite -desmethyldiazepam is up to 100 hours.
Indications
Indications for use include:
- Anxiety, agitation, and tension states.
- Basic sedation, preoperative medication.
- Agitation associated with acute anxiety and panic attacks.
- Motor agitation and delirium tremens.
- Status epilepticus and other convulsive states.
- Eclampsia.
- Muscle cramps, spastic conditions.
Dosage
According to the drug label. Diazepam is administered perorally, parenterally, intranasally, and rectally.
Abuse
Like other benzodiazepines, diazepam is abused as a depressant narcotic.
Contraindications
- Hypersensitivity
- Respiratory failure
- Severe liver dysfunction
- Sleep apnea syndrome
- Myasthenia gravis
For complete precautions, see the drug label.
Interactions
Diazepam is a substrate of CYP3A and CYP2C19 and corresponding interactions are possible. Central depressant drugs and alcohol may potentiate the adverse effects of diazepam.
Adverse effects
The most common adverse effects are fatigue, drowsiness, and muscle weakness. Benzodiazepines can lead to dependence and cause withdrawal symptoms on discontinuation.
