Products
Chlordiazepoxide was synthesized in the 1950s by Leo Sternbach at Hoffmann-La Roche and became the first active ingredient in the benzodiazepine group to be marketed in 1960 (Librium). In many countries, it is currently only available in combination with clidinium bromide or amitriptyline (Librax, Limbitrol). In other countries, the monopreparation Librium is still available.
Structure and properties
Chlordiazepoxide (C16H14ClN3O, Mr = 299.8 g/mol) is a white to pale yellow crystalline powder that is practically insoluble in water. It is also present in some drugs as chlordiazepoxide hydrochloride, which is soluble in water. Chlordiazepoxide is a 5-aryl-1,4-benzodiazepine.
Effects
Chlordiazepoxide (ATC N05BA02) has antianxiety, muscle relaxant, and sedative properties. The effects are due to allosteric binding to the GABA receptor and enhancement of the effects of GABA, the major inhibitory neurotransmitter in the brain.
Indications
For the treatment of tension, agitation, and anxiety states and for the therapy of sleep disorders.
Dosage
According to the professional information. Tablets are usually administered in the evening. The duration of therapy should be kept as short as possible and should not exceed one to three months.
Abuse
Like all benzodiazepines, bromazepam can be abused as a depressant intoxicant. Abuse is dangerous, especially in combination with other depressant and respiratory depressant medications and with alcohol.
Contraindications
- Hypersensitivity
- History of dependence (alcohol, medications, intoxicants).
- Myasthenia gravis
- Severe respiratory failure
- Sleep apnea syndrome
- Severe hepatic insufficiency
For complete precautions, see the drug label.
Interactions
Drug interactions are possible with central depressant medications, alcohol, CYP inhibitors, and muscle relaxants, among others.
Adverse effects
The most common possible adverse effects include fatigue, drowsiness, faintness, dizziness, lightheadedness, ataxia, headache, prolonged reaction time, confusion, and anterograde amnesia. Chlordiazepoxide can cause withdrawal symptoms and be addictive if discontinued rapidly.
