Chlordiazepoxide, trade name Librium among others, is a sedative and hypnotic medication of the benzodiazepine class; it is used to treat anxiety, insomnia and symptoms of withdrawal from alcohol and other drugs.
Chlordiazepoxide has a medium to long half-life but its active metabolite has a very long half-life. The drug has amnesic, anticonvulsant, anxiolytic, hypnotic, sedative and skeletal muscle relaxant properties.
Chlordiazepoxide was patented in 1958 and approved for medical use in 1960. It was the first benzodiazepine to be synthesized and the discovery of chlordiazepoxide was by pure chance. Chlordiazepoxide and other benzodiazepines were initially accepted with widespread public approval but were followed with widespread public disapproval and recommendations for more restrictive medical guidelines for its use.
Chlordiazepoxide is indicated for the short-term (2–4 weeks) treatment of anxiety that is severe and disabling or subjecting the person to unacceptable distress. It is also indicated as a treatment for the management of acute alcohol withdrawal syndrome.
It can sometimes be prescribed to ease symptoms of irritable bowel syndrome combined with clidinium bromide as a fixed dose medication, Librax.
Use of chlordiazepoxide should be avoided in individuals with the following conditions:
Myasthenia gravis
Acute intoxication with alcohol, narcotics, or other psychoactive substances
Ataxia
Severe hypoventilation
Acute narrow-angle glaucoma
Severe liver deficiencies (hepatitis and liver cirrhosis decrease elimination by a factor of 2)
Severe sleep apnea
Hypersensitivity or allergy to any drug in the benzodiazepine class
Chlordiazepoxide is generally considered an inappropriate benzodiazepine for the elderly due to its long elimination half-life and the risks of accumulation. Benzodiazepines require special precaution if used in the elderly, pregnancy, children, alcohol- or drug-dependent individuals and individuals with comorbid psychiatric disorders.
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A divergent and regiocontrolled Pd-catalyzed domino sequence involving an intramol. N-arylation and an intermol. Heck reaction has been developed, providing rapid access to functionalized benzodiazepine-2,5-diones, e.g. I. The starting materials were synth ...