[7] 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.

[8] It can sometimes be prescribed to ease symptoms of irritable bowel syndrome (IBS) combined with clidinium bromide as a fixed dose medication, Librax.

Possible adverse effects from benzodiazepine use during pregnancy include, miscarriage, malformation, intrauterine growth retardation, functional deficits, carcinogenesis and mutagenesis.

Serotonin is closely involved in regulating mood and may be one of the causes of feelings of depression in rats using chlordiazepoxide or other benzodiazepines.

[20] The Committee of Review of Medicines, who carried out an extensive review of benzodiazepines including chlordiazepoxide, found—and were in agreement with the US Institute of Medicine and the conclusions of a study carried out by the White House Office of Drug Policy and the US National Institute on Drug Abuse—that there was little evidence that long-term use of benzodiazepines was beneficial in the treatment of insomnia due to the development of tolerance.

[23] An individual who has consumed excess chlordiazepoxide may display some of the following symptoms: Chlordiazepoxide is typically used under controlled conditions for specific syndromes and sees far less frequent usage when compared to newer drugs of the same class and thus is unlikely to be encountered in a clinical emergency setting as a stand-alone drug causing life-threatening concern.

In cases of suspected overdose, supportive care and observation are most often indicated and provided incrementally in relation to severity and duration of symptoms.

Flumazenil is uniquely poised as an "antidote" that specifically counteracts damaging central nervous system affect induced via benzodiazepine mechanism of action - though is not generally indicated in relation to the severity of symptoms where other treatment options exist, and often has numerous damaging consequences that must be carefully weighted before any potential administration.

[24] Chlordiazepoxide acts on benzodiazepine allosteric sites that are part of the GABAA receptor/ion-channel complex and this results in an increased binding of the inhibitory neurotransmitter GABA to the GABAA receptor thereby producing inhibitory effects on the central nervous system and body similar to the effects of other benzodiazepines.

This has been found by measuring sodium-dependent high affinity choline uptake in vitro after pretreatment of the mice in vivo with chlordiazepoxide.

[31] The half-life of chlordiazepoxide increases significantly in the elderly, which may result in prolonged action as well as accumulation of the drug during repeated administration.

Delayed body clearance of the long half-life active metabolite also occurs in those over 60 years of age, which further prolongs the effects of the drugs with additional accumulation after repeated dosing.

The serendipity involved in the invention of this class of compounds was matched by the trials and errors of the pharmacologists in the discovery of the tranquilizing activity of the benzodiazepines.

The discovery of Librium in 1957 was due largely to the dedicated work and observational ability of a gifted technician, Beryl Kappell.

For some seven years she had been screening compounds by simple animal tests for muscle relaxant activity using myanesin as a standard and then meprobamate and chlorpromazine when they became available.

During studies, chlordiazepoxide induced muscle relaxation and a quieting effect on laboratory animals like mice, rats, cats, and dogs.

[37] In 1963, Carl F. Essig of the Addiction Research Center of the National Institute of Mental Health stated that meprobamate, glutethimide, ethinamate, ethchlorvynol, methyprylon and chlordiazepoxide were drugs whose usefulness “can hardly be questioned.” However, Essig labeled these “newer products” as “drugs of addiction,” like barbiturates, whose habit-forming qualities were more widely known.