Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2019 Publisher: Mylan Products Ltd, Station Close, Potters Bar, Hertfordshire, EN6 1TL, United Kingdom
Pharmacotherapeiutic group: Psycholeptica, anxiolytics, benzodiazepine derivatives
ATC code: N05BA02
Chlordiazepoxide is a psychotropic substance from the class of 1,4-benzodiazepines with tension, excitement, anxiety attenuating properties and sedative and hypnotic effects. Chlordiazepoxide shows muscle relaxant and anticonvulsant effects
Chlordiazepoxide has a low affinity as an agonist at specific benzodiazepine receptors located on GABA-ergic neurones. Stimulation of benzodiazepine receptors potentates the actions of GABA. GABA-ergic neurones are inhibitory in the nervous system. This results in diminution of various 5-HT, dopamine and noradrenergic neurotransmitter system effects.
Librium is well absorbed, with peak blood levels being achieved one or two hours after administration.
Steady-state levels are usually reached within three days.
Chlordiazepoxide is metabolised to desmethyl-chlordiazepoxide. Demoxepam and desmethyldiazepam are also found in the plasma of patients on continuous treatment. The active metabolite desmethyl-chlordiazepoxide has an accumulation half-life of 10–18 hours; that of demoxepam has been recorded as 21–78 hours.
Steady-state levels of these active metabolites are reached after 10-15 days, with metabolite concentrations which are similar to those of the parent drug.
The drug has a half-life is of 6-30 hours.
No clear correlation has been demonstrated between the blood levels of Librium and its clinical effects.
In in-vivo and in-vitro studies with chlordiazepoxide, there are indications for a mutagenic effect. Nevertheless, in similar test systems results are negative. The relevance of the positive findings is currently unclear.
In carcinogenicity studies in mice an increase of liver tumours was seen at high doses, especially in males, whereas no increase of tumour incidence was seen in rats.
In animal studies increased resorption rates, increased incidence of stillbirth and neonatal death, malformation of the scull (exencephaly, cleft palate), lung anomalies and changes in the urogenital tract as well as behavioural disorders and neurochemical changes have been observed in the offspring.
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