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Diazepam belongs to the group of benzodiazepines that have an anxiolytic, muscle relaxant, sedative and anticonvulsant effect. Benzodiazepines exert central depressant actions on spinal reflexes, mediated in part by the brainstem reticular system.
Diazepam administered orally is rapidly and completely absorbed from the gastrointestinal tract, reaching maximum plasma concentrations between 30 and 90 minutes after ingestion. For the distribution of Diazepam and its metabolites, they are largely bound to plasma proteins between 85 and 95%. They cross the blood-brain and placental barriers, and are also found in breast milk in relatively low concentrations. The steady state volume of distribution is 0.8-1.0 l/kg. The distribution half-life reaches up to 3 hours.
Diazepam is mainly metabolized to pharmacologically active metabolites such as Temazepam, N-desmethyl-diazepam and oxazepam.
The elimination of Diazepam after oral administration is biphasic, with a decrease in the concentration-time profile in plasma, with an initial phase of rapid and extensive distribution, followed by a prolonged terminal elimination phase that can be up to 48 hours.
Diazepam and its metabolites are mainly excreted in the urine, predominantly in their conjugated forms. The terminal elimination half-life of the active metabolite N-desmethyl-diazepam is about 100 hours.
In special situations the half-life of Diazepam could be prolonged, for example in newborns, the elderly or patients with liver disease. The half-life of Diazepam does not change in patients with renal deficiency.
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Diazepam was first synthesized by Leo Sternbach and commercialized by Hoffmann-La Roche. Between 1968 and 1982, it became the highest-selling medication in the United States, with over two billion tablets sold in 1978 alone. The patent for Valium expired in 1985, and now more than 500 different brands of Diazepam are available worldwide. It is included on the World Health Organization’s List of Essential Medicines, which identifies the most effective and safe medications needed within a health system. Buy Valium Diazepam online
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