Diazepam, 7-Chlor-2,3-dihydro-1-methyl-5-phenyl-1H-1,4-benzodiazepine-2-one
C16H13ClN2O, M = 284,76 g/mol
Benzodiazepine (long-working) T1/2 24 to 48 h, metabolite 50 to 80 hours, dismantling slows down with increasing age
Trade Marks: Valium®, Faustan®, Stesolid®, Tranquase® (more than 100 generics)
Application for the symptomatic treatment of acute and chronic tensions, excitation and fear conditions, as muscel relaxants for the therapy of epilepsy accumulations as well as sleeping drug.
Reciprocal effects
Diazepam strengthens the effect of other muscel relaxanta as well as of laughing gas and analgesics. The effect of diazepam is strengthened by alcohol. Cimetidin restrains the dismantling at the Cytochrome P450 and extends therfore the effect of diazepam.
Adverse Effects
Diazepam impairs reactivity and causes with an uptake over a longer period a psychological, in addition, physical dependence. Withdrawal symptoms arise when suddently set off. An overdose can lead to intoxication-similar conditions, so-called "Valium Trips".
Analytics
Therapeutic blood level 0.2 to 2 µg/ml. Metabolites: Methyldiazepam, Temazepam, Oxazepam
History
Diazepam was already synthesized in the 50's of L.H. Sternbach and marked in 1963 by Hoffmann LaRoche under the label Valium®.
Today, Diazepam is listed by the WHO list of "indispensable medicines" and is available in more than 100 generics. Valium was used occasionally for physical drug withdrawal and even also used overdosed by the dependents as drug replacement.
