Diazepam

Other Names

7-chlor-1,3-dihydro-1-methyl-5-phenyl-2H-1,4benzodiazepin-2-on, sleeping pill, tranquilizer, Valium

Substance type: benzodiazepine

Diazepam, better known as Valium, was originally synthesized in the laboratory and introduced as a therapeutic drug (psychopharmaca, tranquilizer) in the 1960s. The substance produces sedative, euphoric, and especially anxiolytic (anxietyreducing) effects (Henningfield 1988, 17,35*). During the investigation of diazepam's pharmacology, it was discovered that the human nervous system has a special receptor for this molecule, known as the benzodiazepine receptor or the [3H] -diazepam receptor. Luk et al. (1983) found three isoflans in the urine of cattle that may possibly dock (as neurotransmitters) in the benzodiazepine receptor. It is known that the kavapyrones (cf. Piper methysticum) bind to the [3H] -diazepam receptor.

Recently, flavonoids in the buds of the South American linden tree (Tilia tomentosa Moench; Tiliaceae; cf. tila) were found to bind to the benzodiazepine receptor. A substance found in Passiflora caerulea 1. (cf. Passiflora spp.), 5,7-dihydroxyflavone, also docks to the same location (Viola et al. 1994). The benzodiazepine receptor has been shown to be present in all vertebrates, suggesting that it appeared at a very early date in the evolution of the nervous system and has been preserved into the present. This indicates that it plays an important function in the nervous system and that there are endogenous substances that bind to it in order to transmit certain messages (Muller 1988). But what do these substances look like? At first they were thought to be polypeptides, but then traces of diazepam and desmethyldiazepam were discovered in the brains of humans and other animals. Because diazepam and its initial metabolite appear in breast milk and the placenta after the ingestion of Valium (Wessen et al. 1985), it was first believed that the diazepam must have been introduced into the body from outside" But when diazepam was subsequently also found to be present in brains that dated to a time before the discovery of Valium synthesis, it was concluded that diazepam was not a synthetic chemical at all but a naturally occurring neurotransmitter in the nervous system (Muller 1988). Thus it was demonstrated that "Valium, the very symbol of chemical psychopharmaca" (Zehentauer 1992, 121 *), is actually a natural substance.

Pharmacologists were surprised when subsequent research demonstrated the presence of diazepam and desmethyldiazepam in potatoes (Solanum tuberosum 1.; cf. Solanum spp.) and in such diverse grains as wheat (Triticum aestivum 1.; cf. beer), corn/maize (Zea mays), and rice (Oryza sativa 1.; cf. sake) (Muller 1988). Valium, in other words, is a natural active constituent in plants. However, the concentration in these plants is so low that a person would likely not notice any Valium effects even after consuming a whole sack of potatoes. Valium is one of the most widely used sedative drugs in modern society and is normally prescribed for the treatment of anxiety and sleeping disorders.498 Not surprisingly, Valium also finds use as a recreational drug in some circles, particularly in combination with other substances. Its euphoric properties can be greatly affected by alcohol, which can at times counteract the sedative properties, resulting in powerful stimulating effects. Valium is one of the more commonly used psychopharmaca in the music scene. Several rock bands, including the classic "space rock" band Hawkwind CValium 10," 1978), have dedicated titles to the substance.

Commercial Forms and Regulations

Valium is available by prescription only. In the United States, it is listed as a Schedule IV drug under the Controlled Substances Act.

Literature

Flesch, Peter. 1996. SchlafstOrungen bei iilteren Patienten: Auf Benzodiazepine kann meist verzichtet werden. Jatros Neurologie 12:6-7 (interview).

Henningsfield, Jack E. 1988. Barbiturates: Sleeping potion or intoxicant. The Encyclopedia of

Psychoactive Drugs. London, Toronto, and New York: Burke Publishing Company.

Luk, Kin-Chun, Lorraine Stern, Manfred Weigele,

Robert A. O'Brien, and Nena Sprit. 1983.

Isolation and identification of "diazepam-like"

compounds from bovine urine. Journal of

Natural Products 46 (6): 852-61.

Muller, Walter E. 1988. Sind Benzodiazipine 100%

Natur? Deutsche Apotheker Zeitung126 (13): 672-74.

Viola, H., C. Wolfman, M. Levi de Stein, C.

Wasowski, C. Pena, J. H. Medina, and A. C.

Paladini. 1994. Isolation of pharmacologically

active benzodiazepine receptor ligands from Tilia

tomentosa (Tiliaceae). Journal of

Psychopharmacology 44:47-53.

Wesson, Donald R, Susan Camber, Martha Harkey,

and David E. Smith. 1985. Diazepam and

desmethyldiazepam in breast milk. Journal of

Psychoactive Drugs 17 (1): 55-56.