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.

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