Addictive Potential: Medium
Emergency Room Visits Yearly: Unknown
Mandatory Minimum Sentence: Not more than 3 years
Mechanism of Action: Increases the Neurotransmitter GABA(A)
Diazepam, marketed under brand names Valium, Stesolid, Diazemuls, Seduxen, Bosaurin, Diapam, Antenex, Ducene, Apozepam and Pax. It possesses anxiolytic, anticonvulsant, sedative, skeletal muscle relaxant, and amnestic properties.
Diazepam is a benzodiazepine that binds to a specific subunit on the GABA(A) receptor at a site that is distinct from the endogenous GABA molecule. The GABA(A) receptor is an inhibitory channel which, when activated, decreases neurologic activity.
Diazepam appears to act on areas of the limbic system, thalamus and hypothalamus, inducing anxiolytic effects. Its actions are due to the enhancement of GABA activity.
Diazepam was the second benzodiazepine to be invented by Leo Sternbach of Hoffmann-La Roche, and was approved for use in 1963. It is five times more potent than its predecessor, chlordiazepoxide, which it quickly surpassed in terms of sales. After this initial success, other pharmaceutical companies began to introduce other benzodiazepine derivatives.
The benzodiazepines gained popularity among medical professionals as an improvement upon barbiturates, which have a comparatively narrow therapeutic index, and are far more sedating at therapeutic doses. The benzodiazepines are also far less dangerous; death rarely results from diazepam overdose, except in cases where it is consumed with large amounts of other depressants (such as alcohol or other sedatives).
Diazepam was the top-selling pharmaceutical in the United States from 1969 to 1982, with peak sales in 1978 of 2.3 billion pills. In 1966, The Rolling Stones released the song “Mother’s Little Helper,” which is about a mother needing the “little yellow pill” to get through the day.
While psychiatrists continue to prescribe diazepam for the short-term relief of anxiety, neurology has taken the lead in prescribing diazepam for the palliative treatment of certain types of epilepsy and spastic activity. It is also the first line of defense for a rare disorder called stiff-person syndrome.