|Common names||Valium, Diastat, “Mother’s Little Helper”, Apaurin|
diazepam was patented in 1955 by the pharmaceutical company hoffman-la roche. it has been one of the most frequently prescribed medications in the world since its launch in 1963. it is commonly used to treat a wide range of conditions including anxiety, panic attacks, insomnia, seizures, muscle spasms, and restless legs syndrome. diazepam is a core medicine in the world health organization’s essential drugs list, the minimum medical needs for a basic health-care system.
subjective effects include anxiety suppression, sedation, and muscle relaxation. diazepam has a rapid onset of action compared to other benzodiazepines. however, it is generally considered to have lesser recreational effects compared to benzodiazepines like clonazepam (klonopin) and alprazolam (xanax).
diazepam is considered to have low toxicity. however, it has moderate abuse potential and produces physical and psychological dependence with extended use. additionally, it can contribute to death by respiratory depression if combined with alcohol, opiates, and other depressants. it is highly advised to use harm reduction practices if using this substance.
it should be noted that the sudden discontinuation of benzodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death. it is highly recommended to taper one’s dose by gradually lowering the amount taken each day for a prolonged period of time instead of stopping abruptly.
history and culture
following chlordiazepoxide (librium), which was approved for use in 1960, diazepam was the second benzodiazepine invented by leo sternbach of pharmaceutical company hoffman-la roche. released in 1963 as an improved version of librium, diazepam became incredibly popular and quickly surpassed it in sales, helping roche to become a pharmaceutical industry giant. after this initial success, other pharmaceutical companies began to introduce other benzodiazepine derivatives.
the benzodiazepines gained popularity among medical professionals as an improvement over barbiturates, which have a comparatively narrow therapeutic index, and are far more sedative 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 opioids). benzodiazepine drugs such as diazepam initially had widespread public support, but with time the view changed to one of growing criticism and calls for restrictions on their prescription.
marketed by roche using an advertising campaign conceived by the william douglas mcadams agency under the leadership of arthur sackler, diazepam was the top-selling pharmaceutical in the united states from 1969 to 1982, with peak annual sales in 1978 of 2.3 billion valium tablets. 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.
diazepam is a drug of the benzodiazepine class. benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at r1 and r4. at r1, diazepam is substituted with methyl group. further, the benzodiazepine ring is bonded at r5 to an aromatic phenyl ring. the benzyl ring of the bicyclic core is substituted at r7 with a chlorine group. diazepam also contains an oxygen group double bonded to r2 of its diazepine ring to form a ketone. this oxygen substitution at r2 is shared with other benzodiazepine drugs with the suffix -azepam.
benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (gaba) by acting on its receptors. as this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of diazepam on the nervous system.
the anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.