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The Benzodiazepine Class of Research Chemicals

The Benzodiazepine Class of Research Chemicals

The family of research chemicals called the Benzodiazepines, BZDs and ‘benzos’, are a class of psychoactive compounds which all share a common feature – a diazepine ring fused with a benzene ring.

The first benzodiazepine drug was discovered in the mid-1950s by Leo Sternbach, and was first marketed in the early 1960s. The most famous benzodiazepine, Valium (benzodiazepine diazepam) was first prescribed in 1963. Just fourteen years later, benzodiazepines were the most prescribed family of drugs worldwide.

Benzodiazepines work by increasing the effect of a aeurotransmitter called GABA (gamma-aminobutyric acid) upon a receptor named after it, the GABAA receptor. The classic effects of the benzodiazepine class of chemicals are:

  • Anticonvulsant properties
  • Reduction of anxiety
  • Relaxation of skeletal muscles
  • Sleep (hypnotic properties)

Common side effects of high doses are dissociation and anterograde amnesia (the temporary loss of ability to form memories), aggression and disinhibition of some undesirable behaviours.

Due to these properties, various benzodiazepines have been used to treat such disorders as:

  • Agitation
  • Anxiety
  • Insomnia
  • Muscle spasm
  • Seizure disorders
  • And even alcohol withdrawal

There are three categories of benzodiazepines: short, intermediate and long-acting. The longer acting class is commonly used for treating anxiety disorders, whist the short and intermediate classes are more commonly prescribed for insomnia. Most benzodiazepines are considered safe for short term use, though they can be habit forming.

Long term use of many benzodiazepine chemicals can result in decreasing effectiveness (tolerance) various physical or psychological side effects, and even physical dependence (addiction) and withdrawal symptoms. The elderly are generally at higher risk of these side effects than younger patients.

Overdose of benzodiazepines is likely to cause deep unconsciousness, and can certainly be dangerous, but they are considered much less toxic than barbiturates, which they have largely replaced. When combined with central nervous system depressants, like any of the opioids or alcohol, the likelihood of fatal overdose skyrockets. As these chemicals are often taken in combination with these drugs, this danger should not be overlooked.

 

Benzodiazepines - Pharmacology

Benzodiazepines are all linked by a similar overall chemical structure, so they share a common pharmacology. Most benzodiazepine-related effects rely on allosteric effects on the GABAA receptor, increasing its inhibitory effects. This is the core of the benzodiazepine family’s beneficial and harmful effects alike.

GABA works to reduce the excitability of neural connections by binding to the GABAA receptor, and making the neuron less likely to be stimulated.

Essentially, this family of research chemicals makes the function of existing GABA more efficient. The result is that communication between neurons is both slowed and reduced in volume, and many of the brain’s systems and processes are calmed.

The reason different benzodiazepines have so many varying effects is that there are many different types of GABAA receptors in the brain, and each responds differently to different BZDs. Particular neural ‘circuits’ tend to have particular types of receptors, so different processes are reduced by different BZDs, resulting in different psychoactive effects in the subject. However, all GABAA receptors respond to all BZDs to some degree, so it is virtually impossible to isolate one type of effect using benzodiazepines