Benzodiazepines

The core structure of benzodiazepines

Benzodiazepines (also referred to as benzos) are psychoactive drugs that act as central nervous system depressants. These drugs work by magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors. The prominent effects of benzodiazepines include sedation, muscle relaxation, disinhibition, and amnesia. Short-acting benzodiazepines are recommended for treating insomnia while long-acting ones are recommended for the treatment of anxiety disorders.

Chemistry

Benzodiazepine is a heterocyclic compound comprised of a benzene ring fused to a diazepine ring. Benzodiazepine drugs are substituted 1,4-benzodiazepines with different side groups attached to the central structure.

Pharmacology

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site on the GABAA receptor and modulating the function of the GABA receptor, the most prolific inhibitory receptor within the brain. The GABA chemical and receptor system mediates inhibitory (or calming effects) of alprazolam on the nervous system.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects. These effects are listed and defined in detail within their own dedicated articles below:

• Sedation
• Amnesia
• Thought deceleration
• Disinhibition
• Motor control loss - Lack of coordination may result in falls and injuries, in particular, in the elderly. Another result of motor control loss is the impairment of driving skills and the increased likelihood of road traffic accidents.
• Muscle relaxation
• Delusions of sobriety - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others.
• Physical euphoria
• Information processing suppression
• Dizziness

Paradoxical effects

Paradoxical reactions such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%). These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.

Examples

• Alprazolam
• Clonazepam
• Clonazolam
• Diazepam
• Diclazepam
• Flubromazolam
• Flubromazepam
• Nifoxipam
• Lorazepam
• Phenazepam
• Pyrazolam
• Temazepam
• Zopiclone

Toxicity and harm potential

Radar plot showing relative physical harm, social harm, and dependence of benzodiazepines in comparison to other drugs.

Lethal dosage

The median lethal dosage varies wildly between specific substances within the benzodiazepine class. It is because of this that one should always fully research the substance before administering it to themselves or others.

Tolerance and addiction potential

Tolerance will develop to the sedative-hypnotic effects within a couple of days. Withdrawal symptoms or rebound symptoms may occur after ceasing treatment abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.

Discontinuation

It is notoriously difficult to discontinue use of benzodiazepines, and potentially life threatening for tolerant individuals using regularly to do so without tapering their dose over a period of weeks. Benzodiazepines are positive allosteric modulators of GABA receptors, so as the brain is calibrated to operate with higher than usual inhibition, the number of GABA receptors expressed is reduced via downregulation. Abrupt discontinuation following chronic use of benzodiazepines causes rebound stimulation which presents as anxiety, insomnia and restlessness while the body attempts to return to homeostasis.

There is an increased risk of seizure following discontinuation of benzodiazepines. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal. It is safest to reduce the dose each day by a very small amount, for a couple of weeks until close to abstinence. If using a short-half life benzodiazepine, a longer acting variety such as diazepam can be substituted. Symptoms may still be present, but their severity will be reduced significantly. Small amounts of ethanol can also help to reduce the symptoms.

Duration and severity of symptoms depends on a number of factors including the half life of the drug used, tolerance and the duration of abuse. Major symptoms will usually start within just a few days after discontinuation and persist for around a week for shorter lasting benzodiazepines. Benzodiazepines with longer half-lives will exhibit discontinuation symptoms with a slow onset and extended duration.

Recipes and preparation methods

• Benzodiazepine solution - if one's benzos are in powder form they are unlikely to weigh out accurately without the most expensive of scales due to their extreme potency. To avoid this one can dissolve the benzodiazepine volumetrically into a solution and dose it accurately based upon the methodological instructions linked within this tutorial here.

See also

• Understanding Benzodiazepines by Steven M. Juergens MD
• Psychoactive substance index
• Entactogens
• Etizolam
• Stimulants
• Hallucinogens
• Depressants