Benzodiazepines
Learn more about benzodiazepines, the central nervous system depressants among the most commonly prescribed drugs in the world.
Overview
Common Nicknames
Vallies, jellies, blues, and benzos
Drug Class
Depressant
Drug Form
Pills
Route of Administration
Swallowed
What is the science of Benzodiazepines?
Benzodiazepines quickly diffuse through the blood-brain barrier and primarily work by interacting with GABA-A receptors. These receptors are special proteins in the brain that help regulate nerve activity. They are activated by a chemical called gamma-aminobutyric acid (GABA), which is the main neurotransmitter responsible for calming down nerve signals in the central nervous system.
Benzodiazepines bind at a site that is distinct from the GABA binding site, increasing the affinity of GABA to the receptor and potentiating the response of the receptor to GABA. The potentiation of the effects of GABA, which works as a depressor on the central nervous system, causes sedative effects.
Because of their quick diffusion and influence on the inhibitory neurotransmitter GABA, benzodiazepines have rapid sedative effects, causing relaxation. This makes them attractive medications for those struggling with sleep and anxiety.
What are the risks?
Benzodiazepines are considered relatively safe to use in the treatment of a variety of disorders. However, due to the development of tolerance, which causes users to need increasing doses for the same symptom relief, there is a severe potential for dependence. This is why benzodiazepines are usually not recommended to use for longer than four weeks.
When benzodiazepines are taken in high doses, they can cause unpleasant and potentially harmful effects. Overdosing can lead to slurred speech, dizziness, hostile or erratic behaviour, and impaired motor coordination. Impaired motor coordination can increase the risk of fall and injuries, and the risk of traffic accidents.
In more severe cases, overdosing can lead to depressed breathing and loss of consciousness. This can happen from benzodiazepines alone, but often arises from a combination with other sedatives like alcohol or opioids. Combining benzodiazepines and opioids increases the risk of non-fatal and fatal overdose, particularly due to respiratory depression.
As benzodiazepines can cause anterograde amnesia, which is the inability to form new memories after taking the drug, in combination with their sedative effects, they are commonly associated with drug-facilitated sexual assaults (DFSA).
In some cases, the use of benzodiazepines has been associated with a higher risk on suicide attempt and suicide. Benzodiazepines are known to increase impulsivity and aggression, traits that can lead to a dissociated type of aggression and impulsive actions that elevate the risk on suicidal behaviour. While benzodiazepines are useful for acute symptom relief in anxiety and insomnia, their potential to increase suicide risk calls for careful use, especially in patients with coexisting mental health issues.
How might the drug make you feel?
Benzodiazepines calm the nervous system, which reduces anxiety, relaxes the mind and muscles, and decreases alertness and concentration. Common side effects are drowsiness, lethargy, and fatigue. Another common side effect is anterograde amnesia, which is the inability to form new memories after taking the drug. In higher doses, the sedative effects of benzodiazepines become stronger. They can then cause impaired motor coordination, dizziness, slurred speech, blurry vision and mood swings.
For some people, benzodiazepines can cause paradoxical or disinhibitory reactions. Characteristic symptoms are excessive talkativeness, increased activity level, excitement, agitation, aggression and confusion. Important risk factors for paradoxical effects are older age and dementia, but also history of alcohol use and affective disorder have been associated with a higher risk of paradoxical effects from benzodiazepines.
Is Benzodiazepines addictive, and what are the long-term effects?
One-off, occasional or short-term use of benzodiazepines is unlikely to result in the development of dependence. However, when the substance is being used for a longer period, users can develop a physical and psychological addiction. The main driving factor for dependence is the development of tolerance, as users need higher doses for the same symptom relief.
There are two main groups of people who develop benzodiazepine dependence. The first group consists of people who sought medical help during increased anxiety or sleeplessness, but continued using the medication beyond the recommended time-frame or at doses outside the recommended range. The second group consists of people actively seeking out the sedative effects of benzodiazepines, as benzodiazepine dependence is often accompanied by dependence on other substances and / or alcohol. In this case, benzodiazepines are abused to reduce the withdrawal effects of the other substances and to enhance or prolong the effects of the other substance.
Short-acting and high-potency benzodiazepines (like Xanax) are more addictive than long-acting benzodiazepines (like Valium). People who suffer from a substance use disorder are at higher risk of developing benzodiazepine dependence.
Harm Reduction and Drug-Drug Interactions
Short-term, occasional medical or recreational use of benzodiazepines has a relatively low risk of harm. However, there are dangerous sides to the use of benzodiazepines, especially when they are mixed with other substances or when they are taken in higher doses or for longer periods than subscribed.
A first sign of the possible development of benzodiazepine dependence is when you start developing a tolerance for the substance’s effects. In order to avoid developing dependence, it is advised to not take benzodiazepines for longer than four weeks.
It is not advised to combine benzodiazepines with other substances. When you are mixing them, it is important to be aware of the potential risks. Combining benzodiazepines with substances that are also central nervous system depressants, like alcohol and opioids, can lead to a greater risk of severe sedation, respiratory depression, coma, or even death. Combining benzodiazepines with stimulants, like speed and cocaine, leads to a greater risk of taking high doses or overdosing, as the substances can mask each other’s effects.
When someone is overdosing on benzodiazepines it is important to help them, as overdosing can lead to depressed breathing and loss of consciousness. When you notice slower breathing or unconsciousness, there are a few things you should do:
Place the person on their side so that their airway is not blocked if they vomit.
Do not leave the person alone, as their condition might get worse.
Monitor the person and if they a) become unresponsive; b) vomit while unconscious; or c) have slow breathing, make sure to call emergency services.
Let the medical team know what the person has taken, if you know.
Medical Uses
Benzodiazepines are used in general medicine, psychiatry, neurology, internal medicine, and in the field of anaesthesia, for the treatment of many clinical disorders.
Due to their sedative effects calming the nervous system, benzodiazepines are used short-term to treat sleep problems (hypnotics) and anxiety disorders (anxiolytics). They are also used to ease distress, panic, and fear.
Benzodiazepines also relax muscles and have anticonvulsant effects, which makes them useful in treating the withdrawal effects of alcohol, where they work to ease agitation as well as preventing seizures, muscle spasms and shaking. Due to this anticonvulsant effect, it can be used for people with epilepsy.
Benzodiazepines are preferred medicines for so many clinical disorders because of their fast state of action, efficiency, low number of collateral effects, and minimal acute toxicity in comparison to other medications. However, due to the risk of both mental and physical addiction, they are often not used long term.
Myths and Misconceptions
Benzodiazepines are safe for long-term daily use
While effective short-term, tolerance develops within weeks and long-term use increases risks of dependence and cognitive impairment. Clinical guidelines recommend limiting use to 2-4 weeks due to diminishing benefits and accumulating harms.
Mixing benzodiazepines with alcohol is just extra sedating
Combining benzodiazepines and alcohol dramatically increases overdose risk through synergistic respiratory depression. This combination is involved in a significant proportion of fatal overdoses and emergency department visits, as both substances enhance each other's depressant effects unpredictably.