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  • How Benzodiazepines Work | Pharmacology, Uses, & Risks

    Published on March 30, 2021

    When benzodiazepines like Librium and Valium came onto the scene in the early 1960s, they were revolutionary. 

    Not only was this new class of drugs effective in treating anxiety disorders and insomnia, but they were far safer than older drugs, like barbiturates, that were used for the same purpose.

    Unfortunately, while benzodiazepines are generally safe and have become one of the most commonly prescribed classes of drugs in the United States, they are not without risks or potential for abuse.

    To understand these risks, as well as the common side effects associated with benzodiazepine use and abuse, we need to first understand how benzodiazepines work inside the body.

     Benzodiazepine Pharmacology

    All benzodiazepine drugs, also known as benzos, share a similar chemical structure with minor differences that influence how quickly the particular drug is absorbed, it’s potency, and how long it lasts in the body. 

    Benzodiazepine Action

    In each case, the drug is absorbed into the bloodstream and transported to the brain, where it binds to GABA A receptors in your neurons and increases their excitability towards the gamma-aminobutyric acid (GABA) neurotransmitter. 

    This increases the effect of the GABA already in your body, leading to sedation, or a calming effect on your brain and central nervous system (CNS). 

    Effects Of Benzodiazepines

    Benzos are known as minor tranquilizers and have a variety of effects on the body related to relaxation, including:

    • sedative effects, a reduction in activity in your brain and CNS that leads to lower blood pressure, slowed breathing, and reduced heart rate
    • hypnotic effects, causing drowsiness or sleep
    • anxiolytic effects, decreasing the mental and physical effects of anxiety or stress
    • anticonvulsant effects, preventing or decreasing the severity of muscle spasms or convulsions
    • muscle relaxant effects, relaxing tight or tense muscles and decreasing overall muscle tone

    Uses Of Benzos

    Because benzodiazepines have such a wide range of effects, they are often used to treat a variety of different conditions. These commonly include:

    Anxiety Disorders

    Both short- and long-acting benzodiazepines are used to help control a wide-range of anxiety disorders and panic disorders, from chronic conditions to sudden panic attacks, by prompting the body to relax. However, they should not be used for more than a few weeks.

    Insomnia & Certain Sleep Disorders

    Insomnia, which is often co-occurring with anxiety disorders, is also commonly treated with benzodiazepines thanks to their calming effects. Generally, short-acting benzodiazepines with short-term effects are most effective for this purpose.

    Seizure Disorders

    Fast-acting benzodiazepines can help prevent injury and mitigate seizures by relaxing muscle tone before, during, and after seizure events, though other drugs are preferred for cases of long-term epilepsy. 

    Alcohol Withdrawal

    Long half-life benzodiazepines are commonly used to help control withdrawal symptoms during alcohol detoxification. This makes potentially severe withdrawal symptoms more tolerable, and can help reduce the risk of dangerous or even deadly complications.  


    Major depression is often treated with a combination of antidepressant drugs and benzodiazepines, a combination which has been shown to be more effective than antidepressants alone in improving depression in the first weeks of treatment.

    Differences Between Specific Benzodiazepines

    Benzodiazepines are often sorted by half life and potency. 

    Low potency, short half-life benzos include:

    • oxazepam (Serax)
    • temazepam (Restoril)

    High potency, short-half-life benzos include:

    • alprazolam (Xanax)
    • lorazepam (Ativan)
    • triazolam (Halcion)
    • midazolam (Versed)

    Low potency, long half-life benzos include: 

    • chlordiazepoxide (Librium)
    • clorazepate (Tranxene)
    • diazepam (Valium)
    • flurazepam (Dalmane and Dalmadorm)

    High potency, long half-life benzos include:

    • clonazepam (Klonopin)
    • flunitrazepam (Rohypnol, a common date rape drug that is illegal in the United States)

    Risks Associated With Benzodiazepine Abuse

    Use of benzodiazepines is associated with a variety of risks. These include:

    Adverse Effects

    Benzos drugs are often known to cause side effects ranging from lightheadedness and unsteadiness to memory issues, constipation, dry mouth, and a number of others.

    Intoxication & Overdose

    Taking larger quantities of benzodiazepines can increase their depressant effects, resulting in intoxication.

    They may also be taken with other drugs, especially alcohol and opioids, to increase or alter the experience, though this greatly increases the risk of dangerous overdose symptoms including respiratory depression, which can be fatal.

    Dependence & Tolerance

    Those prescribing benzodiazepines should only do so for short periods of time. After even just a few weeks of taking these drugs, it’s possible to develop physiological dependence, resulting in potentially serious and prolonged withdrawal symptoms when use is discontinued. 

    This risk is increased if the drug is abused in higher doses.

    Mental Health Effects

    Long-term effects of benzodiazepine abuse include an increased risk of memory and mental health issues including Alzheimer’s disease and dementia, vertigo, and other issues.

    Benzodiazepine Detox 

    If you or a loved one stops taking benzodiazepines after developing dependence, you should expect a period of potentially severe or even dangerous withdrawal symptoms while your body adjusts. This may include suicidal ideation.

    Ark Behavioral Health provides a variety of rehabilitation services to help support you through every stage of this process. To learn more, please contact us today.

    Written by Ark Behavioral Health Editorial Team
    ©2022 Ark National Holdings, LLC. | All Rights Reserved.
    This page does not provide medical advice.

    Harvard Health - Benzodiazepines (and the alternatives)
    Drug Enforcement Administration (DEA) - Drug Fact Sheet: Benzodiazepines
    U.S. Food and Drug Administration (FDA) - FDA requiring Boxed Warning updated to improve safe use of benzodiazepine drug class

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