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Benzodiazepines Mechanism Of Action: Why Learn How It Works?

Last Updated: December 18, 2019

Authored by Sharon Levy, MD, MPH

Benzodiazepines belong to a category of drugs known as CNS (central nervous system) depressants. Also called benzos, these drugs are commonly prescribed for a broad range of health issues, more specifically sought for its muscle relaxing, antiepileptic, and anti-anxiety effects.
Despite its potential benefits, failure to understand benzodiazepines mechanism of action or ignoring drug interactions can seriously endanger a patient’s life, with a high potential for overdose leading to death. Based on figures revealed by the National Institute on Drug Abuse, about a third of all cases of opioid overdose also involve benzos.
Learn more about benzodiazepines mechanism of action and pharmacology to understand how taking this drug can be beneficial and risky for a patient at the same time.

How Do Benzodiazepines Work?

Benzodiazepines mechanism of action is inhibitory. That means they slow down the activity of neurons located in the central nervous system. Benzodiazepines mechanism of action work by the following:

  • First, benzos target the GABA-A (gamma-aminobutyric acid) receptors. GABA-A receptors function by inhibiting synapses that enable movement, anxiety, and other active brain activities.
  • Second, benzodiazepines improve the binding of GABA to GABA-A receptors, thereby enhancing the inhibitory effect of GABA.
  • Third, they help open up chloride channels, permitting more chloride ions to enter the neuron. As a result, the neuron becomes less responsive to becoming excited.

It makes benzos effective for delivering the following therapeutic results:

  • Improve the quality of sleep
  • Lessen anxiety
  • Decrease the intensity and frequency of tremors
  • Promote muscle relaxation
  • Reduce panic attacks
  • Block or reduce pain associated with outpatient medical and dental procedures

Benzodiazepines Pharmacokinetics

Benzodiazepines structure is characterized to be a combination of a benzene ring and a diazepine ring. It is consistent across different types, and all deliver their therapeutic benefits by increasing GABA receptor activity, which, in turn, inhibits neuron function. This results in a calming effect. However, it may be differentiated based on benzodiazepines pharmacology. Using the half-life of benzodiazepines as a critical differentiator, benzos are further broken down into three sub-divisions.

Various types of benzos in pills and capsules.

Based on the pharmacokinetics of benzodiazepines, these drugs may be grouped into the following:

Short-Acting Benzodiazepines

This class of benzodiazepines consists of drugs belonging to the following generic classes, abbreviated as “ATOM” drugs:

Intermediate-Acting Benzos

Benzos that behave this way include drugs falling under the following generic names, abbreviated as “FuN TLC”:

Long-Acting Benzos

Drugs that fall under the following generic names of benzos are considered long-acting:

  • Flurazepam
  • Diazepam
  • Chlordiazepoxide
  • Clorazepate

Barbiturates Vs. Benzodiazepines Mechanism Of Action

Barbiturates precede benzodiazepines, then a new class of drugs that have only been introduced in the market in the early years of the 1960s. At the time of its launch, the mechanism of action of benzodiazepines were deemed safer and more effective than barbiturates. Medical professionals deem that benzos continue to be safer even when compared to other newer alternative tranquilizers and sedatives.

Two blisters of barbs and benzos on blue background
In fact, benzos are generally classified under Schedule IV of controlled substances, which indicates a low potential for abuse.

Benzodiazepines Precautions

Based on the benzodiazepines mechanism of action, benzos can be beneficial in many ways if taken with care. Keep in mind that benzos build tolerance, and with it, drug dependence may follow. Benzos can also lead to lethal drug overdose and other life-threatening symptoms, including lowered blood pressure and slowed breathing.

Portrait Of Smiling Female Doctor
Here are some important points on how to practice care when using benzos:

  • Inform the attending physician of all medicines and supplements being taken at the time of prescription. Drug interaction is possible with benzos and can be even lethal when combined with opioids.
  • Taking benzos while pregnant may lead to abortion. Make sure to rule out possible pregnancy before taking benzos.
  • Take them only in a prescribed route of administration. Do not crush, snort, or use in any other way.
  • Doctor prescribed frequency and dosage must be strictly followed.
  • Use benzos only for the duration recommended by a medical professional. Extended use of benzodiazepines may inevitably lead to a substance use disorder.
  • Be vigilant with any change or symptom of addiction that may develop while using these drugs. Make sure to discuss it with a qualified professional.

In case benzo dependence is suspected, the person affected must immediately seek professional support and treatment for addiction.
Abrupt benzodiazepines withdrawal may be risky, dangerous to health, and possibly lead to life-threatening conditions.

Page Sources

  1. National Institute on Drug Abuse, Benzodiazepines and Opioids,
  2. Harvard Health Publishing, Benzodiazepines (and the alternatives),
  3. U.S. DEPARTMENT OF JUSTICE, Controlled Substance Schedules,

Published on: December 5th, 2019

Updated on: December 18th, 2019

About Author

Sharon Levy, MD, MPH

After successful graduation from Boston University, MA, Sharon gained a Master’s degree in Public Health. Since then, Sharon devoted herself entirely to the medical niche. Sharon Levy is also a certified addiction recovery coach.


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