How do Benzodiazepines Work and What Are They Used For?

Benzodiazepines are a class of psychoactive drugs, meaning that they change your mental state by altering the way your brain and nervous system function. Created in the 1960’s, benzodiazepines are still some of the most widely prescribed class of medications today.

The primary effects of all benzodiazepines are:

• Hypnotic (sleep)

• Anxiolytic (anxiety)

• Anti-seizure (reduce seizures and convulsions)

• Muscle relaxant (reduce pain and tension)

• Amnesic (tends to affect long and short term memory).

Benzos have a relaxing calming effect and are most commonly used for anxiety though there are many reasons doctors prescribe them, including panic attacks, depression, seizures, convulsions, insomnia, muscle tension, general anesthesia and sedation for surgery.

Types of benzodiazepines

Here is a list of various types of Benzodiazepines:

• alprazolam (Xanax, Xanax XR, Xanor, Tafil)

• bromazepam (Lexotan, Lexomil)

• chlordiazepoxide (Librium, Nova-Pam)

• clobazam (Frisium)

• clonazepam (Klonopin, Rivotril)

• clorazepate (Tranxene)

• diazepam (Valium, D-Pam, Pro-Pam)

• estazolam (Prosom is a discontinued brand in the US)

• flunitrazepam (Rohypnol)

• flurazepam (Dalmane)

• halazepam (Paxipam)

• ketazolam (Anxon)

• loprazolam (Dormonoct)

• lorazepam (Ativan, Tavor, Temesta)

• lormetazepam (Noctamid)

• midazolam, (Versed, Hypnovel, Dormicum)

• nitrazepam (Mogadon, Insoma, Nitrados)

• oxazepam (Serax (discontinued in the US, Serapax, Serenid, Benzotran)

• prazepam (Centrax)

• quazepam (Doral)

• temazepam (Restoril, Euhypnos, Normison, Sompam)

• triazolam (Halcion, Hypam, Tricam)

Some less common benzos include adinazolam, bretazenil, brotizolam, camazepam, cinolazepam, clotiazepam, cloxazolam, delorazepam, etizolam, fludiazepam, haloxazolam, oxazolam, nimetazepam, nordazepam, phenazepam, pinazepam, tetrazepam, tofisopam. Also Librax / Libraxin (a combination of chlordiazepoxide and clidinium).

Short or long acting?

Benzos are usually classified by how long they take to work and stay in your system. They include:

• Short-acting - These include drugs like Versed (used prior to surgery for anxiety), Halcion (for insomnia) and Tranxene (anti-anxiety).

• Intermediate-acting – Drugs including Xanax and Ativan as well as Restoril and Klonopin fall into this category.

• Long-acting – Valium and Librium are examples of long-acting benzos.

On one end of the benzo spectrum, your body reacts quickly to the short acting drugs, so you feel the effects quickly and they rapidly leave your system.  On the other end, the long-acting drugs take more time to produce the stated effects but remain in your system over a much more significant amount of time. This leads to a discussion of half lives, which is very important when tapering your benzo.

What are neurotransmitters?

The exact mechanism of action of benzodiazepines is not fully understood, but it’s widely believed they work by affecting neurotransmitters in the brain.

Neurotransmitters are chemicals that nerves release in order to communicate with other nearby nerves. 

Neurotransmitters tell your heart to beat, lungs to breathe, and stomach to digest and so on.

They play a major role in shaping our everyday life and controlling our bodily functions.

Currently more than 100 chemical messengers have been uniquely identified.

Neurotransmitters can be classified by their function:

• Excitatory - these have an excitatory effect on the neuron - creating stimulating effects in the body.

• Inhibitory - these have inhibitory effects on the neuron - producing calming effects in the body.

• Modulatory - these are sometimes called neuromodulators and they are capable of affecting a large number of neurons at once.

Some neurotransmitters can create both excitatory and inhibitory effects depending upon the type of receptors that are present.

In order to try to understand how Benzodiazepines work, we first need to learn about the neurotransmitters glutamate and gamma-aminobutyric acid (GABA).

GABA and glutamate

• GABA and glutamate are the major neurotransmitters in our brains. They have a complex and interconnected relationship. Both have important roles to play in many aspects of our physical and mental health. They are supposed to work together, in a homeostatic relationship.

• GABA is inhibitory (calming) and glutamate is excitatory (stimulating).

• GABA and glutamate work together to control many processes, including the brain’s overall level of excitation. Like all neurotransmitters, too much or too little of either one can create issues.

• High levels of GABA produce can produce sedation and relaxation, while high levels of glutamate can produce anxiety, fear, insomnia and stress.

• When you’re low in GABA, your mind gets stuck in the “on” position and you might find yourself overstimulated, overwhelmed and anxious. Using a car as an analogy, the same way your gas pedal and brakes in your car work together to control speed, GABA puts the brakes on brain activity to counter the gas pedal effects of glutamate.

benzos are minor tranquilizers

It is thought that benzodiazepines work by enhancing the effect of the neurotransmitter GABA.

This enhancing effect occurs at the GABA-A receptor, essential triggering a tranquilizing chemical in your brain.

In other words, they depress the activity of your central nervous system (CNS), producing hypnotic, sedative, muscle relaxant, anti-anxiety, and anticonvulsant effects.

Put simply, when you feel stressed or anxious, your brain becomes overexcited and GABA is a neurotransmitter that slows down that activity, calming your brain.

Benzos increase these effects, keeping your brain in a tranquilized state.

It is believed that benzo withdrawal symptoms stem in part from a decreased GABAergic calming/inhibitory function and an increase in glutamatergic stimulating/excitatory function.