Evidence Based
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Etizolam: Potential Uses, Mechanisms, and Medical Controversies

Written by Puya Yazdi, MD | Last updated:
Jonathan Ritter
Matt Carland
Medically reviewed by
Jonathan Ritter, PharmD, PhD (Pharmacology), Matt Carland, PhD (Neuroscience) | Written by Puya Yazdi, MD | Last updated:

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Etizolam is a drug that is chemically quite similar to benzodiazepines. It has been used in some countries to help treat anxiety and panic disorders, although it is not and has never been FDA-approved for medical use in many countries, including the United States. What’s the story behind this drug, and why do medical practitioners tend to avoid it? Read on to learn more about this drug, how it works, and why many people consider it to be risky!

Disclaimer: This post is not a recommendation or endorsement for etizolam. This medication has not been FDA-approved for any medical uses in the United States, and also cannot be legally prescribed or purchased in many other countries as well. We have written this post for informational purposes only, and our goal is solely to inform people about the science behind etizolam’s effects, possible mechanisms, and associated risks.

What is Etizolam?

Etizolam is similar to benzodiazepines, although it has a slightly different chemical structure, making it a “thienodiazepine” (for the chemistry afficionados out there, this means its molecule contains a “thiophene ring” as opposed to a “benzene ring”).

It also has generally similar effects to benzodiazepines, such as reducing anxiety, alleviating convulsions, promoting unconsciousness and/or sleep (hypnotic/sedative effects), and relaxing the skeletal muscles [1].

Etizolam was originally developed in Japan during the early 1980s as a treatment for anxiety – especially for anxiety symptoms when they occur as a part of other major psychiatric disorders, such as depression, panic disorder, and generalized anxiety disorder (GAD). It also sometimes used for insomnia-related conditions, although this is relatively less common [1].

While this drug has been approved for medical applications in some countries – including Japan, Italy, and India – etizolam has not ever been approved by the FDA for medical use in the United States, where it remains “unscheduled”.

This means that it is not available to buy or use through a pharmacy – nor even can your doctor legally write a prescription for it.

At this point you might be wondering, if this drug has been approved in other countries, and is potentially effective, what’s up with its unusual legal status in other countries such as the US? In short, the answer to this has to do with the fact that etizolam is considered to have very high abuse potential [2, 3].

For example, etizolam is more easily absorbed and processed (metabolized) by the body. These chemical and molecular features cause its effects to be up to 6 times stronger than those of an identical dose of other chemically-related drugs, such as diazepam [1].

However, it’s in large part exactly because of this dramatically-increased potency that the medical establishment has some serious reservations about it [2, 3].

Anti-anxiety (anxiolytic) drugs – including benzodiazepines such as diazepam and opioids such as oxycodone and hydrocodone – are already some of the most widely abused prescription drugs out there, and their relatively widespread availability in countries in the US has played a major role in many ongoing addiction epidemics.

Since addiction is already a major social and public health issue with these types of drugs, you might be able to see now why the medical establishment would be hesitant to introduce a version of these drugs that is 6x stronger (and hence much more easily abusable).

Some researchers have reported that etizolam can sometimes be found and ordered online – but obviously this is not recommended. In addition to the well-established risks of abuse and addiction with this drug, buying unregulated substances online means you have no way of being sure what you’re actually getting, and could open yourself up to any number of significant dangers.

Mechanism of Action

Because etizolam is chemically structurally similar to benzodiazepines, its mechanisms are believed to be fairly similar as well.

The vast majority of etizolam’s main effects on anxiety and sleep most likely arise through the activation (agonism) of GABA receptors – particularly the GABAA receptor subtype [1, 2].

GABA is the primary “inhibitory” neurotransmitter used throughout the brain. Hence, medications that target this system can have therapeutic effects on symptoms like anxiety by effectively “shutting down” the regions of the brain responsible for producing these feelings.

That’s a simplified explanation, anyways. If you want to dive into more of the details and intricacies behind the GABAergic system and how it works – or some of the more common medical drugs and other compounds or supplements that deal with this system – we recommend checking out our dedicated SelfDecode posts on GABA and natural ways to increase it.

Potential Medical Uses of Etizolam (UNAPPROVED)

The following sections describe some of the research that has been done on the potential medical applications of etizolam.

However, keep in mind that while there is generally fairly strong evidence in favor of etizolam’s efficacy in several health conditions, it’s where its safety is concerned that the issues arise.

Etizolam’s lack of safety is generally why the following uses have not been approved by the FDA. Therefore, the information discussed throughout this post is provided for informational purposes only.

Fortunately, if you suffer from anxiety-related issues, there are a large number of safe and legal medication options to consider, as well as many “natural” or “complementary” strategies that can potentially be tried in addition to conventional medical treatment. By discussing your health and treatment options with your doctor, he- or she will be able to advise you on the overall safest and most effective treatment approaches based on your specific medical needs.

1) Treating Anxiety

According to a few double-blind studies, etizolam has been reported to be relatively effective at treating anxiety and depressive symptoms in human patients [4, 5].

For example, etizolam is reported to reduce anxiety, and has even shown some signs of being a potentially effective antidepressant [6].

Similarly, one double-blind study with 30 female subjects reported that etizolam was generally effective at reducing anxiety and depressive activity [7].

When paired with other treatments, it may also potentially alleviate symptoms of panic disorder [8, 9].

Once again, while the effectiveness of etizolam is not really in question, it’s the lack of safety – such as the very high risk for abuse and addiction – where etizolam falls short. If you believe you are experiencing significant symptoms of anxiety, talk to your doctor about many of the legal and safer alternatives to etizolam to find out the best treatment option for you.

Other Potential Uses of Etizolam (UNAPPROVED)

1) Pain

One early study has reported that etizolam may help alleviate pain for up to thirty minutes at a time, but that it is not the ideal form of treatment (especially compared to other pain-killing medications, which are generally more effective) [10].

In one study in young female patients, etizolam combined with a non-steroidal anti-inflammatory drug was reported to be a potentially effective treatment for tension-type headaches [11].

This drug has also been reported to be effective in treating pain related to irritable colon syndrome in patients with concurrent chronic anxiety conditions [12].

2) Vertigo

One early study has reported that low doses of etizolam reduced self-reported scores on evaluations of dizziness in patients with benign paroxysmal positional vertigo [13].

3) Elevated Blood Pressure

According to a single preliminary study, etizolam was reported to improve blood pressure indicators (systolic and diastolic blood pressure) in patients with elevated blood pressure (hypertension) [14].

Warnings and Cautions

In the few clinical studies that have been done with etizolam, it has been generally reported to be well-tolerated by most patients, and appears to produce relatively few side effects [15].

However, there have been several cases of toxicity, and the drug itself is also highly addictive [15, 3].

According to one report (case study), children may be at particular risk of negative reactions to etizolam, and may even show “paradoxical” reactions, such as stimulation-like effects (even though this drug normally has the exact opposite effect [16].

Genetics Related to Etizolam

CYP2C19

The CYP2C19 gene creates a protein that metabolizes etizolam. Specific genetic variants (‘AG’ and ‘AA’ genotypes) for the single nucleotide polymorphism (SNP) rs4244285 are poor metabolizers of etizolam. This mutation is also sometimes referred to as the “CYP2C19*2” polymorphism [17].

Takeaway

So, what can we conclude about etizolam? While it may have a few potentially useful therapeutic effects, the significant concerns about its safety – especially regarding its very high potential for abuse and addiction – have prevented it from being legally approved for any medical applications in most countries.

For this reason, it’s not legal to buy or even prescribe in many countries, including the US.

However, this is probably not such a bad thing: after all, for people with anxiety-related health conditions, there are still very many alternative medical treatments available out there which work essentially just as well, and which are also much less risky when it comes to the possibility of becoming addicted or dependent.

As always, if you think you may be experiencing anxiety-related symptoms, talk to your doctor so that he or she can help you determine the best treatment plan for your individual health needs.

About the Author

Puya Yazdi

Puya Yazdi

MD
Dr. Puya Yazdi is a physician-scientist with 14+ years of experience in clinical medicine, life sciences, biotechnology, and nutraceuticals.
As a physician-scientist with expertise in genomics, biotechnology, and nutraceuticals, he has made it his mission to bring precision medicine to the bedside and help transform healthcare in the 21st century.He received his undergraduate education at the University of California at Irvine, a Medical Doctorate from the University of Southern California, and was a Resident Physician at Stanford University. He then proceeded to serve as a Clinical Fellow of The California Institute of Regenerative Medicine at The University of California at Irvine, where he conducted research of stem cells, epigenetics, and genomics. He was also a Medical Director for Cyvex Nutrition before serving as president of Systomic Health, a biotechnology consulting agency, where he served as an expert on genomics and other high-throughput technologies. His previous clients include Allergan, Caladrius Biosciences, and Omega Protein. He has a history of peer-reviewed publications, intellectual property discoveries (patents, etc.), clinical trial design, and a thorough knowledge of the regulatory landscape in biotechnology.He is leading our entire scientific and medical team in order to ensure accuracy and scientific validity of our content and products.

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