Brotizolam (Lendormin): Uses, Safety, & Harm Reduction Tips

By Jermaine Walters Last Updated: November 02, 2022
Last Updated: November 02, 2022
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Brotizolam is a sedative and hypnotic drug in the benzodiazepine family. It also possesses anticonvulsant and anxiolytic properties.

Brotizolam is one of the most potent yet well-tolerated hypnotic drugs currently available. It’s active at sub-milligram doses (roughly 50 times more potent than diazepam (Valium). 

The main advantages of brotizolam are its short half-life, low dosage, and fast-acting sedative effects. Studies show that brotizolam can decrease the latent period for sleep, reduce the number of awakenings, and increase the overall duration of sleep [1].

Like most benzodiazepines, brotizolam is prescribed only for a short period. Long-term use of brotizolam, or other benzodiazepines, carries a high risk of dependence [2].

The powerful nature and wide availability of this drug also make it a popular option for recreational use. It’s often combined with stimulants like cocaine, methamphetamine, or MDMA to counteract the sedative action and bring out the intoxicating profile inherent to most benzodiazepines. 

Brotizolam Specs

StatusApproved 💊
Common Dosage0.125–0.25 mg
PubChem ID2451
CAS#57801-81-7

IUPAC Name: 2-Bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine

Other names: Lendormin, Lindormin, Goodmin, Brometon, Sorentmin

Metabolism: Before renal excretion, Brotizolam is metabolized almost completely into hydroxylated compounds, 1-methyl-hydroxy- and the 4-hydroxy-derivatives.

Duration of Effects: Brotizolam is a short-acting sedative drug with a half-life of about 4.4 hours [3]. 

What is the Dose of Brotizolam?

The usual dose of brotizolam is 0.25 mg once daily for up to 2 weeks (for insomnia). It’s available in tablet form in doses of 0.125 mg, 0.25 mg and 0.5 mg [2].

Compared to other benzodiazepines, brotizolam is very strong — roughly equivalent in potency to triazolam (Halcion), twice times as potent as alprazolam (Xanax), and 50 times as strong as diazepam (Valium)

Dosage Equivalent Calculator: Brotizolam

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**Caution:** Benzodiazepines have a narrow therapeutic window. Dose equivalents may not be accurate in higher doses.

This calculator does not substitute for clinical experience and is meant to serve only as a reference for determining oral benzodiazepine equivalence.

Please consult a medical practitioner before taking benzodiazepines.

How Does Brotizolam Work?

Brotizolam is a central nervous system depressant. It lowers the brain’s electrical activity by binding to gamma-aminobutyric acid (GABA) receptors [2].

GABA is one of the most important inhibitory neurotransmitters that act by binding to specific GABA receptors in the central and peripheral nervous system. When GABA or other compounds with similar chemical structure binds to GABA receptors, it reduces neuronal transmission [4].

There are three types of GABA receptors: GABA-A, GABA-B, and GABA-C receptors. Among these, GABA-A receptors are the major binding site of most benzodiazepines. Brotizolam also has a similar structure as clonazepam, which falls under 1,4-benzodiazepines. Therefore, the mechanism of action of brotizolam is highly similar to that of clonazepam, with both drugs binding to GABA-A receptors [5]. 

Brotizolam acts with a similar mechanism as clonazepam. Although definitive studies on its action on GABA receptors are lacking, it is believed to act as a positive allosteric modulator on the γ-amino butyric acid (GABA)-A receptor. It binds to the α and γ subunits of the GABA receptor, which causes a conformational change in the receptor’s chloride channel resulting in hyperpolarization. This increases the affinity of GABA to GABA receptors, thereby enhancing its inhibitory effects. This activity of brotizolam is responsible for its sedative, hypnotic, and anxiolytic effects [6]. 

Is Brotizolam Safe? Risks & Side Effects

The adverse effects of brotizolam are similar to that of short-acting benzodiazepines. The most common side effects include drowsiness, dizziness, tinnitus (ringing in the ears), dry mouth, difficulty concentrating, and headaches. Brotizolam does not affect the respiratory and cardiovascular system like other drug classes (namely opiates).

Brotizolam is highly addictive and should not be used for more than two weeks at a time. The more frequently one takes brotizolam, the more likely they are to need it. Once dependency forms, the original symptoms the drug was used to treat become much worse. Users dependent on brotizolam experience severe anxiety, insomnia, muscle tension, and mood swings whenever the effects of the drug wear off. 

The risks of overdose on brotizolam alone are low. However, the risk increases dramatically when combined with other drugs or alcohol. 

Common Side Effects Of Brotizolam

The side effects of taking brotizolam within the recommended dosage range are generally mild.

You should consult your doctor if these side effects persist or hamper day-to-day activities.

Side effects of brotizolam may include:

  • Drowsiness
  • Dizziness
  • Headache
  • Blurring of vision
  • Dizziness
  • Decreased sex drive
  • Frequent urination
  • Increased salivation
  • Lightheadedness
  • Low mood
  • Muscle weakness
  • Problems with thinking and memory
  • Sleep disturbance with vivid dreams
  • Unsteadiness and problems with balance

Serious side effects of brotizolam include:

  • Difficulty breathing
  • Jaundice
  • Amnesia (memory loss)
  • Hallucinations
  • Liver failure
  • Excessive bleeding
  • Suicidal thoughts
  • Anaphylaxis (severe allergic reaction)

These side effects are rare. If you experience any of these side effects, you need to tell your doctor immediately.

Harm Reduction Tips: Brotizolam

Brotizolam carries a high risk of tolerance and dependence. The key to avoiding this issue is to avoid using the drug for more than two weeks and follow the recommended dosage schedule provided by your doctor. 

Recreational use of brotizolam can lead to problems with addiction and abuse in subtle ways you may not notice until it’s too late. Consider why you’re using the drug, whether or not your relationship with this substance is healthy, or if you’re seeking the drug as an escape from other, more complicated problems.

Accidental injury is also common while using benzodiazepines. It’s wise to avoid driving or operating heavy machinery after taking benzos like brotizolam.

Brotizolam may enhance the effect of centrally acting drugs, including neuroleptics, tranquilizers, antidepressants, hypnotics, antiepileptics, antihistamines, analgesics, and anesthetics. It may also increase the effect of muscle relaxants. Combining brotizolam with alcohol, GHB, phenibut, Z-drugs, barbiturates, or other sedative medications can lead to overdose and death. 

Benzodiazepine Harm Reduction Tips:

  1. 🥣 Don’t mix — Mixing benzodiazepines with other depressants (alcohol, GHB, phenibut, barbiturates, opiates) can be fatal. 
  2. ⏳ Take frequent breaks or plan for a short treatment span — Benzodiazepines can form dependence quickly, so it’s important to stop using the drug periodically.
  3. 🥄 Always stick to the proper dose — The dosage of benzos can vary substantially. Some drugs require 20 or 30 mg; others can be fatal in doses as low as 3 mg.
  4. 💊 Be aware of contraindications — Benzodiazepines are significantly more dangerous in older people or those with certain medical conditions.
  5. 🧪 Test your drugs — If ordering benzos from unregistered vendors (online or street vendors), order a benzo test kit to ensure your pills contain what you think they do.
  6. 💉 Never snort or inject benzos — Not only does this provide no advantage, but it’s also extremely dangerous. Benzos should be taken orally. 
  7. 🌧 Recognize the signs of addiction — Early warning signs are feeling like you’re not “yourself” without the drug or hiding your habits from loved ones. 
  8. ⚖️ Understand the laws where you live — In most parts of the world, benzodiazepines are only considered legal if given a prescription by a medical doctor. 
  9. 📞 Know where to go if you need help — Help is available for benzodiazepine addiction; you just have to ask for it. Look up “addiction hotline” for more information where you live. (USA: 1-800-662-4357; Canada: 1-866-585-0445; UK: 0300-999-1212). 

Similar Benzodiazepines 

Brotizolam is a potent benzodiazepine analogue most closely related to nitrazepam, flunitrazepam, and triazolam. There are several other benzodiazepines with similar functions as that of brotizolam.

Brotizolam vs. Other Benzodiazepines

BrotizolamLorazepamFlurazepamTriazolam
Chemical CompositionTriazolothienodiazepineBenzodiazepineBenzodiazepineBenzodiazepine
Route of AdministrationOralOralOralOral
Onset of ActionFastSlowFastFast
Peak concentration1 to 2 hours1 to 2 hours0.5 to 1 hour1 to 2 hours
Duration of effectShort-actingIntermediate-actingLong-actingShort-acting
Mechanism of actionActs on GABA-A receptorActs on GABA-A receptorActs on GABA-A receptorActs on GABA-A receptor
Medical UsesInsomniaInsomnia, anxiety disorders, epilepsyInsomniaInsomnia
Source: Griffin, C. E., Kaye, A. M., Bueno, F. R., & Kaye, A. D. (2013).

Natural Alternatives To Benzodiazepines

There are a few natural alternatives to benzodiazepines that work by increasing the activity of GABA.

However, there are not enough studies to back them for therapeutic use. So, before using any natural alternative to clonazepam, it is best to consult your doctor.

Some natural alternatives to benzodiazepines include:

Lavender essential oil

Lavender oil (Lavandula spp.) has long been used in traditional medicine as a remedy for muscle spasms, insect bites, and infections. Recent findings suggest that it also possesses sedative, anxiolytic, anticonvulsant, and mood-stabilizing properties. Researchers believe that these effects may be due to antioxidant, anticholinergic, and neuroprotective activities. Also, it has minimal side effects and withdrawal symptoms [7].

Valerian Root

Valerian root (Valeriana officinalis) has been found to naturally increase the amount of gamma-aminobutyric acid (GABA) in the brain. Although it has been used for hundreds of years as a natural remedy for sleep disorders, it has only recently garnered interest from the scientific community for its sedative and hypnotic effects. So far, few studies on valerian root hypothesize that it both increases GABA release and acts on GABA-A receptors [8].

Kava

Kava (Piper methysticum) is a popular anxiolytic consumed in the form of tea. It is preferred by those seeking a natural remedy for insomnia as it is easily available and is not habit-forming. Researchers believe that its stress-relieving effects may be due to its action on GABA receptors [9]. 

Kava (Piper methysticum)

Gotu Kola 

Centella asiatica, also known as Gotu kola, is a herb with antiepileptic, anxiolytic, sedative, and antidepressant effects. Its neuroprotective and antiepileptic effects are believed to result from increased GABA activity in the central nervous system [10].

L-theanine 

L-theanine is one of the active compounds in green tea. The anxiolytic effects of green tea rely on a similar modulation of the GABA receptors found in benzodiazepines. However, unlike benzodiazepines, L-theanine is much less potent and doesn’t impair cognition, cause drowsiness, or intoxicate users [11].

Chamomile

Chamomile is a popular herb taken in the form of tea to treat sleep disorders, relieve anxiety, and provide relief from gastrointestinal issues. Its anxiolytic effects may be due to its ability to modulate important neurotransmitters in the central and peripheral nervous system, such as serotonin, GABA, noradrenaline, and dopamine [12].

Brotizolam FAQs

How will brotizolam make me feel?

Brotizolam lowers anxiety and can simulate a feeling of relaxation and sleepiness. When you first start this drug, you may feel drowsy and your sleep cycle may also be hampered.

How long does it take brotizolam to kick in?

Brotizolam is a short-acting drug with a fast onset of action. It starts showing its effects within 15 to 30 minutes. 

Will I become addicted after taking brotizolam?

If taken for a short time, the risk of drug dependence is low with brotizolam. But if you take it for a long period (more than two weeks or so), there is a high risk of addiction and abuse. 

Do I need to avoid any foods or drinks while taking brotizolam?

The desired effect of brotizolam is impaired by the consumption of food containing caffeine, such as coffee, tea, carbonated drinks, and chocolate. 

Consumption of alcoholic beverages while under the effects of brotizolam should be strictly avoided. Mixing alcohol with benzodiazepines carries a high risk of accidental injury and overdose. 


References

  1. Roehrs, T., Zorick, F., Koshorek, G. L., Wittig, R., & Roth, T. (1983). Effects of acute administration of brotizolam in subjects with disturbed sleep. British Journal of Clinical Pharmacology, 16(S2), 371S-376S.
  2. Langley, M. S., & Clissold, S. P. (1988). Brotizolam. Drugs, 35(2), 104-122.
  3. National Center for Biotechnology Information (2022). PubChem Compound Summary for CID 2451, Brotizolam. 
  4. DeVane, C. L., Ware, M. R., & Lydiard, R. B. (1991). Pharmacokinetics, pharmacodynamics, and treatment issues of benzodiazepines: alprazolam, adinazolam, and clonazepam. Psychopharmacology bulletin, 27(4), 463-473.
  5. Jenner, P., Pratt, J. A., & Marsden, C. D. (1986). Mechanism of action of clonazepam in myoclonus in relation to effects on GABA and 5-HT. Advances in neurology, 43, 629-643.
  6. Griffin, C. E., Kaye, A. M., Bueno, F. R., & Kaye, A. D. (2013). Benzodiazepine pharmacology and central nervous system–mediated effects. Ochsner Journal, 13(2), 214-223.
  7. Koulivand, L. the nervous system, Evid. Based Complement. Altern. Med, (2013), 681304.
  8. Gohil, K. J., Patel, J. A., & Gajjar, A. K. (2010). Pharmacological review on Centella asiatica: a potential herbal cure-all. Indian journal of pharmaceutical sciences, 72(5), 546.
  9. Chua, H. C., Christensen, E. T., Hoestgaard-Jensen, K., Hartiadi, L. Y., Ramzan, I., Jensen, A et al. (2016). Kavain, the major constituent of the anxiolytic kava extract, potentiates GABAA receptors: functional characteristics and molecular mechanism. PLoS One, 11(6), e0157700.
  10. Gohil, K. J., Patel, J. A., & Gajjar, A. K. (2010). Pharmacological review on Centella asiatica: a potential herbal cure-all. Indian journal of pharmaceutical sciences, 72(5), 546.
  11. Higashiyama, A., Htay, H. H., Ozeki, M., Juneja, L. R., & Kapoor, M. P. (2011). Effects of l-theanine on attention and reaction time response. Journal of Functional Foods, 3(3), 171-178.
  12. Mao, J. J., Li, Q. S., Soeller, I., Rockwell, K., Xie, S. X., & Amsterdam, J. D. (2014). Long-Term Chamomile Therapy of Generalized Anxiety Disorder: A Study Protocol for a Randomized, Double-Blind, Placebo-Controlled Trial. Journal of clinical trials, 4(5), 188.