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Brotizolam

Brotizolam molecule structureBrotizolam molecule structure
Lendormin, Lendorm, Lindormin, Bondormin, Noctilan
Chemical Class
Thienotriazolodiazepine

Brotizolam is a sedative-hypnotic of the thienotriazolodiazepine class, a benzodiazepine analog patented in 1974 and introduced into medical use in 1984.citation needed It is prescribed for short-term treatment of severe insomnia in parts of Europe, Israel, and Japan. Brotizolam is notable for its exceptional potency and rapid elimination, producing effects comparable to triazolam and midazolam. As with other benzodiazepines, it carries risks of respiratory depression when combined with other depressants, as well as amnesia and habit formation.

Dosage & Duration

Dosage

Doses are population estimates that vary widely between individuals.

Threshold~100 µg
Light100-200 µg
Moderate200-400 µg
Strong400-600 µg
Heavy600+ µg

Duration

After Effects1-4 hours
Half-life
3.6-7.9 hours

Subjective Effects

Legacy content. A statistically backed ontology from Mindstate Design Labs is coming soon.

Brotizolam produces an experience dominated by rapid, heavy sedation and anxiety relief, consistent with its use as a highly potent, short-acting hypnotic for severe insomnia. Its character closely resembles short-acting benzodiazepines such as triazolam, with pronounced hypnotic, muscle relaxant, and amnesic components and little in the way of sensory alteration. Residual effects such as drowsiness and impaired cognitive and motor function can persist into the following day, particularly at doses above 0.5-1 mg.

Physical

The body load centers on strong sedation and skeletal muscle relaxation, accompanied by ataxia, clumsiness, slurred speech, and general impairment of motor function. Dizziness, fatigue, and headache are common, while nausea, vomiting, palpitations, hypotension, and respiratory depression occur less often.

Sedation

Sedation is the defining physical effect, appropriate to a hypnotic used for sleep induction.

Uncomfortable

DizzinessHeadaches

Cognitive

The headspace is calm and anxiety-suppressed but clouded, with confusion and anterograde amnesia commonly accompanying moderate to high doses. Paradoxical reactions such as anxiety, aggression, or violent behavior occur infrequently.

Paradoxical

Paradoxical reactions occur in a minority of users.

Suppressions

Suppressive effects dominate the mental state, in line with the compound's hypnotic and anxiolytic profile.

Confusion

Visual

Visual effects are not a typical feature of brotizolam.

Pharmacology

Pharmacodynamics

Brotizolam acts as a positive allosteric modulator of the GABA-A receptor at the benzodiazepine binding site.citation needed Through this mechanism, it produces anxiolytic, anticonvulsant, hypnotic, sedative, and skeletal muscle relaxant effects. It is considered pharmacologically similar to other short-acting hypnotic benzodiazepines such as triazolam and midazolam.

Pharmacokinetics

Brotizolam is rapidly absorbed following administration and is rapidly eliminated, with an average half-life of 4.4 hours (range 3.6–7.9 hours).citation needed It is metabolized into two primary metabolites: a 4-hydroxy derivative with far less potency than the parent compound, and a 1-methylhydroxy derivative thought to have comparable activity. However, the 1-methylhydroxy metabolite is not present in measurable plasma concentrations following a single dose in healthy subjects, so neither metabolite contributes significantly to the overall pharmacological effect in humans.

Interactions

Caution

Use caution

These combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.

1,2-BenzodiazepineAbametapirAcetazolamideAcetophenazineAgomelatine
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Tolerance

Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.

Full Tolerance
Tolerance to the hypnotic effects develops with repeated use, which is why clinical treatment is typically limited to 2-4 weeks to minimize tolerance development and dependence.
Cross Tolerance

Benzodiazepines, Thienodiazepines, Other GABA-A positive allosteric modulators

Harm Potential

Addiction & Dependence

Psychological

Moderate

Brotizolam has recognized potential for abuse and is classified as habit-forming.citation needed Abuse was significant enough in Hong Kong during the late 1980s and 1990s to warrant government reclassification as a Dangerous Drug, with regulatory controls subsequently extended to all benzodiazepines.

Physical

Moderate

Physical dependence can develop with regular use.1 Treatment is recommended for only 2-4 weeks for severe insomnia.citation needed Mild rebound insomnia may occur when treatment is stopped, indicating physiological adaptation to the drug.

Psychosis Risk

Hallucinations and paradoxical reactions including aggression, anxiety, and violent behavior are listed as less common side effects.citation needed These psychiatric disturbances appear to be uncommon at recommended doses.

History & Culture

Development and Commercialization

Brotizolam was first patented in 1974.citation needed The compound's synthesis was subsequently documented by Weber, Bauer, Danneberg, and Kuhn through a 1978 United States patent. The substance entered clinical practice a decade after its initial patent in 1984, finding adoption

Legality

By Country

Controlled / restricted4
Canada flagCanadaRestricted
Taiwan flagTaiwanRestricted
Ukraine flagUkraineRestricted
United Kingdom flagUnited KingdomRestricted
Prescription11
Austria flagAustriaPrescription medicine
Germany flagGermanyPrescription only
Israel flagIsraelPrescription only
Italy flagItalyPrescription medicine
Japan flagJapanPrescription medicine
Luxembourg flagLuxembourgPrescription medicine
Netherlands flagNetherlandsPrescription medicine
Poland flagPolandPrescription only
Portugal flagPortugalPrescription medicine
Singapore flagSingaporePrescription only
Spain flagSpainPrescription medicine
Legal / decriminalized1
Belgium flagBelgiumLegal (regulated)
Not scheduled2
United States flagUnited StatesNot approved
Hong Kong flagHong KongDangerous Drug

References

Source Pages

  1. DrugBank
  2. DrugBank: Benzodiazepine category
  3. PsychonautWiki: Benzodiazepines
  4. PsychonautWiki: Dangerous Combinations
  5. PsychonautWiki: Thienodiazepines
  6. TripSit Factsheet: Brotizolam
  7. TripSit Wiki: Drug Combinations
  8. TripSit Wiki: Uncommon Benzodiazepines
  9. Wikipedia

Citations

  1. Lendormin 0.25mg tablets (Brotizolam) – Core Safety Profile, European PSUR Work Sharing Project. College ter Beoordeling van Geneesmiddelen (CBG-MEB) (2009). https://db.cbg-meb.nl/veegactie/csp/brotizolam-3-2009.pdf1
  2. Kenneth K.C. Lee, Thomas Y.K. Chan, Anthony W.K. Chan, Grace S.N. Lau, & Julian A.J.H. Critchley. (1995). Use and abuse of benzodiazepines in Hong Kong 1990-1993--the impact of regulatory changes. Journal of Toxicology. Clinical Toxicology, 33(6), 597–602. https://doi.org/10.3109/155636595090106151234
  3. European Medicines Agency. (2023-07-06). List of nationally authorised medicinal products: brotizolam, Procedure No. PSUSA/00000444/202212. European Medicines Agency. https://www.ema.europa.eu/en/documents/psusa/brotizolam-list-nationally-authorised-medicinal-products-psusa00000444202212_en.pdf123456
  4. Royal Decree of 6 September 2017 regulating narcotic drugs and/or psychotropic substances, Annex III. ejustice.just.fgov.be (n.d.). http://www.ejustice.just.fgov.be/eli/arrete/2017/09/06/2017031231/justel1
  5. Royal Decree of 6 September 2017 regulating narcotic drugs and/or psychotropic substances, Annex III. afmps.be (n.d.). https://www.afmps.be/sites/default/files/content/INSP/NARC/annex%20III_non%20official%20consolidated%20version.pdf1
  6. Bulletin: Controlled Substances Licensed Dealers Regulations — Benzodiazepines and Other Targeted Substances. canada.ca (n.d.). https://www.canada.ca/en/health-canada/services/health-concerns/reports-publications/controlled-substances-precursor-chemicals/bulletin-controlled-substances-licensed-dealers-regulations-benzodiazepines-other-targeted-substances.html1
  7. German Federal Government. (n.d.). Betäubungsmittelgesetz (BtMG) – Anlage III (zu § 1 Abs. 1): verkehrsfähige und verschreibungsfähige Betäubungsmittel. gesetze-im-internet.de. https://www.gesetze-im-internet.de/btmg_1981/anlage_iii.html1
  8. Betäubungsmittelgesetz § 13 Verschreibung und Abgabe auf Verschreibung. gesetze-im-internet.de (n.d.). https://www.gesetze-im-internet.de/btmg_1981/__13.html1
  9. Pharmacy Society of Hong Kong. (2011). Consolidated List of Poisons, Antibiotics and Dangerous Drugs – Schedule 1, Part I Dangerous Drugs (Cap.134). Hong Kong Pharmaceutical Journal, 18(4 (Supplement)). http://www.pshk.hk/uploads/files/HKPJ/v18n4supp.pdf1
  10. Pharmacists Ordinance [New Version], 1981 (official government PDF). gov.il (n.d.). https://www.gov.il/BlobFolder/service/application-for-cosmetic-import-permits/en/pkudat-rokhim.pdf1

Further Reading

  1. Drug-Do: Benzos
  2. PubChem: Brotizolam
  3. Tripsitter: Brotizolam Harm Reduction

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Recent changes8 human edits · latest

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19 August 2026

  1. Lyrea · Changed a word in Subjective Effects › Notes › Overview

  2. Lyrea · Changed a word in Dosage & Duration › Routes 1 › Dose ranges › Threshold

24 January 2026

  1. Josie Kins · Updated the article · also 1,4-Butanediol, 1B-LSD, 1cP-AL-LAD and 573 more

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