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Ketazolam

Ketazolam molecule structureKetazolam molecule structure
Chemical Class

Ketazolam is a long-acting depressant in the 1,4-benzodiazepine class. It belongs to the benzodiazepine class, which has anxiolytic, hypnotic-sedative, muscle-relaxant, and anticonvulsant actions.1 It is used to manage anxiety, insomnia, and spasticity. Its effectiveness for anxiety is similar to diazepam,2 while adverse effects, including sedation, appear to be less pronounced and tend to be milder when they occur.3 Ketazolam is habit-forming.4

Dosage & Duration

Dosage

Doses are population estimates that vary widely between individuals.

Threshold~5 mg
Light5-15 mg
Moderate15-30 mg
Strong30-60 mg
Heavy60+ mg

Duration

Onset30-90 minutes
After Effects2-12 hours
Total8-12 hours

Subjective Effects

Subjective Effects not written up yet

Pharmacology

Pharmacodynamics

Ketazolam positively modulates GABA-A receptors by binding at their benzodiazepine site. This enhances GABA-mediated chloride conductance, making neurons less likely to fire. The binding site lies at the interface between alpha and gamma subunits, with alpha-1, alpha-2, alpha-3, and alpha-5 subunits able to participate.

Pharmacokinetics

Ketazolam undergoes sequential metabolic conversion beginning in the blood, and a half-life of 26-200 hours is reported. Its downstream products are eliminated mainly in urine, predominantly after glucuronide conjugation.5 Ketazolam is classified as a CYP3A4 substrate and inhibitor, with inhibitor strength unspecified, and as a P-glycoprotein substrate. Computational predictions suggest intestinal absorption, intestinal cell permeability, and blood-brain barrier penetration, as well as inhibition of CYP2C9 and CYP2C19. Predictions differ on whether it inhibits P-glycoprotein.

Interactions

Interactions not written up yet

An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.

Check TripSit

Tolerance

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

Full Tolerance
Tolerance to ketazolam's therapeutic effects develops over 15 days of chronic use.

Harm Potential

Addiction & Dependence

Psychological

Ketazolam can be habit-forming.8

Physical

Chronic ketazolam use can cause physical dependence, with benzodiazepine withdrawal symptoms following discontinuation or dose reduction.

Toxicity

Central nervous system

Ketazolam overdose can cause somnolence, confusion, coma, and reduced reflexes.9

History & Culture

In Canada, ketazolam was marketed as Loftran by SmithKline Beecham from December 31, 1992, to September 12, 1996. In South Africa, GlaxoSmithKline marketed it under the brand name Solatran.

Legality

International

Ketazolam is approved or marketed in some countries, but the approved jurisdictions are not specified.

By Country

Illegal1
United States flagUnited StatesIllegal
Controlled / restricted1
Canada flagCanadaRestricted

References

Citations

  1. Ficha técnica Ketazolam Adamed 15 mg cápsulas duras. Agencia Española de Medicamentos y Productos Sanitarios (2014). https://cima.aemps.es/cima/dochtml/ft/56259/FT_56259.html1
  2. Ketazolam and diazepam in anxiety: a controlled study. Journal of Clinical Pharmacology / PubMed (1980). https://doi.org/10.1002/j.1552-4604.1980.tb01673.x1
  3. Ketazolam Compared to Diazepam and Placebo in the Treatment of Anxiety. Journal of International Medical Research (1980). https://doi.org/10.1177/0300060580008006151
  4. Prospecto Ketazolam Adamed 45 mg cápsulas duras. Agencia Española de Medicamentos y Productos Sanitarios (n.d.). https://cima.aemps.es/cima/dochtml/p/56261/P_56261.html1
  5. Ficha técnica Ketazolam Adamed 30 mg cápsulas duras. Agencia Española de Medicamentos y Productos Sanitarios (2014). https://cima.aemps.es/cima/dochtml/ft/56260/FT_56260.html1
  6. Solatran — Fachinformation. Swissmedic (2022). https://swissmedicinfo-pro.ch/showText.aspx?authNr=42286&lang=DE&supportMultipleResults=1&textType=FI1
  7. Toxicological analysis on forensic investigation in drug related cases; pharmacological information on 88 psychoactive substances in “Narcotics and Psychotropics Control Act” in Japan. Medical Mass Spectrometry (2022). https://doi.org/10.24508/mms.2022.06.0071
  8. Ficha técnica Ketazolam Adamed 45 mg cápsulas duras. Agencia Española de Medicamentos y Productos Sanitarios (2014). https://cima.aemps.es/cima/dochtml/ft/56261/FT_56261.html1
  9. Ketazolam - TOX Seup. TOX Seup (n.d.). https://toxseup.org/ketazolam/1
  10. Controlled Drugs and Substances Act — Schedule IV. laws-lois.justice.gc.ca (n.d.). https://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-12.html1

Article Status

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