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Mexazolam

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Subjective Effects
Interactions
Legality
Mexazolam molecule structureMexazolam molecule structure
Open in Piru
Chemical Class
Benzodiazepine

Dosage & Duration

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Dosage

Doses are population estimates that vary widely between individuals.

Threshold~0.25 mg
Light0.25-0.5 mg
Moderate0.5-1.5 mg
Strong1.5-2 mg
Heavy2-3 mg

Duration

Onset5-45 minutes
After Effects1-12 hours
Total4-8 hours

Subjective Effects

Subjective Effects not written up yet

Pharmacology

Pharmacodynamics

Mexazolam enhances GABA-A receptor activity at the benzodiazepine site through an active metabolite. It potentiates GABA currents at receptors containing α2 or α3 subunits, supporting its anxiolytic action. Its effect on current amplitude at α1-containing receptors is minimal.

Pharmacokinetics

Mexazolam undergoes extensive hepatic metabolism, primarily through oxidation by CYP3A isoforms, including CYP3A4, producing two principal active metabolites. Elimination is biphasic, with an initial distribution half-life of approximately 1.4 hours associated with rapid tissue uptake and first-pass metabolism, followed by a terminal half-life of about 76 hours. Plasma protein binding exceeds 90%, and gradual release from peripheral tissues contributes to the prolonged terminal phase. The active metabolites have elimination half-lives of 130-200 hours and further prolong its action.

Interactions

Interactions not written up yet

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

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Tolerance

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

Full Tolerance
During treatment, mexazolam retained its therapeutic anxiolytic effects at 1 week, but by 3 weeks its effectiveness had fallen to the level of placebo.

Harm Potential

Addiction & Dependence

Psychological

Mexazolam can be habit-forming.2

History & Culture

Mexazolam was marketed under the trade names Melex3 and Sedoxil4 and was investigated in clinical trials for anxiety.5

Legality

Legality not written up yet

References

Citations

  1. Voltage-clamp evidence of GABAA receptor subunit-specific effects: pharmacodynamic fingerprint of chlornordiazepam, the major active metabolite of mexazolam, as compared to alprazolam, bromazepam, and zolpidem. Pharmacological Reports / PubMed (2022). https://doi.org/10.1007/s43440-022-00411-x1
  2. Sedoxil, 1 mg, tablet — Summary of Product Characteristics. BIAL (2015). https://academy.bial.com/regional/wp-content/uploads/2022/04/SmPC-Sedoxil-Albania.pdf1
  3. Pharmaceuticals and Medical Devices Safety Information No. 342. Pharmaceuticals and Medical Devices Agency (2017). https://www.pmda.go.jp/files/000217869.pdf1
  4. SEDOXIL patient information leaflet. Malta Medicines Authority (n.d.). https://medicinesauthority.gov.mt/file.ashx?f=19BDEC85EF4B3E34216BC01F021CD08CBEF8D778C6CBD15C1
  5. Mexazolam: Clinical Efficacy and Tolerability in the Treatment of Anxiety. Neurology and Therapy (2014). https://doi.org/10.1007/s40120-014-0016-71

Article Status

  • Josie Kins avatar
    Step 1 · Automated synthesis

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