Ethyl loflazepate
Ethyl loflazepate is a prodrug benzodiazepine licensed as an anxiolytic in some countries (e.g. Japan and France as Meilax/Victan). It is metabolised to long-acting active metabolites including descarbethoxyloflazepate. It is included here because it circulates on the grey market. Like other benzodiazepines it potentiates GABA-A signalling to produce anxiolysis and sedation.
01 Overview
Ethyl loflazepate is a prodrug that is converted in the body to active metabolites with long half-lives, giving a slow onset and prolonged, relatively smooth anxiolytic effect. It has genuine clinical use as a long-acting anxiolytic in a handful of countries.
Outside those markets it is sold as an unregulated research chemical of variable purity. Its long duration favours accumulation, and it carries the standard benzodiazepine risks of dependence and withdrawal.
02 Mechanism
Prodrug metabolised to active benzodiazepines that act as positive allosteric modulators at the GABA-A benzodiazepine site.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Common | 1–2 mg/day | Oral | Reflects licensed anxiolytic dosing; onset is slow. |
| Strong | 2–4 mg/day | Oral | Upper clinical range. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| AnxiolysisLong, smooth reduction in anxiety. | Anecdotal | ||
| SedationMild to moderate sedation. | Anecdotal | ||
| Muscle relaxationSkeletal muscle relaxation. | Anecdotal |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Dependence and withdrawalTolerance, dependence and a protracted withdrawal syndrome with rebound anxiety and seizure risk. | Severe | Common with regular use | Anecdotal | |
| Respiratory depressionSuppressed respiration, markedly worse with opioids or alcohol. | Life-threatening | Uncommon alone, higher with CNS depressants | Anecdotal | |
| Accumulation and prolonged impairmentCumulative sedation and impaired coordination from long-lived metabolites. | Moderate | Common | Anecdotal |