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What is Etizolam?

Etizolam is a fast acting synthetic depressant substance belonging to a chemical class of thienodiazepine, and is known to produce anti-anxiety, disinhibition, muscle relaxation and sedative effects that are similar to benzodiazepine. They are found to be effective using oral or sublingual route of administration.

Etizolam is also structurally analogous to benzodiazepines, wherein the benzene ring is substituted by a thiophene ring; hence the name of class is thienodiazepine. Thiopene is a 5 membered aromatic ring that contains one sulfur atom.

Etizolam core consists of a thiophene ring that is fused with a seven membered diazepine ring which have two nitrogen constituents located at R1 and R4. At R7 of this bicyclic structure, an ethyl chain is attached. Also a R₂ ‘chlorine substituted phenyl ring is attached at R5 location of the structure.

Etizolam consists of a methylated triazole ring that is bonded at R1 and R2 of its diazepine ring, which makes its similar to benzodiazepine drugs belonging to triazolobenzodiazepines, recognized by the suffix of “ –zolam”.

Etizolam is comparatively a new and popular research chemical, and its first appearance was as a gray market research chemical in 2011, however its origin as a medical drug can be dated back to 1990s, where it was used as an anti-anxiety in many countries of the world (Brand name: Etilaam and Etizest).

It is not a controlled substance and anecdotal reports stating its potency which is comparatively less, as 1mg of etizolam is equivalent to 0.5mg of alprazolam/ clonazepam or 10mg of diazepam. It is often regarded as less potent and sedating form of alprazolam when compared in relation to its speed of onset, duration of action and possible recreational purpose.

It is an addictive and high-dependence forming drug and abrupt discontinuation of these substances can potentiate life-threatening withdrawal symptoms, so gradual dose tapering must be observed.

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Bioactivity of Etizolam

It has hypnotic, sedative, anxiolytic, anti-convulsant, skeletal muscle relaxant and amnesic properties.

Etizolam potent hypnotic activity can be related to other short acting benzodiazepines. The etizolam has been reported to act as a full agonist at a benzodiazepine receptor site where it exhibits a range of therapeutic and adverse effects.

The pharmacological activity is produced by virtue of the thienodiazepines bonding to a benzodiazepine receptor site, where it is reported to significantly enhance the efficiency and effects of the neurotransmitter gamma amino butyric acid (GABA) by acting on their receptors.

This receptor is the most abundantly occurring inhibitory receptor set present inside brain; therefore its modulation consequently produces sedating/ calming effect of etizolam on the nervous system.

Expected Physical effects of Etizolam

It can cause muscle relaxation, physical euphoria, loss of motor control, respiratory depression, increased libido, stimulation of appetite, suppression of seizure and temporary erectile dysfunction. It causes dizziness and is a dangerous rapidly acting sedative substance that can lead to complete unconsciousness on repeated doses.

It produces cognitive euphoria, disinhibition, memory suppression i.e. amnesia, delusions of sobriety due to cognitive impairment, ego inflation, emotionality and motivation suppression. Under the effect of drug, thought deceleration, suppression of analysis and temporary impairment in information processing ability is seen.

All of these effects contribute towards compulsive redosing, which may cause overdosing of drug as the user forgets, which consequently presents with an amnesic black out state.

An increased anxiety, aggression, irritability, violence and suicidal behavior may rarely develop and are most likely occur among recreational abusers or patients getting high-dose regimes. The after effects include rebound anxiety, dream potentiation or suppression, residual sleepiness, irritability and altered thought processing.

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Dosage Information for Etizolam

The minimum dose required to produce depressant effect is 0.2 – 0.5 mg. For mild effects, a dose of 0.5 – 1 mg is sufficient, but most commonly 1 – 2 mg is given and are available as in pill or pellet form, powder or dispensed on a blotter paper sheet. Strong depressant effects are seen when given in dosage of 2 – 5 mg and overdose has been observed in individuals taking more than 5 mg quantity of drug or when taken with other depressants.

The total duration of action is 5 – 7 hours, with onset seen within 15 – 25 minutes and peak effects shown after 2 – 3 hours. However, their after-effects remain for about 6 – 24 hours after the last dose taken.

Other names for Etizolam

4-(2-Chlorophenyl)-2-ethyl-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine

Brand names: Etilaam, Etizest, Sedekopan, Pasaden, Depas etc.

*The information contained in this article is for educational purposes only. We have tried to be as factual as possible but this doesn’t mean that the information is 100% accurate.