Etizolam

There is a high incidence of death due to respiratory depression when benzodiazepines are combined with depressants such as opiates, alcohol or other GABAergic substances.

Etizolam
The skeletal formula of Etizolam.
Chemical Nomenclature
Common names	Etizolam
Substitutive name	Etilaam, Etizest
Systematic name	7-(2-Chlorophenyl)-4-ethyl-13-methyl-3-thia-1,8,11,12-tetraazatricyclo[8.3.0.02,6] trideca-2(6),4,7,10,12-pentaene
Class Membership
Psychoactive class	Depressant
Chemical class	Thienodiazepine
Routes of Administration
Oral Dosage WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. Threshold < 0.5 mg Light 0.5 mg Common 1 - 2 mg Strong 3 - 5 mg Heavy > 5 mg Duration Total 3 - 8 hours Onset 15 - 60 minutes Peak 1 - 2 hours Offset 2 - 3 hours Afterglow 3 - 6 hours

Summary sheet: Etizolam

Etizolam (trade names Etilaam and Etizest) is a short-acting psychoactive drug of the thienodiazepine class which has been shown to produce depressant, anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, and amnestic effects. Etizolam, like benzodiazepines, binds to modulatory sites on the GABA gamma-aminobutyric acid receptors. Etizolam is not commonly prescribed and is not recognised as a controlled substance in many parts of the world, leading to its rise in popularity as a product of many research chemical vendors.

Etizolam has a relatively fast onset of action and symptomatic relief. 1mg of etizolam is approximately equivalent to 10mg diazepam. For anxiety disorders associated with depression, 1 mg can be administered several times over the course of a day. Smaller doses may alleviate symptoms of panic and can be used before bed for relief of insomnia.

Chemistry

Etizolam is a structural relative of benzodiazepines, whereby the benzene ring has been replaced by a thiophene ring, classifying it as a thienodiazepine. Thiophene is a five member aromatic ring with one sulfur atom. Etizolam contains a thiophene ring fused to a diazepine ring, which is a seven member ring with the two nitrogen constituents located at R₁ and R₄. This forms the thienodiazepine core of etizolam. An ethyl chain is bound to this bicyclic structure at R₇. Additionally, a R₂' fluorine substituted phenyl ring is bound to this structure at R₅. Etizolam also contains a methylated triazole ring fused to and incorporating R₁ and R₂ of its diazepine ring. Etizolam shares this fused triazole ring substitution with certain benzodiazepine drugs, called triazolobenzodiazepines, distinguished by the suffix "-zolam".

Pharmacology

Thienodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors. As this site is the most prolific inhibitory receptor within the brain, its modulation results in the sedating (or calming effects) of etizolam on the nervous system.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects

The physical effects of etizolam can be broken down into several components which progressively intensify proportional to dosage.

These are described below and generally include:

• Sedation - In terms of energy level alterations, this drug has the potential to be extremely sedating and often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
• Motor control loss
• Respiratory depression
• Muscle relaxation
• Dizziness
• Temporary erectile dysfunction

Cognitive effects

The cognitive effects of etizolam can be broken down into several components which progressively intensify proportional to dosage. The general head space of etizolam is described by many as one of recreationally intense sedation and decreased inhibition. It contains a large number of typical depressant cognitive effects.

The most prominent of these cognitive effects generally include:

• Anxiety suppression
• Thought deceleration
• Disinhibition
• Information processing suppression
• Compulsive redosing
• Amnesia
• Delusions of sobriety - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others.

Paradoxical effects

Paradoxical reactions to benzodiazepines such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%).

These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.

Toxicity and harm potential

Blepharospasm

Blepharospasms (twitching eyelid) can occur with long-term use. Rarely, erythema annulare centrifugum skin lesions have been reported.

Lethal dosage

The lethal dose of etizolam has not been established; however, like many benzodiazepines, it has a large therapeutic index and margin of safety. Complications may arise when administered in excess. Intentional overdoses have been reported.

As with all GABAergic drugs, overdose can be lethal when mixed with other depressants including alcohol or opioids.

Tolerance and addiction potential

Tolerance will develop to the sedative-hypnotic effects within a couple of days of repeated administration. Abrupt discontinuation of etizolam following regular dosing over several days can result in a withdrawal phase which includes rebound symptoms such as increased anxiety and insomnia. It is possible to gradually reduce the dose over the course of several days, which will lengthen the duration of the withdrawal period, but reduce the perceived intensity.

Thienodiazepine discontinuation is notoriously difficult; it is potentially life-threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of seizure following discontinuation of Etizolam. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Etizolam may not be cross-tolerant with some other thienodiazepines or benzodiazapienes such as diazepam, meaning the tolerances to these substances develop independently. This also means that the consumption of diazepam or similar substances may not fully relieve the withdrawal symptoms of etizolam or provide relief from the potentially lethal withdrawal symptoms whatsoever.

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

• Depressants (1,4-Butanediol, 2-methyl-2-butanol, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances also potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Stimulants - It is dangerous to combine benzodiazepines with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of benzodiazepines, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of benzodiazepines will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dosing a certain amount of benzodiazepines per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.

Legal issues

• United States: In August 2014, a Connecticut man was charge with the possession of etizolam after being involved with a DUI. In the same month, the state of Arkansas listed etizolam as a Schedule I drug under their drug scheduling guidelines.
• Germany: Phenazepam and etizolam were controlled in Germany in July 2013.
• Poland: Etizolam may be scheduled under the Act on Counteracting Drug Addiction and the State Sanitary Inspection -Article 27c.
• United Kingdom: Etizolam is not controlled as of July 2013.

Preparation methods

Preparation methods for this compound within our preparation index include:

• Volumetric liquid dosing

See also

• Responsible use
• Psychoactive substance index
• Alcohol
• Benzodiazepines
• Depressants
• Volumetric liquid dosing

External links

• Etizolam (Erowid)
• Etizolam (Wikipedia)