Etizolam

Death may occur when thienodiazepines are combined with depressants such as opiates, benzodiazepines, alcohol or other GABAergic substances.

It is strongly discouraged to consume moderate to heavy dosages of these substances together.

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. See responsible use section. DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation. This dosage and duration information has been sourced from TripSit Threshold 0.2 - 0.5 mg Light 0.5 - 1 mg Common 1 - 2 mg Strong 2 - 5 mg Heavy 5 mg + Duration Total 5 - 8 hours Onset 15 - 60 minutes Peak 1 - 2 hours Offset 2 - 3 hours After effects 6 - 24 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 depressants, anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, depressant and amnestic effects. 1mg of etizolam is approximately equivalent to 10mg diazepam.

This compound is not commonly prescribed and is not recognized as a controlled substance in many parts of the world, leading to its rise in popularity as a product of many research chemical vendors.

Similar to benzodiazepines, the sudden discontinuation of thienodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death. It is highly recommended to taper one's dose by gradually lowering the amount taken each day for a prolonged period of time instead of stopping abruptly.

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Etizolam is a structural relative of benzodiazepines, whereby the benzene ring has been replaced by a thiophene ring, classifying it as a thienodiazepine.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 set 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

• 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.
• Physical euphoria
• 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 depressants cognitive effects.

The most prominent of these cognitive effects generally include:

• Anxiety suppression
• Thought deceleration
• Analysis suppression
• Disinhibition
• Information processing suppression
• Compulsive redosing
• Amnesia
• Cognitive euphoria - This effect is generally achieved only at high doses.
• Emotion suppression - Although this compound primarily suppresses anxiety, it also dulls other emotions in a manner which is distinct but less intensive than that of antipsychotics.
• 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. It most commonly occurs at heavy dosages.

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

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

Main article: Research chemicals § Toxicity and harm potential

Etizolam likely has a low toxicity relative to dose. However, it is potentially lethal when mixed with depressants like alcohol or opioids.

It is strongly recommended that one use harm reduction practices when using this drug.

Tolerance and addiction potential

Etizolam is extremely physically and psychologically addictive. When multiple doses of etizolam, or lorazepam, were administered to rat neurons, lorazepam caused downregulation of alpha-1 benzodiazepine binding sites (tolerance/dependence), while etizolam caused an increase in alpha-2 benzodiazepine binding sites (reverse tolerance to anti-anxiety effects). Tolerance to the anticonvulsant effects of lorazepam was observed, but no significant tolerance to the anticonvulsant effects of etizolam was observed. Etizolam therefore has a reduced liability to induce tolerance, and dependence when compared with classic benzodiazepines.

Tolerance will, however, develop to the sedative-hypnotic effects within a couple of days of continuous use. After cessation, the tolerance returns to baseline in 7 - 14 days. However, in certain cases this may take significantly longer in a manner which is proportional to the duration and intensity of one's long-term usage.

Withdrawal symptoms or rebound symptoms may occur after ceasing treatment abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction. For more information on tapering from thienodiazepines in a controlled manner, please see this guide.

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 also an increased risk of seizure following discontinuation of thienodiazepines. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Etizolam presents cross-tolerance with all benzodiazepines and thienodiazepines, meaning that after its consumption all thienodiazepines will have a reduced effect.

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 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 thienzodiazepines with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of thienzodiazepines, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of thienzodiazepines 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 thienzodiazepines 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 - It is illegal to produce, supply, or import this drug under the Psychoactive Substance Act, which came into effect on May 26th, 2016.

Preparation methods

Preparation methods for this compound within our tutorial index include:

• Volumetric liquid dosing

See also

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

External links

• ETIZOLAM
• Etizolam (Erowid)
• Etizolam (Wikipedia)
• Etizolam (TripSit)
• Etizolam.com