Etizolam Powder

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Etizolam Powder Etizolam (marketed under many brand names) is a thienodiazepine derivative which is a benzodiazepine analog.

The etizolam molecule differs from a benzodiazepine in that the benzene ring has been replaced by a thiophene ring and triazole ring has been fused, making the drug a thienotriazolodiazepine. It possesses amnesic, anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties.

It was patented in 1972 and approved for medical use in 1983.

Pharmacology

Etizolam, a thienodiazepine derivative, is absorbed fairly rapidly, with peak plasma levels achieved between 30 minutes and 2 hours. It has a mean elimination half life of about 3.5 hours.

Etizolam possesses potent hypnotic properties, and is comparable with other short-acting benzodiazepines. Etizolam acts as a full agonist at the benzodiazepine receptor to produce its range of therapeutic and adverse effects.

According to the Italian P.I. sheet, etizolam belongs to a new class of diazepines, thienotriazolodiazepines. This new class is easily oxidized, rapidly metabolized, and has a lower risk of accumulation, even after prolonged treatment.

Etizolam has an anxiolytic action about 6 times greater than that of diazepam. Etizolam produces, especially at higher dosages, a reduction in time taken to fall asleep, an increase in total sleep time, and a reduction in the number of awakenings.

During tests, there were no substantial changes in deep sleep; however, it may reduce REM sleep. In EEG tests of healthy volunteers, etizolam showed some similar characteristics to tricyclic antidepressants.

Interactions

Itraconazole and fluvoxamine slow down the rate of elimination of etizolam, leading to accumulation of etizolam, therefore increasing its pharmacological effects. Carbamazepine speeds up the metabolism of etizolam, resulting in reduced pharmacological effects.

Overdose

Cases of intentional suicide by overdose using etizolam in combination with GABA agonists have been reported. Although etizolam has a lower LD50 than certain benzodiazepines, the LD50 is still far beyond the prescribed or recommended dose.

Flumazenil, a GABA antagonist agent used to reverse benzodiazepine overdoses, inhibits the effect of etizolam as well as classical benzodiazepines such as diazepam and chlordiazepoxide.

Etizolam overdose deaths are rising  for instance, the National Records of Scotland report on drug-related deaths, implicated 548 deaths from street Etizolam in 2018, almost double the number from 2017 (299) and only six years from the first recorded death (in 2012).

The 548 deaths were 45% of all drug-related deaths in Scotland in 2018.

Misuse

Etizolam is a drug of potential misuse. Cases of etizolam dependence have been documented in the medical literature.

However, conflicting reports from the World Health Organization, made public in 1991, dispute the misuse claims. Since 1991, cases of etizolam misuse and addiction have substantially increased, due to varying levels of accessibility and cultural popularity.

Chemical and physical data

Formula: C17H15ClN4S

Molar mass: 342.07 g/mol g·mol1

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