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 replace 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
olerance, dependence and withdrawal
Abrupt or rapid discontinuation from etizolam, as with benzodiazepines, may result in the appearance of the benzodiazepine withdrawal syndrome, including rebound insomnia. Neuroleptic malignant syndrome, a rare event in benzodiazepine withdrawal, has been documented in a case of abrupt withdrawal from etizolam. This is particularly relevant given etizolam’s short half life relative to benzodiazepines such as diazepam resulting in a more rapid drug level decrease in blood plasma levels.
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In a study that compared the effectiveness of etizolam, alprazolam, and bromazepam for the treatment of generalized anxiety disorder, all three drugs retained their effectiveness over 2 weeks, but etizolam became more effective from 2 weeks to 4 weeks. Administering .5 mg etizolam twice daily did not induce cognitive deficits over 3 weeks when compared to placebo.
When multiple doses of etizolam, or lorazepam, are administer 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 is observe, but no significant tolerance to the anticonvulsant effects of etizolam observe. Etizolam therefore has a reduced liability to induce tolerance, and dependence, compared with classic benzodiazepines
Etizolam, a thienodiazepine derivative, is absorbe fairly rapidly, with peak plasma levels achieve between 30 minutes and 2 hours. It has a mean elimination half life of about 3.4 hours. Etizolam possesses potent hypnotic properties, and is comparable with other short-acting benzodiazepines. Etizolam acts as a full agonist at the benzodiazepine/GABAa receptor to produce its range of therapeutic and adverse effects