Etizolam

Etizolam (marketed under the brand name Etilaam, Etizola, Sedekopan, Pasaden or Depas) is a thienodiazepine drug which is a benzodiazepine analog. The etizolam molecule differs from most other benzodiazepines in that the benzene ring has been replaced by a thiophene ring. It possesses amnesic, anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties.

Etizolam

Indications   Short-term treatment of insomnia Short-term treatment of anxiety or panic attacks, if a benzodiazepine is required Dosage   For anxiety: 0.50-1 mg two or three times per day (maximum 2 mg per day) For insomnia: 1-2 mg before bedtime A 1mg dose of etizolam is approximately equivalent to that of 10mg of diazepam long term use cause Blepharospasms Tolerance, dependence and withdrawal Abrupt or over rapid withdrawal from etizolam as with other benzodiazepines may result in the appearance of the benzodiazepine withdrawal syndrome, including rebound insomnia. A neuroleptic malignant syndrome, a rare event in benzodiazepine withdrawal has been documented in a case of abrupt withdrawal from etizolam Contraindications and special caution Benzodiazepines require special precaution if used in the elderly, during pregnancy, in children, alcohol or drug-dependent individuals and individuals with comorbid psychiatric disorders. Pharmacology Etizolam a thienodiazepine benzodiazepine derivative, is absorbed fairly rapidly with peak plasma levels achieved between 30 minutes and 2 hours and has a mean elimination half life of about 3 and a half hours. However, its pharmacologically active metabolite alpha-hydroxyetizolam which has the same potency as etizolam is eliminated more slowly with a mean half life of just over 8 hours. So it can be classified as a short-medium action benzodiazepine. Etizolam possesses potent hypnotic properties. Etizolam acts as a full agonist at the benzodiazepine receptor to produce its range of therapeutic as well as adverse effects. Similar to other benzodiazepines etizolam binds unselectively to benzodiazepine receptor subtypes. In addition etizolam unlike most other benzodiazepines (some of which can increase levels of estradiol) has prolactogenic effects leading to an increase in prolactin blood levels. 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 not substantial changes in deep sleep. There is a reduction of REM sleep. In EEG tests of healthy volunteers Etizolam showed some characteristics of tricyclic antidepressants. Interactions Itraconazole and fluvoxamine slow down the rate of elimination of etizolam leading to accumulation of etizolam and thus increased pharmacological effects. Carbamazepine speeds up the metabolism of etizolam resulting in reduced pharmacological effects of etizolam.